HRP20180916T1 - Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba - Google Patents
Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba Download PDFInfo
- Publication number
- HRP20180916T1 HRP20180916T1 HRP20180916TT HRP20180916T HRP20180916T1 HR P20180916 T1 HRP20180916 T1 HR P20180916T1 HR P20180916T T HRP20180916T T HR P20180916TT HR P20180916 T HRP20180916 T HR P20180916T HR P20180916 T1 HRP20180916 T1 HR P20180916T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- phenyl
- trans
- compound according
- cyclopropylamino
- Prior art date
Links
- 101000615488 Homo sapiens Methyl-CpG-binding domain protein 2 Proteins 0.000 title 1
- 102100021299 Methyl-CpG-binding domain protein 2 Human genes 0.000 title 1
- 101100334370 Schizosaccharomyces pombe (strain 972 / ATCC 24843) fas2 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 37
- 208000012902 Nervous system disease Diseases 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 208000025966 Neurological disease Diseases 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- XBBRLCXCBCZIOI-DLBZAZTESA-N vafidemstat Chemical compound O1C(N)=NN=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 XBBRLCXCBCZIOI-DLBZAZTESA-N 0.000 claims 5
- -1 C-amido Chemical group 0.000 claims 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000004202 carbamide Substances 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 150000003456 sulfonamides Chemical class 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- RAIPHJJURHTUIC-UHFFFAOYSA-N 1,3-thiazol-2-amine Chemical compound NC1=NC=CS1 RAIPHJJURHTUIC-UHFFFAOYSA-N 0.000 claims 1
- MCRPCHPLDTWWIQ-ZWKOTPCHSA-N 3-[4-[(1s,2r)-2-[(2-amino-1,3-thiazol-5-yl)methylamino]cyclopropyl]phenyl]phenol Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(O)C=CC=2)C1 MCRPCHPLDTWWIQ-ZWKOTPCHSA-N 0.000 claims 1
- LHGWKSSSHJWPDK-RBUKOAKNSA-N 3-[4-[(1s,2r)-2-[(2-aminopyrimidin-5-yl)methylamino]cyclopropyl]phenyl]phenol Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(O)C=CC=2)C1 LHGWKSSSHJWPDK-RBUKOAKNSA-N 0.000 claims 1
- QNMAQELYEAAQOX-DOTOQJQBSA-N 3-[5-[(1s,2r)-2-[(2-amino-1,3-thiazol-5-yl)methylamino]cyclopropyl]pyridin-2-yl]phenol Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=C(O)C=CC=2)C1 QNMAQELYEAAQOX-DOTOQJQBSA-N 0.000 claims 1
- HQKNDJJROYDZDO-FUHWJXTLSA-N 3-[5-[(1s,2r)-2-[(2-aminopyrimidin-5-yl)methylamino]cyclopropyl]pyridin-2-yl]phenol Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=C(O)C=CC=2)C1 HQKNDJJROYDZDO-FUHWJXTLSA-N 0.000 claims 1
- VJOTYGQWNUGGSP-DLBZAZTESA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]-1,2,4-oxadiazol-3-amine Chemical compound NC1=NOC(CN[C@H]2[C@@H](C2)C=2C=CC(OCC=3C=CC=CC=3)=CC=2)=N1 VJOTYGQWNUGGSP-DLBZAZTESA-N 0.000 claims 1
- UKYBJIFGAZGUOR-RBUKOAKNSA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]-1,3-thiazol-2-amine Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 UKYBJIFGAZGUOR-RBUKOAKNSA-N 0.000 claims 1
- HJWZUPRHNBJKHE-VQTJNVASSA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]pyrimidin-2-amine Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 HJWZUPRHNBJKHE-VQTJNVASSA-N 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 230000007419 viral reactivation Effects 0.000 claims 1
Classifications
-
- 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
- A61K31/433—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
-
- 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
- A61K31/4439—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
- A61K31/495—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
-
- 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
- A61K31/53—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
- C07D237/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
- C07D241/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
- C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
- C07D253/06—1,2,4-Triazines
- C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
- C07D253/07—1,2,4-Triazines having three 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
- C07D261/14—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
- C07D263/28—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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
- C07D263/48—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
- C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
- C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
- C07D277/38—Nitrogen atoms
- C07D277/40—Unsubstituted amino or imino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
- C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
- C07D285/135—Nitrogen atoms
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D417/12—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 chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Molecular Biology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biotechnology (AREA)
- Hospice & Palliative Care (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (29)
1. Spoj, naznačen time, da ima Formulu (I) ili njegova farmaceutski prihvatljiva sol ili njegov solvat:
u kojoj:
(A) je aril-skupina ili heteroaril-skupina, pri čemu navedena aril-skupina ili navedena heteroaril-skupina ima n supstituenata (R3);
(B) je –O-CH2-fenil ili fenil, pri čemu navedeni fenil ili dio molekule fenila obuhvaćen u navedenom –O-CH2-fenilu, ima n supstituenata (R2);
(D) je monociklička heteroaril-skupina, pri čemu navedena heteroaril-skupina ima jedan supstituent (R1), i nadalje time, da je navedena heteroaril-skupina kovalentno vezana na ostatak molekule preko prstenskog atoma ugljika;
(R1) je –NH2;
svaki (R2) je neovisno odabran od sljedećih: alkil, alkenil, alkinil, ciklil, amino, amido, C-amido, alkilamino, hidroksil, nitro, halo, haloalkil, haloalkoksi, cijano, sulfinil, sulfonil, sulfonamid, alkoksi, acil, karboksil, karbamat ili urea;
svaki (R3) je neovisno odabran od sljedećih: alkil, alkenil, alkinil, ciklil, amino, amido, C-amido, alkilamino, hidroksil, nitro, halo, haloalkil, haloalkoksi, cijano, sulfinil, sulfonil, sulfonamid, alkoksi, acil, karboksil, karbamat ili urea; i
n je neovisno 0, 1, 2, 3, ili 4.
