JP2014502979A5 - - Google Patents
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- JP2014502979A5 JP2014502979A5 JP2013549707A JP2013549707A JP2014502979A5 JP 2014502979 A5 JP2014502979 A5 JP 2014502979A5 JP 2013549707 A JP2013549707 A JP 2013549707A JP 2013549707 A JP2013549707 A JP 2013549707A JP 2014502979 A5 JP2014502979 A5 JP 2014502979A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- substituted
- aryl
- cycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000003118 aryl group Chemical group 0.000 claims 51
- 125000001475 halogen functional group Chemical group 0.000 claims 47
- 125000000217 alkyl group Chemical group 0.000 claims 41
- 150000001875 compounds Chemical class 0.000 claims 38
- 125000000753 cycloalkyl group Chemical group 0.000 claims 34
- 125000001424 substituent group Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 239000003814 drug Substances 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- 206010020772 Hypertension Diseases 0.000 claims 4
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- SHIPWMSSVUHKSG-UHFFFAOYSA-N 1-[1-[3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl]indazol-4-yl]-3-methylsulfonylurea Chemical compound N1=CC2=C(NC(=O)NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(Cl)C=C1 SHIPWMSSVUHKSG-UHFFFAOYSA-N 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000016998 Conn syndrome Diseases 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 206010020571 Hyperaldosteronism Diseases 0.000 claims 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 206010028594 Myocardial fibrosis Diseases 0.000 claims 2
- 208000004880 Polyuria Diseases 0.000 claims 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 2
- 208000001647 Renal Insufficiency Diseases 0.000 claims 2
- 206010041277 Sodium retention Diseases 0.000 claims 2
- 241000209149 Zea Species 0.000 claims 2
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 claims 2
- 235000002017 Zea mays subsp mays Nutrition 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 206010003119 arrhythmia Diseases 0.000 claims 2
- 230000006793 arrhythmia Effects 0.000 claims 2
- 150000003943 catecholamines Chemical class 0.000 claims 2
- 235000005822 corn Nutrition 0.000 claims 2
- 230000003205 diastolic effect Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000035619 diuresis Effects 0.000 claims 2
- 230000029142 excretion Effects 0.000 claims 2
- 201000006370 kidney failure Diseases 0.000 claims 2
- 239000011777 magnesium Substances 0.000 claims 2
- 229910052749 magnesium Inorganic materials 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- MFVSIGTZCBDQNQ-UHFFFAOYSA-N n-[1-[1-(4-chlorophenyl)-1-(1-hydroxycyclopropyl)propyl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C1(O)CC1)(CC)C1=CC=C(Cl)C=C1 MFVSIGTZCBDQNQ-UHFFFAOYSA-N 0.000 claims 2
- WJAQRAZQVWRUDA-UHFFFAOYSA-N n-[1-[1-(4-chlorophenyl)-1-(2-cyanocyclopropyl)propyl]indazol-4-yl]methanesulfonamide Chemical compound C=1C=C(Cl)C=CC=1C(N1C2=CC=CC(NS(C)(=O)=O)=C2C=N1)(CC)C1CC1C#N WJAQRAZQVWRUDA-UHFFFAOYSA-N 0.000 claims 2
