DE15187654T1 - Antivirales Mittel - Google Patents
Antivirales Mittel Download PDFInfo
- Publication number
- DE15187654T1 DE15187654T1 DE15187654.7T DE15187654T DE15187654T1 DE 15187654 T1 DE15187654 T1 DE 15187654T1 DE 15187654 T DE15187654 T DE 15187654T DE 15187654 T1 DE15187654 T1 DE 15187654T1
- Authority
- DE
- Germany
- Prior art keywords
- optionally substituted
- ring
- solvate
- pharmaceutically acceptable
- acceptable salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000003443 antiviral agent Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 9
- 125000004429 atom Chemical group 0.000 claims abstract 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims 19
- 239000012453 solvate Substances 0.000 claims 19
- 125000003107 substituted aryl group Chemical group 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- -1 nitro, hydroxy Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000002947 alkylene group Chemical group 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 6
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000004450 alkenylene group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 230000002452 interceptive effect Effects 0.000 claims 4
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 claims 3
- 125000004509 1,3,4-oxadiazol-2-yl group Chemical group O1C(=NN=C1)* 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 claims 1
- 125000004505 1,2,4-oxadiazol-5-yl group Chemical group O1N=CN=C1* 0.000 claims 1
- 125000004515 1,2,4-thiadiazol-3-yl group Chemical group S1N=C(N=C1)* 0.000 claims 1
- 125000004516 1,2,4-thiadiazol-5-yl group Chemical group S1N=CN=C1* 0.000 claims 1
- 125000001305 1,2,4-triazol-3-yl group Chemical group [H]N1N=C([*])N=C1[H] 0.000 claims 1
- 125000004521 1,3,4-thiadiazol-2-yl group Chemical group S1C(=NN=C1)* 0.000 claims 1
- 229940099797 HIV integrase inhibitor Drugs 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 125000005140 aralkylsulfonyl group Chemical group 0.000 claims 1
- 125000004659 aryl alkyl thio group Chemical group 0.000 claims 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 125000005110 aryl thio group Chemical group 0.000 claims 1
- 125000005164 aryl thioalkyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004281 furazan-3-yl group Chemical group [H]C1=NON=C1* 0.000 claims 1
- 125000004994 halo alkoxy alkyl group Chemical group 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005253 heteroarylacyl group Chemical group 0.000 claims 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 1
- 125000005367 heteroarylalkylthio group Chemical group 0.000 claims 1
- 125000005326 heteroaryloxy alkyl group Chemical group 0.000 claims 1
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 1
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims 1
- 125000005368 heteroarylthio group Chemical group 0.000 claims 1
- 239000003084 hiv integrase inhibitor Substances 0.000 claims 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 1
- 125000002140 imidazol-4-yl group Chemical group [H]N1C([H])=NC([*])=C1[H] 0.000 claims 1
- 125000001793 isothiazol-3-yl group Chemical group [H]C1=C([H])C(*)=NS1 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- LHKVDVFVJMYULK-UHFFFAOYSA-N nitrosylazide Chemical compound [N-]=[N+]=NN=O LHKVDVFVJMYULK-UHFFFAOYSA-N 0.000 claims 1
- 125000004287 oxazol-2-yl group Chemical group [H]C1=C([H])N=C(*)O1 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000004289 pyrazol-3-yl group Chemical group [H]N1N=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 claims 1
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 claims 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 claims 1
- 125000000464 thioxo group Chemical group S=* 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/38—2-Pyrrolones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/40—Radicals substituted by oxygen atoms
- C07D307/46—Doubly bound oxygen atoms, or two oxygen atoms singly bound to the same carbon atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
- C07D311/24—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrane Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
Verbindung der Formel (I):wobei RC und RD zusammen genommen mit den angrenzenden Kohlenstoffatomen einen Ring bilden, der kondensiert sein kann, Y Hydroxy ist; Z O ist; RA ein durch die Formeldargestellter Rest ist, wobei der Ring C ein aromatischer Heterocyclus ist, der N enthält, wobei mindestens ein Atom, angrenzend an das Atom an der Bindestelle, ein nicht substituiertes N-Atom ist; wobei die gestrichelte Linie die Anwesenheit oder Abwesenheit einer Bindung darstellt, oder ein durch die Formel ...
Claims (20)
