AR044818A1 - Acidos pirrolidin 1-2 dicarboxilicos-1-[4-(etinil-fenil)amida]-2-[(fenil)-amido] derivados y procedimiento para preparar dichos compuestos - Google Patents
Acidos pirrolidin 1-2 dicarboxilicos-1-[4-(etinil-fenil)amida]-2-[(fenil)-amido] derivados y procedimiento para preparar dichos compuestosInfo
- Publication number
- AR044818A1 AR044818A1 ARP040102129A ARP040102129A AR044818A1 AR 044818 A1 AR044818 A1 AR 044818A1 AR P040102129 A ARP040102129 A AR P040102129A AR P040102129 A ARP040102129 A AR P040102129A AR 044818 A1 AR044818 A1 AR 044818A1
- Authority
- AR
- Argentina
- Prior art keywords
- hal
- cooh
- phenyl
- atoms
- mono
- Prior art date
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- 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
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Los nuevos compuestos de la fórmula (1), en donde significan: R es H, X, A, X-CO- o A-CO-; R1 es H, =O, Hal, X, A, OH, OA, A-COO-, A-CONH-, A-CONA-, N3, NH2, NO2, CN, COOH, COOA, CONH2, CON(A)2, O-alilo, -O-propargilo, O-bencilo, =N-OH, =N-OA, OCH2CH(OH)CH2OH, A-O-CO-(CH2)m-O-, -O(CH2)mCOOH u -O(CH2)mOA; R2 es H, Hal o A; R3 es un heterociclo monocíclico saturado, insaturado o aromático con 1 a 4 átomos de N, o y/o S, que puede ser insustituido o mono, di o trisustituido con Hal, A, OA, CN, (CH2)nOH, NR4R5, =NH, =N-OH, =N-OA, COOA y/o el oxígeno del carbonilo (=O), o CONR4R5; R2 y R3 juntos también -CH=CH-NH- o -CH2-CH2-NH, en donde un átomo de H puede estar sustituido con A-CO- o A-O-CO-; R4, R5 son independientes entre sí, H o A; R4 y R5 juntos también una cadena de alquileno con 3, 4 o 5 átomos de C que también puede estar sustituido sustituida con A, Hal, OA y/o el oxígeno del carbonilo (=CO); X-arilo es arilo, arilalquilo, Het o Het-alquilo, fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OH, NH2, NO2, CN, COOH, COOA, CONH2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2, SO2A, -CH2-COOH u -OCH2-COOH; Het es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con Hal, A, bencilo, cicloalquilo, OH, NH2, NHCONH2, NO2, CN, -CH2-COOH, -CH2-CONH2, NHCOA, NR3SO2A, CHO, SO2NH2, SO2A y/o el oxígeno del carbonilo; A es alquilo ramificado, ramificado o cíclico con C1-10, en donde también 1-7 átomos de H pueden estar reemplazados por F y/o cloro; Hal es F, Cl, Br o I; m es 1, 2, 3, 4, 5 ó 6; n es 0, 1, 2, 3, 4, 5 ó 6, así como sus derivados, sales, solvatos y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores del factor de coagulación Xa y pueden emplearse para la profilaxis y/o la terapia de enfermedades tromboembólicas y para el tratamiento de tumores.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10327428A DE10327428A1 (de) | 2003-06-18 | 2003-06-18 | Ethinylprolinderivate |
| DE10329457A DE10329457A1 (de) | 2003-04-03 | 2003-07-01 | Ethinylprolinderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR044818A1 true AR044818A1 (es) | 2005-10-05 |
Family
ID=33553467
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040102129A AR044818A1 (es) | 2003-06-18 | 2004-06-18 | Acidos pirrolidin 1-2 dicarboxilicos-1-[4-(etinil-fenil)amida]-2-[(fenil)-amido] derivados y procedimiento para preparar dichos compuestos |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US7557222B2 (es) |
| EP (1) | EP1633346B1 (es) |
| JP (1) | JP5015593B2 (es) |
| KR (1) | KR20060023154A (es) |
| CN (1) | CN1809346A (es) |
| AR (1) | AR044818A1 (es) |
| AT (1) | ATE337000T1 (es) |
| AU (1) | AU2004246766B2 (es) |
| BR (1) | BRPI0411466A (es) |
| CA (1) | CA2529453C (es) |
| DE (1) | DE502004001289D1 (es) |
| ES (1) | ES2271894T3 (es) |
| MX (1) | MXPA05013536A (es) |
| PE (1) | PE20050229A1 (es) |
| TW (1) | TW200504012A (es) |
| WO (1) | WO2004110433A1 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102004004731A1 (de) * | 2004-01-30 | 2005-08-18 | Merck Patent Gmbh | Harnstoffderivate |
| DE102004016605A1 (de) * | 2004-04-03 | 2005-10-20 | Merck Patent Gmbh | Thiocarbamoylproline |