- CJPUIMBIYSFFNZ-UHFFFAOYSA-N n-[1-[1-(4-chlorophenyl)-1-(3-ethyl-1,2,4-oxadiazol-5-yl)propyl]indol-4-yl]methanesulfonamide Chemical compound CCC1=NOC(C(CC)(C=2C=CC(Cl)=CC=2)N2C3=CC=CC(NS(C)(=O)=O)=C3C=C2)=N1 CJPUIMBIYSFFNZ-UHFFFAOYSA-N 0.000 claims 2
- BLEKXSOYNCRHJN-UHFFFAOYSA-N n-[1-[2-(4-chlorophenyl)-1-hydroxybutan-2-yl]-2,3-dihydroindol-4-yl]methanesulfonamide Chemical compound C1CC(C(=CC=C2)NS(C)(=O)=O)=C2N1C(CO)(CC)C1=CC=C(Cl)C=C1 BLEKXSOYNCRHJN-UHFFFAOYSA-N 0.000 claims 2
- MFVGPPNQHPWGHH-UHFFFAOYSA-N n-[1-[2-(4-chlorophenyl)-1-hydroxybutan-2-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CO)(CC)C1=CC=C(Cl)C=C1 MFVGPPNQHPWGHH-UHFFFAOYSA-N 0.000 claims 2
- VAXYUCJZSOERFN-UHFFFAOYSA-N n-[1-[2-amino-3-(4-chlorophenyl)pentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)N)(CC)C1=CC=C(Cl)C=C1 VAXYUCJZSOERFN-UHFFFAOYSA-N 0.000 claims 2
- MPFHSFBLSWLVNH-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-hydroxypentan-3-yl]-6-fluoroindol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(C(C)O)(CC)C1=CC=C(Cl)C=C1 MPFHSFBLSWLVNH-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000011591 potassium Substances 0.000 claims 2
- 229910052700 potassium Inorganic materials 0.000 claims 2
- 208000013846 primary aldosteronism Diseases 0.000 claims 2
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 claims 1
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- XKDXIJIYBQRHLO-UHFFFAOYSA-N N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(C(F)(F)F)C=C1 Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(C(F)(F)F)C=C1 XKDXIJIYBQRHLO-UHFFFAOYSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 229960002478 aldosterone Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- ACWKJSZJAGAKFW-UHFFFAOYSA-N n-[1-(1-cyano-3-phenylpentan-3-yl)-6-fluoroindazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(CCC#N)(CC)C1=CC=CC=C1 ACWKJSZJAGAKFW-UHFFFAOYSA-N 0.000 claims 1
- KPNWZECOXIHMCY-RUDMXATFSA-N n-[1-[(e)-3-(4-chlorophenyl)-1-cyanopent-1-en-3-yl]-6-fluoroindazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(\C=C\C#N)(CC)C1=CC=C(Cl)C=C1 KPNWZECOXIHMCY-RUDMXATFSA-N 0.000 claims 1
- YTFLEIJWHIGTBJ-UHFFFAOYSA-N n-[1-[1-cyano-3-(4-methoxyphenyl)pentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCC#N)(CC)C1=CC=C(OC)C=C1 YTFLEIJWHIGTBJ-UHFFFAOYSA-N 0.000 claims 1
- GDMIJALDCNMNQA-UHFFFAOYSA-N n-[1-[1-cyano-3-[4-(trifluoromethyl)phenyl]pentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCC#N)(CC)C1=CC=C(C(F)(F)F)C=C1 GDMIJALDCNMNQA-UHFFFAOYSA-N 0.000 claims 1
- SGVBASQJFIRYMK-UHFFFAOYSA-N n-[1-[2-(4-chlorophenyl)-1-methoxybutan-2-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(COC)(CC)C1=CC=C(Cl)C=C1 SGVBASQJFIRYMK-UHFFFAOYSA-N 0.000 claims 1
- GKBSBEVPPBUZJM-UHFFFAOYSA-N n-[1-[2-hydroxy-3-[4-(trifluoromethyl)phenyl]pentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)O)(CC)C1=CC=C(C(F)(F)F)C=C1 GKBSBEVPPBUZJM-UHFFFAOYSA-N 0.000 claims 1
- IJYBFZDFUPLFBM-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-1-cyanopentan-3-yl]-6-fluoroindol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(CCC#N)(CC)C1=CC=C(Cl)C=C1 IJYBFZDFUPLFBM-UHFFFAOYSA-N 0.000 claims 1