2. Spoj prema zahtjevu 1, naznačen time, da (A) je fenil, piridinil, tiofenil, pirolil, furanil, ili tiazolil, i nadalje time, da (A) ima n supstituenata (R3).
3. Spoj prema zahtjevu 1, naznačen time, da (A) je fenil ili piridil, i nadalje time, da navedeni fenil ili navedeni piridil ima n supstituenata (R3).
4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time, da (A) ima n supstituenata (R3).
5. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time, da (B) ima 0 ili 1 supstituent (R2).
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da (D) je tiazolil, oksadiazolil, oksazolil, izoksazolil, tiadiazolil, triazinil, piridazinil, pirazinil, piridinil, ili pirimidinil, i nadalje time, da navedeni tiazolil, navedeni oksadiazolil, navedeni oksazolil, navedeni izoksazolil, navedeni tiadiazolil, navedenitriazinil, navedeni piridazinil, navedeni pirazinil, navedeni piridinil, ili navedeni pirimidinil ima jedan supstituent (R1).
7. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time, da (D) je oksadiazolil, pri čemu navedeni oksadiazolil ima jedan supstituent (R1).
8. Spoj prema bilo kojem od zahtjeva 1 do 7, naznačen time, da (R2) je neovisno odabran od hidroksila, halo ili haloalkila.
9. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time, da su supstituenti na dijelu molekule ciklopropila u trans-konfiguraciji.
10. Spoj prema zahtjevu 1, naznačen time, da je navedeni spoj odabran od sljedećih:
5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)pirimidin-2-amin;
5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)tiazol-2-amin;
5-(((trans)-2-(6-(3-trifluorometil)fenil)piridin-3-il)ciklopropilamino)metil)pirimidin-2-amin;
5-(((trans)-2-(6-(3-trifluorometil)fenil)piridin-3-il)ciklopropilamino)metil)tiazol-2-amin;
3-(5-((trans)-2-((2-aminopirimidin-5-il)metilamino)ciklopropil)piridin-2-il)fenol;
3-(5-((trans)-2-((2-aminotiazol-5-il)metilamino)ciklopropil)piridin-2-il)fenol;
4'-((trans)-2-((2-aminopirimidin-5-il)metilamino)ciklopropil)bifenil-3-ol;
4'-((trans)-2-((2-aminotiazol-5-il)metilamino)ciklopropil)bifenil-3-ol;
5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,2,4-oksadiazol-3-amin;
5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin;
ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
11. Spoj prema zahtjevu 1, naznačen time, da navedeni spoj je:
5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
12. Spoj prema bilo kojem od zahtjeva 9 do 11, naznačen time, da navedeni spoj je optički aktivan stereoizomer.
13. Spoj prema bilo kojem od zahtjeva 9 do 12, naznačen time, da navedeni spoj je (-) stereoizomer.
14. Spoj prema bilo kojem od zahtjeva 9 do 12, naznačen time, da navedeni spoj je (+) stereoizomer.
15. Spoj prema zahtjevu 1, naznačen time, da navedeni spoj je:
(-) 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
16. Farmaceutski pripravak, naznačen time, da on obuhvaća spoj prema bilo kojem od zahtjeva 1 do 15 i farmaceutski prihvatljiv nosač.
17. Spoj prema bilo kojem od zahtjeva 1 do 15, ili farmaceutski pripravak prema zahtjevu 16, naznačen time, da se upotrebljava kao lijek.
18. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji neurološke bolesti ili neurološkog poremećaja.
19. Spoj za uporabu prema zahtjevu 18, naznačen time, da navedeni spoj je:
5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
20. Spoj za uporabu prema zahtjevu 18, naznačen time, da navedeni spoj je:
(-) 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
21. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 20, naznačen time, da
je navedena neurološka bolest ili navedeni neurološki poremećaj odabrana/odabran od sljedećih: depresija, Alzheimerova bolest, Huntingtonova bolest, Parkinsonova bolest, amiotrofna lateralna skleroza, frontotemporalna demencija ili demencija s Lewy tijelima.
22. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Alzheimerova bolest.
23. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Huntingtonova bolest.
24. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Parkinsonova bolest.
25. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je amiotrofna lateralna skleroza.
26. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji raka.
27. Spoj za uporabu prema zahtjevu 26, naznačen time, da je navedeni rak odabran od sljedećih: rak prostate, rak dojke, rak pluća, kolorektalni rak, rak mozga, rak kože, rak krvi, leukemija, limfom, ili mijelom.
28. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji virusne infekcije.
29. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji virusne reaktivacije nakon latentnog stanja.
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP10171342 | 2010-07-29 | ||
EP11160738 | 2011-03-31 | ||
EP11160731 | 2011-03-31 | ||
EP11160728 | 2011-03-31 | ||
PCT/EP2011/062949 WO2012013728A1 (en) | 2010-07-29 | 2011-07-27 | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
EP11749119.1A EP2598482B1 (en) | 2010-07-29 | 2011-07-27 | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20180916T1 true HRP20180916T1 (hr) | 2018-08-10 |
Family
ID=44514682
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20180916TT HRP20180916T1 (hr) | 2010-07-29 | 2018-06-12 | Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba |
Country Status (25)
Country | Link |
---|---|
US (3) | US9181198B2 (hr) |
EP (2) | EP2598482B1 (hr) |
JP (2) | JP6054868B2 (hr) |
KR (1) | KR101866858B1 (hr) |
CN (2) | CN103124724B (hr) |
AU (1) | AU2011284688B2 (hr) |
BR (1) | BR112013002164B1 (hr) |
CA (1) | CA2806008C (hr) |
CY (1) | CY1120586T1 (hr) |
DK (1) | DK2598482T3 (hr) |
ES (1) | ES2674747T3 (hr) |
HR (1) | HRP20180916T1 (hr) |
HU (1) | HUE037937T2 (hr) |
IL (1) | IL224389A (hr) |
LT (1) | LT2598482T (hr) |
ME (1) | ME03085B (hr) |
MX (1) | MX341732B (hr) |
NO (1) | NO2598482T3 (hr) |
PL (1) | PL2598482T3 (hr) |
PT (1) | PT2598482T (hr) |
RS (1) | RS57331B1 (hr) |
RU (1) | RU2611437C2 (hr) |
SI (1) | SI2598482T1 (hr) |
TR (1) | TR201809057T4 (hr) |
WO (1) | WO2012013728A1 (hr) |
Families Citing this family (77)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010043721A1 (en) | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
US8993808B2 (en) | 2009-01-21 | 2015-03-31 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
MX338041B (es) | 2009-09-25 | 2016-03-30 | Oryzon Genomics Sa | Inhibidores de demetilasa-1 especificos de lisina y su uso. |
US8946296B2 (en) | 2009-10-09 | 2015-02-03 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use |
US9186337B2 (en) | 2010-02-24 | 2015-11-17 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae |
WO2011106574A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
ES2607081T3 (es) | 2010-04-19 | 2017-03-29 | Oryzon Genomics, S.A. | Inhibidores de desmetilasa específica de lisina-1 y su uso |
EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
LT2598482T (lt) * | 2010-07-29 | 2018-07-10 | Oryzon Genomics, S.A. | Demetilazės lsd1 inhibitoriai arilciklopropilamino pagrindu ir jų medicininis panaudojimas |
WO2012045883A1 (en) * | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
WO2012107499A1 (en) | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
WO2012107498A1 (en) | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
EP2688568B1 (en) | 2011-03-25 | 2019-06-19 | Glaxosmithkline Intellectual Property (No. 2) Limited | Cyclopropylamines as lsd1 inhibitors |
EP2741741A2 (en) | 2011-05-19 | 2014-06-18 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for inflammatory diseases or conditions |
EP2750671A2 (en) | 2011-05-19 | 2014-07-09 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
CA2849564C (en) | 2011-10-20 | 2020-10-20 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
BR112014009306B1 (pt) * | 2011-10-20 | 2021-07-20 | Oryzon Genomics S.A. | Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1 |
WO2014058071A1 (ja) * | 2012-10-12 | 2014-04-17 | 武田薬品工業株式会社 | シクロプロパンアミン化合物およびその用途 |
CN102863341B (zh) * | 2012-10-22 | 2014-05-07 | 南通大学 | 一种(1r,2s)-2-芳基环丙胺衍生物的化学合成方法 |
EP2740474A1 (en) * | 2012-12-05 | 2014-06-11 | Instituto Europeo di Oncologia S.r.l. | Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
WO2014194280A2 (en) * | 2013-05-30 | 2014-12-04 | The Board of Regents of the Nevada System of Higher Education on behalf of the University of | Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells |
DK3030323T3 (da) | 2013-08-06 | 2019-07-15 | Imago Biosciences Inc | Kdm1a-inhibitorer til behandlingen af sygdom |
TWI664164B (zh) | 2014-02-13 | 2019-07-01 | 美商英塞特控股公司 | 作為lsd1抑制劑之環丙胺 |
WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
SG10201806849WA (en) | 2014-02-13 | 2018-09-27 | Incyte Corp | Cyclopropylamines as lsd1 inhibitors |
MA39732A (fr) | 2014-04-11 | 2021-05-26 | Takeda Pharmaceuticals Co | Composé de cyclopropanamine et son utilisation |
US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
JP2017528452A (ja) | 2014-08-25 | 2017-09-28 | ユニバーシティ・オブ・キャンベラUniversity of Canberra | がん幹細胞を調節するための組成物およびその使用 |
EA039196B1 (ru) * | 2014-10-08 | 2021-12-16 | Инсайт Корпорейшн | Циклопропиламины в качестве ингибиторов lsd1 |
WO2016123387A1 (en) * | 2015-01-30 | 2016-08-04 | Genentech, Inc. | Therapeutic compounds and uses thereof |
MX2017010291A (es) | 2015-02-12 | 2017-12-07 | Imago Biosciences Inc | Inhibidores de kdm1a para el tratamiento de enfermedades. |
JP6995623B2 (ja) | 2015-04-03 | 2022-01-14 | インサイト・コーポレイション | Lsd1阻害剤としてのヘテロ環式化合物 |
EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
CA2987876A1 (en) * | 2015-06-12 | 2016-12-15 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
TWI765860B (zh) | 2015-08-12 | 2022-06-01 | 美商英塞特公司 | Lsd1抑制劑之鹽 |
US10059668B2 (en) | 2015-11-05 | 2018-08-28 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
MA43318A (fr) | 2015-11-27 | 2018-10-03 | Taiho Pharmaceutical Co Ltd | Nouveau composé de biphényle ou un sel de celui-ci |
WO2017109061A1 (en) * | 2015-12-23 | 2017-06-29 | Ieo - Istituto Europeo Di Oncologia S.R.L. | Spirocyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
JP6916795B2 (ja) | 2015-12-29 | 2021-08-11 | ミラティ セラピューティクス, インコーポレイテッド | Lsd1阻害剤 |
CN107176927B (zh) * | 2016-03-12 | 2020-02-18 | 福建金乐医药科技有限公司 | 组蛋白去甲基化酶lsd1抑制剂 |
SG10201913290QA (en) | 2016-03-15 | 2020-03-30 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for the treatment of hematological malignancies |
AU2017233898B2 (en) | 2016-03-15 | 2022-12-15 | Oryzon Genomics, S.A. | Combinations of LSD1 inhibitors for use in the treatment of solid tumors |
US11034991B2 (en) | 2016-03-16 | 2021-06-15 | Oryzon Genomics S.A. | Methods to determine KDM1A target engagement and chemoprobes useful therefor |
CN107200706A (zh) | 2016-03-16 | 2017-09-26 | 中国科学院上海药物研究所 | 一类氟取代的环丙胺类化合物及其制备方法、药物组合物和用途 |
MX2018012901A (es) | 2016-04-22 | 2019-06-06 | Incyte Corp | Formulaciones de inhibidor de demetilasa 1 especifica para lisina (lsd1). |
RS58951B1 (sr) | 2016-06-10 | 2019-08-30 | Oryzon Genomics Sa | Lečenje multiple skleroze |
WO2018035259A1 (en) | 2016-08-16 | 2018-02-22 | Imago Biosciences, Inc. | Methods and processes for the preparation of kdm1a inhibitors |
US20190256930A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
CN110087644A (zh) * | 2016-11-17 | 2019-08-02 | 赛途公司 | 作为骨骼肌肥大诱导物的lsd1抑制剂 |
WO2018106984A1 (en) | 2016-12-09 | 2018-06-14 | Constellation Pharmaceuticals, Inc. | Markers for personalized cancer treatment with lsd1 inhibitors |
RU2763898C9 (ru) | 2017-01-24 | 2022-03-18 | Цспц Чжунци Фармасьютикал Текнолоджи (Шицзячжуан) Ко., Лтд. | Ингибитор lsd1, а также способ его получения и его применение |
JP6843979B2 (ja) | 2017-05-26 | 2021-03-17 | 大鵬薬品工業株式会社 | 新規なビフェニル化合物又はその塩 |
RU2765153C2 (ru) | 2017-05-26 | 2022-01-26 | Тайхо Фармасьютикал Ко., Лтд. | Усилитель противоопухолевого эффекта с применением нового соединения бифенила |
AU2018276611B2 (en) * | 2017-05-31 | 2022-01-06 | Taiho Pharmaceutical Co., Ltd. | Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1 |
JP2020152641A (ja) * | 2017-07-07 | 2020-09-24 | 国立研究開発法人理化学研究所 | リジン特異的脱メチル化酵素1阻害活性を有する新規化合物、その製造方法及びその用途 |
AU2018309372A1 (en) * | 2017-08-03 | 2020-01-30 | Oryzon Genomics, S.A. | Methods of treating behavior alterations |
WO2019068326A1 (en) | 2017-10-05 | 2019-04-11 | Université D'aix-Marseille | INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES |
US11578059B2 (en) | 2018-05-11 | 2023-02-14 | Imago Biosciences. Inc. | KDM1A inhibitors for the treatment of disease |
EP3825309B1 (en) * | 2018-07-20 | 2023-09-06 | CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. | Salt of lsd1 inhibitor and a polymorph thereof |
US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
CN112672994B (zh) * | 2018-09-13 | 2022-09-13 | 南昌弘益药业有限公司 | 作为lsd1抑制剂的杂螺环类化合物及其应用 |
CN113631164A (zh) | 2019-03-20 | 2021-11-09 | 奥莱松基因组股份有限公司 | 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法 |
MX2021011256A (es) | 2019-03-20 | 2021-10-01 | Oryzon Genomics Sa | Metodos de tratamiento del trastorno limite de la personalidad. |
CN114341366A (zh) | 2019-07-05 | 2022-04-12 | 奥莱松基因组股份有限公司 | 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法 |
CN114615979A (zh) | 2019-09-03 | 2022-06-10 | 奥莱松基因组股份有限公司 | 用于治疗孤独症谱系障碍的伐菲德司他 |
WO2021228146A1 (zh) * | 2020-05-12 | 2021-11-18 | 石药集团中奇制药技术(石家庄)有限公司 | 一种lsd1抑制剂的用途 |
EP3964204A1 (en) | 2020-09-08 | 2022-03-09 | Université d'Aix-Marseille | Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues |
EP4319732A1 (en) | 2021-04-08 | 2024-02-14 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for treating myeloid cancers |
CN113582906B (zh) * | 2021-08-24 | 2023-05-16 | 郑州大学 | 二氟苯环丙胺类化合物及其制备方法和应用 |
WO2023217758A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
WO2023217784A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
Family Cites Families (131)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3106578A (en) | 1960-09-16 | 1963-10-08 | Smith Kline French Lab | Nu-phenethyl-2-phenylcyclopropylamine derivatives |
US3365458A (en) | 1964-06-23 | 1968-01-23 | Aldrich Chem Co Inc | N-aryl-n'-cyclopropyl-ethylene diamine derivatives |
US3532749A (en) * | 1965-05-11 | 1970-10-06 | Aldrich Chem Co Inc | N'-propargyl-n**2-cyclopropyl-ethylenediamines and the salts thereof |
US3532712A (en) | 1967-09-29 | 1970-10-06 | Aldrich Chem Co Inc | N'-cyclopropyl ethylenediamine derivatives |
US3471522A (en) | 1967-09-29 | 1969-10-07 | Aldrich Chem Co Inc | N-cyclopropyl-n'-furfuryl-n'-methyl ethylene diamines |
US3654306A (en) | 1970-01-26 | 1972-04-04 | Robins Co Inc A H | 5-azaspiro(2.4)heptane-4 6-diones |
US3758684A (en) | 1971-09-07 | 1973-09-11 | Burroughs Wellcome Co | Treating dna virus infections with amino purine derivatives |
US4530901A (en) | 1980-01-08 | 1985-07-23 | Biogen N.V. | Recombinant DNA molecules and their use in producing human interferon-like polypeptides |
US4409243A (en) | 1981-11-09 | 1983-10-11 | Julian Lieb | Treatment of auto-immune and inflammatory diseases |
US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
GB9311282D0 (en) | 1993-06-01 | 1993-07-21 | Rhone Poulenc Rorer Ltd | New compositions of matter |
EP1275635A1 (en) | 1994-10-21 | 2003-01-15 | Nps Pharmaceuticals, Inc. | Calcium receptor-active compounds |
US5652258A (en) | 1995-05-30 | 1997-07-29 | Gliatech, Inc. | 2-(4-imidazoyl) cyclopropyl derivatives |
US20040132820A1 (en) | 1996-02-15 | 2004-07-08 | Jean Gosselin | Agents with leukotriene B4-like antiviral (DNA) and anti-neoplastic activities |
GB9615730D0 (en) | 1996-07-26 | 1996-09-04 | Medical Res Council | Anti-viral agent 1 |
US5961987A (en) | 1996-10-31 | 1999-10-05 | University Of Iowa Research Foundation | Ocular protein stimulants |
DE19647615A1 (de) | 1996-11-18 | 1998-05-20 | Bayer Ag | Verfahren zur Herstellung von Cyclopropylaminen |
SE9702772D0 (sv) | 1997-07-22 | 1997-07-22 | Astra Pharma Prod | Novel compounds |
AR017014A1 (es) | 1997-07-22 | 2001-08-22 | Astrazeneca Ab | Compuestos de triazolo [4,5-d]pirimidina, composiciones farmaceuticas, uso de los mismos para preparar medicamentos y procesos para la preparacionde dichos compuestos |
AU1631699A (en) | 1997-12-18 | 1999-07-05 | E.I. Du Pont De Nemours And Company | Cyclohexylamine arthropodicides and fungicides |
US6809120B1 (en) | 1998-01-13 | 2004-10-26 | University Of Saskatchewan Technologies Inc. | Composition containing propargylamine for enhancing cancer therapy |
WO1999036406A1 (en) * | 1998-01-16 | 1999-07-22 | Medivir Ab | Antivirals |
WO1999054440A1 (en) | 1998-04-21 | 1999-10-28 | Micromet Gesellschaft Für Biomedizinische Forschung Mbh | CD19xCD3 SPECIFIC POLYPEPTIDES AND USES THEREOF |
SE9802206D0 (sv) | 1998-06-22 | 1998-06-22 | Astra Pharma Inc | Novel compounds |
GB2344337A (en) | 1998-12-02 | 2000-06-07 | Fcp | Carton having a rim |
TWI229674B (en) | 1998-12-04 | 2005-03-21 | Astra Pharma Prod | Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses |
MY132006A (en) | 2000-05-26 | 2007-09-28 | Schering Corp | ADENOSINE A2a RECEPTOR ANTAGONISTS |
TWI290549B (en) * | 2000-06-02 | 2007-12-01 | Astrazeneca Ab | Process for the preparation of cyclopropyl carboxylic acid ester and derivatives |
JP2001354563A (ja) | 2000-06-09 | 2001-12-25 | Sankyo Co Ltd | 置換ベンジルアミン類を含有する医薬 |
US8519005B2 (en) | 2000-07-27 | 2013-08-27 | Thomas N. Thomas | Compositions and methods to prevent toxicity of antiinflammatory agents and enhance their efficacy |
EP1193268A1 (en) | 2000-09-27 | 2002-04-03 | Applied Research Systems ARS Holding N.V. | Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein Junkinases |
KR100947185B1 (ko) | 2000-12-21 | 2010-03-15 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 조성물 |
WO2002079152A1 (en) | 2001-03-29 | 2002-10-10 | Bristol-Myers Squibb Company | Cyclopropylindole derivatives as selective serotonin reuptake inhibitors |
RU2332415C2 (ru) * | 2001-04-27 | 2008-08-27 | Вертекс Фармасьютикалз Инкорпорейтед | Производные пиразола, полезные в качестве ингибиторов протеинкиназы |
DE10123163A1 (de) | 2001-05-09 | 2003-01-16 | Gruenenthal Gmbh | Substituierte Cyclohexan-1,4-diaminderivate |
US20030008844A1 (en) | 2001-05-17 | 2003-01-09 | Keryx Biopharmaceuticals, Inc. | Use of sulodexide for the treatment of inflammatory bowel disease |
US7544675B2 (en) | 2002-04-18 | 2009-06-09 | Ucb, S.A. | Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions |
US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
CA2484209C (en) | 2002-05-03 | 2013-06-11 | Exelixis, Inc. | Protein kinase modulators and methods of use |
EP1505966A4 (en) | 2002-05-10 | 2006-08-30 | Bristol Myers Squibb Co | 1,1-DISUBSTITUTED CYCLOALKYL DERIVATIVES AS FACTOR XA HEMMER |
US7456222B2 (en) | 2002-05-17 | 2008-11-25 | Sequella, Inc. | Anti tubercular drug: compositions and methods |
US6951961B2 (en) | 2002-05-17 | 2005-10-04 | Marina Nikolaevna Protopopova | Methods of use and compositions for the diagnosis and treatment of infectious disease |
US20040033986A1 (en) | 2002-05-17 | 2004-02-19 | Protopopova Marina Nikolaevna | Anti tubercular drug: compositions and methods |
EP1506172B1 (en) | 2002-05-20 | 2011-03-30 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
US7611704B2 (en) | 2002-07-15 | 2009-11-03 | Board Of Regents, The University Of Texas System | Compositions and methods for treating viral infections using antibodies and immunoconjugates to aminophospholipids |
SE0202539D0 (sv) | 2002-08-27 | 2002-08-27 | Astrazeneca Ab | Compounds |
ATE384724T1 (de) | 2002-12-13 | 2008-02-15 | Smithkline Beecham Corp | Cyclopropylverbindungen als ccr5 antagonisten |
US20040229955A1 (en) | 2003-01-08 | 2004-11-18 | Andersen Niels H. | Antibacterial agents |
US7223785B2 (en) | 2003-01-22 | 2007-05-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
GB0303439D0 (en) | 2003-02-14 | 2003-03-19 | Pfizer Ltd | Antiparasitic terpene alkaloids |
US7186832B2 (en) | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
WO2004096135A2 (en) | 2003-04-24 | 2004-11-11 | Merck & Co., Inc. | Inhibitors of akt activity |
ATE384039T1 (de) | 2003-07-03 | 2008-02-15 | Lilly Co Eli | Indanderivate als muscarinrezeptoragonisten |
AU2004270733B2 (en) | 2003-09-11 | 2011-05-19 | Itherx Pharma, Inc. | Cytokine inhibitors |
JP4870562B2 (ja) | 2003-09-12 | 2012-02-08 | メルク セローノ ソシエテ アノニム | 糖尿病の治療のためのスルホンアミド誘導体 |
CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
WO2005041971A1 (en) | 2003-10-21 | 2005-05-12 | Merck & Co., Inc. | Triazolo-pyridazine compounds and derivatives thereof useful in the treatment of neuropathic pain |
US7026339B2 (en) | 2003-11-07 | 2006-04-11 | Fan Yang | Inhibitors of HCV NS5B polymerase |
ZA200605248B (en) | 2003-12-15 | 2007-10-31 | Japan Tobacco Inc | Cyclopropane compounds and pharmaceutical use thereof |
US20080058356A1 (en) | 2003-12-15 | 2008-03-06 | Neurocrine Biosciences, Inc. | 2,6 Bisheteroaryl-4-Aminopyrimidines as Adenosine Receptor Antagonists |
CN1894206A (zh) | 2003-12-15 | 2007-01-10 | 日本烟草产业株式会社 | N-取代的n-磺酰氨基环丙烷化合物和其药学应用 |
US7399825B2 (en) | 2003-12-24 | 2008-07-15 | Lipps Binie V | Synthetic peptide, inhibitor to DNA viruses |
EP1756103A2 (en) | 2004-04-26 | 2007-02-28 | Pfizer, Inc. | Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors |
US20090275099A1 (en) | 2004-04-27 | 2009-11-05 | Regents Of The University Of Michigan | Methods and compositions for treating diseases and conditions associated with mitochondrial function |
CN1950326A (zh) * | 2004-06-28 | 2007-04-18 | 特瓦药物精化学品股份有限公司 | 托莫西汀的光学拆分和重新利用方法 |
DE102004057594A1 (de) | 2004-11-29 | 2006-06-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Substitueirte Pteridine zur Behandlung von entzündlichen Erkrankungen |
ATE554184T1 (de) | 2004-12-16 | 2012-05-15 | Harvard College | Durch das nukleäre aminoxidase-homolog lsd1 vermittelte histondemethylierung |
ES2349544T3 (es) | 2005-02-18 | 2011-01-04 | Universitätsklinikum Freiburg | Control de la expresión génica dependiente de receptores de andrógenos inhibiendo la actividad de amina oxidasa de la demetilasa lisina-específica (lsd1). |
US20060275366A1 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Controlled-release formulation |
US7273882B2 (en) | 2005-06-21 | 2007-09-25 | Bristol-Myers Squibb Company | Aminoacetamide acyl guanidines as β-secretase inhibitors |
EP1741708A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals |
EP2305695A3 (en) | 2005-07-25 | 2011-07-27 | Intermune, Inc. | Macrocyclic inhibitors of Hepatitis C virus replication |
CA2619005A1 (en) | 2005-08-10 | 2007-02-22 | Johns Hopkins University | Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors |
WO2007025144A1 (en) | 2005-08-24 | 2007-03-01 | University Of Illinois - Chicago | 5-ht2c receptor agonists as anorectic agents |
GB0517740D0 (en) | 2005-08-31 | 2005-10-12 | Novartis Ag | Organic compounds |
TW200745067A (en) | 2006-03-14 | 2007-12-16 | Astrazeneca Ab | Novel compounds |
TWI388547B (zh) | 2006-05-18 | 2013-03-11 | Syngenta Participations Ag | 新穎殺微生物劑 |
US8198301B2 (en) | 2006-07-05 | 2012-06-12 | Hesheng Zhang | Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors |
EP2521786B1 (en) | 2006-07-20 | 2015-06-24 | Vical Incorporated | Compositions for vaccinating against hsv-2 |
WO2008033466A2 (en) | 2006-09-14 | 2008-03-20 | Combinatorx (Singapore) Pre. Ltd. | Compositions and methods for treatment of viral diseases |
WO2008127734A2 (en) | 2007-04-13 | 2008-10-23 | The Johns Hopkins University | Lysine-specific demethylase inhibitors |
