AR034307A1 - Derivados de acido 6-oxo-octahidro-pirido[2,1a][2]benzoazepina-4-carboxilico, procedimiento para su preparacion y la preparacion de un intermediario, composicion farmaceutica, un metodo para su preparacion y el uso de los mismos para la preparacion de un medicamento - Google Patents
Derivados de acido 6-oxo-octahidro-pirido[2,1a][2]benzoazepina-4-carboxilico, procedimiento para su preparacion y la preparacion de un intermediario, composicion farmaceutica, un metodo para su preparacion y el uso de los mismos para la preparacion de un medicamentoInfo
- Publication number
- AR034307A1 AR034307A1 ARP020101321A ARP020101321A AR034307A1 AR 034307 A1 AR034307 A1 AR 034307A1 AR P020101321 A ARP020101321 A AR P020101321A AR P020101321 A ARP020101321 A AR P020101321A AR 034307 A1 AR034307 A1 AR 034307A1
- Authority
- AR
- Argentina
- Prior art keywords
- preparation
- aryl
- alkyl
- oxo
- hydrogen
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 239000002253 acid Substances 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 abstract 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 abstract 1
- 206010007559 Cardiac failure congestive Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 102000003729 Neprilysin Human genes 0.000 abstract 1
- 108090000028 Neprilysin Proteins 0.000 abstract 1
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 abstract 1
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000005982 diphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- -1 methylenedioxy ring Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Derivado del ácido 6-oxo-octahidro-benzopiridoazepin-4-carboxílico, que comprende un compuesto de Fórmula (1), en la que: R1 es hidrógeno, -CH2OC(O)C(CH3)3, o un grupo acilo; R2 es hidrógeno, -CH2O-C(O)C(CH3)3, un alquilo C1-4, arilo, aril-alquilo C1-4 o difenilmetilo; X es -(CH2)n-, en la que n es un entero 0 ó 1, -S-, -O-, un resto de Fórmula (2) ó (3), en la que R3 es hidrógeno, un alquilo C1-4, arilo o aril-(alquilo C1-4), y R4 es -CF3, alquilo C1-10, arilo o aril-(alquilo C1-4); B1 y B2 son, cada uno independientemente, hidrógeno, hidroxi u -OR5, en la que R5 es alquilo C1-4, arilo o aril-(alquilo C1-4) o, en la que, B1 y B2 están unidos a átomos de C adyacentes, pudiendo tomarse B1 y B2 conjuntamente con dichos átomos de C adyacentes para formar un anillo de benceno o metilendioxi; o sus sales farmacéuticamente aceptables o sus estereoisómeros. Asimismo se describen y reivindican composiciones farmacéuticas que incorporan estos compuestos, y procedimientos para preparar dichos compuestos, intermediarios y composiciones farmacéuticas. El uso de dichos compuestos para la preparación de un medicamento para la inhibición de la enzima convertidora de angiotensina y endopeptidasa neutra, y para el tratamiento de la hipertensión y de la insuficiencia cardíaca congestiva.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28330501P | 2001-04-12 | 2001-04-12 | |
| GBGB0119305.1A GB0119305D0 (en) | 2001-04-12 | 2001-08-08 | Mercaptoacetylamide derivatives,a process for their preparation and their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR034307A1 true AR034307A1 (es) | 2004-02-18 |
Family
ID=23085405
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020101321A AR034307A1 (es) | 2001-04-12 | 2002-04-10 | Derivados de acido 6-oxo-octahidro-pirido[2,1a][2]benzoazepina-4-carboxilico, procedimiento para su preparacion y la preparacion de un intermediario, composicion farmaceutica, un metodo para su preparacion y el uso de los mismos para la preparacion de un medicamento |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US6602866B2 (es) |