- MEYHTWPUOMJOCY-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-1-cyanopentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCC#N)(CC)C1=CC=C(Cl)C=C1 MEYHTWPUOMJOCY-UHFFFAOYSA-N 0.000 claims 1
- YEHIJPNUIZWGGR-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-1-cyanopentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCC#N)(CC)C1=CC=C(Cl)C=C1 YEHIJPNUIZWGGR-UHFFFAOYSA-N 0.000 claims 1
- MEWKDHXUQFVKCB-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-1-hydroxypentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCO)(CC)C1=CC=C(Cl)C=C1 MEWKDHXUQFVKCB-UHFFFAOYSA-N 0.000 claims 1
- RFDLKVRSKTZRCU-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl]-6-fluoroindol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(C(C)(C)O)(CC)C1=CC=C(Cl)C=C1 RFDLKVRSKTZRCU-UHFFFAOYSA-N 0.000 claims 1
- XTYMFUDXUREQRD-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(Cl)C=C1 XTYMFUDXUREQRD-UHFFFAOYSA-N 0.000 claims 1
- JOXVIBCCAPTBEO-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(Cl)C=C1 JOXVIBCCAPTBEO-UHFFFAOYSA-N 0.000 claims 1
- WPKHBXGUDHAVIU-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-oxopentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)=O)(CC)C1=CC=C(Cl)C=C1 WPKHBXGUDHAVIU-UHFFFAOYSA-N 0.000 claims 1
- LMIREAGAYXEEGR-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-6-hydroxyhexan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCCO)(CC)C1=CC=C(Cl)C=C1 LMIREAGAYXEEGR-UHFFFAOYSA-N 0.000 claims 1
- MQLOOLGWCJSOPP-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)pentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CC)(CC)C1=CC=C(Cl)C=C1 MQLOOLGWCJSOPP-UHFFFAOYSA-N 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 0 *C(*)(*)[n]1ncc2c1cccc2* Chemical compound *C(*)(*)[n]1ncc2c1cccc2* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161434543P | 2011-01-20 | 2011-01-20 | |
| US61/434,543 | 2011-01-20 | ||
| PCT/CN2012/070597 WO2012097744A1 (en) | 2011-01-20 | 2012-01-19 | Mineralocorticoid receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014502979A JP2014502979A (ja) | 2014-02-06 |
| JP2014502979A5 true JP2014502979A5 (enExample) | 2015-02-26 |
| JP6078004B2 JP6078004B2 (ja) | 2017-02-08 |
Family
ID=46515166
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013549707A Expired - Fee Related JP6078004B2 (ja) | 2011-01-20 | 2012-01-19 | ミネラルコルチコイド受容体拮抗薬 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US8933113B2 (enExample) |
| EP (1) | EP2665707B1 (enExample) |
| JP (1) | JP6078004B2 (enExample) |
| KR (1) | KR20140009291A (enExample) |
| CN (1) | CN103384661B (enExample) |
| AU (1) | AU2012208837B2 (enExample) |
| CA (1) | CA2824344A1 (enExample) |
| ES (1) | ES2618812T3 (enExample) |
| MX (1) | MX351305B (enExample) |
| RU (1) | RU2598842C2 (enExample) |
| WO (1) | WO2012097744A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20140009291A (ko) * | 2011-01-20 | 2014-01-22 | 머크 샤프 앤드 돔 코포레이션 | 미네랄로코르티코이드 수용체 길항제 |
| WO2013135674A1 (en) * | 2012-03-12 | 2013-09-19 | Syngenta Participations Ag | Insecticidal 2-aryl-acetamide compounds |
| IN2014KN02993A (enExample) | 2012-07-17 | 2015-05-08 | Glaxosmithkline Ip No 2 Ltd | |
| AR091731A1 (es) | 2012-07-19 | 2015-02-25 | Merck Sharp & Dohme | Antagonistas del receptor de mineralocorticoides |
| JP6371284B2 (ja) | 2012-08-22 | 2018-08-08 | コーネル ユニヴァーシティー | ファスシンを阻害する方法 |
| US9522141B2 (en) | 2012-12-20 | 2016-12-20 | Merck Sharp & Dohme Corp. | Indazole compounds as aldosterone synthase inhibitors |
| TWI667233B (zh) | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
| EP3097077A1 (en) * | 2014-01-21 | 2016-11-30 | Glaxosmithkline Intellectual Property (No. 2) Limited | Crystalline forms of (r)-1 -(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)indoline-5-carbonitrile |
| CA2940144C (en) | 2014-02-20 | 2023-06-13 | Cornell University | Substituted indazol-3-yl derivatives and pharmaceutical compositions thereof useful as inhibitor of fascin |
| IL286839B (en) | 2016-02-19 | 2022-08-01 | Pmv Pharmaceuticals Inc | Propyne-indole compounds |
| WO2018069148A1 (de) | 2016-10-11 | 2018-04-19 | Bayer Pharma Aktiengesellschaft | Kombination enthaltend sgc aktivatoren und mineralocorticoid-rezeptor-antagonisten |
| CA3039734A1 (en) | 2016-10-11 | 2018-04-19 | Bayer Pharma Aktiengesellschaft | Combination containing sgc stimulators and mineralocorticoid receptor antagonists |
| WO2018153898A1 (de) | 2017-02-22 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Selektive partielle adenosin a1 rezeptor-agonisten in kombination mit mineralocorticoid-rezeptor-antagonisten |
| DE102017008472A1 (de) | 2017-09-08 | 2018-05-03 | Bayer Pharma Aktiengesellschaft | Kombination enthaltend PDE5 Inhibitoren und Mineralocorticoid-Rezeptor-Antagonisten |
| EP3886854A4 (en) | 2018-11-30 | 2022-07-06 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| KR20210153056A (ko) | 2019-03-18 | 2021-12-16 | 리네트 케이. 니만 | 인슐린 감수성 개선 방법 |
| KR102838154B1 (ko) | 2019-09-23 | 2025-07-28 | 피엠브이 파마슈티컬스 인코포레이티드 | 돌연변이체 p53 기능을 회복시키기 위한 방법 및 화합물 |
| CA3096145A1 (en) * | 2019-10-11 | 2021-04-11 | Royal Bank Of Canada | System and method of machine learning using embedding networks |
| MX2022015793A (es) | 2020-06-24 | 2023-02-27 | Pmv Pharmaceuticals Inc | Terapia de combinacion para tratamiento de cancer. |
| CN111675646B (zh) * | 2020-06-24 | 2023-04-07 | 郑州轻工业大学 | 利用古龙酸结晶母液制备2-氨基-3-(5-羟基吲哚)丙酸的方法 |
Family Cites Families (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB705652A (en) * | 1948-10-01 | 1954-03-17 | Farbewerke Hoechst Ag | Manufacture of 3-aminopropane compounds |
| US4342767A (en) | 1980-01-23 | 1982-08-03 | Merck & Co., Inc. | Hypocholesteremic fermentation products |
| US4444784A (en) | 1980-08-05 | 1984-04-24 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
| MX7065E (es) | 1980-06-06 | 1987-04-10 | Sankyo Co | Un procedimiento microbiologico para preparar derivados de ml-236b |
| US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
| US4845079A (en) | 1985-01-23 | 1989-07-04 | Luly Jay R | Peptidylaminodiols |
| US5066643A (en) | 1985-02-19 | 1991-11-19 | Sandoz Ltd. | Fluorine and chlorine statine or statone containing peptides and method of use |
