[go: up one dir, main page]

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 compuestos

Info

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
Application number
ARP040102129A
Other languages
English (en)
Inventor
Mederski Werner Dr
Tsaklakidis Christos Dr
Dipl Chem Dorsch Dieter Dr
Cezanne Bertram Dr
Gleitz Johannes Dr
Original Assignee
Merck Patent Gmbh
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from DE10327428A external-priority patent/DE10327428A1/de
Priority claimed from DE10329457A external-priority patent/DE10329457A1/de
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR044818A1 publication Critical patent/AR044818A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (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.
ARP040102129A 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 AR044818A1 (es)

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)

* Cited by examiner, † Cited by third party
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
US7601752B2 (en) 2005-11-16 2009-10-13 Hoffmann-La Roche Inc. Pyrrolidine derivatives
EP1818330A1 (de) * 2006-02-14 2007-08-15 Boehringer Ingelheim Pharma GmbH & Co.KG Substituierte Prolinamide, deren Herstellung und deren Verwendung als Arzneimittel
AU2007251614B2 (en) * 2006-05-16 2013-01-17 Boehringer Ingelheim International Gmbh Substituted prolinamides, production thereof and their use as drugs
CA2691849A1 (en) 2007-06-28 2008-12-31 Novartis Ag Kallikrein 7 modulators
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
US9056859B2 (en) 2010-10-29 2015-06-16 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
RU2014110401A (ru) 2011-08-19 2015-09-27 Мерк Шарп И Доум Корп. Ингибиторы внешнего медуллярного калиевого канала почек
US9527830B2 (en) 2011-09-16 2016-12-27 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2771005B1 (en) 2011-10-25 2016-05-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013062900A1 (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
EP2773206B1 (en) 2011-10-31 2018-02-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9493474B2 (en) 2011-10-31 2016-11-15 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2790511B1 (en) 2011-12-16 2016-09-14 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
EP2925322B1 (en) 2012-11-29 2018-10-24 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
US9765074B2 (en) 2013-03-15 2017-09-19 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP3027625B1 (en) 2013-07-31 2018-05-30 Merck Sharp & Dohme Corp. Spiro-fused derivatives of piperidine useful for the treatment of inter alia hypertension and acute or chronic heart failure
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
EP3095786A4 (en) * 2014-01-14 2017-10-11 Sumitomo Dainippon Pharma Co., Ltd. Condensed 5-oxazolidinone derivative
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU776053B2 (en) * 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
WO2002079145A1 (en) 2001-03-30 2002-10-10 Millennium Pharmaceuticals, Inc. BENZAMIDE INHIBITORS OF FACTOR Xa
US7312235B2 (en) * 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
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

Also Published As

Publication number Publication date
EP1633346A1 (de) 2006-03-15
US20070093472A1 (en) 2007-04-26
JP5015593B2 (ja) 2012-08-29
CN1809346A (zh) 2006-07-26
CA2529453A1 (en) 2004-12-23
WO2004110433A1 (de) 2004-12-23
EP1633346B1 (de) 2006-08-23
JP2006527708A (ja) 2006-12-07
ATE337000T1 (de) 2006-09-15
DE502004001289D1 (de) 2006-10-05
CA2529453C (en) 2012-10-02
US7557222B2 (en) 2009-07-07
TW200504012A (en) 2005-02-01
KR20060023154A (ko) 2006-03-13
ES2271894T3 (es) 2007-04-16
AU2004246766B2 (en) 2009-09-17
PE20050229A1 (es) 2005-04-12
AU2004246766A1 (en) 2004-12-23
BRPI0411466A (pt) 2006-07-11
MXPA05013536A (es) 2006-03-09

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
ECSP066414A (es) Derivados de malonamida que bloquean la actividad de gama-secretasa
AR036114A1 (es) Tetrahidroimidazol[1,2-a]pirazinas y tetrahidrotriazol[4,3-a]pirazinas como inhibidores de la dipeptidil peptidasa utiles para el tratamiento o la prevencion de la diabetes
PE20060570A1 (es) Compuestos de quinazolina e isoquinolina piperidilo sustituidos como inhibidores de fosfodiesterasa pde-10
ECSP056131A (es) Compuestos de carbonilo
PE20141855A1 (es) Benzotienilo-pirrolotriazinas disustituidas y sus usos
PE20091002A1 (es) Analogos dipeptidos como inhibidores del factor de coagulacion
AR057109A1 (es) Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis
AR067506A1 (es) Derivados de quinazolinamida
PE20110062A1 (es) N-(3-(3,5-dimetoxifenetil)-1h-pirazol-5-il)-4-(3,4-dimetilpiperazin-1-il)benzamida y sales del mismo
HRP20080429T3 (en) Disubstituted pyrazolobenzodiazepines useful as inhibitors for cdk2 and angiogesis, and for the treatment of breast, colon, lung and prostate cancer
CY1108230T1 (el) Παραγωγα 2-(1η-ινδολυλοσουλφανυλ)-βενζυλαμινης ως ssri
RU2008145701A (ru) Производные пурина для применения в качестве агонистов аденозинового рецептора a2a
AR116115A1 (es) Dimetil amino azetidina amidas como inhibidores de jak
DE602004028150D1 (de) Aminopyrazolderivate als gsk-3-inhibitoren
DE502004005033D1 (de) Substituierte 2-aminotetraline zur behandlung von depressionen
BRPI0410979A (pt) composto, composição farmacêutica, e, métodos para tratar uma doença em um animal mediada pela catepsina s e para tratar um paciente submetido a uma terapia
ES2255190T3 (es) Compuestos indol 2,3-sustituidos como inhibidores de cox-2.
AR115965A1 (es) Derivados heteroaromáticos de carboxamida como inhibidores de la calicreína plasmática
AR053554A1 (es) Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos
PE20071132A1 (es) Compuestos macrociclicos como inhibidores del factor viia
AR130094A1 (es) Inhibidores de inflamasoma nlrp3
EA201070366A1 (ru) 3-метил-2-((2s)-2-(4-(3-метил-1,2,4-оксадиазол-5-ил)фенил)морфолино)-6-(пиримидин-4-ил)пиримидин-4(3н)-он в качестве ингибитора тау-протеинкиназы
PE20021060A1 (es) Empleo de amidas de acidos antranilicos como medicamento para el tratamiento de arritmias, asi como preparados farmaceuticos que las contienen

Legal Events

Date Code Title Description
FB Suspension of granting procedure