BR0209652A - Derivados de dipeptìdeos possuindo um grupo 2-tioacila n-terminal, como inibidores de vasopeptidase - Google Patents
Derivados de dipeptìdeos possuindo um grupo 2-tioacila n-terminal, como inibidores de vasopeptidaseInfo
- Publication number
- BR0209652A BR0209652A BR0209652-8A BR0209652A BR0209652A BR 0209652 A BR0209652 A BR 0209652A BR 0209652 A BR0209652 A BR 0209652A BR 0209652 A BR0209652 A BR 0209652A
- Authority
- BR
- Brazil
- Prior art keywords
- terminal
- dipeptide derivatives
- thioacyl group
- vasopeptidase inhibitors
- inhibitors
- Prior art date
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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P9/04—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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
"DERIVADOS DE DIPEPTìDEOS POSSUINDO UM GRUPO 2-TIOACILA N-TERMINAL, COMO INIBIDORES DE VASOPEPTIDASE". A presente invenção refere-se a compostos da fórmula: onde R, R~ 1~, COOR~ 2~, R~ 3~-R~ 7~, alk e X possuem o significado como acima, sendo úteis como inibidores duplos de enzima de conversão de angiotensina e endopeptidase neutra, bem como inibidores de enzima de conversão de endotelina.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US29108801P | 2001-05-15 | 2001-05-15 | |
US33957501P | 2001-12-11 | 2001-12-11 | |
PCT/EP2002/005293 WO2002092622A2 (en) | 2001-05-15 | 2002-05-14 | Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BR0209652A true BR0209652A (pt) | 2004-07-13 |
Family
ID=26966569
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR0209652-8A BR0209652A (pt) | 2001-05-15 | 2002-05-14 | Derivados de dipeptìdeos possuindo um grupo 2-tioacila n-terminal, como inibidores de vasopeptidase |
Country Status (23)
Country | Link |
---|---|
US (3) | US6777443B2 (pt) |
EP (2) | EP2239268A1 (pt) |
JP (1) | JP4390458B2 (pt) |
KR (1) | KR100908152B1 (pt) |
CN (1) | CN1649893A (pt) |
AR (1) | AR035890A1 (pt) |
AU (1) | AU2002314067B2 (pt) |
BR (1) | BR0209652A (pt) |
CA (1) | CA2449292A1 (pt) |
CO (1) | CO5540347A2 (pt) |
CZ (1) | CZ20033077A3 (pt) |
HU (1) | HUP0304084A3 (pt) |
IL (1) | IL158772A0 (pt) |
MX (1) | MXPA03010403A (pt) |
MY (1) | MY127495A (pt) |
NO (1) | NO20035084L (pt) |
NZ (1) | NZ529438A (pt) |
PE (1) | PE20030042A1 (pt) |
PL (1) | PL366786A1 (pt) |
RU (1) | RU2298559C2 (pt) |
SK (1) | SK14032003A3 (pt) |
TW (1) | TWI295996B (pt) |
WO (1) | WO2002092622A2 (pt) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6777443B2 (en) * | 2001-05-15 | 2004-08-17 | Novartis Ag | Dipeptide derivatives |
US7199261B2 (en) * | 2001-07-06 | 2007-04-03 | Teva Pharmaceutical Industries Ltd | Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives |
ATE342261T1 (de) * | 2001-09-21 | 2006-11-15 | Novartis Pharma Gmbh | Pyranderivate als inhibitoren von ace und nep |
DE60315795T2 (de) * | 2002-01-17 | 2008-06-05 | Novartis Ag | Pharmazeutische zusammensetzung enthaltend valsartan und nep-inhibitoren |
US7468390B2 (en) | 2002-01-17 | 2008-12-23 | Novartis Ag | Methods of treatment and pharmaceutical composition |
SI1515717T1 (sl) * | 2002-06-13 | 2009-02-28 | Novartis Ag | Kalcijeve soli statinov, izvedenih iz indola |
ATE493973T1 (de) | 2004-06-04 | 2011-01-15 | Teva Pharma | Irbesartan enthaltende pharmazeutische zusammensetzung |
EP1827448A1 (en) * | 2004-12-15 | 2007-09-05 | Solvay Pharmaceuticals GmbH | Pharmaceutical compositions comprising nep-inhibitors, inhibitors of the endogenous endothelin producing system and hmg coa reductase inhibitors |
EP1858518A1 (en) * | 2005-03-14 | 2007-11-28 | Orion Corporation | A combination treatment for enhancing diuresis |
US7390789B2 (en) * | 2005-09-13 | 2008-06-24 | William H Simmons | Thio-containing inhibitors of aminopeptidase P, and compositions thereof |
US7400236B2 (en) | 2005-10-21 | 2008-07-15 | Gm Global Technology Operations, Inc. | Vehicular lane monitoring system utilizing front and rear cameras |
AR057882A1 (es) | 2005-11-09 | 2007-12-26 | Novartis Ag | Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra |
US20120157387A1 (en) * | 2006-11-28 | 2012-06-21 | Apotex Technologies Inc. | Orally bioavailable d-gamma-glutamyl-d-tryptophan |
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 |
JP2011506459A (ja) | 2007-12-11 | 2011-03-03 | セラヴァンス, インコーポレーテッド | 抗高血圧剤としての二重作用性ベンゾイミダゾール誘導体およびその使用 |
WO2009134741A1 (en) | 2008-04-29 | 2009-11-05 | 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 |
ES2441419T3 (es) | 2009-07-22 | 2014-02-04 | Theravance, Inc. | Agentes antihipertensivos de doble acción basados en oxazol |
WO2011090929A1 (en) | 2010-01-19 | 2011-07-28 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
US20150011484A1 (en) * | 2011-03-31 | 2015-01-08 | Aptoex Technologies, Inc. | Prodrugs of d-gamma-glutamyl-d-tryptophan and d-gamma-glutamyl-l-tryptophan |
US9212206B1 (en) * | 2014-11-24 | 2015-12-15 | William H Simmons | 4-Fluoro-Thio-containing inhibitors of APP2, compositions thereof and method of use |
WO2018002673A1 (en) | 2016-07-01 | 2018-01-04 | N4 Pharma Uk Limited | Novel formulations of angiotensin ii receptor antagonists |
UY38072A (es) | 2018-02-07 | 2019-10-01 | Novartis Ag | Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos |
WO2019213386A1 (en) * | 2018-05-04 | 2019-11-07 | New Mexico Tech University Research Park Corporation | Proteasome inhibitors |
CN113956183B (zh) * | 2021-10-28 | 2023-06-20 | 成都市科隆化学品有限公司 | 一种Boc-Ser(Bzl)-OH及其制备方法 |
Family Cites Families (27)
Publication number | Priority date | Publication date | Assignee | Title |
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AU6733190A (en) | 1989-11-27 | 1991-06-26 | Santen Pharmaceutical Co. Ltd. | Amino acid derivative |
FR2679564A1 (fr) | 1991-07-23 | 1993-01-29 | Inst Nat Sante Rech Med | Nouveaux acylmercaptoalcanoldipeptides, leur preparation et les compositions qui les contiennent. |
ES2108855T3 (es) | 1992-07-21 | 1998-01-01 | Ciba Geigy Ag | Derivados de acido oxamico como agentes hipocolesteremicos. |
US5432186A (en) * | 1993-11-16 | 1995-07-11 | Ciba-Geigy Corporation | Cyclic amino acid derivatives |
US5508266A (en) | 1994-06-22 | 1996-04-16 | Ciba-Geigy Corporation | Gem-disubstituted amino acid derivatives |
US6162828A (en) | 1995-03-31 | 2000-12-19 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
DE69632821T2 (de) * | 1995-04-25 | 2005-08-25 | Daiichi Fine Chemical Co., Ltd., Takaoka | In wasser hochlöslicher metalloproteinase-inhibitor |
DE69627483T2 (de) | 1995-05-10 | 2004-04-01 | Darwin Discovery Ltd., Slough | Peptidartige stoffe, die metalloproteinasen und die tnf-freisetzung hemmen, und ihre therapeutische verwendung |
JPH11507352A (ja) * | 1995-06-07 | 1999-06-29 | ジンタ・インコーポレイテッド | 新規カルバメート基本カチオン性脂質 |
US6245809B1 (en) * | 1996-12-09 | 2001-06-12 | Cor Therapeutics Inc. | Integrin antagonists |
US6492421B1 (en) * | 1997-07-31 | 2002-12-10 | Athena Neurosciences, Inc. | Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4 |
DE19745151A1 (de) | 1997-10-14 | 1999-04-15 | Basf Ag | Neue Verbindungen zur Behandlung von Krankheiten, die mit der biologischen Wirkung von Endothelin assoziiert sind |
FR2770844A1 (fr) | 1997-11-10 | 1999-05-14 | Inst Nat Sante Rech Med | Inhibiteurs de toxines clostridiales et compositions pharmaceutiques les contenant |
EP1030853A1 (en) * | 1997-11-12 | 2000-08-30 | Ariad Pharmaceuticals, Inc. | Novel signal transduction inhibitors, compositions containing them |
RU2000129510A (ru) | 1998-04-23 | 2002-11-10 | Новартис АГ (CH) | Определенные тиольные ингибиторы эндотелинпревращающих ферментов |
JP3646062B2 (ja) | 1998-04-23 | 2005-05-11 | ノバルティス アクチエンゲゼルシャフト | エンドセリン変換酵素のヘテロアリール置換チオール型阻害剤 |
ES2188277T3 (es) | 1998-12-31 | 2003-06-16 | Aventis Pharma Inc | Inhibidores selectivos de mmp-12. |
FR2788526B1 (fr) | 1999-01-20 | 2002-07-05 | Inst Nat Sante Rech Med | Composes tripeptidiques utiles a titre d'hinhibiteurs selectifs de l'aminopeptidase a et compositions pharmaceutiques correspondantes |
CO5160290A1 (es) | 1999-03-29 | 2002-05-30 | Novartis Ag | Derivados de acido fenoxifeniloxamico sustituido . |
US6503949B1 (en) * | 1999-05-17 | 2003-01-07 | Noro Nordisk A/S | Glucagon antagonists/inverse agonists |
GB9917909D0 (en) * | 1999-07-31 | 1999-09-29 | Synphar Lab Inc | Cysteine protease inhibitors |
CA2383002A1 (en) * | 1999-08-27 | 2001-03-08 | Cytovia, Inc. | Substituted .alpha.-hydroxy acid caspase inhibitors and the use thereof |
US6803383B2 (en) * | 2000-03-27 | 2004-10-12 | The Scripps Research Institute | Inhibition of angiogenesis and tumor growth |
CA2405496A1 (en) | 2000-04-03 | 2001-10-11 | Richard A. Reeves | Vasopeptidase inhibitors to treat isolated systolic hypertension |
SK14612002A3 (sk) | 2000-04-12 | 2003-05-02 | Novartis Ag | Farmaceutická kompozícia obsahujúca inhibítor aldosterónsyntázy prípadne v kombinácii s antagonistom AT1-receptora a jej použitie |
US20020013307A1 (en) | 2000-05-23 | 2002-01-31 | Pablo Lapuerta | Use of vasopeptidase inhibitors to treat or slow the progression of cognitive dysfunction and to treat and/or prevent dementia |
US6777443B2 (en) * | 2001-05-15 | 2004-08-17 | Novartis Ag | Dipeptide derivatives |
-
2002
- 2002-05-09 US US10/142,693 patent/US6777443B2/en not_active Expired - Fee Related
- 2002-05-13 AR ARP020101736A patent/AR035890A1/es unknown
- 2002-05-14 CA CA002449292A patent/CA2449292A1/en not_active Abandoned
- 2002-05-14 NZ NZ529438A patent/NZ529438A/en unknown
- 2002-05-14 TW TW091110028A patent/TWI295996B/zh not_active IP Right Cessation
- 2002-05-14 SK SK1403-2003A patent/SK14032003A3/sk not_active Application Discontinuation
- 2002-05-14 WO PCT/EP2002/005293 patent/WO2002092622A2/en active IP Right Grant
- 2002-05-14 EP EP10164769A patent/EP2239268A1/en not_active Withdrawn
- 2002-05-14 CZ CZ20033077A patent/CZ20033077A3/cs unknown
- 2002-05-14 IL IL15877202A patent/IL158772A0/xx unknown
- 2002-05-14 JP JP2002589505A patent/JP4390458B2/ja not_active Expired - Fee Related
- 2002-05-14 CN CNA028118499A patent/CN1649893A/zh active Pending
- 2002-05-14 KR KR1020037014849A patent/KR100908152B1/ko not_active IP Right Cessation
- 2002-05-14 MY MYPI20021740A patent/MY127495A/en unknown
- 2002-05-14 EP EP02740600A patent/EP1392720A2/en not_active Withdrawn
- 2002-05-14 PL PL02366786A patent/PL366786A1/xx unknown
- 2002-05-14 HU HU0304084A patent/HUP0304084A3/hu unknown
- 2002-05-14 RU RU2003134153/04A patent/RU2298559C2/ru not_active IP Right Cessation
- 2002-05-14 BR BR0209652-8A patent/BR0209652A/pt not_active IP Right Cessation
- 2002-05-14 AU AU2002314067A patent/AU2002314067B2/en not_active Ceased
- 2002-05-14 MX MXPA03010403A patent/MXPA03010403A/es active IP Right Grant
- 2002-05-15 PE PE2002000407A patent/PE20030042A1/es not_active Application Discontinuation
-
2003
- 2003-11-14 NO NO20035084A patent/NO20035084L/no not_active Application Discontinuation
- 2003-12-02 CO CO03105928A patent/CO5540347A2/es not_active Application Discontinuation
-
2004
- 2004-07-02 US US10/884,150 patent/US6992105B2/en not_active Expired - Fee Related
-
2005
- 2005-10-21 US US11/255,827 patent/US20060058242A1/en not_active Abandoned
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 10A ANUI DADE. |
|
B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: NAO APRESENTADA A GUIA DE CUMPRIMENTO DE EXIGENCIA. REFERENTE A 10A ANUIDADE. |