[go: up one dir, main page]

PE20020484A1 - Derivados de pirimidina como inhibidores de la enzima conversor de endotelina - Google Patents

Derivados de pirimidina como inhibidores de la enzima conversor de endotelina

Info

Publication number
PE20020484A1
PE20020484A1 PE2001000709A PE2001000709A PE20020484A1 PE 20020484 A1 PE20020484 A1 PE 20020484A1 PE 2001000709 A PE2001000709 A PE 2001000709A PE 2001000709 A PE2001000709 A PE 2001000709A PE 20020484 A1 PE20020484 A1 PE 20020484A1
Authority
PE
Peru
Prior art keywords
alkyl
endothelin
pyrimidine derivatives
inhibitors
benzyloximethyl
Prior art date
Application number
PE2001000709A
Other languages
English (en)
Inventor
Daniel Bur
Alexander Chucholowski
Johannes Aebi
Henrietta Dehmlow
Original Assignee
Hoffmann La Roche
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20020484A1 publication Critical patent/PE20020484A1/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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)

Abstract

SE REFIERE A DERIVADOS DE PIRIMIDINA DE FORMULA I DONDE R1 ES H, ALQUILCARBONILO, ARILCARBONILO; R2 ES ALQUILO, ALQUINILO, HIDROXIALQUILO, CARBOXIALQUILO, ALCOXICARBONILO, ENTRE OTROS; R3 Y R4 SON H, ALQUILO, ALQUILCICLOALQUILO, ALQUILCICLOALQUILALQUILO, ENTRE OTROS; R5 ES H, ALQUILO, ARILO, ARILALQUILOXICARBONIILO, ALQUILCARBONILO; X1, X2, X3 Y X4 SON CH, N; NO MAS DE 2 X1, X2, X3 Y X4 SON NITROGENO; Y ES O, NR5; SON COMPUESTOS PREFERIDOS (3R,5S)-1-PIRIMIDIN-2-IL-5-(2,4,5-TRIFLUORO-BENCILOXIMETIL)-PIRROLIDIN-3-TIOL, TRIFLUOROACETATO; (3R,5S)-1-(6-FENIL-PIRIDAZIN-3-IL)-5-(2,4,5-TRIFLUORO-BENCILOXIMETIL)-PIRROLIDIN-3-TIOL, ENTRE OTROS.TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS PUEDEN SER UTILES PARA EL TRATAMIENTO DE TRASTORNOS CAUSADOS POR LA ACTIVIDAD DE LA ENZIMA CONVERSOR DE ENDOTELINA COMO ISQUEMIA DE MIOCARDIO, INSUFICIENCIA CARDIACA CONGESTIVA, ARRITMIA, HIPERTENSION, HIPERTENSION PULMONAR, ASMA, VASOESPASMO CEREBRAL
PE2001000709A 2000-07-19 2001-07-16 Derivados de pirimidina como inhibidores de la enzima conversor de endotelina PE20020484A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00114950 2000-07-19

Publications (1)

Publication Number Publication Date
PE20020484A1 true PE20020484A1 (es) 2002-06-06

Family

ID=8169227

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001000709A PE20020484A1 (es) 2000-07-19 2001-07-16 Derivados de pirimidina como inhibidores de la enzima conversor de endotelina

Country Status (15)

Country Link
US (1) US6660738B2 (es)
EP (1) EP1303507A1 (es)
JP (1) JP3983662B2 (es)
KR (1) KR100551853B1 (es)
CN (1) CN1443184A (es)
AR (1) AR030940A1 (es)
AU (1) AU2001285836A1 (es)
BR (1) BR0112656A (es)
CA (1) CA2415681C (es)
MX (1) MXPA03000504A (es)
PA (1) PA8522201A1 (es)
PE (1) PE20020484A1 (es)
UY (1) UY26845A1 (es)
WO (1) WO2002006271A1 (es)
ZA (1) ZA200300161B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004089294A2 (en) 2003-04-04 2004-10-21 Incyte Corporation Compositions, methods and kits relating to her-2 cleavage
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
WO2009120094A2 (en) * 2008-03-27 2009-10-01 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
CA2897279C (en) 2013-01-23 2020-12-29 Astrazeneca Ab Aminopyrazine derivatives and pharmaceutical compositions thereof for use in the treatment of cancer
SMT202200134T1 (it) 2018-03-08 2022-05-12 Incyte Corp Composti di amminopirazindiolo come inibitori di pi3k-y
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3579888D1 (de) * 1984-11-08 1990-10-31 Sumitomo Pharma Carbapenemverbindungen und deren herstellung.
AU631671B2 (en) * 1989-08-04 1992-12-03 Banyu Pharmaceutical Co., Ltd. 2-(2-vinylpyrrolidinylthio)carbapenem derivatives
US5360798A (en) * 1991-07-04 1994-11-01 Shionogi Seiyaku Kabushiki Kaisha Aminooxypyrrolidinylthiocarbapenem compounds
US5317016A (en) * 1991-08-20 1994-05-31 Shionogi Seiyaku Kabushiki Kaisha Pyrrolidylthiocarbapenem derivative
TR199800157T1 (xx) * 1995-07-31 1998-06-22 Shionogi & Co.,Ltd. Fosfolipaz A2 inhibit�r� aktivitesi olan pirolidin t�revleri.
AU2995497A (en) * 1996-07-26 1997-11-19 Dr. Reddy's Research Foundation Thiazolidinedione compounds having antidiabetic, hypolipidaemic, antihypertensive properties, process for their preparation and pharmaceutical compositions thereof
BR9712792A (pt) * 1996-08-28 1999-12-14 Procter & Gamble Inibidores de metaloprotease bidentada.
CA2301590C (en) * 1997-09-12 2007-05-01 Merck Frosst Canada & Co. 2-aminopyridines as inhibitors of cyclooxygenase-2
US6329418B1 (en) * 1998-04-14 2001-12-11 The Procter & Gamble Company Substituted pyrrolidine hydroxamate metalloprotease inhibitors

