RU2343153C2 - Производные 7-арил-3,9-диазабицикло(3.3.1)-нон-6-ена - ингибиторы ренина - Google Patents
Производные 7-арил-3,9-диазабицикло(3.3.1)-нон-6-ена - ингибиторы ренина Download PDFInfo
- Publication number
- RU2343153C2 RU2343153C2 RU2004134320/04A RU2004134320A RU2343153C2 RU 2343153 C2 RU2343153 C2 RU 2343153C2 RU 2004134320/04 A RU2004134320/04 A RU 2004134320/04A RU 2004134320 A RU2004134320 A RU 2004134320A RU 2343153 C2 RU2343153 C2 RU 2343153C2
- Authority
- RU
- Russia
- Prior art keywords
- phenyl
- diazabicyclo
- propyl
- trifluorophenoxy
- carboxylic acid
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- -1 benzo[b]thienyl Chemical group 0.000 claims abstract 75
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 54
- 239000000203 mixture Substances 0.000 claims abstract 19
- 125000000217 alkyl group Chemical group 0.000 claims abstract 17
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims abstract 14
- 150000003839 salts Chemical class 0.000 claims abstract 7
- 239000002904 solvent Substances 0.000 claims abstract 7
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 6
- 229910052736 halogen Inorganic materials 0.000 claims abstract 4
- 125000004076 pyridyl group Chemical group 0.000 claims abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 3
- 230000000694 effects Effects 0.000 claims abstract 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 3
- FTNJQNQLEGKTGD-UHFFFAOYSA-N 1,3-benzodioxole Chemical compound C1=CC=C2OCOC2=C1 FTNJQNQLEGKTGD-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims abstract 2
- 239000003814 drug Substances 0.000 claims abstract 2
- 150000002367 halogens Chemical group 0.000 claims abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims abstract 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 31
- GCJYLAWVUWEHLW-UHFFFAOYSA-N n-[(2-chlorophenyl)methyl]cyclopropanamine Chemical compound ClC1=CC=CC=C1CNC1CC1 GCJYLAWVUWEHLW-UHFFFAOYSA-N 0.000 claims 27
- SASNBVQSOZSTPD-UHFFFAOYSA-N n-methylphenethylamine Chemical compound CNCCC1=CC=CC=C1 SASNBVQSOZSTPD-UHFFFAOYSA-N 0.000 claims 17
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 15
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 15
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 9
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 7
- KJYVKUQRRKDPAX-UHFFFAOYSA-N n-[(2,3-dichlorophenyl)methyl]cyclopropanamine Chemical compound ClC1=CC=CC(CNC2CC2)=C1Cl KJYVKUQRRKDPAX-UHFFFAOYSA-N 0.000 claims 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 6
- 125000004494 ethyl ester group Chemical group 0.000 claims 6
- CRIMYHBFDHWKQY-UHFFFAOYSA-N n-[(2,3-dimethylphenyl)methyl]cyclopropanamine Chemical compound CC1=CC=CC(CNC2CC2)=C1C CRIMYHBFDHWKQY-UHFFFAOYSA-N 0.000 claims 6
- XOJVVFBFDXDTEG-UHFFFAOYSA-N pristane Chemical compound CC(C)CCCC(C)CCCC(C)CCCC(C)C XOJVVFBFDXDTEG-UHFFFAOYSA-N 0.000 claims 6