| US4894437A (en) | 1985-11-15 | 1990-01-16 | The Upjohn Company | Novel renin inhibiting polypeptide analogs containing S-aryl-D- or L- or DL-cysteinyl, 3-(arylthio)lactic acid or 3-(arylthio)alkyl moieties |
| US4885292A (en) | 1986-02-03 | 1989-12-05 | E. R. Squibb & Sons, Inc. | N-heterocyclic alcohol renin inhibitors |
| US5089471A (en) | 1987-10-01 | 1992-02-18 | G. D. Searle & Co. | Peptidyl beta-aminoacyl aminodiol carbamates as anti-hypertensive agents |
| US4980283A (en) | 1987-10-01 | 1990-12-25 | Merck & Co., Inc. | Renin-inhibitory pepstatin phenyl derivatives |
| US5034512A (en) | 1987-10-22 | 1991-07-23 | Warner-Lambert Company | Branched backbone renin inhibitors |
| US5063207A (en) | 1987-10-26 | 1991-11-05 | Warner-Lambert Company | Renin inhibitors, method for using them, and compositions containing them |
| US5055466A (en) | 1987-11-23 | 1991-10-08 | E. R. Squibb & Sons, Inc. | N-morpholino derivatives and their use as anti-hypertensive agents |
| US5036054A (en) | 1988-02-11 | 1991-07-30 | Warner-Lambert Company | Renin inhibitors containing alpha-heteroatom amino acids |
| US5036053A (en) | 1988-05-27 | 1991-07-30 | Warner-Lambert Company | Diol-containing renin inhibitors |
| DE3841520A1 (de) | 1988-12-09 | 1990-06-13 | Hoechst Ag | Enzymhemmende harnstoffderivate von dipeptiden, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung |
| US5106835A (en) | 1988-12-27 | 1992-04-21 | American Cyanamid Company | Renin inhibitors |
| FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| US5063208A (en) | 1989-07-26 | 1991-11-05 | Abbott Laboratories | Peptidyl aminodiol renin inhibitors |
| US5098924A (en) | 1989-09-15 | 1992-03-24 | E. R. Squibb & Sons, Inc. | Diol sulfonamide and sulfinyl renin inhibitors |
| US5104869A (en) | 1989-10-11 | 1992-04-14 | American Cyanamid Company | Renin inhibitors |
| US5114937A (en) | 1989-11-28 | 1992-05-19 | Warner-Lambert Company | Renin inhibiting nonpeptides |
| US5064965A (en) | 1990-03-08 | 1991-11-12 | American Home Products Corporation | Renin inhibitors |
| US5095119A (en) | 1990-03-08 | 1992-03-10 | American Home Products Corporation | Renin inhibitors |
| US5075451A (en) | 1990-03-08 | 1991-12-24 | American Home Products Corporation | Pyrrolimidazolones useful as renin inhibitors |
| US5071837A (en) | 1990-11-28 | 1991-12-10 | Warner-Lambert Company | Novel renin inhibiting peptides |
| JP2648897B2 (ja) | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
| JPH0977744A (ja) * | 1995-09-12 | 1997-03-25 | Kyowa Hakko Kogyo Co Ltd | インドール誘導体 |
| GB9523948D0 (en) * | 1995-11-23 | 1996-01-24 | Univ East Anglia | Process for preparing n-benzyl indoles |
| PL186907B1 (pl) | 1995-12-22 | 2004-03-31 | Kowa Co | Kompozycja farmaceutyczna stabilizowana czynnikiem zasadowym |
| AU1856997A (en) | 1996-02-02 | 1997-08-22 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
| CA2356162A1 (en) | 1998-12-22 | 2000-06-29 | Eli Lilly And Company | Substituted tricyclics |
| ATE362468T1 (de) | 2000-07-25 | 2007-06-15 | Merck & Co Inc | N-substituierte indole mit anwendung in der behandlung von diabetes |