US7906513B2 (en) | 2007-04-26 | 2011-03-15 | Enanta Pharmaceuticals, Inc. | Hydrazide-containing hepatitis C serine protease inhibitors |
CN101842361B (zh) | 2007-06-27 | 2013-06-05 | 阿斯利康(瑞典)有限公司 | 吡嗪酮衍生物及其在治疗肺病中的用途 |
EP2187883A2 (en) | 2007-08-10 | 2010-05-26 | Genelabs Technologies, Inc. | Nitrogen containing bicyclic chemical entities for treating viral infections |
CN101842360B (zh) | 2007-09-17 | 2014-12-17 | 艾伯维巴哈马有限公司 | 抗感染嘧啶及其用途 |
US20100016262A1 (en) | 2007-10-18 | 2010-01-21 | Yale University | Compositions and methods for reducing hepatotoxicity associated with drug administration and treating non-alcoholic fatty liver disease, non-alcoholic steatohepatitis and associated cirrhosis |
US8299123B2 (en) | 2007-10-19 | 2012-10-30 | Boehringer Ingelheim International Gmbh | CCR10 antagonists |
JP5517153B2 (ja) | 2007-12-26 | 2014-06-11 | 塩野義製薬株式会社 | グリコペプチド抗生物質配糖化誘導体 |
WO2009109991A2 (en) | 2008-01-23 | 2009-09-11 | Sun Pharma Advanced Research Company Ltd., | Novel hydrazide containing tyrosine kinase inhibitors |
NZ586831A (en) | 2008-01-28 | 2012-02-24 | Janssen Pharmaceutica Nv | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace) |
JP5746612B2 (ja) | 2008-03-19 | 2015-07-08 | オーリムメッド・ファルマ・インコーポレーテッド | 中枢神経系疾患および障害の治療に有効な新規化合物 |
NZ600207A (en) | 2008-03-27 | 2013-09-27 | Gruenenthal Chemie | Substituted 4-aminocyclohexane derivatives |
JP5705720B2 (ja) | 2008-04-16 | 2015-04-22 | ポートラ ファーマシューティカルズ, インコーポレイテッド | Sykまたはjakキナーゼ阻害剤としての2,6−ジアミノ−ピリミジン−5−イル−カルボキサミド |
WO2009153197A1 (en) | 2008-06-18 | 2009-12-23 | F. Hoffmann-La Roche Ag | Halo-substituted pyrimidodiazepines as plkl inhibitors |
WO2010011845A2 (en) | 2008-07-24 | 2010-01-28 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Methods of preventing or treating viral infection or reactivation after latency in a host using inhibitors of the lsd1 protein |
EP2331542B1 (en) | 2008-08-01 | 2016-07-27 | The United States of America, as Represented by The Secretary, Department of Health and Human Services | A3 adenosine receptor antagonists and partial agonists |
US8048887B2 (en) | 2008-09-11 | 2011-11-01 | Bristol-Myers Squibb Company | Compounds for the treatment of hepatitis C |
WO2010043721A1 (en) | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
US8993808B2 (en) | 2009-01-21 | 2015-03-31 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
WO2010085749A2 (en) | 2009-01-23 | 2010-07-29 | Northwestern University | Potent and selective neuronal nitric oxide synthase inhibitors with improved membrane permeability |
MX2011008982A (es) | 2009-02-27 | 2011-09-15 | Enata Pharmaceuticals Inc | Inhibidores del virus de la hepatitis c. |
AU2010247414B2 (en) | 2009-05-15 | 2013-08-01 | Novartis Ag | Aryl pyridine as aldosterone synthase inhibitors |
US8389580B2 (en) * | 2009-06-02 | 2013-03-05 | Duke University | Arylcyclopropylamines and methods of use |
EP2258865A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer |
WO2010143582A1 (ja) | 2009-06-11 | 2010-12-16 | 公立大学法人名古屋市立大学 | フェニルシクロプロピルアミン誘導体及びlsd1阻害剤 |
WO2011022489A2 (en) | 2009-08-18 | 2011-02-24 | The Johns Hopkins University | (bis) urea and (bis) thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders |
WO2011031934A1 (en) | 2009-09-11 | 2011-03-17 | Enanta Pharmaceuticals, Inc. | Hepatitis c virus inhibitors |
MX338041B (es) | 2009-09-25 | 2016-03-30 | Oryzon Genomics Sa | Inhibidores de demetilasa-1 especificos de lisina y su uso. |
US8946296B2 (en) | 2009-10-09 | 2015-02-03 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use |
WO2011057262A2 (en) | 2009-11-09 | 2011-05-12 | Evolva Inc. | Treatment of infections with tp receptor antagonists |
US9186337B2 (en) | 2010-02-24 | 2015-11-17 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae |
WO2011106574A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
US20130197088A1 (en) | 2010-03-12 | 2013-08-01 | Robert A. Casero, JR. | Compositions and Methods for Combinations of Oligoamines with 2-Difluoromethylornithine (DFMO) |
ES2607081T3 (es) | 2010-04-19 | 2017-03-29 | Oryzon Genomics, S.A. | Inhibidores de desmetilasa específica de lisina-1 y su uso |
PL2560949T3 (pl) | 2010-04-20 | 2017-01-31 | Università Degli Studi Di Roma "La Sapienza" | Pochodne tranylocyprominy jako inhibitory demetylazy histonowej LSD1 i/lub LSD2 |
US20130150577A1 (en) | 2010-04-20 | 2013-06-13 | Actavis Group Ptc Ehf | Novel process for preparing phenylcyclopropylamine derivatives using novel intermediates |
CN103003231A (zh) | 2010-06-30 | 2013-03-27 | 阿特维斯集团公司 | 制备苯基环丙基胺衍生物的新方法及其用于制备替卡格雷的用途 |
LT2598482T (lt) | 2010-07-29 | 2018-07-10 | Oryzon Genomics, S.A. | Demetilazės lsd1 inhibitoriai arilciklopropilamino pagrindu ir jų medicininis panaudojimas |
EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
WO2012034116A2 (en) | 2010-09-10 | 2012-03-15 | The Johns Hopkins University | Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders |
US20130303545A1 (en) | 2010-09-30 | 2013-11-14 | Tamara Maes | Cyclopropylamine derivatives useful as lsd1 inhibitors |
WO2012045883A1 (en) | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
WO2012107498A1 (en) | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
WO2012107499A1 (en) | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
EP2688568B1 (en) | 2011-03-25 | 2019-06-19 | Glaxosmithkline Intellectual Property (No. 2) Limited | Cyclopropylamines as lsd1 inhibitors |
EP2750671A2 (en) | 2011-05-19 | 2014-07-09 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
EP2741741A2 (en) | 2011-05-19 | 2014-06-18 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for inflammatory diseases or conditions |
CA2849564C (en) | 2011-10-20 | 2020-10-20 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
BR112014009306B1 (pt) | 2011-10-20 | 2021-07-20 | Oryzon Genomics S.A. | Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1 |
-
2011
- 2011-07-27 LT LTEP11749119.1T patent/LT2598482T/lt unknown
- 2011-07-27 AU AU2011284688A patent/AU2011284688B2/en active Active
- 2011-07-27 HU HUE11749119A patent/HUE037937T2/hu unknown
- 2011-07-27 KR KR1020137004877A patent/KR101866858B1/ko active IP Right Grant
- 2011-07-27 PT PT117491191T patent/PT2598482T/pt unknown
- 2011-07-27 BR BR112013002164-0A patent/BR112013002164B1/pt active IP Right Grant
- 2011-07-27 CN CN201180047286.3A patent/CN103124724B/zh active Active
- 2011-07-27 EP EP11749119.1A patent/EP2598482B1/en active Active
- 2011-07-27 MX MX2013000968A patent/MX341732B/es active IP Right Grant
- 2011-07-27 NO NO11749119A patent/NO2598482T3/no unknown
- 2011-07-27 DK DK11749119.1T patent/DK2598482T3/en active
- 2011-07-27 ES ES11749119.1T patent/ES2674747T3/es active Active
- 2011-07-27 PL PL11749119T patent/PL2598482T3/pl unknown
- 2011-07-27 CN CN201510197250.3A patent/CN104892525A/zh active Pending
- 2011-07-27 CA CA2806008A patent/CA2806008C/en active Active
- 2011-07-27 JP JP2013521139A patent/JP6054868B2/ja active Active
- 2011-07-27 RU RU2013108702A patent/RU2611437C2/ru active
- 2011-07-27 SI SI201131504T patent/SI2598482T1/sl unknown
- 2011-07-27 ME MEP-2018-163A patent/ME03085B/me unknown
- 2011-07-27 RS RS20180684A patent/RS57331B1/sr unknown
- 2011-07-27 EP EP18165419.5A patent/EP3375775A1/en not_active Withdrawn
- 2011-07-27 WO PCT/EP2011/062949 patent/WO2012013728A1/en active Application Filing
- 2011-07-27 US US13/812,366 patent/US9181198B2/en active Active
- 2011-07-27 TR TR2018/09057T patent/TR201809057T4/tr unknown
-
2013
- 2013-01-24 IL IL224389A patent/IL224389A/en active IP Right Grant
-
2015
- 2015-09-09 US US14/848,649 patent/US9708309B2/en active Active
-
2016
- 2016-09-23 JP JP2016186185A patent/JP2017039740A/ja active Pending
-
2017
- 2017-06-15 US US15/623,866 patent/US10233178B2/en active Active
-
2018
- 2018-06-12 HR HRP20180916TT patent/HRP20180916T1/hr unknown
- 2018-06-22 CY CY181100649T patent/CY1120586T1/el unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20180916T1 (hr) | Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba | |
JP2013535460A5 (hr) | ||
HRP20100677T1 (hr) | IMIDAZO[1,2-a]PIRIDINSKI SPOJEVI KAO INHIBITORI VEGF-R2 | |
JP2016506960A5 (hr) | ||
IL264982B (en) | Hetero(aryl)cyclopropylamine compounds as lsd1 inhibitors | |
RU2008146995A (ru) | N-(2-тиазолил)амидные производные в качестве ингибиторов gsk-3 | |
JP2019517487A5 (hr) | ||
MY148375A (en) | Delta and epsilon crystal forms of imatinib mesylate | |
JP2012507566A5 (hr) | ||
JP2017533968A5 (hr) | ||
JP2016512520A5 (hr) | ||
JP2008516986A5 (hr) | ||
HRP20140156T1 (hr) | Acetamidi supstituirani s n-(hetero)aril,2-(hetero)aril, koji se upotrebljavaju kao wnt-signalni modulatori | |
JP2017538785A5 (hr) | ||
JP2016506962A5 (hr) | ||
JP2013533879A5 (hr) | ||
RU2017126128A (ru) | Конденсированные бициклические соединения для лечения заболевания | |
GEP20156389B (en) | Oxazolidin-2-one compounds and their usage as pi3ks inhibitors | |
BRPI0820112B8 (pt) | derivados de isoxazol-piridina, seu uso e processos de preparação e medicamento | |
JP2010031025A5 (hr) | ||
RU2013143028A (ru) | Тиазолилфенилбензолсульфонамидопроизводные в качестве ингибиторов киназ | |
JP2016506961A5 (hr) | ||
JP2020502092A5 (hr) | ||
BR112012001031A8 (pt) | Compostos espiro amino adequados para o tratamento de inter alia distúrbios do sono e toxicodependência | |
HRP20100724T1 (hr) | Supstituirani biciklički derivati pirimidona |