| KR (1) | KR100910929B1 (es) |
| AR (1) | AR034307A1 (es) |
| CR (1) | CR7074A (es) |
| DK (1) | DK1381605T3 (es) |
| EC (1) | ECSP034782A (es) |
| GB (1) | GB0119305D0 (es) |
| GT (1) | GT200200069A (es) |
| IL (1) | IL158289A (es) |
| MY (1) | MY128226A (es) |
| PE (1) | PE20021079A1 (es) |
| RS (1) | RS50919B (es) |
| TN (1) | TNSN03083A1 (es) |
| TW (1) | TWI319764B (es) |
| UA (1) | UA75647C2 (es) |
| UY (1) | UY27255A1 (es) |
| ZA (1) | ZA200307096B (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1481960A4 (en) * | 2002-02-04 | 2005-04-06 | Kaneka Corp | PROCESS FOR OBTAINING OPTICALLY ACTIVE 2-HALOGENO-CARBOXYLIC ACIDS |
| TW200838501A (en) | 2007-02-02 | 2008-10-01 | Theravance Inc | Dual-acting antihypertensive agents |
| TWI448284B (zh) * | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| TWI406850B (zh) * | 2007-06-05 | 2013-09-01 | Theravance Inc | 雙效苯并咪唑抗高血壓劑 |
| US7834041B2 (en) * | 2007-09-07 | 2010-11-16 | Theravance, Inc. | Dual-acting antihypertensive agents |
| EP2234608A2 (en) | 2007-12-11 | 2010-10-06 | Viamet Pharmaceuticals, Inc. | Metalloenzyme inhibitors using metal binding moieties in combination with targeting moieties |
| CA2705921A1 (en) | 2007-12-11 | 2009-06-18 | Theravance, Inc. | Dual-acting benzoimidazole derivatives and their use as antihypertensive agents |
| EP2297113A1 (en) | 2008-04-29 | 2011-03-23 | Theravance, Inc. | Dual-acting antihypertensive agents |
| US7863309B2 (en) | 2008-07-24 | 2011-01-04 | Theravance, Inc. | Dual-acting antihypertensive agents |
| WO2011005674A1 (en) | 2009-07-07 | 2011-01-13 | Theravance, Inc. | Dual-acting pyrazole antihypertensive agents |
| JP2012533626A (ja) | 2009-07-22 | 2012-12-27 | セラヴァンス， インコーポレーテッド | 二重作用オキサゾール降圧剤 |
| EP2526095A1 (en) | 2010-01-19 | 2012-11-28 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
| EP2651900B1 (en) | 2010-12-15 | 2015-08-19 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| CA2817368C (en) | 2010-12-15 | 2019-12-31 | Theravance, Inc. | Neprilysin inhibitors |
| US8449890B2 (en) | 2011-02-17 | 2013-05-28 | Theravance, Inc. | Neprilysin inhibitors |
| EP2675795B1 (en) | 2011-02-17 | 2016-04-20 | Theravance Biopharma R&D IP, LLC | Substituted aminobutyric derivatives as neprilysin inhibitors |
| EP2714648B1 (en) | 2011-05-31 | 2017-08-16 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| JP5959075B2 (ja) | 2011-05-31 | 2016-08-02 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | ネプリライシン阻害剤 |
| EP2714662B1 (en) | 2011-05-31 | 2017-10-11 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| WO2013181332A1 (en) | 2012-05-31 | 2013-12-05 | Theravance, Inc. | Nitric oxide donor neprilysin inhibitors |
| WO2013184898A1 (en) | 2012-06-08 | 2013-12-12 | Theravance, Inc. | Neprilysin inhibitors |
| AU2013271537B2 (en) | 2012-06-08 | 2017-05-11 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| JP6092390B2 (ja) | 2012-08-08 | 2017-03-08 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | ネプリライシン阻害剤 |
| HUE034210T2 (hu) | 2013-03-05 | 2018-02-28 | Theravance Biopharma R&D Ip Llc | Neprilizininhibitorok |