| AU2006314637A1 (en) | 2005-11-16 | 2007-05-24 | F. Hoffmann-La Roche Ag | Novel pyrrolidine derivatives as inhibitors of coagulation factor Xa |
| EP1818330A1 (de) | 2006-02-14 | 2007-08-15 | Boehringer Ingelheim Pharma GmbH & Co.KG | Substituierte Prolinamide, deren Herstellung und deren Verwendung als Arzneimittel |
| EP2051975B1 (de) | 2006-05-16 | 2012-09-12 | Boehringer Ingelheim International GmbH | Substituierte prolinamide, deren herstellung und deren verwendung als arzneimittel |
| KR20100027159A (ko) * | 2007-06-28 | 2010-03-10 | 노파르티스 아게 | 칼리크레인 7 조절제 |
| US8673920B2 (en) * | 2009-05-06 | 2014-03-18 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9073882B2 (en) | 2010-10-27 | 2015-07-07 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| EP2632464B1 (en) | 2010-10-29 | 2015-04-29 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| AU2012299227A1 (en) | 2011-08-19 | 2014-02-20 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| TW201317213A (zh) | 2011-09-16 | 2013-05-01 | Merck Sharp & Dohme | 腎外髓質鉀通道抑制劑 |
| WO2013062900A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2013062892A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9139585B2 (en) | 2011-10-31 | 2015-09-22 | Merck Sharp & Dohme Corp. | Inhibitors of the Renal Outer Medullary Potassium channel |
| US9108947B2 (en) | 2011-10-31 | 2015-08-18 | Merck Sharp & Dohme Corp. | Inhibitors of the Renal Outer Medullary Potassium channel |
| WO2013066718A2 (en) | 2011-10-31 | 2013-05-10 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2013090271A1 (en) | 2011-12-16 | 2013-06-20 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| GB201209138D0 (en) * | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
| AR092031A1 (es) | 2012-07-26 | 2015-03-18 | Merck Sharp & Dohme | Inhibidores del canal de potasio medular externo renal |
| US9777002B2 (en) | 2012-11-29 | 2017-10-03 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9573961B2 (en) | 2012-12-19 | 2017-02-21 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2014126944A2 (en) | 2013-02-18 | 2014-08-21 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| EP2968288B1 (en) | 2013-03-15 | 2018-07-04 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2015017305A1 (en) | 2013-07-31 | 2015-02-05 | Merck Sharp & Dohme Corp | Inhibitors of the renal outer medullary potassium channel |
| WO2015065866A1 (en) | 2013-10-31 | 2015-05-07 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| JP6337750B2 (ja) * | 2013-11-22 | 2018-06-06 | 小野薬品工業株式会社 | 化合物 |
| CN106103453A (zh) | 2014-01-14 | 2016-11-09 | 大日本住友制药株式会社 | 缩合5‑噁唑烷酮衍生物 |
| WO2016127358A1 (en) | 2015-02-12 | 2016-08-18 | Merck Sharp & Dohme Corp. | Inhibitors of renal outer medullary potassium channel |
| CN109796439B (zh) * | 2019-01-18 | 2020-05-19 | 西安交通大学 | 一种羟脯氨酸类肽衍生物及其制备方法和应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU776053B2 (en) * | 2000-03-31 | 2004-08-26 | Astellas Pharma Inc. | Diazepan derivatives or salts thereof |
| US7312235B2 (en) * | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
| ATE368643T1 (de) * | 2001-03-30 | 2007-08-15 | Millennium Pharm Inc | Faktor xa benzamidin inhibitoren |
| US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| DE102004014945A1 (de) * | 2004-03-26 | 2005-10-13 | Merck Patent Gmbh | Prolinylderivate |
-
2004
- 2004-05-27 KR KR1020057024102A patent/KR20060023154A/ko not_active Application Discontinuation
- 2004-05-27 AU AU2004246766A patent/AU2004246766B2/en not_active Ceased
- 2004-05-27 CN CNA2004800169550A patent/CN1809346A/zh active Pending
- 2004-05-27 ES ES04735007T patent/ES2271894T3/es not_active Expired - Lifetime
- 2004-05-27 MX MXPA05013536A patent/MXPA05013536A/es not_active Application Discontinuation
- 2004-05-27 US US10/561,227 patent/US7557222B2/en not_active Expired - Fee Related
- 2004-05-27 BR BRPI0411466-3A patent/BRPI0411466A/pt not_active Application Discontinuation