- Verbindung der Formel (I): wobei RC und RD zusammen genommen mit den angrenzenden Kohlenstoffatomen einen Ring bilden, der kondensiert sein kann, Y Hydroxy ist; Z O ist; RA ein durch die Formel dargestellter Rest ist, wobei der Ring C ein aromatischer Heterocyclus ist, der N enthält, wobei mindestens ein Atom, angrenzend an das Atom an der Bindestelle, ein nicht substituiertes N-Atom ist; wobei die gestrichelte Linie die Anwesenheit oder Abwesenheit einer Bindung darstellt, oder ein durch die Formel dargestellter Rest ist, wobei X O ist; RB ein aus der Substitutionsgruppe A ausgewählter Substituent ist; mindestens eines von dem von RC und RD gebildeten Ring, Ring C und RB mit einem Rest -Z1-Z2-Z3-R1 substituiert ist, wobei Z1 und Z3 jeweils unabhängig eine Bindung, gegebenenfalls substituiertes Alkylen oder gegebenenfalls substituiertes Alkenylen sind; Z2 eine Bindung, gegebenenfalls substituiertes Alkylen, gegebenenfalls substituiertes Alkenylen, -CH(OH)-, -S-, -SO-, -SO2-, -SO2NR2-, -NR2SO2-, -O-, -NR2-, -NR2CO-, -CONR2-, -C(=O)-O-, -O-C(=O)- oder -CO- ist; R2 Wasserstoff, gegebenenfalls substituiertes Alkyl, gegebenenfalls substituiertes Alkenyl, gegebenenfalls substituiertes Aryl oder gegebenenfalls substituiertes Heteroaryl ist; R1 gegebenenfalls substituiertes Aryl, gegebenenfalls substituiertes Heteroaryl, gegebenenfalls substituiertes Cycloalkyl, gegebenenfalls substituiertes Cycloalkenyl oder gegebenenfalls substituierter Heterocyclus ist, wobei der von RC und RD gebildete Ring, der Ring C oder RB gegebenenfalls mit einem nicht interferierenden Substituenten substituiert ist an einer Position, an der sich der Rest -Z1-Z2-Z3-R1 nicht befindet (wobei Z1, Z2, Z3 und R1 wie vorstehend definiert sind); die Substitutionsgruppe A aus Alkyl, Alkoxy, Hydroxy, gegebenenfalls substituiertem Amino, gegebenenfalls substituiertem Cycloalkyl, gegebenenfalls substituiertem Cycloalkenyl, gegebenenfalls substituiertem Heterocyclus, gegebenenfalls substituiertem Aryl oder gegebenenfalls substituiertem Heteroaryl besteht, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 1, wobei der von RC und RD gebildete Ring ein 5- bis 6-gliedriger Ring ist, der (ein) Heteroatom(e) enthalten kann und damit kondensiert sein kann, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 2, wobei der von RC und RD gebildete Ring ein 5- bis 6-gliedriger Ring ist, der (ein) Heteroatom(e) O und/oder N enthalten kann und mit einem Benzolring kondensiert ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 3, wobei der von RC und RD gebildete Ring ein 6-gliedriger Ring ist, der (ein) Heteroatom(e) N enthält und mit einem Benzolring kondensiert ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 3, wobei der von RC und RD gebildete Ring ein 6-gliedriger Ring ist, der (ein) Heteroatom(e) N enthält, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach einem der Ansprüche 1 bis 5, wobei die nicht interferierenden Substituenten unabhängig ausgewählt sind aus Wasserstoff, Halogen, Alkoxycarbonyl, Carboxy, Alkyl, Alkoxy, Alkoxyalkyl, Nitro, Hydroxy, Hydroxyalkyl, Alkenyl, Alkinyl, Alkylsufonyl, gegebenenfalls substituiertem Amino, Alkylthio, Alkylthioalkyl, Haloalkyl, Haloalkoxy, Haloalkoxyalkyl, gegebenenfalls substituiertem Cycloalkyl, gegebenenfalls substituiertem Cycloalkenyl, gegebenenfalls substituiertem Heterocyclus, Oxo, Thioxo, Nitroso, Azid, Amidino, Guanidino, Cyano, Isocyano, Mercapto, gegebenenfalls substituiertem Carbamoyl, Sulfamoyl, Sulfoamino, Formyl, Alkylcarbonyl, Alkylcarbonyloxy, Hydrazino, Morpholino, gegebenenfalls substituiertem Aryl, gegebenenfalls substituiertem Heteroaryl, gegebenenfalls substituiertem Aralkyl, gegebenenfalls substituiertem Heteroarylalkyl, gegebenenfalls substituiertem Aryloxy, gegebenenfalls substituiertem Heteroaryloxy, gegebenenfalls substituiertem Arylthio, gegebenenfalls substituiertem Heteroarylthio, gegebenenfalls substituiertem Aralkyloxy, gegebenenfalls substituiertem Heteroarylalkyloxy, gegebenenfalls substituiertem Aralkylthio, gegebenenfalls substituiertem Heteroarylalkylthio, gegebenenfalls substituiertem Aryloxyalkyl, gegebenenfalls substituiertem Heteroaryloxyalkyl, gegebenenfalls substituiertem Arylthioalkyl, gegebenenfalls substituiertem Heteroarylthioalkyl, gegebenenfalls substituiertem Arylsulfonyl, gegebenenfalls substituiertem Heteroarylsulfonyl, gegebenenfalls substituiertem Aralkylsulfonyl und gegebenenfalls substituiertem Heteroarylalkylsulfonyl, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach einem der Ansprüche 1 bis 5, wobei der nicht interferierende Substituent an dem von RC und RD gebildete Ring ausgewählt ist aus Wasserstoff, Halogen, Alkyl, Aralkyl, Cycloalkyl, gegebenenfalls substituiertem Aryl, Alkoxy, Alkoxyalkyl, gegebenenfalls substituiertem Amino, Hydroxyalkyl, Alkenyl, Alkoxycarbonylalkyl, Heteroarylalkyl oder Hydroxy; und der nicht interferierende Substituent an RB ausgewählt ist aus Halogen, Alkyl, Aralkyl, Cycloalkyl, gegebenenfalls substituiertem Aryl, Alkoxy, Alkoxyalkyl, gegebenenfalls substituiertem Amino, Hydroxyalkyl, Alkenyl, Alkoxycarbonylalkyl, Heteroarylakyl oder Hydroxy, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach einem der Ansprüche 1 bis 7, wobei Z1 eine Bindung oder Alkylen ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach einem der Ansprüche 1 bis 8, wobei Z3 eine Bindung oder Alkylen ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach einem der Ansprüche 1 bis 9, wobei Z1, Z2 und Z3 nicht gleichzeitig Bindungen sind, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach einem der Ansprüche 1 bis 10, wobei R1 gegebenenfalls substituiertes Cycloalkyl, gegebenenfalls substituiertes Aryl oder gegebenenfalls substituiertes Heteroaryl ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 11, wobei R1 gegebenenfalls substituiertes Cycloalkyl ausgewählt aus C3- bis C6-Cycloalkyl, gegebenenfalls substituiertes Aryl ausgewählt aus Phenyl oder Naphthyl, oder gegebenenfalls substituiertes Heteroaryl ausgewählt aus monocyclischem aromatischen heterocyclischem Rest oder kondensiertem aromatischen heterocyclischem Rest ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 12, wobei gegebenenfalls substituiertes Heteroaryl ein monocyclischer aromatischer heterocyclischer Rest ist.
- Verbindung nach einem der Ansprüche 11 bis 13, wobei der Substituent von gegebenenfalls substituiertem Cycloalkyl, gegebenenfalls substituiertem Aryl und gegebenenfalls substituiertem Heteroaryl ausgewählt ist aus Alkyl, Haloalkyl, Halogen oder Alkoxy, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach einem der Ansprüche 1 bis 14, wobei der Ring C Imidazol-2-yl, Imidazol-4-yl, Pyrazol-3-yl, Triazol-3-yl, Tetrazol-5-yl, Oxazol-2-yl, Oxazol-4-yl, Isoxaxol-3-yl, Thiazol-2-yl, Thiazol-4-yl, 1,3,4-Thiadiazol-2-yl, 1,2,4-Thiadiazol-5-yl, 1,2,4-Thiadiazol-3-yl, 1,3,4-Oxadiazol-2-yl, 1,2,4-Oxadiazol-5-yl, 1,2,4-Oxadiazol-3-yl, Isothiazol-3-yl, Pyridin-2-yl, Pyridazin-3-yl, Pyradin-2-yl, Pyrimidin-2-yl, Pyrimidin-4-yl oder Furazan-3-yl ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 15, wobei der Ring C Pyridin-2-yl, Pyrimidin-2-yl, 1,3,4-Oxadiazol-2-yl, 1,2,4-Triazol-3-yl, oder Imidazol-2-yl ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung der Formel (I): wobei RC und RD zusammen genommen mit den angrenzenden Kohlenstoffatomen einen 5- bis 6-gliedrigen Heterocylus bilden, der (ein) Atom(e) N und/oder O enthalten kann und mit einem Benzolring kondensiert sein kann; Y Hydroxy, Mercapto oder Amino ist; Z O, S oder NH ist; RA ein durch die Formel dargestellter Rest ist, wobei der Ring C ein aromatischer Heterocyclus ist, der N enthält, wobei mindestens ein Atom, angrenzend an das Atom an der Bindestelle, ein nicht substituiertes N-Atom ist; die gestrichelte Linie die Anwesenheit oder Abwesenheit einer Bindung darstellt, oder ein durch die Formel dargestellter Rest ist, wobei X O, S oder NH ist; RB Alkyl, Alkoxy, Hydroxy, gegebenenfalls substituiertes Amino, gegebenenfalls substituiertes Aryl, gegebenenfalls substituiertes Heteroaryl, gegebenenfalls substituiertes Cycloalkyl, gegebenenfalls substituiertes Cycloalkenyl oder gegebenenfalls substituierter Heterocyclus ist; mindestens eines von dem von RC und RD gebildeten Ring, Ring C und RB mit einem Rest der Formel -Z1-Z2-Z3-R1 substituiert ist, wobei Z1 und Z3 jeweils unabhängig eine Bindung, gegebenenfalls substituiertes Alkylen oder gegebenenfalls substituiertes Alkenylen sind; Z2 eine Bindung, gegebenenfalls substituiertes Alkylen, gegebenenfalls substituiertes Alkenylen, -CH(OH)-, -S-, -SO-, -SO2-, -SO2N(R2)-, -N(R2)SO2-, -O-, -N(R2)-, -N(R2)CO-, -CON(R2)-, -C(=O)-O-, -O-C(=O) oder -CO- ist; R2 Wasserstoff, gegebenenfalls substituiertes Alkyl, gegebenenfalls substituiertes Alkenyl, gegebenenfalls substituiertes Aryl oder gegebenenfalls substituiertes Heteroaryl ist; R1 gegebenenfalls substituiertes Aryl, gegebenenfalls substituiertes Heteroaryl, gegebenenfalls substituiertes Cycloalkyl, gegebenenfalls substituiertes Cycloalkenyl oder gegebenenfalls substituierter Heterocyclus ist; und der von RC und RD gebildete Ring, der Ring C oder RB gegebenenfalls mit 1 bis 3 Substituenten substituiert ist ausgewählt aus Wasserstoff, Alkyl, Aralkyl, Cycloalkyl, gegebenenfalls substituiertem Aryl, Alkoxy, Alkoxyalkyl, gegebenenfalls substituiertem Amino, Hydroxyalkyl, Alkenyl, Alkoxycarbonylalkyl, Heteroarylalkyl und Hydroxy, an einer Position, an der sich die obige Formel -Z1-Z2-Z3-R1 nicht befindet (wobei Z1, Z2, Z3 und R1 wie vorstehend definiert sind), oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 17, wobei der von RC und RD gebildete Ring ein 5-oder 6-gliedriger Heterocylcus ist, der ein O- und/oder N-Atom enthalten kann und mit einem Benzolring kondensiert sein kann; Y Hydroxy ist; Z O ist; X O ist; der von RC und RD gebildete Ring gegebenenfalls mit 1 bis 3 Substituenten substituiert ist ausgewählt aus Wasserstoff, Alkyl, Aralkyl, Cycloalkyl, gegebenenfalls substituiertem Aryl, Alkoxy, Alkoxyalkyl, gegebenenfalls substituiertem Amino, Hydroxyalkyl, Alkenyl, Alkoxycaronylalkyl und Heteroarylalkyl, und der Ring C und RB gegebenenfalls mit 1 bis 3 Substituenten substituiert ist ausgewählt aus Alkyl, Amino, Halogen und Hydroxy, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 17 oder 18, wobei mindestens eines von der von RC und RD gebildete Ring, der Ring C und RB mit einem Rest der Formel -Z1-Z2-Z3-R1 substituiert ist, wobei Z1 eine Bindung oder Alkylen ist; Z2 Alkylen oder -O- ist; Z3 eine Bindung oder Alkylen ist; R1 gegebenenfalls substituiertes Aryl oder gegebenenfalls substituiertes Heteroaryl ist, oder ein pharmazeutisch verträgliches Salz oder Solvat davon.
- Verbindung nach Anspruch 1 bis 19 oder ein pharmazeutisch verträgliches Salz oder Solvat davon zur Verwendung als HIV-Integrase-Inhibitor.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2001245071 | 2001-08-10 | ||
JP2001245071 | 2001-08-10 | ||
JP2001370860 | 2001-12-05 | ||
JP2001370860 | 2001-12-05 | ||
JP2002191483 | 2002-06-28 | ||
JP2002191483 | 2002-06-28 | ||
EP15187654.7A EP3042894A1 (de) | 2001-08-10 | 2002-08-08 | Antivirales mittel |
Publications (1)
Publication Number | Publication Date |
---|---|
DE15187654T1 true DE15187654T1 (de) | 2016-12-01 |
Family
ID=27347328
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE15187654.7T Pending DE15187654T1 (de) | 2001-08-10 | 2002-08-08 | Antivirales Mittel |
DE10178132.6T Pending DE10178132T1 (de) | 2001-08-10 | 2002-08-08 | Antivirales Mittel |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE10178132.6T Pending DE10178132T1 (de) | 2001-08-10 | 2002-08-08 | Antivirales Mittel |
Country Status (16)
Country | Link |
---|---|
US (3) | US20040229909A1 (de) |
EP (4) | EP1422218B1 (de) |
JP (3) | JP4338192B2 (de) |
KR (2) | KR20100087209A (de) |
CN (2) | CN100491349C (de) |
AT (2) | ATE550320T1 (de) |
BR (1) | BR0211750A (de) |
CA (1) | CA2452769C (de) |
CY (2) | CY20162200001T2 (de) |
DE (2) | DE15187654T1 (de) |
DK (2) | DK3042894T1 (de) |
ES (3) | ES2587564T1 (de) |
MX (1) | MXPA04000646A (de) |
PT (1) | PT2266958T (de) |
TW (1) | TWI327137B (de) |
WO (1) | WO2003016275A1 (de) |
Families Citing this family (134)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2587564T1 (es) | 2001-08-10 | 2016-10-25 | Shionogi & Co., Ltd. | Agente antiviral |
DK1441734T3 (da) | 2001-10-26 | 2007-06-11 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase |
IL161337A0 (en) | 2001-10-26 | 2004-09-27 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase |
WO2004004657A2 (en) | 2002-07-09 | 2004-01-15 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
KR20050087865A (ko) | 2002-12-27 | 2005-08-31 | 이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티에스.피.에이. | HIV 인테그라제 억제제로서 유용한테트라하이드로-4H-피리도[1,2-a]피리미딘 및 관련화합물 |
US7135467B2 (en) | 2003-01-13 | 2006-11-14 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
JP4607469B2 (ja) * | 2003-01-29 | 2011-01-05 | 三洋化成工業株式会社 | ウレタン樹脂及びその粉体の製造方法 |
EP1611125A1 (de) * | 2003-02-07 | 2006-01-04 | Vertex Pharmaceuticals Incorporated | Heteroaryl-substituierte pyrrole als proteinkinase-hemmer |
US20050014753A1 (en) * | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
US7037908B2 (en) | 2003-04-24 | 2006-05-02 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
TW200526635A (en) * | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
CN101014571A (zh) * | 2004-01-30 | 2007-08-08 | 默克公司 | 用作hiv整合酶抑制剂的n-苄基-3,4-二羟基吡啶-2-羧酰胺类和n-苄基-2,3-二羟基吡啶-4-羧酰胺类化合物 |
CN1930161A (zh) | 2004-03-09 | 2007-03-14 | P·安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
US7820680B2 (en) | 2004-03-09 | 2010-10-26 | Merck & Co., Inc. | HIV integrase inhibitors |
EA200601654A1 (ru) * | 2004-03-09 | 2007-02-27 | Мерк Энд Ко., Инк. | Ингибиторы интегразы вич |
US7619086B2 (en) * | 2004-03-09 | 2009-11-17 | Merck & Co., Inc. | HIV integrase inhibitors |
US7538112B2 (en) * | 2004-05-07 | 2009-05-26 | Merck & Co., Inc. | HIV integrase inhibitors |
US7115601B2 (en) * | 2004-05-18 | 2006-10-03 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
JP2008502741A (ja) * | 2004-06-09 | 2008-01-31 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害薬 |
US7550463B2 (en) | 2004-09-15 | 2009-06-23 | Shionogi & Co., Ltd. | Carbamoylpyridone derivatives having inhibitory activity against HIV integrase |
WO2006068760A2 (en) | 2004-11-19 | 2006-06-29 | The Regents Of The University Of California | Anti-inflammatory pyrazolopyrimidines |
JP5317257B2 (ja) * | 2005-02-21 | 2013-10-16 | 塩野義製薬株式会社 | Hivインテグラーゼ阻害活性を有する2環性カルバモイルピリドン誘導体 |
CN101146811B (zh) | 2005-03-31 | 2012-01-11 | P.安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
LT3284520T (lt) | 2005-04-28 | 2019-09-25 | Viiv Healthcare Company | Policiklinis karbamoilpiridono darinys, turintis živ integrazę slopinantį poveikį |
US7741315B2 (en) * | 2005-05-10 | 2010-06-22 | Merck Sharp & Dohme Corp. | HIV integrase inhibitors |
JP2006342115A (ja) * | 2005-06-10 | 2006-12-21 | Shionogi & Co Ltd | Hivインテグラーゼ阻害活性を有する多環性化合物 |
US7939537B2 (en) * | 2005-10-04 | 2011-05-10 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | HIV integrase inhibitors |
KR20080064182A (ko) | 2005-10-27 | 2008-07-08 | 시오노기세야쿠 가부시키가이샤 | Hiv 인테그라아제 억제활성을 가지는 다환성카르바모일피리돈 유도체 |
WO2007054105A2 (en) * | 2005-11-14 | 2007-05-18 | H. Lundbeck A/S | Method for the preparation of escitalopram |
MX2008012928A (es) | 2006-04-04 | 2009-03-06 | Univ California | Antagonistas de pi3-cinasa. |
US20100056516A1 (en) * | 2006-07-17 | 2010-03-04 | Williams Peter D | 1-hydroxy naphthyridine compounds as anti-hiv agents |
US20110130397A1 (en) * | 2006-09-22 | 2011-06-02 | Soongyu Choi | Pyrrolinone compounds as inhibitors of bacterial peptidyl trna hydrolase and uses thereof |
AU2007313293A1 (en) * | 2006-10-18 | 2008-04-24 | Merck & Co., Inc. | HIV integrase inhibitors |
WO2009046448A1 (en) | 2007-10-04 | 2009-04-09 | Intellikine, Inc. | Chemical entities and therapeutic uses thereof |
CN104926815B (zh) | 2008-01-04 | 2017-11-03 | 英特利凯恩有限责任公司 | 某些化学实体、组合物和方法 |
US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
EP2095819A1 (de) * | 2008-02-28 | 2009-09-02 | Maastricht University | N-Benzyl-Imidazolderivate und deren Verwendung als Aldosteronsynthaseinhibitoren |
US8993580B2 (en) | 2008-03-14 | 2015-03-31 | Intellikine Llc | Benzothiazole kinase inhibitors and methods of use |
JP5547099B2 (ja) | 2008-03-14 | 2014-07-09 | インテリカイン, エルエルシー | キナーゼ阻害剤および使用方法 |
DE102008028905A1 (de) | 2008-06-18 | 2009-12-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate |
WO2010000030A1 (en) | 2008-07-02 | 2010-01-07 | Avexa Limited | Thiazopyrimidinones and uses thereof |
CA2729663A1 (en) | 2008-07-02 | 2010-01-07 | Avexa Limited | Compounds having antiviral properties |
CA2729656A1 (en) * | 2008-07-02 | 2010-01-07 | Avexa Limited | Imidazopyrimidinones and uses thereof |
BRPI0915231A2 (pt) | 2008-07-08 | 2018-06-12 | Intellikine Inc | compostos inibidores de quinase e métodos de uso |
US20110224223A1 (en) | 2008-07-08 | 2011-09-15 | The Regents Of The University Of California, A California Corporation | MTOR Modulators and Uses Thereof |
US20100041653A1 (en) * | 2008-08-15 | 2010-02-18 | Burnham Institute For Medical Research | Composition and methods for the design and development of metallo-enzyme inhibitors |
WO2010036380A1 (en) | 2008-09-26 | 2010-04-01 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
BRPI0920605A8 (pt) * | 2008-10-06 | 2016-04-26 | Merck Sharp & Dohme | Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, método para o tratamento ou profilaxia de infecção pelo hiv ou para o tratamento, profilaxia, ou retardo no início ou progressão da aids em um paciente em necessidade deste. |
US8697709B2 (en) | 2008-10-16 | 2014-04-15 | The Regents Of The University Of California | Fused ring heteroaryl kinase inhibitors |
US8476282B2 (en) | 2008-11-03 | 2013-07-02 | Intellikine Llc | Benzoxazole kinase inhibitors and methods of use |
EP2427195B1 (de) | 2009-05-07 | 2019-05-01 | Intellikine, LLC | Heterocyclische verbindungen und ihre verwendung |
JP2012532849A (ja) * | 2009-07-10 | 2012-12-20 | ビバリス | C型肝炎ns5bポリメラーゼの阻害剤としての1−(6員アゾ複素環式)−ピロリン−2−オン化合物、その医薬組成物、およびそれらの治療上の使用 |
US8980899B2 (en) | 2009-10-16 | 2015-03-17 | The Regents Of The University Of California | Methods of inhibiting Ire1 |
JP5766690B2 (ja) | 2010-04-12 | 2015-08-19 | 塩野義製薬株式会社 | インテグラーゼ阻害活性を有するピリドン誘導体 |
CN103002738A (zh) | 2010-05-21 | 2013-03-27 | 英特利凯恩有限责任公司 | 用于激酶调节的化学化合物、组合物和方法 |
CN101967209B (zh) * | 2010-10-20 | 2012-11-07 | 南京大学 | 一种n-乙酰基乙二胺螯合树脂及其制备方法 |
AU2011326427B2 (en) | 2010-11-10 | 2016-01-07 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
GB201020076D0 (en) * | 2010-11-26 | 2011-01-12 | Liverpool School Tropical Medicine | Antimalarial compounds |
BR112013017670B1 (pt) | 2011-01-10 | 2022-07-19 | Infinity Pharmaceuticals, Inc | Processos de preparação de isoquinolinonas e formas sólidas de isoquinolinonas |
WO2012148540A1 (en) | 2011-02-23 | 2012-11-01 | Intellikine, Llc | Combination of kanase inhibitors and uses threof |
AR088218A1 (es) | 2011-07-19 | 2014-05-21 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos utiles como inhibidores de pi3k |
WO2013012915A1 (en) | 2011-07-19 | 2013-01-24 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
CA2846431A1 (en) | 2011-08-29 | 2013-03-07 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
WO2013077921A2 (en) | 2011-09-02 | 2013-05-30 | The Regents Of The University Of California | Substituted pyrazolo[3,4-d]pyrimidines and uses thereof |
WO2013048982A1 (en) | 2011-09-27 | 2013-04-04 | Bristol-Myers Squibb Company | Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors |
EP2760828B1 (de) | 2011-09-27 | 2015-10-21 | Bristol-Myers Squibb Company | Als endothellipasehemmer verwendbare pyrrolinoncarboxamidverbindungen |
WO2013048928A1 (en) | 2011-09-27 | 2013-04-04 | Bristol-Myers Squibb Company | Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors |
AU2012321762A1 (en) | 2011-10-12 | 2014-04-17 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative having integrase-inhibiting activity |
WO2013068875A1 (en) | 2011-11-11 | 2013-05-16 | Pfizer Inc. | 2-thiopyrimidinones |
US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
JP6183053B2 (ja) * | 2012-08-22 | 2017-08-23 | 宇部興産株式会社 | テトラヒドロピラニルピリミジン化合物の製造方法 |
RU2015115631A (ru) | 2012-09-26 | 2016-11-20 | Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния | Модулирование ire1 |
US9714243B2 (en) | 2012-12-17 | 2017-07-25 | Merck Sharp & Dohme Corp. | 4-pyridinonetriazine derivatives as HIV integrase inhibitors |
PT3608325T (pt) | 2012-12-21 | 2022-10-17 | Gilead Sciences Inc | Compostos carbamoílpiridona policíclicos e sua utilização farmacêutica |
US9481667B2 (en) | 2013-03-15 | 2016-11-01 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
CN103172581A (zh) * | 2013-04-07 | 2013-06-26 | 杨国成 | 一种5-氨基-3-巯基-1,2,4-三氮唑晶体及其制备方法 |
EP2986291B1 (de) | 2013-04-16 | 2020-05-27 | Merck Sharp & Dohme Corp. | 4-pyridonderivatverbindungen und verwendungen davon als hiv-integrase-hemmer |
GB201308217D0 (en) | 2013-05-08 | 2013-06-12 | Ucl Business Plc | Compounds and their use in therapy |
CN104148018B (zh) * | 2013-05-14 | 2018-04-20 | 上海亨臻实业有限公司 | 抗体亲和纯化材料及其用途 |
ME02977B (de) | 2013-05-17 | 2018-10-20 | Merck Sharp & Dohme | Kondensierte tricyclische heterocyclische verbindungen als hiv-integrase-hemmer |
US9951079B2 (en) | 2013-06-13 | 2018-04-24 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as HIV integrase inhibitors |
NO2865735T3 (de) | 2013-07-12 | 2018-07-21 | ||
PT3019503T (pt) | 2013-07-12 | 2017-11-27 | Gilead Sciences Inc | Compostos carbamoílpiridona- policíclicos e seu uso para o tratamento de infecções por hiv |
WO2015048363A1 (en) | 2013-09-27 | 2015-04-02 | Merck Sharp & Dohme Corp. | Substituted quinolizine derivatives useful as hiv integrase inhibitors |
US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
MY175778A (en) | 2013-10-04 | 2020-07-08 | Infinity Pharmaceuticals Inc | Heterocyclic compounds and uses thereof |
WO2015117094A1 (en) * | 2014-02-03 | 2015-08-06 | American Life Science Pharmaceuticals, Inc. | Compositions and methods for synthesizing (2s,3s)-trans-epoxysuccinyl-l-leucyl-amido-3-methylbutane ethyl ester |
CN106456628A (zh) | 2014-03-19 | 2017-02-22 | 无限药品股份有限公司 | 用于治疗PI3K‑γ介导的障碍的杂环化合物 |
WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
NO2717902T3 (de) | 2014-06-20 | 2018-06-23 | ||
TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
US10065930B2 (en) | 2014-08-06 | 2018-09-04 | Eisai R&D Management Co., Ltd. | Method for producing pyrimidine-1-ol compound, and intermediate thereof |
WO2016027879A1 (ja) | 2014-08-22 | 2016-02-25 | 塩野義製薬株式会社 | インテグラーゼ阻害活性を有する多環性ピリドン誘導体 |
WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
PL3277691T3 (pl) | 2015-04-02 | 2019-07-31 | Gilead Sciences, Inc. | Policykliczne związki karbamoilopirydonowe i ich zastosowanie farmaceutyczne |
CR20170498A (es) | 2015-05-05 | 2018-01-26 | Pfizer | 2-tiopirimidinonas |
WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
WO2017048702A1 (en) | 2015-09-14 | 2017-03-23 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same |
CN105237406A (zh) * | 2015-10-14 | 2016-01-13 | 湖南华腾制药有限公司 | (r)-(-)-1-甲基-3-***的合成方法 |
US10611747B2 (en) | 2015-11-09 | 2020-04-07 | Forge Therapeutics, Inc. | Pyrone based compounds for treating bacterial infections |
EP3374350B1 (de) | 2015-11-09 | 2022-01-05 | Forge Therapeutics, Inc. | Hydroxypyridinon- und hydroxypyrimidinon-basierte verbindungen zur behandlung von bakteriellen infektionen |
WO2017087257A1 (en) | 2015-11-17 | 2017-05-26 | Merck Sharp & Dohme Corp. | Amido-substituted pyridotriazine derivatives useful as hiv integrase inhibitors |
EP3389380B1 (de) | 2015-12-15 | 2021-07-21 | Merck Sharp & Dohme Corp. | Spirocyclische chinolizinderivate zur verwendung als hiv-integrase-inhibitoren |
WO2017113288A1 (en) | 2015-12-31 | 2017-07-06 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
WO2017153919A1 (en) | 2016-03-08 | 2017-09-14 | Novartis Ag | Tricyclic compounds useful to treat orthomyxovirus infections |
US10759806B2 (en) | 2016-03-17 | 2020-09-01 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors |
WO2017190050A1 (en) * | 2016-04-28 | 2017-11-02 | Cornell University | Inhibitors of soluble adenylyl cyclase |
US10919914B2 (en) | 2016-06-08 | 2021-02-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
MX2018016227A (es) | 2016-06-24 | 2019-07-08 | Infinity Pharmaceuticals Inc | Terapias de combinacion. |
CN107773562B (zh) * | 2016-08-25 | 2020-04-07 | 清华大学 | 化合物在抗登革和寨卡病毒感染中的应用 |
JOP20170169A1 (ar) | 2016-08-29 | 2019-01-30 | Novartis Ag | مركبات بيريدازين ثلاثية الحلقة مندمجة تفيد في علاج العدوى بفيروس أورثوميكسو |
JOP20190130A1 (ar) | 2016-12-02 | 2019-06-02 | Merck Sharp & Dohme | مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv) |
RU2749043C2 (ru) | 2016-12-02 | 2021-06-03 | Мерк Шарп И Доум Корп. | Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич |
CN106810458B (zh) * | 2016-12-31 | 2019-05-03 | 武汉工程大学 | 一种拆分dl-2-氨基丙醇制备l-2-氨基丙醇的方法 |
EP3573984A4 (de) | 2017-01-26 | 2020-07-29 | Merck Sharp & Dohme Corp. | Als hiv-integrase-inhibitoren nützliche, substituierte chinolizinderivate |
CN110431224A (zh) * | 2017-03-13 | 2019-11-08 | 帝斯曼知识产权资产管理有限公司 | 锌双核簇转录调控因子缺陷型菌株 |
WO2018166855A1 (en) | 2017-03-16 | 2018-09-20 | Basf Se | Heterobicyclic substituted dihydroisoxazoles |
US11021471B2 (en) * | 2017-05-10 | 2021-06-01 | Forge Therapeutics, Inc. | Antibacterial compounds |
MX2020002944A (es) | 2017-09-14 | 2020-09-28 | Daiichi Sankyo Co Ltd | Compuesto que tiene estructura ciclica. |
EP3759113A1 (de) | 2018-02-28 | 2021-01-06 | Novartis AG | 10-(diphenyl)methyl)-4-hydroxy-8,9,9a,10-tetrahydro-7h-pyrrolo [1',2':4,5] pyrazino[1,2-b] pyridazin-3,5-dionderivate und verwandte verbindungen als inhibitoren der orthomyxovirus-replikation zur behandlung von influenza |
CN108658784B (zh) * | 2018-04-26 | 2020-12-18 | 联化科技股份有限公司 | (r)-1-(4-甲基苯基)乙胺的合成方法 |
JP7495395B2 (ja) | 2018-09-20 | 2024-06-04 | ブラックスミス メディシンズ,インク. | 抗菌性化合物 |
UA127747C2 (uk) | 2018-10-23 | 2023-12-20 | Басф Се | Трициклічні пестицидні сполуки |
WO2020132820A1 (zh) * | 2018-12-24 | 2020-07-02 | 广东莱佛士制药技术有限公司 | 一种3-(苄氧基)-4-氧代-4h-吡喃-2-羧酸的合成方法 |
RU2717101C1 (ru) | 2019-06-03 | 2020-03-18 | Андрей Александрович Иващенко | Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2Н-пиридо[1,2-a]пиразин-7-карбоксамиды - ингибиторы интегразы ВИЧ, способы их получения и применения |
US20200398978A1 (en) | 2019-06-20 | 2020-12-24 | Bell Helicopter Textron Inc. | Low-drag rotor blade extension |
CN110563943A (zh) * | 2019-09-09 | 2019-12-13 | 中国科学院长春应用化学研究所 | 一种生物基聚合物及其制备方法 |
WO2021195260A1 (en) | 2020-03-25 | 2021-09-30 | Forge Therapeutics, Inc. | Lpxc inhibitor and methods of making |
CN115427408A (zh) | 2020-04-14 | 2022-12-02 | 巴斯夫欧洲公司 | 杀害虫的三环化合物 |
KR20230074174A (ko) | 2020-09-21 | 2023-05-26 | 란도스 바이오파마, 인크. | Nlrx1 리간드 |
Family Cites Families (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3244725A (en) | 1964-09-21 | 1966-04-05 | Taub William | 4, 5-diacyl-3-hydroxy-3-pyrrolin-2-ones |
US4298743A (en) * | 1979-09-11 | 1981-11-03 | Merck & Co., Inc. | 4-(Substituted phenyl thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones |
DE3820176A1 (de) | 1987-12-18 | 1989-06-29 | Bayer Ag | Verfahren zur herstellung von phosphorsaeurederivaten und zwischenprodukten |
WO1992002523A1 (en) | 1990-08-02 | 1992-02-20 | Sankei Pharmaceutical Company Limited | Novel cephalosporin compound |
WO1992006954A2 (en) | 1990-10-15 | 1992-04-30 | Pfizer Inc. | Pyrrolidine dione derivatives |
JPH06100445A (ja) * | 1992-07-06 | 1994-04-12 | Banyu Pharmaceut Co Ltd | 抗腫瘍剤 |
JPH06100405A (ja) * | 1992-08-07 | 1994-04-12 | Yoshitomi Pharmaceut Ind Ltd | 水中防汚剤 |
WO1998011876A1 (de) | 1996-09-18 | 1998-03-26 | Marigen S.A. | Bioflavonol-glykosid-perester und ihre aufarbeitung zu pharmakologisch wirksamen konzentraten und ultramikroemulsionen |
CA2326166A1 (en) | 1998-03-26 | 1999-10-07 | Shionogi & Co., Ltd. | Indole derivatives with antiviral activity |
EP1082121A4 (de) | 1998-06-03 | 2003-02-05 | Merck & Co Inc | Hiv-integraseinhibitoren |
EP1083897A4 (de) | 1998-06-03 | 2003-01-02 | Merck & Co Inc | Hiv integrase-inhibitoren |
JP2002517390A (ja) | 1998-06-03 | 2002-06-18 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害薬 |
US6610692B1 (en) | 1998-10-30 | 2003-08-26 | Merck & Co., Inc. | Thrombin inhibitors |
GB2345058A (en) | 1998-12-01 | 2000-06-28 | Cerebrus Pharm Ltd | Hydroxypyridone compounds useful in the treatment of oxidative damage to the central nervous system |
ATE411286T1 (de) | 1998-12-25 | 2008-10-15 | Shionogi & Co | Aromatische heterocyclen mit hiv integrase inhibierenden eigenschaften |
AU5880600A (en) | 1999-06-25 | 2001-01-31 | Merck & Co., Inc. | 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof |
AU6731100A (en) | 1999-09-02 | 2001-04-10 | Shionogi & Co., Ltd. | Integrase inhibitors containing aromatic heterocycle derivatives |
JP2001270884A (ja) | 2000-03-23 | 2001-10-02 | Mitsubishi-Tokyo Pharmaceuticals Inc | ピリミドン誘導体 |
US20040039060A1 (en) * | 2000-06-14 | 2004-02-26 | Ryuichi Kiyama | Inhibitor for enzyme having two divalent metal ions as active centers |
WO2002036734A2 (en) | 2000-10-12 | 2002-05-10 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors |
ATE430745T1 (de) | 2000-10-12 | 2009-05-15 | Merck & Co Inc | Aza- und polyaza naphthalenyl karboxamide als inhibitoren der hiv-integrase |
AU1532802A (en) | 2000-10-12 | 2002-04-22 | Merck & Co Inc | Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors |
KR20030078958A (ko) | 2001-03-01 | 2003-10-08 | 시오노기세이야쿠가부시키가이샤 | Hiv 인테그라제 저해 활성을 갖는 질소 함유의헤테로아릴 화합물 |
JP4176477B2 (ja) | 2001-03-01 | 2008-11-05 | 塩野義製薬株式会社 | Hivインテグラーゼ阻害活性を有する含窒素芳香族複素環誘導体 |
ES2587564T1 (es) | 2001-08-10 | 2016-10-25 | Shionogi & Co., Ltd. | Agente antiviral |
WO2003030897A1 (en) * | 2001-10-03 | 2003-04-17 | Ucb, S.A. | Pyrrolidinone derivatives |
IL161337A0 (en) | 2001-10-26 | 2004-09-27 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase |
DK1441734T3 (da) | 2001-10-26 | 2007-06-11 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase |
WO2004004657A2 (en) | 2002-07-09 | 2004-01-15 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
TW200526635A (en) * | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
CN101014571A (zh) | 2004-01-30 | 2007-08-08 | 默克公司 | 用作hiv整合酶抑制剂的n-苄基-3,4-二羟基吡啶-2-羧酰胺类和n-苄基-2,3-二羟基吡啶-4-羧酰胺类化合物 |
US9328075B2 (en) | 2011-05-05 | 2016-05-03 | St. Jude Children's Research Hospital | Pyrimidinone compounds and methods for treating influenza |
-
2002
- 2002-08-08 ES ES15187654.7T patent/ES2587564T1/es active Pending
- 2002-08-08 ES ES10178132.6T patent/ES2572030T3/es not_active Expired - Lifetime
- 2002-08-08 EP EP02749384A patent/EP1422218B1/de not_active Revoked
- 2002-08-08 CN CNB028198697A patent/CN100491349C/zh not_active Expired - Fee Related
- 2002-08-08 DE DE15187654.7T patent/DE15187654T1/de active Pending
- 2002-08-08 CN CN2009101282803A patent/CN101513402B/zh not_active Expired - Fee Related
- 2002-08-08 EP EP09177978A patent/EP2181985B1/de not_active Expired - Lifetime
- 2002-08-08 KR KR1020107012655A patent/KR20100087209A/ko not_active Application Discontinuation
- 2002-08-08 EP EP10178132.6A patent/EP2266958B1/de not_active Revoked
- 2002-08-08 AT AT02749384T patent/ATE550320T1/de active
- 2002-08-08 MX MXPA04000646A patent/MXPA04000646A/es active IP Right Grant
- 2002-08-08 US US10/485,394 patent/US20040229909A1/en not_active Abandoned
- 2002-08-08 PT PT101781326T patent/PT2266958T/pt unknown
- 2002-08-08 DK DK15187654.7T patent/DK3042894T1/da unknown
- 2002-08-08 KR KR1020047002062A patent/KR100977701B1/ko active IP Right Grant
- 2002-08-08 ES ES02749384T patent/ES2383262T3/es not_active Expired - Lifetime
- 2002-08-08 JP JP2003521202A patent/JP4338192B2/ja not_active Expired - Fee Related
- 2002-08-08 WO PCT/JP2002/008108 patent/WO2003016275A1/ja active Application Filing
- 2002-08-08 DK DK10178132.6T patent/DK2266958T1/da unknown
- 2002-08-08 DE DE10178132.6T patent/DE10178132T1/de active Pending
- 2002-08-08 BR BR0211750-9A patent/BR0211750A/pt not_active Application Discontinuation
- 2002-08-08 AT AT09177978T patent/ATE530520T1/de not_active IP Right Cessation
- 2002-08-08 CA CA2452769A patent/CA2452769C/en not_active Expired - Fee Related
- 2002-08-08 EP EP15187654.7A patent/EP3042894A1/de not_active Withdrawn
- 2002-08-09 TW TW091117986A patent/TWI327137B/zh not_active IP Right Cessation
-
2009
- 2009-03-11 JP JP2009057635A patent/JP5207392B2/ja not_active Expired - Lifetime
-
2012
- 2012-08-09 JP JP2012176768A patent/JP2012236852A/ja active Pending
-
2015
- 2015-01-23 US US14/603,979 patent/US9572813B2/en not_active Expired - Fee Related
-
2016
- 2016-05-10 CY CY20162200001T patent/CY20162200001T2/el unknown
- 2016-11-18 US US15/356,343 patent/US20170066754A1/en not_active Abandoned
- 2016-11-25 CY CY20162200002T patent/CY20162200002T2/el unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
DE15187654T1 (de) | Antivirales Mittel | |
CA2484159A1 (en) | Heteroaryl substituted spirocyclic sulfamides for inhibition of gamma secretase | |
Das et al. | Recent developments of 2-aminothiazoles in medicinal chemistry | |
T Chhabria et al. | Thiazole: A review on chemistry, synthesis and therapeutic importance of its derivatives | |
US8492545B2 (en) | Aminothiazole compounds as kinase inhibitors and methods of using the same | |
RU2216533C2 (ru) | Новые трициклические производные (варианты), фармацевтическая композиция (варианты), способ подавления иммуной реакции или лечения и/или предупреждения аллергических заболеваний (варианты) | |
Kashyap et al. | Thiazoles: having diverse biological activities | |
RU2375363C2 (ru) | Пирролотриазиновые производные анилина, полезные в качестве ингибиторов киназы | |
Trotsko | Antitubercular properties of thiazolidin-4-ones–A review | |
JP2005511608A5 (de) | ||
JP2009530281A5 (de) | ||
JP2006517220A5 (de) | ||
RU2009115179A (ru) | Кристаллические формы соединения тиазолидиндиона и способ его получения | |
Pola | Significance of thiazole-based heterocycles for bioactive systems | |
US20040097566A1 (en) | 2-Substituted thiazolidinone and oxazolidinone derivatives for the inhibition of phosphatases and the treatment of cancer | |
CA2480880A1 (en) | Inhibitors of akt activity | |
RU2013143028A (ru) | Тиазолилфенилбензолсульфонамидопроизводные в качестве ингибиторов киназ | |
CA2657594A1 (en) | Pyrrolotriazine kinase inhibitors | |
JP2021500335A5 (de) | ||
CA2457410A1 (en) | Compounds effecting glucokinase | |
JP2007523905A5 (de) | ||
JP2006515858A5 (de) | ||
Horiuchi et al. | Discovery of novel thieno [2, 3-d] pyrimidin-4-yl hydrazone-based cyclin-dependent kinase 4 inhibitors: synthesis, biological evaluation and structure–activity relationships | |
RU2017107506A (ru) | Конденсированные 11-членные соединения и содержащие их сельскохозяйственные/садоводческие фунгициды | |
RU2015111133A (ru) | Ингибиторы тирозинкиназы брутона |