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 5
- CEQDKNLDFWAMEL-UHFFFAOYSA-N n-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]cyclopropanamine Chemical compound FC(F)(F)C1=CC=CC(CNC2CC2)=C1Cl CEQDKNLDFWAMEL-UHFFFAOYSA-N 0.000 claims 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 150000004702 methyl esters Chemical class 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- QWMNTOVGKJAROU-UHFFFAOYSA-N n-[(2-chlorophenyl)methyl]ethanamine Chemical compound CCNCC1=CC=CC=C1Cl QWMNTOVGKJAROU-UHFFFAOYSA-N 0.000 claims 4
- BTBDLUOYLCXSMK-UHFFFAOYSA-N n-[(3,5-dimethoxyphenyl)methyl]cyclopropanamine Chemical compound COC1=CC(OC)=CC(CNC2CC2)=C1 BTBDLUOYLCXSMK-UHFFFAOYSA-N 0.000 claims 4
- 235000019260 propionic acid Nutrition 0.000 claims 4
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims 4
- IVEWTCACRDEAOB-UHFFFAOYSA-N 2-(2-methoxyphenyl)acetic acid Chemical compound COC1=CC=CC=C1CC(O)=O IVEWTCACRDEAOB-UHFFFAOYSA-N 0.000 claims 3
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- HWDVTQAXQJQROO-UHFFFAOYSA-N cyclopropylazanide Chemical compound [NH-]C1CC1 HWDVTQAXQJQROO-UHFFFAOYSA-N 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- SBKDFWWYKALTKE-UHFFFAOYSA-N n-[(2-bromophenyl)methyl]cyclopropanamine Chemical compound BrC1=CC=CC=C1CNC1CC1 SBKDFWWYKALTKE-UHFFFAOYSA-N 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000003070 2-(2-chlorophenyl)ethyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000006179 2-methyl benzyl group Chemical group [H]C1=C([H])C(=C(C([H])=C1[H])C([H])([H])*)C([H])([H])[H] 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000001721 carbon Chemical group 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- CUPDQCKBQJVOMC-UHFFFAOYSA-N n-[(2-fluoro-5-methoxyphenyl)methyl]cyclopropanamine Chemical compound COC1=CC=C(F)C(CNC2CC2)=C1 CUPDQCKBQJVOMC-UHFFFAOYSA-N 0.000 claims 2
- ORZRHMRDNOCKDU-UHFFFAOYSA-N n-[(3,4-dimethoxyphenyl)methyl]cyclopropanamine Chemical compound C1=C(OC)C(OC)=CC=C1CNC1CC1 ORZRHMRDNOCKDU-UHFFFAOYSA-N 0.000 claims 2
- VALINFAZSMPKJJ-UHFFFAOYSA-N n-[(3-chlorophenyl)methyl]cyclopropanamine Chemical compound ClC1=CC=CC(CNC2CC2)=C1 VALINFAZSMPKJJ-UHFFFAOYSA-N 0.000 claims 2
- NUPAMNLYORQZRV-UHFFFAOYSA-N n-[(3-methoxyphenyl)methyl]cyclopropanamine Chemical compound COC1=CC=CC(CNC2CC2)=C1 NUPAMNLYORQZRV-UHFFFAOYSA-N 0.000 claims 2
- LJBFNXZKZYKGFY-UHFFFAOYSA-N n-[(3-methylphenyl)methyl]cyclopropanamine Chemical compound CC1=CC=CC(CNC2CC2)=C1 LJBFNXZKZYKGFY-UHFFFAOYSA-N 0.000 claims 2
- ANCFTHKEGKDXKD-UHFFFAOYSA-N n-[[3-(trifluoromethoxy)phenyl]methyl]cyclopropanamine Chemical compound FC(F)(F)OC1=CC=CC(CNC2CC2)=C1 ANCFTHKEGKDXKD-UHFFFAOYSA-N 0.000 claims 2
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- UGRMITBWUVWUEB-UHFFFAOYSA-N 1-$l^{1}-oxidanyl-3-methylbenzene Chemical group CC1=CC=CC([O])=C1 UGRMITBWUVWUEB-UHFFFAOYSA-N 0.000 claims 1
- DTJKAALGEAHUIV-UHFFFAOYSA-N 2-(2-chlorophenyl)-n-methylethanamine Chemical compound CNCCC1=CC=CC=C1Cl DTJKAALGEAHUIV-UHFFFAOYSA-N 0.000 claims 1
- UCAUHTUMXIYKFJ-UHFFFAOYSA-N 2-(2-methoxyphenyl)-n-methylethanamine Chemical compound CNCCC1=CC=CC=C1OC UCAUHTUMXIYKFJ-UHFFFAOYSA-N 0.000 claims 1
- HNJWKRMESUMDQE-UHFFFAOYSA-N 2-(3,4-dimethoxyphenyl)-n-methylethanamine Chemical compound CNCCC1=CC=C(OC)C(OC)=C1 HNJWKRMESUMDQE-UHFFFAOYSA-N 0.000 claims 1
- ZAIUACXHBBABJZ-UHFFFAOYSA-N 2-(3-chlorophenyl)-n-methylethanamine Chemical compound CNCCC1=CC=CC(Cl)=C1 ZAIUACXHBBABJZ-UHFFFAOYSA-N 0.000 claims 1
- MCGDBHZRFQKLBT-UHFFFAOYSA-N 2-(3-methoxyphenyl)-n-methylethanamine Chemical compound CNCCC1=CC=CC(OC)=C1 MCGDBHZRFQKLBT-UHFFFAOYSA-N 0.000 claims 1
- VCSUCPDSYSXLEX-UHFFFAOYSA-N 2-(4-chlorophenyl)-n-methylethanamine Chemical compound CNCCC1=CC=C(Cl)C=C1 VCSUCPDSYSXLEX-UHFFFAOYSA-N 0.000 claims 1
- SOUBMUUVTHTRBB-UHFFFAOYSA-N CC(C)(C(Cl)(Cl)Cl)OC(C)(C)C(Cl)(Cl)Cl Chemical compound CC(C)(C(Cl)(Cl)Cl)OC(C)(C)C(Cl)(Cl)Cl SOUBMUUVTHTRBB-UHFFFAOYSA-N 0.000 claims 1
- HTTQMLBCRUJDSN-ZNLMSAFMSA-N C[C@@H](CC(N([C@H](C1)CNC2)[C@H]2C(C(O)=O)=C1C1=CC=C(CC(C)OC(C(F)=CC=C2F)=C2F)C=C1)=O)O.ClC1=C(CNC2CC2)C=CC=C1 Chemical compound C[C@@H](CC(N([C@H](C1)CNC2)[C@H]2C(C(O)=O)=C1C1=CC=C(CC(C)OC(C(F)=CC=C2F)=C2F)C=C1)=O)O.ClC1=C(CNC2CC2)C=CC=C1 HTTQMLBCRUJDSN-ZNLMSAFMSA-N 0.000 claims 1
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 claims 1
- JCMWSVNNSPUNER-UHFFFAOYSA-N N,O-dimethyltyramine Chemical compound CNCCC1=CC=C(OC)C=C1 JCMWSVNNSPUNER-UHFFFAOYSA-N 0.000 claims 1
- CDDQBIWIOSSSDK-ORLCUPCUSA-N N[C@@H](CO)C(N1C[C@H](C(C(O)=O)=C(C2)C3=CC=C(CCCOC(C(F)=CC=C4F)=C4F)C=C3)N[C@H]2C1)=O.ClC1=C(CNC2CC2)C=CC=C1 Chemical compound N[C@@H](CO)C(N1C[C@H](C(C(O)=O)=C(C2)C3=CC=C(CCCOC(C(F)=CC=C4F)=C4F)C=C3)N[C@H]2C1)=O.ClC1=C(CNC2CC2)C=CC=C1 CDDQBIWIOSSSDK-ORLCUPCUSA-N 0.000 claims 1
- BHHGXPLMPWCGHP-UHFFFAOYSA-N Phenethylamine Chemical compound NCCC1=CC=CC=C1 BHHGXPLMPWCGHP-UHFFFAOYSA-N 0.000 claims 1
- 125000005605 benzo group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- HROUFMHZMXWOHI-UHFFFAOYSA-N n-(1,3-benzodioxol-5-ylmethyl)cyclopropanamine Chemical compound C=1C=C2OCOC2=CC=1CNC1CC1 HROUFMHZMXWOHI-UHFFFAOYSA-N 0.000 claims 1
- ILHIZUJWNGLALK-UHFFFAOYSA-N n-(2-phenylethyl)cyclopropanamine Chemical compound C1CC1NCCC1=CC=CC=C1 ILHIZUJWNGLALK-UHFFFAOYSA-N 0.000 claims 1
- VNFABSKAJCALBZ-UHFFFAOYSA-N n-[(2-chloro-6-fluorophenyl)methyl]cyclopropanamine Chemical compound FC1=CC=CC(Cl)=C1CNC1CC1 VNFABSKAJCALBZ-UHFFFAOYSA-N 0.000 claims 1
- UZYPFBRRGVZJNV-UHFFFAOYSA-N n-[(2-fluorophenyl)methyl]cyclopropanamine Chemical compound FC1=CC=CC=C1CNC1CC1 UZYPFBRRGVZJNV-UHFFFAOYSA-N 0.000 claims 1
- WYQUCNZBUBLJHN-UHFFFAOYSA-N n-[(2-methylphenyl)methyl]cyclopropanamine Chemical compound CC1=CC=CC=C1CNC1CC1 WYQUCNZBUBLJHN-UHFFFAOYSA-N 0.000 claims 1
- WRRVCXHKEDNRNB-UHFFFAOYSA-N n-[(3,5-difluorophenyl)methyl]cyclopropanamine Chemical compound FC1=CC(F)=CC(CNC2CC2)=C1 WRRVCXHKEDNRNB-UHFFFAOYSA-N 0.000 claims 1
- VRDMJNOXKZMLTF-UHFFFAOYSA-N n-[(6-chloro-1,3-benzodioxol-5-yl)methyl]cyclopropanamine Chemical compound ClC1=CC=2OCOC=2C=C1CNC1CC1 VRDMJNOXKZMLTF-UHFFFAOYSA-N 0.000 claims 1
- NJHZDGHFBLATGX-UHFFFAOYSA-N n-[2-(2-chlorophenyl)ethyl]cyclopropanamine Chemical compound ClC1=CC=CC=C1CCNC1CC1 NJHZDGHFBLATGX-UHFFFAOYSA-N 0.000 claims 1
- AOMAZSZEDRDSIF-UHFFFAOYSA-N n-[[3-(trifluoromethyl)phenyl]methyl]cyclopropanamine Chemical compound FC(F)(F)C1=CC=CC(CNC2CC2)=C1 AOMAZSZEDRDSIF-UHFFFAOYSA-N 0.000 claims 1
- USBAUXJPPHVCTF-UHFFFAOYSA-N n-benzylcyclopropanamine Chemical compound C=1C=CC=CC=1CNC1CC1 USBAUXJPPHVCTF-UHFFFAOYSA-N 0.000 claims 1
- WOHOHPONCSKXSQ-UHFFFAOYSA-N n-ethyl-2-phenylethanamine Chemical compound CCNCCC1=CC=CC=C1 WOHOHPONCSKXSQ-UHFFFAOYSA-N 0.000 claims 1
- MLHBZVFOTDJTPK-UHFFFAOYSA-N n-methyl-3-phenylpropan-1-amine Chemical compound CNCCCC1=CC=CC=C1 MLHBZVFOTDJTPK-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 239000002461 renin inhibitor Substances 0.000 claims 1
- 229940086526 renin-inhibitors Drugs 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000001647 Renal Insufficiency Diseases 0.000 abstract 1
- 125000003787 chinoxalinyl group Chemical group 0.000 abstract 1
- 201000006370 kidney failure Diseases 0.000 abstract 1
- CPJSUEIXXCENMM-UHFFFAOYSA-N phenacetin Chemical compound CCOC1=CC=C(NC(C)=O)C=C1 CPJSUEIXXCENMM-UHFFFAOYSA-N 0.000 abstract 1
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- 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
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged 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
- A61K31/495—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
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0204705 | 2002-04-29 | ||
| EPPCT/EP02/04705 | 2002-04-29 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2004134320A RU2004134320A (ru) | 2005-08-27 |
| RU2343153C2 true RU2343153C2 (ru) | 2009-01-10 |
Family
ID=29286070
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004134320/04A RU2343153C2 (ru) | 2002-04-29 | 2003-04-08 | Производные 7-арил-3,9-диазабицикло(3.3.1)-нон-6-ена - ингибиторы ренина |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7427613B2 (enExample) |
| EP (1) | EP1501830B1 (enExample) |
| JP (1) | JP4041123B2 (enExample) |
| KR (1) | KR100783863B1 (enExample) |
| CN (1) | CN1649870A (enExample) |
| AT (1) | ATE527261T1 (enExample) |
| AU (1) | AU2003233963B2 (enExample) |
| BR (1) | BR0309498A (enExample) |
| CA (1) | CA2483241C (enExample) |
| CL (1) | CL2003002042A1 (enExample) |
| CO (1) | CO5631443A2 (enExample) |
| EC (1) | ECSP045378A (enExample) |
| ES (1) | ES2372931T3 (enExample) |