- 2004-05-27 EP EP04735007A patent/EP1633346B1/de not_active Expired - Lifetime
- 2004-05-27 CA CA2529453A patent/CA2529453C/en not_active Expired - Fee Related
- 2004-05-27 DE DE502004001289T patent/DE502004001289D1/de not_active Expired - Lifetime
- 2004-05-27 JP JP2006515798A patent/JP5015593B2/ja not_active Expired - Fee Related
- 2004-05-27 AT AT04735007T patent/ATE337000T1/de not_active IP Right Cessation
- 2004-05-27 WO PCT/EP2004/005717 patent/WO2004110433A1/de not_active Application Discontinuation
- 2004-06-14 PE PE2004000589A patent/PE20050229A1/es not_active Application Discontinuation
- 2004-06-16 TW TW093117389A patent/TW200504012A/zh unknown
- 2004-06-18 AR ARP040102129A patent/AR044818A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US7557222B2 (en) | 2009-07-07 |
| JP5015593B2 (ja) | 2012-08-29 |
| AU2004246766B2 (en) | 2009-09-17 |
| AU2004246766A1 (en) | 2004-12-23 |
| ES2271894T3 (es) | 2007-04-16 |
| US20070093472A1 (en) | 2007-04-26 |
| CN1809346A (zh) | 2006-07-26 |
| EP1633346A1 (de) | 2006-03-15 |
| MXPA05013536A (es) | 2006-03-09 |
| WO2004110433A1 (de) | 2004-12-23 |
| KR20060023154A (ko) | 2006-03-13 |
| CA2529453A1 (en) | 2004-12-23 |
| EP1633346B1 (de) | 2006-08-23 |
| PE20050229A1 (es) | 2005-04-12 |
| DE502004001289D1 (de) | 2006-10-05 |
| JP2006527708A (ja) | 2006-12-07 |
| ATE337000T1 (de) | 2006-09-15 |
| TW200504012A (en) | 2005-02-01 |
| CA2529453C (en) | 2012-10-02 |
| BRPI0411466A (pt) | 2006-07-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR044818A1 (es) | Acidos pirrolidin 1-2 dicarboxilicos-1-[4-(etinil-fenil)amida]-2-[(fenil)-amido] derivados y procedimiento para preparar dichos compuestos | |
| AR043833A1 (es) | Derivados de 1,2 diazol. metodo de preparacion y composiciones farmaceuticas | |
| PE20071132A1 (es) | Compuestos macrociclicos como inhibidores del factor viia | |
| PE20020504A1 (es) | N-acilsulfonamidas promotoras de apoptosis | |
| PE20141855A1 (es) | Benzotienilo-pirrolotriazinas disustituidas y sus usos | |
| AR053554A1 (es) | Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos | |
| PE20110062A1 (es) | N-(3-(3,5-dimetoxifenetil)-1h-pirazol-5-il)-4-(3,4-dimetilpiperazin-1-il)benzamida y sales del mismo | |
| CY1111733T1 (el) | Παραγωγα 2-(1η-ινδολυλοσουλφανυλ)-βενζυλαμινης ως ssri | |
| AR061238A1 (es) | Compuestos de oxilmilo macrociclico inhibidores de proteasa de hepatitis c | |
| PE20191557A1 (es) | Compuestos de pirimidinil-pyridiloxi-naftil y metodos para tratar enfermedades y trastornos relacionados con ire1 | |
| RU2008145701A (ru) | Производные пурина для применения в качестве агонистов аденозинового рецептора a2a | |
| AR061735A1 (es) | Derivados de indazol, composiciones farmaceuticas y uso de los mismos | |
| ATE307810T1 (de) | Imidazol-2-carbonsäureamid derivate als raf- kinase-inhibitoren | |
| EA200600503A1 (ru) | Производные малонамида, блокирующие активность <sub>&gamma;</sub>- секретазы | |
| AR039385A1 (es) | Derivados de tioxantina como inhibidores de la mieloperoxidasa | |
| CY1107985T1 (el) | Ccr1 ανταγωνιστες για την αγωγη μεταξυ αλλων απομυελινωτικης φλεγμονωδους νοσου | |
| DE602004028150D1 (de) | Aminopyrazolderivate als gsk-3-inhibitoren | |
| AR046643A1 (es) | Derivados de pirrol | |
| EA201170607A1 (ru) | Акриламидопроизводные, применимые как ингибиторы перехода митохондриальной проницаемости | |
| PE20061155A1 (es) | Derivados de indolinona como agentes para el tratamiento o la prevencion de enfermedades fibroticas | |
| AR046086A1 (es) | Derivados de 1,3- benzoxazolilo como inhibidores de quinasa | |
| ES2255190T3 (es) | Compuestos indol 2,3-sustituidos como inhibidores de cox-2. | |
| AR065798A1 (es) | Usos terapeuticos de la 4-[2-(4-metilfenilsulfanil)fenil]piperidina | |
| AR048326A1 (es) | Derivados de prolinilo | |
| AR115965A1 (es) | Derivados heteroaromáticos de carboxamida como inhibidores de la calicreína plasmática |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |