HRP20151336T1 - Tetrahidroizokinolin-1-on derivat ili njegova sol - Google Patents

Tetrahidroizokinolin-1-on derivat ili njegova sol Download PDF

Info

Publication number
HRP20151336T1
HRP20151336T1 HRP20151336TT HRP20151336T HRP20151336T1 HR P20151336 T1 HRP20151336 T1 HR P20151336T1 HR P20151336T T HRP20151336T T HR P20151336TT HR P20151336 T HRP20151336 T HR P20151336T HR P20151336 T1 HRP20151336 T1 HR P20151336T1
Authority
HR
Croatia
Prior art keywords
alkylene
alkyl
group
halogen
aryl
Prior art date
Application number
HRP20151336TT
Other languages
English (en)
Inventor
Hiroyuki Hisamichi
Itsuro Shimada
Tsukasa Ishihara
Tomofumi Takuwa
Takafumi Shimizu
Noriko Ishikawa
Kyoichi Maeno
Norio Seki
Original Assignee
Seldar Pharma Inc.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40075016&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20151336(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Seldar Pharma Inc. filed Critical Seldar Pharma Inc.
Publication of HRP20151336T1 publication Critical patent/HRP20151336T1/hr

Links

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
    • A61K31/435—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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/435—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
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/695—Silicon compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • C07D409/12—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 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Claims (12)