| HR (1) | HRP20041132A2 (enExample) |
| IL (1) | IL164767A0 (enExample) |
| IS (1) | IS7545A (enExample) |
| MA (1) | MA27305A1 (enExample) |
| MX (1) | MXPA04010608A (enExample) |
| NO (1) | NO20045042L (enExample) |
| NZ (1) | NZ536750A (enExample) |
| PL (1) | PL372141A1 (enExample) |
| RU (1) | RU2343153C2 (enExample) |
| TW (1) | TW200514786A (enExample) |
| UA (1) | UA80821C2 (enExample) |
| WO (1) | WO2003093267A1 (enExample) |
| ZA (1) | ZA200408283B (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004234040A1 (en) * | 2003-04-28 | 2004-11-11 | Actelion Pharmaceuticals Ltd | Diazabicyclononene and tetrahydropyridine derivatives as renin inhibitors |
| RU2005137174A (ru) * | 2003-04-30 | 2006-03-27 | Актелион Фармасьютикалз Лтд. (Ch) | Азабициклононеновые производные |
| WO2004096799A1 (en) * | 2003-04-30 | 2004-11-11 | Actelion Pharmaceuticals Ltd | Tropane derivatives and their use as ace inhibitors |
| EP1622685A1 (en) * | 2003-04-30 | 2006-02-08 | Actelion Pharmaceuticals Ltd. | 9-azabicyclo[3.3.1]non-6-ene derivatives with a heteroatom at the 3-position as renin inhibitors |
| KR20060015573A (ko) * | 2003-05-02 | 2006-02-17 | 액테리온 파마슈티칼 리미티드 | 신규한 디아자비시클로노넨 유도체 |
| WO2004105762A1 (en) * | 2003-05-30 | 2004-12-09 | Actelion Pharmaceuticals Ltd | Medical use of diazabicyclononene derivatives as inhibitors of parasite aspartic proteases |
| WO2005040120A1 (en) * | 2003-10-09 | 2005-05-06 | Actelion Pharmaceuticals Ltd | Tetrahydropyridine derivatives |
| JP2007508262A (ja) * | 2003-10-13 | 2007-04-05 | アクテリオン ファマシューティカルズ リミテッド | 新規ジアザビシクロノネン誘導体およびその使用 |
| JP2007509099A (ja) * | 2003-10-23 | 2007-04-12 | アクテリオン ファマシューティカルズ リミテッド | 新規ジアザビシクロノネンおよび新規極性側鎖を有するテトラヒドロピリジン誘導体 |
| WO2005054243A1 (en) * | 2003-12-05 | 2005-06-16 | Actelion Pharmaceuticals Ltd | Diazabicyclononene derivatives and their use as renin inhibitors |
| AU2004295092A1 (en) * | 2003-12-05 | 2005-06-16 | Actelion Pharmaceuticals Ltd. | Azabicyclooctene and other tetrahydropyridine derivatives with a new side-chain |
| WO2006021403A1 (en) * | 2004-08-25 | 2006-03-02 | Actelion Pharmaceuticals Ltd | Bicyclononene derivatives |
| ATE462703T1 (de) * | 2004-08-25 | 2010-04-15 | Actelion Pharmaceuticals Ltd | Bicyclononen-derivate als renin-inhibitoren |
| WO2006021399A2 (en) * | 2004-08-25 | 2006-03-02 | Actelion Pharmaceuticals Ltd | Azabicyclononene derivatives as renin inhibitors |
| WO2006021401A2 (en) * | 2004-08-25 | 2006-03-02 | Actelion Pharmaceuticals Ltd | Bicylononene derivatives |
| AR052263A1 (es) * | 2004-12-08 | 2007-03-07 | Actelion Pharmaceuticals Ltd | Derivado de diazabiciclononeno |
| WO2006063610A1 (en) * | 2004-12-17 | 2006-06-22 | Actelion Pharmaceuticals Ltd | Heteroaryl substituted diazabicyclononene derivatives |
| GB0428526D0 (en) | 2004-12-30 | 2005-02-09 | Novartis Ag | Organic compounds |