| ATE306272T1 (de) | 2000-08-28 | 2005-10-15 | Pharmacia Corp | Verwendung von einem aldosteron-rezeptor- antagonisten zur verbesserung der kognitiven funktion |
| MXPA03006772A (es) * | 2001-01-29 | 2004-10-15 | Dimensional Pharm Inc | Indoles sustituidos y su uso como antogonistas de integrina. |
| AU2003265681A1 (en) | 2002-08-29 | 2004-03-19 | Merck And Co., Inc. | Indoles having anti-diabetic activity |
| AU2004207740A1 (en) * | 2003-01-22 | 2004-08-12 | Eli Lilly And Company | Indole-derivative modulators of steroid hormone nuclear receptors |
| CN1960973A (zh) | 2004-03-30 | 2007-05-09 | 惠氏公司 | 作为去甲肾上腺素(ne)与血清素(5－h t)活性和单胺重摄取的调控剂以治疗血管舒缩症状(vms)的1－(1h－吲哚－1－基)－3－(4－甲基哌嗪－1－基)－1－苯基丙烷－2－醇衍生物和相关化合物 |
| US7414052B2 (en) * | 2004-03-30 | 2008-08-19 | Wyeth | Phenylaminopropanol derivatives and methods of their use |
| US7517899B2 (en) * | 2004-03-30 | 2009-04-14 | Wyeth | Phenylaminopropanol derivatives and methods of their use |
| CN1960980A (zh) | 2004-03-30 | 2007-05-09 | 惠氏公司 | 作为单胺再摄取调控剂治疗血管舒缩症状（vms）的杂环苯基氨基丙醇衍生物 |
| EP1756096B1 (en) * | 2004-05-03 | 2009-08-12 | F.Hoffmann-La Roche Ag | Indolyl derivatives as liver-x-receptor modulators |
| ES2340180T3 (es) * | 2004-06-01 | 2010-05-31 | F.Hoffmann-La Roche Ag | 3-amino-1-arilpropil-indoles como inhibidores de reabsorcion de monoaminas. |
| CN101309904A (zh) | 2005-09-29 | 2008-11-19 | 惠氏公司 | 作为单胺再摄取调节剂用于治疗血管舒缩症状(vasomotorsymptoms，vms)的1－(1h－吲哚－1－基)－3－(甲基氨基)－1－苯基丙－2－醇衍生物和相关化合物 |
| CA2672464A1 (en) | 2006-12-12 | 2008-06-19 | Wyeth | Dihydrobenzofuranyl derivatives and methods of their use |
| JP2009077744A (ja) | 2007-09-25 | 2009-04-16 | Shinichiro Matsubara | 雪上滑走板 |
| DE102008030206A1 (de) | 2008-06-25 | 2009-12-31 | Bayer Schering Pharma Aktiengesellschaft | 3-Cyanoalky- und 3-Hydroxyalkyl-Indole und ihre Verwendung |
| DE102008030207A1 (de) | 2008-06-25 | 2009-12-31 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 7-Sulfanylmethyl-, 7-Sulfinylmethyl- und 7-Sulfonylmethyl-Indole und ihre Verwendung |
| RU2011147181A (ru) * | 2009-04-22 | 2013-05-27 | Янссен Фармацевтика Нв | Азетидинилдиамиды в качестве ингибиторов моноациглицерин-липазы |
| KR20140009291A (ko) * | 2011-01-20 | 2014-01-22 | 머크 샤프 앤드 돔 코포레이션 | 미네랄로코르티코이드 수용체 길항제 |
-
2012
- 2012-01-19 KR KR1020137019134A patent/KR20140009291A/ko not_active Ceased
- 2012-01-19 CA CA2824344A patent/CA2824344A1/en not_active Abandoned
- 2012-01-19 AU AU2012208837A patent/AU2012208837B2/en not_active Ceased
- 2012-01-19 EP EP12736795.1A patent/EP2665707B1/en active Active
- 2012-01-19 CN CN201280005921.6A patent/CN103384661B/zh not_active Expired - Fee Related
- 2012-01-19 RU RU2013138569/04A patent/RU2598842C2/ru not_active IP Right Cessation
- 2012-01-19 MX MX2013008431A patent/MX351305B/es active IP Right Grant
- 2012-01-19 ES ES12736795.1T patent/ES2618812T3/es active Active
- 2012-01-19 US US13/979,875 patent/US8933113B2/en active Active
- 2012-01-19 JP JP2013549707A patent/JP6078004B2/ja not_active Expired - Fee Related
- 2012-01-19 WO PCT/CN2012/070597 patent/WO2012097744A1/en not_active Ceased
-
2014
- 2014-12-02 US US14/557,980 patent/US9403807B2/en active Active
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