1. Derivat tetrahidroizokinolin-1-ona predstavljen formulom (I) ili njegova farmaceutski prikladna sol: [image] gdje simboli u formuli imaju sljedeća značenja: R1: (C1-6 alkilen koji može biti supstituiran skupinom izabranom iz grupe koju čini fenil koji može biti supstituiran s halogenom, C1-6 alkilom ili -OR0, i -OH)-OH, ili cikloalkil supstituiran skupinom izabranom iz grupe koju čine -OR0, - N(R0)2, -N(R0)C(O)R0, -N(R0)C(O)-C1-6 alkilen-OR0, -N(R0)S(O)2-C1-6 alkil, i heterociklička skupina, R0: međusobno jednaki ili različiti, svaki predstavlja -H ili C1-6 alkil, R2: fenil koji može biti supstituiran s halogenom ili -OR0, R3: -H, R4: -N(R0)-O-C1-6alkilen-(aril ili heteroaril, od kojih svaki može biti supstituiran skupinom izabranom iz grupe G6), Grupa G6: halogen, C1-6 alkil koji može biti supstituiran s -OR0, halogen-C1-6 alkil koji može biti supstituiran s -OR0, -CN, -N(R0)2, -CO2R0, -CO2-C1-6 alkilen-aril, -C(O)N(R0)2, C1-6 alkilen-OC(O)R0, C1-6 alkilen-OC(O)aril, C1-6 alkilen-CO2R0, halogen-C1-6 alkilen-CO2R0, C1-6 alkilen-CO2-C1-6 alkilen-aril, C1-6alkilen-C(O)N(R0)2, halogen-C1-6 alkilen-C(O)N(R0)2, -O-C1-6 alkilen-CO2R0, -O-C1-6 alkilen-CO2-C1-6 alkilen-aril, -O-C1-6 alkilen-C(O)N(R0)2, -O-halogen-C1-6 alkilen-CO2R0, -O-halogen-C1-6 alkilen-C(O)N(R0)2, -C(O)N(R0)S(O)2-C1-6 alkil, C1-6 alkilen-C(O)N(R0)S(O)2-C1-6 alkil, -S(O)2-C1-6 alkil, -S(O)2N(R0)2, heterociklička skupina, -C(=NH)NH2, -C(-NH)=NO-C(O)O-C1-10 alkil, -C(=NOH)NH2, -C(O)N=C(N(R0)2)2, -N(R0)C(O)R0, -N(R0)C(O)-C1-6 alkilen-OR0, -N(R0)C(O)OR0, -N(R0)S(O)2-C1-6 alkil, -C(aril)3, i okso, gdje "aril" i "heterociklička skupina" u Grupi G6 svaki može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0, -O-halogen-C1-6 alkil, okso, i tiokso (=S), m: cijeli broj od 0 do 3, i R5: C1-6 alkil, halogen-C1-6 alkil, halogen, nitro, -OR0, -O-halogen-C1-6 alkil, -N(R0)2, -O-C1-6 alkilen-CO2R0, ili -O-C1-6 alkilen-aril, gdje aril u R5 može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0 i -O-halogen-C1-6 alkil.
2. Spoj kako je opisan prema zahtjevu 1, gdje R4 jest -NH-O-C1-6alkilen-(fenil, piridil, N-oksidopiridil, tienil, ili tiazolil, od kojih svaki može biti supstituiran skupinom izabranom iz grupe koju čine halogen, -OR0, C1-6 alkilen-OR0, -CO2R0, C1-6 alkilen-CO2R0, i -OC1-6 alkilen-CO2R0).
3. Spoj kako je opisan prema zahtjevu 2, gdje je R1 cikloalkil supstituiran skupinom izabranom iz grupe koju čine -OR0, -N(R0)2, -N(R0)C(O)R0, -N(R0)C(O)-C1-6alkilen-OR0, -N(R0)S(O)2-C1-6 alkil, i heterociklička skupina.
4. Spoj kako je opisan prema zahtjevu 3, gdje m je jednako 0.
5. Spoj kako je opisan prema zahtjevu 4, gdje je R1 cikloheksil supstituiran skupinom izabranom iz grupe koju čine -OR0, -N(R0)C(O)R0 i -N(R0)S(O)2-C1-6 alkil.
6. Spoj kako je opisan prema zahtjevu 1, a koji se izabire iz grupe koju čine: (3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-1-okso-N-(piridin-2-ilmetoksi)-1,2,3,4-tetrahidroizokinolin-4-karboksamid, (3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-N-[(1-oksidopiridin-2-il)metoksi]-1-okso-1,2,3,4-tetrahidroizokinolin-4-karboksamid, 3-{[({[(3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)-amino]cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-oksi]metil}benzojeva kiselina, (4-{[({[(3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)-amino]-cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-oksi]metil}fenil)octena kiselina, (3-{[({[(3R,4R)-3-(2,4-diklorofenil-2-{(1S,2S)-2-[(metilsulfonil)-amino]cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-oksi]metil}fenoksi)octena kiselina, {3-[2-({[(3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-etil]fenil}(difluoro)octena kiselina, (3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-N-(2-{3-[(metilsulfonil)karbamoil]fenil}etil)-1-okso-1,2,3,4-tetrahidroizokinolin-4-karboksamid, {4-[2-({[(3R,4R)-3-(2,4-diklorofenil)-2-{(1S,2S)-2-[(metilsulfonil)amino]-cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-etil]fenil}octena kiselina, i 4-(3-{[({[(3R,4R)-3-(2,4-diklorofenil)-2-{(18,28)-2-[(metilsulfonil)amino]-cikloheksil}-1-okso-1,2,3,4-tetrahidroizokinolin-4-il]karbonil}amino)-oksi]metil}fenoksi)butan kiselina; ili njegova farmaceutski prikladna sol.