| ATE514697T1 (de) * | 2005-01-28 | 2011-07-15 | Actelion Pharmaceuticals Ltd | 7-ä4-ä2-(2,6-dichloro-4- methylphenoxy)ethoxyüphenylü-3,9- diazabicycloä3.3.1ünon-6-ene-6-carbonsäure- cyclopropyl-(2,3-dimethylbenzyl)amid als renin- hemmer für die behandlung von bluthochdruck |
| BRPI0609890A2 (pt) * | 2005-05-27 | 2010-05-04 | Actelion Pharmaceuticals Ltd | composto, composição farmacêutica, e, uso de um composto |
| GB0514203D0 (en) | 2005-07-11 | 2005-08-17 | Novartis Ag | Organic compounds |
| PT2420491E (pt) | 2005-12-30 | 2013-10-14 | Novartis Ag | Compostos de piperidina 3,5-substituída como inibidores de renina |
| RU2425032C2 (ru) | 2006-02-02 | 2011-07-27 | Актелион Фармасьютикалз Лтд | Вторичные амины в качестве ингибиторов ренина |
| CL2007000595A1 (es) * | 2006-03-08 | 2008-01-04 | Actelion Pharmaceuticals Ltd | Compuestos derivados de piperidina; composicion farmaceutica y uso para el tratamiento y/o profilaxis de enfermedades seleccionadas entre hipertension, insuficiencia cardiaca congestiva e insuficiencia renal entre otras. |
| US8343968B2 (en) | 2007-05-24 | 2013-01-01 | Merck Canada Inc. | Case of renin inhibitors |
| WO2009000811A1 (en) | 2007-06-25 | 2008-12-31 | Novartis Ag | N5-(2-ethoxyethyl)-n3-(2-pyridinyl)-3,5-piperidinedicarboxamide derivatives for use as renin inhibitors |
| WO2009023964A1 (en) | 2007-08-20 | 2009-02-26 | Merck Frosst Canada Ltd. | Renin inhibitors |
| CA2722734C (en) | 2008-05-05 | 2013-11-05 | Merck Frosst Canada Ltd. | 3,4-substituted piperidine derivatives as renin inhibitors |
| CN109721613B (zh) * | 2017-10-27 | 2021-07-30 | 四川科伦博泰生物医药股份有限公司 | 含季铵离子的大环酰胺化合物及其药物组合物和用途 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3509161A (en) * | 1967-07-10 | 1970-04-28 | Boehringer & Soehne Gmbh | 3-phenyl-granatene-(2)-derivatives |
| RU2124013C1 (ru) * | 1993-06-04 | 1998-12-27 | Эли Лилли Энд Компани | Способ получения кристаллического моногидрата лоракарбефа из кристаллического дигидрата лоракарбефа |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9020927D0 (en) | 1990-09-26 | 1990-11-07 | Beecham Group Plc | Pharmaceuticals |
| US5268361A (en) * | 1991-06-07 | 1993-12-07 | Sri International | Hydroxyazido derivatives and related compounds as renin inhibitors |
| KR100384979B1 (ko) | 1995-09-07 | 2003-10-17 | 에프. 호프만-라 로슈 아게 | 심부전증및신부전증치료용의신규한4-(옥시알콕시페닐)-3-옥시-피페리딘 |
| WO1998039328A1 (en) | 1997-03-03 | 1998-09-11 | F.Hoffmann-La Roche Ag | Substituted 2,4-diaminopyrimidines |
| US20060223795A1 (en) * | 2003-05-02 | 2006-10-05 | Oliver Bezencon | Novel diazabicyclononene derivatives |
| WO2005054243A1 (en) * | 2003-12-05 | 2005-06-16 | Actelion Pharmaceuticals Ltd | Diazabicyclononene derivatives and their use as renin inhibitors |
-
2003
- 2003-04-08 AU AU2003233963A patent/AU2003233963B2/en not_active Ceased
- 2003-04-08 RU RU2004134320/04A patent/RU2343153C2/ru not_active IP Right Cessation