| US9585882B2 (en) | 2014-01-30 | 2017-03-07 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| SG11201605965UA (en) | 2014-01-30 | 2016-08-30 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| KR102640906B1 (ko) | 2015-02-11 | 2024-02-27 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 저해제로서 (2s,4r)-5-(5''-클로로-2''-플루오로비페닐-4-일)-4-(에톡시옥살릴아미노)-2-히드록시메틸-2-메틸펜타노익산 |
| EP3259255B1 (en) | 2015-02-19 | 2020-10-21 | Theravance Biopharma R&D IP, LLC | (2r,4r)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid |
| MX2018010727A (es) | 2016-03-08 | 2019-01-24 | Theravance Biopharma R&D Ip Llc | Acido (2s,4r)-5-(5'-cloro-2'-fluoro-[1,1'-bifenil]-4-il)-2-(etoxim etil)-4-(3-hidroxiisoxazol-5-carboxamido)-2-metilpentanoico cristalino, y sus usos. |
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| US3334091A (en) | 1965-03-25 | 1967-08-01 | Sandoz Ag | Sedatives |
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| IE50839B1 (en) | 1980-02-26 | 1986-07-23 | Wyeth John & Brother Ltd | Novel processes for preparing proline derivatives and analogous compounds |
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| US4415496A (en) | 1981-03-23 | 1983-11-15 | Merck & Co., Inc. | Bicyclic lactams |
| GB2128984B (en) | 1982-05-12 | 1985-05-22 | Hoffmann La Roche | Diaza-bicyclic compounds |
| NZ204130A (en) | 1982-05-12 | 1986-03-14 | Hoffmann La Roche | Bicyclic heterocyclic compounds and pharmaceutical compositions |
| US4552889A (en) | 1983-06-09 | 1985-11-12 | Eli Lilly And Company | 3-Mercaptomethyl-2-oxo-1-pyrrolidine acetic acids and use for hypertension |
| US4692438A (en) | 1984-08-24 | 1987-09-08 | Hoffmann-La Roche Inc. | Pyridazo-diazepines, diazocines, and -triazepines having anti-hypertensive activity |
| US4584294A (en) | 1984-11-07 | 1986-04-22 | Merck & Co., Inc. | Fused tricyclic lactams as angiotensin converting enzyme inhibitors and as antihypertensive agents |
| ZA863170B (en) | 1985-04-30 | 1987-12-30 | Lilly Co Eli | 7-substituted bicyclic pyrazolidinones |
| US4973585A (en) | 1986-06-13 | 1990-11-27 | Merrell Dow Pharmaceuticals | Tricyclic lactams active as antihypertensive agents |
| ZA874106B (en) | 1986-06-13 | 1987-12-08 | Merrell Dow Pharmaceuticals Inc. | Novel antihypertensive agent |
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| GB8629875D0 (en) | 1986-12-15 | 1987-01-28 | Hoffmann La Roche | Pyridazodiazepine derivatives |
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| GB8926512D0 (en) | 1989-11-23 | 1990-01-10 | Pfizer Ltd | Therapeutic agents |
| AU7168091A (en) | 1989-12-22 | 1991-07-24 | Schering Corporation | Mercaptocycloacyl aminoacid endopeptidase inhibitors |
| US5430145A (en) * | 1990-10-18 | 1995-07-04 | Merrell Dow Pharmaceuticals Inc. | Mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ace |
| CA2053340C (en) | 1990-10-18 | 2002-04-02 | Timothy P. Burkholder | Mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ace |
| US5491143A (en) | 1990-10-18 | 1996-02-13 | Merrell Dow Pharmaceuticals Inc. | Mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ACE |
| DK0492369T3 (da) | 1990-12-21 | 1997-10-13 | Merrell Pharma Inc | Hidtil ukendte tricycliske amino- og nitro-forbindelser med ACE-hæmmende virkning |
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| FR2679564A1 (fr) | 1991-07-23 | 1993-01-29 | Inst Nat Sante Rech Med | Nouveaux acylmercaptoalcanoldipeptides, leur preparation et les compositions qui les contiennent. |
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| DK0534363T3 (da) | 1991-09-27 | 1997-09-22 | Merrell Pharma Inc | 2-substituerede indan-2-mercaptoacetylamid-forbindelse med inhiberende virkning på enkephalinase og ACE. |
| AU657793B2 (en) | 1991-09-27 | 1995-03-23 | Merrell Pharmaceuticals Inc. | Novel 2-substituted indane-2-carboxyalkyl derivatives useful as inhibitors of enkephalinase and ACE |
| AU668707B2 (en) | 1992-02-14 | 1996-05-16 | Merrell Pharmaceuticals Inc. | Aminoacetylmercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ACE |
| WO1993023403A1 (en) | 1992-05-15 | 1993-11-25 | Merrell Dow Pharmaceuticals Inc. | NOVEL MERCAPTOACETYLAMIDO PYRIDAZO[1,2]PYRIDAZINE, PYRAZOLO[1,2]PYRIDAZINE, PYRIDAZO[1,2-a][1,2]DIAZEPINE AND PYRAZOLO[1,2-a][1,2]DIAZEPINE DERIVATIVES USEFUL AS INHIBITORS OF ENKEPHALINASE AND ACE |
| RU2124503C1 (ru) | 1992-05-18 | 1999-01-10 | И.Р.Сквибб энд Санз, Инк. | Гетероциклические азотсодержащие производные карбоновой кислоты, способ их получения и фармацевтическая композиция |
| US5238932A (en) | 1992-05-20 | 1993-08-24 | Merrell Dow Pharmaceuticals Inc. | Mercaptoacetylamide tricyclic derivatives useful as inhibitors of enkephalinase |
| US5679671A (en) * | 1993-06-11 | 1997-10-21 | Eisai Co., Ltd. | Amino acid derivative |
| US5525723A (en) | 1993-11-18 | 1996-06-11 | Bristol-Myers Squibb Co. | Compounds containing a fused multiple ring lactam |
| DE69416873T2 (de) * | 1994-02-14 | 1999-07-29 | Merrell Pharmaceuticals Inc., Cincinnati, Ohio | Mercaptoacetylamid disulfidderivate als enkephalinase und ace inhibitoren |
| DK0751774T3 (da) * | 1994-03-24 | 2003-12-08 | Merrell Pharma Inc | Hypocholesterolæmiske mercaptoacetylamiddisulfid-derivater |
-
2001
- 2001-08-08 GB GBGB0119305.1A patent/GB0119305D0/en not_active Ceased
-
2002
- 2002-03-04 UA UA20031110184A patent/UA75647C2/uk unknown
- 2002-04-03 RS YUP-787/03A patent/RS50919B/sr unknown
- 2002-04-03 DK DK02732549T patent/DK1381605T3/da active
- 2002-04-03 KR KR1020037013181A patent/KR100910929B1/ko not_active IP Right Cessation
- 2002-04-08 US US10/118,179 patent/US6602866B2/en not_active Expired - Lifetime
- 2002-04-10 TW TW091107133A patent/TWI319764B/zh not_active IP Right Cessation
- 2002-04-10 UY UY27255A patent/UY27255A1/es not_active Application Discontinuation
- 2002-04-10 PE PE2002000294A patent/PE20021079A1/es not_active Application Discontinuation
- 2002-04-10 GT GT200200069A patent/GT200200069A/es unknown
- 2002-04-10 AR ARP020101321A patent/AR034307A1/es active IP Right Grant
- 2002-04-10 MY MYPI20021326A patent/MY128226A/en unknown
-
2003
- 2003-07-08 TN TNPCT/EP2002/003668A patent/TNSN03083A1/en unknown
- 2003-09-11 ZA ZA200307096A patent/ZA200307096B/en unknown
- 2003-09-12 CR CR7074A patent/CR7074A/es not_active Application Discontinuation
- 2003-09-26 EC EC2003004782A patent/ECSP034782A/es unknown
- 2003-10-07 IL IL158289A patent/IL158289A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| MY128226A (en) | 2007-01-31 |
| GB0119305D0 (en) | 2001-10-03 |
| UA75647C2 (en) | 2006-05-15 |
| RS50919B (sr) | 2010-08-31 |
| KR20040008153A (ko) | 2004-01-28 |
| TWI319764B (en) | 2010-01-21 |
| US20020193589A1 (en) | 2002-12-19 |
| DK1381605T3 (da) | 2005-05-09 |
| UY27255A1 (es) | 2002-07-31 |
| TNSN03083A1 (en) | 2005-12-23 |
| IL158289A (en) | 2010-11-30 |
| GT200200069A (es) | 2002-12-17 |
| US6602866B2 (en) | 2003-08-05 |
| KR100910929B1 (ko) | 2009-08-06 |
| YU78703A (sh) | 2006-05-25 |
| ECSP034782A (es) | 2003-12-01 |
| PE20021079A1 (es) | 2003-02-19 |
| CR7074A (es) | 2007-12-04 |
| ZA200307096B (en) | 2004-09-06 |
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