7. Farmaceutski pripravak koji sadrži spoj kako je opisan prema bilo kojem od zahtjeva 1 do 6 ili njegovu farmaceutski prikladnu sol, i farmaceutski prikladan nosač.
8. Farmaceutski pripravak koji sadrži derivat tetrahidroizokinolin-1-ona predstavljen formulom (I’) ili njegovu farmaceutski prikladnu sol, i farmaceutski prikladan nosač: [image] gdje simboli u formuli imaju sljedeća značenja: R1: (C1-6 alkilen koji može biti supstituiran skupinom izabranom iz grupe G1)-OH, cikloalkil koji može biti supstituiran skupinom izabranom iz grupe G2, ili heterociklička skupina koja može biti supstituirana skupinom izabranom iz grupe G2, Grupa G1: halogen, -OR0, -N(R0)(R6), i aril, gdje "aril" u Grupi G1 može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0, i -O-halogen-C1-6 alkil, Grupa G2: halogen, C1-6 alkil, halogen-C1-6 alkil, C1-6 alkilen-OR0,-OR0, -O-halogen-C1-6 alkil, -N(R0)2, -N(R0)-C1-6 alkilen-OR0, -N(R0)-C1-6 alkilen-CO2R0, -N(R0)C(O)R0, -N(R0)C(O)OR0, -N(R0)C(O)-aril, -N(R0)C(O)-C1-6 alkilen-OR0, -N(R0)C(O)-C1-6 alkilen-N(R0)2, -N(R0)C(O)N(R0)2, -N(R0)C(=NR0)-C1-6 alkil, -N(R0)S(O)2-C1-6 alkil, -N(C1-6 alkilen-OR0)-S(O)2-C1-6 alkil, -N(C1-6 alkilen-CO2R0)-S(O)2-C1-6 alkil, -N(R0)S(O)2-C1-6 alkilen-CO2R0, -N(R0)S(O)2-C1-6 alkilen-S(O)2-C1-6 alkil, -N(R0)S(O)2-aril, -N(R0)S(O)2N(R0)2, -S(O)2-C1-6 alkil, -CO2R0, -CO2-C1-6 alkilen-Si(C1-6 alkil)3, -C(O)N(R0)2, -C(O)N(R0)-C1-6 alkilen-OR0, -C(O)N(R0)-C1-6 alkilen-N(R0)2, -C(O)N(R0)-C1-6 alkilen-CO2R0, -C(O)N(R0)-O-C1-6 alkilen-heterociklička skupina, heterociklička skupina, -C(O)R0, -C(O)-C1-6 alkilen-OR0, - C(O)-C1-6 alkilen-N(R0)2, -C(O)-heterociklička skupina, i okso, gdje "aril" i "heterociklička skupina" u Grupi G2 svaki može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0, -O-halogen-C1-6 alkil, i okso; R0: međusobno jednaki ili različiti, svaki predstavlja -H ili C1-6 alkil, R2: fenil koji može biti supstituiran s halogenom, C1-6 alkilom ili -OR0, R3: -H, R4: -N(R0)-O-C1-6 alkilen-(aril ili heteroaril, od kojih svaki može biti supstituiran skupinom izabranom iz grupe G6), Grupa G6: halogen, C1-6 alkil koji može biti supstituiran s -OR0, halogen-C1-6 alkil koji može biti supstituiran s -OR0, -CN, -N(R0)2, -CO2R0, -CO2-C1-6 alkilen-aril, -C(O)N(R0)2, C1-6 alkilen-OC(O)R0, C1-6 alkilen-OC(O)aril, C1-6 alkilen-CO2R0, halogen-C1-6 alkilen-CO2R0, C1-6 alkilen-CO2-C1-6 alkilen-aril, C1-6alkilen-C(O)N(R0)2, halogen-C1-6 alkilen-C(O)N(R0)2, -O-C1-6 alkilen-CO2R0, -O-C1-6 alkilen-CO2-C1-6 alkilen-aril, -O-C1-6 alkilen-C(O)N(R0)2, -O-halogen-C1-6 alkilen-CO2R0, -O-halogen-C1-6 alkilen-C(O)N(R0)2, -C(O)N(R0)S(O)2-C1-6 alkil, C1-6 alkilen-C(O)N(R0)S(O)2-C1-6 alkil, -S(O)2-C1-6 alkil, -S(O)2N(R0)2, heterociklička skupina, -C(=NH)NH2, -C(-NH)=NO-C(O)O-C1-10 alkil, -C(=NOH)NH2, -C(O)N=C(N(R0)2)2, -N(R0)C(O)R0, -N(R0)C(O)-C1-6alkilen-OR0, -N(R0)C(O)OR0, -N(R0)S(O)2-C1-6 alkil, -C(aril)3, i okso, gdje "aril" i "heterociklička skupina" u Grupi G6 svaki može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0, -O-halogen-C1-6 alkil, okso, i tiokso (=S), m: cijeli broj od 0 do 3, R5: C1-6 alkil, halogen-C1-6 alkil, halogen, nitro, -OR0, -O-halogen-C1-6 alkil, -N(R0)2, -O-C-1-6 alkilen-CO2R0, ili -O-C1-6 alkilen-aril, gdje aril u R5 može biti supstituiran skupinom izabranom iz grupe koju čine halogen, C1-6 alkil, halogen-C1-6 alkil, -OR0 i -O-halogen-C1-6 alkil, i R6: R0, -C(O)-R0, -CO2-C1-6 alkil ili -S(O)2-C1-6 alkil.
9. Uporaba spoja predstavljenog formulom (I’) prema zahtjevu 8 ili njegova farmaceutski prikladna sol za proizvodnju terapijskog sredstva za sindrom iritabilnog crijeva.
10. Uporaba spoja kako je opisan prema zahtjevu 1 ili njegove farmaceutski prikladne soli za proizvodnju terapijskog sredstva za rak.
11. Spoj predstavljen formulom (I’) prema zahtjevu 8 ili njegova sol za uporabu u liječenju sindroma iritabilnog crijeva.
12. Spoj kako je opisan prema zahtjevu 1 ili njegova sol za uporabu u liječenju raka.
HRP20151336TT 2007-05-28 2015-12-07 Tetrahidroizokinolin-1-on derivat ili njegova sol HRP20151336T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2007140097 2007-05-28
PCT/JP2008/059621 WO2008146774A1 (ja) 2007-05-28 2008-05-26 テトラヒドロイソキノリン-1-オン誘導体またはその塩
EP08764654.3A EP2149561B1 (en) 2007-05-28 2008-05-26 Tetrahydroisoquinolin-1-one derivative or salt thereof

Publications (1)

Publication Number Publication Date
HRP20151336T1 true HRP20151336T1 (hr) 2016-01-15

Family

ID=40075016

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20151336TT HRP20151336T1 (hr) 2007-05-28 2015-12-07 Tetrahidroizokinolin-1-on derivat ili njegova sol

Country Status (23)

Country Link
US (5) US8486970B2 (hr)
EP (1) EP2149561B1 (hr)
JP (1) JP5336359B2 (hr)
KR (3) KR101830566B1 (hr)
CN (1) CN101668747B (hr)
AU (1) AU2008255815B2 (hr)
BR (1) BRPI0812359A2 (hr)
CA (1) CA2688326C (hr)
CY (1) CY1117004T1 (hr)
DK (1) DK2149561T3 (hr)
ES (1) ES2558677T3 (hr)
HR (1) HRP20151336T1 (hr)
HU (1) HUE026316T2 (hr)
IL (1) IL202301A (hr)
MX (1) MX2009012779A (hr)
PL (1) PL2149561T3 (hr)
PT (1) PT2149561E (hr)
RS (1) RS54429B1 (hr)
RU (1) RU2479578C2 (hr)
SI (1) SI2149561T1 (hr)
TW (1) TWI425945B (hr)
WO (1) WO2008146774A1 (hr)
ZA (1) ZA200908220B (hr)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011029832A1 (de) 2009-09-09 2011-03-17 Vifor (International) Ag Neue thiazol- und oxazol-hepcidin-antagonisten
CN107109701B (zh) * 2014-09-16 2020-10-09 斯坦福国际研究院 通过光纤阵列扫描技术发现亲和试剂和催化剂
JP2019508496A (ja) * 2016-02-15 2019-03-28 チェム−フォルシュングスツェントルン フュル モレクラーレ メディツィン ゲゼルシャフト ミット ベシュレンクテル ハフツング 癌の治療法のためのｔａｆ１阻害剤
EP3490980A4 (en) * 2016-07-22 2020-04-15 Virginia Commonwealth University PRODRUG AND PROTECTED FORMS OF 5-HYDROXYMETHYLFURFURANAL (5-HMF) AND ITS DERIVATIVES
EP3768266A4 (en) * 2018-03-20 2021-12-22 Merck Sharp & Dohme Corp. OXO-TETRAHYDRO-ISOQUINOLINE CARBOXYLIC ACIDS AS STING PROTEIN INHIBITORS
CN110563687B (zh) * 2019-07-23 2022-09-30 上海合全医药有限公司 一种4-(氨基甲基)色烷-3-醇的制备方法
EP4074314A1 (en) * 2021-04-15 2022-10-19 Valdospan GmbH Isoquinoline derivatives for use as antiviral and antitumour agents
CA3214899A1 (en) 2021-04-15 2022-10-20 Lutz Weber Isoquinoline derivatives for use as antiviral and antitumour agents
CN113603625B (zh) * 2021-08-12 2023-03-10 南京卓康医药科技有限公司 一种酮咯酸中间体的合成方法
WO2024083802A1 (en) 2022-10-17 2024-04-25 Valdospan Gmbh Isoquinoline derivatives as protein degraders, e7 degraders, antivirals, tumor therapeutics and immune suppressives

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL110172A (en) * 1993-07-22 2001-10-31 Lilly Co Eli Bicycle compounds and pharmaceuticals containing them
EP1155001A4 (en) 1999-02-22 2003-05-28 Lion Bioscience Ag ISOQUINOLEIN DERIVATIVES AND COMBINATORIAL ISOQUINOLEIN BANKS
WO2001047891A1 (fr) * 1999-12-28 2001-07-05 Eisai Co., Ltd. Composes heterocylciques contenant des groupes de sulfamide
ES2572332T3 (es) * 2000-10-31 2016-05-31 Rensselaer Polytech Inst 2,6-metano-3-benzazocinas sustituidas en posición 8 y morfinanos sustituidos en posición 3 como ligandos de receptores opioides
AR035513A1 (es) * 2000-12-23 2004-06-02 Hoffmann La Roche Derivados de tetrahidropiridina, proceso para prepararlos, composiciones farmaceuticas que los contienen, y uso de dichos compuestos en la preparacion de medicamentos
DE10146867A1 (de) 2001-09-24 2003-04-24 Bayer Ag Tetrahydroisochinoline
AU2003249713A1 (en) * 2002-07-03 2004-01-23 Axys Pharmaceuticals, Inc. 3,4-dihydroisoquinolin-1-one derivatives as inducers of apoptosis
ES2294475T3 (es) * 2003-03-07 2008-04-01 Eli Lilly And Company Derivados de nicotinamida g-sustituidos como antagonistas de receptores de opioides.
GB0305575D0 (en) 2003-03-11 2003-04-16 Glaxo Group Ltd Novel compounds
US7056930B2 (en) * 2003-04-14 2006-06-06 Pfizer Inc. 2-Azabicyclo[3.3.1]nonane derivatives
NZ546834A (en) * 2003-10-01 2010-03-26 Adolor Corp Spirocyclic heterocyclic derivatives and methods of their use
ES2257168B1 (es) * 2004-08-18 2007-06-01 Laboratorios Del Dr Esteve, S.A. Ligandos del receptor 5-ht7.
WO2006045096A2 (en) 2004-10-20 2006-04-27 Resverlogix Corp. Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases
US8163744B2 (en) 2005-03-18 2012-04-24 Nexuspharma, Inc. Tetrahydro-isoquinolin-1-ones for the treatment of cancer
US8101580B2 (en) * 2005-04-21 2012-01-24 Astellas Pharma Inc. Therapeutic agent for irritable bowel syndrome
RU2302417C1 (ru) 2006-03-14 2007-07-10 Иващенко Андрей Александрович 1-оксо-3-(1н-индол-3-ил)-1,2,3,4-тетрагидроизохинолины, способы их получения, комбинаторная библиотека и фокусированная библиотека
RU2303597C1 (ru) * 2006-05-12 2007-07-27 Иващенко Андрей Александрович Фармацевтическая композиция, способы ее получения и применения
WO2008034039A2 (en) * 2006-09-15 2008-03-20 Nexuspharma Inc. Novel tetrahydro-isoquinolines
WO2008112715A2 (en) * 2007-03-12 2008-09-18 Vm Discovery Inc. Novel agents of calcium ion channel modulators
WO2008131779A1 (en) * 2007-04-26 2008-11-06 H. Lundbeck A/S Isoquinolinone derivatives as nk3 antagonists
PT2149560E (pt) * 2007-05-22 2015-07-13 Astellas Pharma Inc Composto de tetra-hidroisoquinolina substituído na posição 1
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms

Also Published As

Publication number Publication date
US10532048B2 (en) 2020-01-14
PT2149561E (pt) 2016-01-07
US20170189390A1 (en) 2017-07-06
SI2149561T1 (sl) 2016-02-29
BRPI0812359A2 (pt) 2015-01-27
PL2149561T3 (pl) 2016-05-31
US20150359787A1 (en) 2015-12-17
RU2009148507A (ru) 2011-07-10
RU2479578C2 (ru) 2013-04-20
US9526719B2 (en) 2016-12-27
CN101668747A (zh) 2010-03-10
KR101830566B1 (ko) 2018-02-20
US20190000832A1 (en) 2019-01-03
KR20100020982A (ko) 2010-02-23
JP5336359B2 (ja) 2013-11-06
CY1117004T1 (el) 2017-04-05
CA2688326A1 (en) 2008-12-04
TWI425945B (zh) 2014-02-11
US9150541B2 (en) 2015-10-06
TW200911251A (en) 2009-03-16
MX2009012779A (es) 2010-02-17
KR101580298B1 (ko) 2016-01-08
CN101668747B (zh) 2012-02-01
US20140058100A1 (en) 2014-02-27
AU2008255815A1 (en) 2008-12-04
AU2008255815B2 (en) 2012-02-02
KR20160139067A (ko) 2016-12-06
ES2558677T3 (es) 2016-02-08
WO2008146774A1 (ja) 2008-12-04
ZA200908220B (en) 2011-02-23
EP2149561B1 (en) 2015-09-09
DK2149561T3 (en) 2015-12-21
JPWO2008146774A1 (ja) 2010-08-19
IL202301A0 (en) 2010-06-30
US8486970B2 (en) 2013-07-16
RS54429B1 (en) 2016-04-28
HUE026316T2 (en) 2016-06-28
IL202301A (en) 2017-07-31
KR101682638B1 (ko) 2016-12-05
KR20150090262A (ko) 2015-08-05
CA2688326C (en) 2016-07-05
US20100227866A1 (en) 2010-09-09
EP2149561A1 (en) 2010-02-03
US10016410B2 (en) 2018-07-10
EP2149561A4 (en) 2011-09-07

Similar Documents

Publication Publication Date Title
HRP20151336T1 (hr) Tetrahidroizokinolin-1-on derivat ili njegova sol
JP2015517981A5 (hr)
HRP20161547T1 (hr) Derivati 5-fluor-n-(piridin-2-il)piridin-2-amina koji sadrže sulfoksiminsku skupinu
JP2013517283A5 (hr)
JP2007519754A5 (hr)
RU2315041C2 (ru) Производные 2,6-хинолинила и 2,6-нафтила, фармацевтические композиции на их основе, их применение в качестве ингибиторов vla-4 и промежуточные соединения
JP2007516983A5 (hr)
WO2006076575B1 (en) Substituted biaryl compounds as factor xia inhibitors
JP2014506599A5 (hr)
MX2009008465A (es) Nuevas 2-aminooxazolinas como ligandos de taar1.
CA2570942A1 (en) Substituted tetrahydro-2h-isoquinolin-1-one derivatives, method for the production thereof, and use of the same as medicament
JP2010501587A5 (hr)
AR089134A1 (es) Arilos y heteroarilos biciclicos inhibidores de los canales de sodio
JP2005513123A5 (hr)
NZ614305A (en) Sulfonamide derivatives as bcl-2-selective apoptosis-inducing agents for the treatment of cancer and immune diseases
BR112012028527A2 (pt) composto de amida, composição farmacêutica e inibidor de 11â-hsd1 compreendendo o dito composto e usos do dito composto
JP2014509298A5 (hr)
JP2015516429A5 (hr)
JP2008516902A5 (hr)
WO2008015280A3 (de) Wässrige wirkstoffkonzentrate mit herbizider wirkung
IL183373A0 (en) 3-[2-(3-acylamino-2-oxo-2h-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives, pharmaceutical compositions containing the same and methods for the preparation thereof
JP2009539938A5 (hr)
JP2013542267A5 (hr)
HRP20140613T1 (hr) Novi intermedijer i postupak koji je koristan za dobivanje {2-[1-(3,5-bi-trifluorometil-benzil)-5-piridin-4-il-1h-[1,2,3]triazol-4-il]-piridin-3-il}-(2-klorofenil)-metanona
CN101547919A (zh) 新型二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途