- 2003-04-08 AT AT03727287T patent/ATE527261T1/de not_active IP Right Cessation
- 2003-04-08 ES ES03727287T patent/ES2372931T3/es not_active Expired - Lifetime
- 2003-04-08 US US10/513,103 patent/US7427613B2/en not_active Expired - Fee Related
- 2003-04-08 MX MXPA04010608A patent/MXPA04010608A/es not_active Application Discontinuation
- 2003-04-08 CA CA2483241A patent/CA2483241C/en not_active Expired - Fee Related
- 2003-04-08 EP EP03727287A patent/EP1501830B1/en not_active Expired - Lifetime
- 2003-04-08 WO PCT/EP2003/003721 patent/WO2003093267A1/en not_active Ceased
- 2003-04-08 HR HR20041132A patent/HRP20041132A2/xx not_active Application Discontinuation
- 2003-04-08 PL PL03372141A patent/PL372141A1/xx not_active Application Discontinuation
- 2003-04-08 JP JP2004501406A patent/JP4041123B2/ja not_active Expired - Fee Related
- 2003-04-08 KR KR1020047016845A patent/KR100783863B1/ko not_active Expired - Fee Related
- 2003-04-08 NZ NZ536750A patent/NZ536750A/xx unknown
- 2003-04-08 IL IL16476703A patent/IL164767A0/xx unknown
- 2003-04-08 BR BR0309498-7A patent/BR0309498A/pt not_active IP Right Cessation
- 2003-04-08 CN CNA038097664A patent/CN1649870A/zh active Pending
- 2003-08-04 UA UA20041109469A patent/UA80821C2/uk unknown
- 2003-10-10 CL CL200302042A patent/CL2003002042A1/es unknown
- 2003-10-23 TW TW092129421A patent/TW200514786A/zh unknown
-
2004
- 2004-10-13 ZA ZA200408283A patent/ZA200408283B/xx unknown
- 2004-10-22 MA MA27914A patent/MA27305A1/fr unknown
- 2004-10-22 CO CO04106347A patent/CO5631443A2/es not_active Application Discontinuation
- 2004-10-22 EC EC2004005378A patent/ECSP045378A/es unknown
- 2004-11-19 NO NO20045042A patent/NO20045042L/no not_active Application Discontinuation
- 2004-11-22 IS IS7545A patent/IS7545A/is unknown
-
2008
- 2008-07-07 US US12/168,666 patent/US20080312242A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3509161A (en) * | 1967-07-10 | 1970-04-28 | Boehringer & Soehne Gmbh | 3-phenyl-granatene-(2)-derivatives |
| RU2124013C1 (ru) * | 1993-06-04 | 1998-12-27 | Эли Лилли Энд Компани | Способ получения кристаллического моногидрата лоракарбефа из кристаллического дигидрата лоракарбефа |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1501830A1 (en) | 2005-02-02 |
| CA2483241A1 (en) | 2003-11-13 |
| TW200514786A (en) | 2005-05-01 |
| ES2372931T3 (es) | 2012-01-27 |
| JP2005527602A (ja) | 2005-09-15 |
| ECSP045378A (es) | 2004-11-26 |
| KR20040101546A (ko) | 2004-12-02 |
| NZ536750A (en) | 2007-02-23 |
| BR0309498A (pt) | 2005-02-15 |
| AU2003233963B2 (en) | 2008-09-11 |
| US20080312242A1 (en) | 2008-12-18 |
| MXPA04010608A (es) | 2004-12-13 |
| PL372141A1 (en) | 2005-07-11 |
| CO5631443A2 (es) | 2006-04-28 |
| HRP20041132A2 (en) | 2006-07-31 |
| ATE527261T1 (de) | 2011-10-15 |
| RU2004134320A (ru) | 2005-08-27 |
| CA2483241C (en) | 2011-05-31 |
| IL164767A0 (en) | 2005-12-18 |
| ZA200408283B (en) | 2006-05-31 |
| UA80821C2 (en) | 2007-11-12 |
| CN1649870A (zh) | 2005-08-03 |
| WO2003093267A1 (en) | 2003-11-13 |
| JP4041123B2 (ja) | 2008-01-30 |
| NO20045042L (no) | 2004-11-19 |
| CL2003002042A1 (es) | 2005-02-04 |
| EP1501830B1 (en) | 2011-10-05 |
| AU2003233963A1 (en) | 2003-11-17 |
| US20050176700A1 (en) | 2005-08-11 |
| MA27305A1 (fr) | 2005-05-02 |
| KR100783863B1 (ko) | 2007-12-10 |
| IS7545A (is) | 2004-11-22 |
| US7427613B2 (en) | 2008-09-23 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2343153C2 (ru) | Производные 7-арил-3,9-диазабицикло(3.3.1)-нон-6-ена - ингибиторы ренина | |
| JP2005527602A5 (enExample) | ||
| RU2005102002A (ru) | Новые производные тетрагидропиридина | |
| RU2320648C2 (ru) | 4,6,7,13-замещенные производные 1-бензил-изохинолина и фармацевтическая композиция, обладающая ингибирующей активностью в отношении гфат | |
| US20240293363A1 (en) | Methods and compositions for improving cognitive function | |
| RU2379292C2 (ru) | Производные пиразола в качестве ингибиторов фосфодиэстеразы 4 | |
| RU2010139806A (ru) | Новые производные пирроло[3,2-d]пиримидин-4-она и их применение в терапии | |
| JP2005532371A5 (enExample) | ||
| AU2022221492A1 (en) | Methods and compositions for improving cognitive function | |
| RU2002117450A (ru) | Новые гетероциклические соединения и их соли и их применение в медицине | |
| RU2006101999A (ru) | Средство для лечения шизофрении на основе гидрированных пиридо(4,3-b)индолов (варианты), фармакологическое средство на его основе и способ его применения | |
| CA2353460A1 (en) | Carboxylic acids and carboxylic acid isosteres of n-heterocyclic compounds | |
| RU2000101813A (ru) | Сульфонамидное соединение | |
| RU2004118719A (ru) | Производные пиперидин-2-она и фармацевтические композиции, содержащие такие соединения в качестве активного ингредиента | |
| JP2009528389A5 (enExample) | ||
| EP2968237A1 (en) | Methods and compositions for improving cognitive function | |
| CA2560293A1 (en) | Substituted 1,4,8-triazaspiro[4.5]decan-2-on compounds | |
| RU2005136986A (ru) | Новые 3,4-дизамещенные производные 1,2,3,6-тетрагидропиридина | |
| AU2004204355B2 (en) | PDE4 inhibitors for the treatment of neoplasms of lymphoid cells | |
| RU2011124960A (ru) | Ингибиторы гликогенсинтаза-киназы 3-бета, содержащие производные 7-гидроксибензоимидазол-4-илметанова | |
| RU2008152181A (ru) | Производные пирролидина, применимые при лечении болезней, которые зависят от активности ренина | |
| RU2024113277A (ru) | Конденсированные бициклические гетероарильные соединения, применимые в качестве ингибиторов nlrp3 | |
| EA044839B1 (ru) | Способы и композиции для улучшения когнитивной функции | |
| RU2005112774A (ru) | Производные пятичленных гетероциклов, способ их получения и их применение в качестве лекарственных средств |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20090409 |