Also Published As

Publication number Publication date
JP3983662B2 (ja) 2007-09-26
AU2001285836A1 (en) 2002-01-30
CA2415681C (en) 2008-05-20
MXPA03000504A (es) 2003-06-24
CA2415681A1 (en) 2002-01-24
KR100551853B1 (ko) 2006-02-13
US6660738B2 (en) 2003-12-09
PA8522201A1 (es) 2002-04-25
AR030940A1 (es) 2003-09-03
KR20030022289A (ko) 2003-03-15
ZA200300161B (en) 2004-04-07
UY26845A1 (es) 2002-01-31
JP2004504317A (ja) 2004-02-12
BR0112656A (pt) 2003-06-24
US20020055632A1 (en) 2002-05-09
WO2002006271A1 (en) 2002-01-24
EP1303507A1 (en) 2003-04-23
CN1443184A (zh) 2003-09-17

Similar Documents

Publication Publication Date Title
AR029216A1 (es) Compuestos inhibidores no peptidicos de la union celular dependiente de vla-4 utiles en el tratamiento de enfermedades inflamatorias, autoinmunes y respiratorias; composicion farmaceutica y procedimiento de tratamiento
PA8501801A1 (es) Inhibidores triciclicos de polimerasas (adp - polirribosas)
CO5251416A1 (es) Inhibidores de intercambio de sodio/protones heterociclicos y metodo
PE20011314A1 (es) DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA COMO INHIBIDORES DE LA FORMACION DE FACTORES DE COAGULACION Xa IXa Y TROMBINA
PE20021011A1 (es) Derivados quinazolinicos como inhibidores de la rho-quinasa
DK1196414T3 (da) Prolægemiddel af carbamathæmmer for IMPDH
PE20010912A1 (es) Derivados arilamina y su aplicacion como agentes antitelomerasa
PE27499A1 (es) Derivados del 2-(purin-9-il)-tetrahidrofuran-3,4-diol
PE20060691A1 (es) Serinamidas sustituidas por benzoilo
EA200400466A1 (ru) Производные пиперазина с антагонистической активностью к рецептору ccr1
CU23210A3 (es) NUEVOS COMPUESTOS DE OXABISPIDINE uTIL EN EL TRATAMIENTO DE ARRITMIAS CARDIACAS
AR040773A1 (es) Pirazoles utiles como inhibidores de gsk-3
SE0202463D0 (sv) Novel compounds
JO2282B1 (en) Oxazole derivatives
PT1261602E (pt) Derivados imidazol-2-carboxamida como inibidores de cinase raf
PE20070790A1 (es) Derivados de 2-aminopirimidina como moduladores de la actividad del receptor de histamina h-4
PE20090649A1 (es) DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1
PE20060589A1 (es) FENILAMINOTIAZOLES SUSTITUIDOS COMO AGONISTAS DE ADENOSINA A1 Y A2b
PE20020484A1 (es) Derivados de pirimidina como inhibidores de la enzima conversor de endotelina
PE20080207A1 (es) DERIVADOS DE 1-N-AMINO-2-IMIDAZOLIDINONAS COMO INHIBIDORES DEL CANAL DE POTASIO Kv1.5
TR200102008T2 (tr) Serebral işemi profilaksı ve tedavisi için piridin türevlerinin kullanımı.
PE20061155A1 (es) Derivados de indolinona como agentes para el tratamiento o la prevencion de enfermedades fibroticas
PE20020333A1 (es) Derivados de pirrolidina como inhibidores de la enzima conversor de endotelina
EA200500133A1 (ru) Производные пирролидина в качестве антагонистов окситоцина
AR035163A1 (es) Compuesto derivado de n-fenil-2-hidroxi-2-metil-3,3,3-trifluoropropanamida, composicion farmaceutica, uso en la fabricacion de un medicamento y proceso para su preparacion

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed