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WO2001021620A3 - Amine derivatives of benzo-4,5-thieno-2,3-d pyrimidines - Google Patents

Amine derivatives of benzo-4,5-thieno-2,3-d pyrimidines Download PDF

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Publication number
WO2001021620A3
WO2001021620A3 PCT/EP2000/008256 EP0008256W WO0121620A3 WO 2001021620 A3 WO2001021620 A3 WO 2001021620A3 EP 0008256 W EP0008256 W EP 0008256W WO 0121620 A3 WO0121620 A3 WO 0121620A3
Authority
WO
WIPO (PCT)
Prior art keywords
amine derivatives
thieno
pyrimidines
benzo
ring
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP2000/008256
Other languages
German (de)
French (fr)
Other versions
WO2001021620A2 (en
Inventor
Volker Eiermann
Rochus Jonas
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Patent GmbH
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 to PL00353319A priority Critical patent/PL353319A1/en
Priority to AU74127/00A priority patent/AU7412700A/en
Priority to KR1020027003415A priority patent/KR20020027652A/en
Priority to CA002387520A priority patent/CA2387520A1/en
Priority to EP00962374A priority patent/EP1212329A2/en
Priority to BR0014052-0A priority patent/BR0014052A/en
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
Priority to JP2001524996A priority patent/JP2003509511A/en
Publication of WO2001021620A2 publication Critical patent/WO2001021620A2/en
Publication of WO2001021620A3 publication Critical patent/WO2001021620A3/en
Priority to NO20021310A priority patent/NO20021310D0/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • 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
    • A61P1/12Antidiarrhoeals
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/02Nasal agents, e.g. decongestants
    • 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
    • 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
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P37/08Antiallergic agents
    • 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
    • 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
    • A61P9/10Drugs 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention relates to the amine derivatives of the formula (I), and to their physiologically acceptable salts and solvates, wherein R?1, R2, R8, R9, R10, R11¿, Q, X, Y, Z, r, ring A and ring C have the meaning indicated in claim 1. The inventive derivatives are characterized by a phosphodiesterase-V inhibiting effect and are used for treating diseases of the cardiovascular system and for the treatment and/or the therapy of potency disorders.
PCT/EP2000/008256 1999-09-17 2000-08-24 Amine derivatives of benzo-4,5-thieno-2,3-d pyrimidines Ceased WO2001021620A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
AU74127/00A AU7412700A (en) 1999-09-17 2000-08-24 Amine derivatives
KR1020027003415A KR20020027652A (en) 1999-09-17 2000-08-24 Amine derivatives
CA002387520A CA2387520A1 (en) 1999-09-17 2000-08-24 Amine derivatives
EP00962374A EP1212329A2 (en) 1999-09-17 2000-08-24 Amine derivatives of benzo[4,5]thieno[2,3-d]pyrimidine
BR0014052-0A BR0014052A (en) 1999-09-17 2000-08-24 Amine derivatives
PL00353319A PL353319A1 (en) 1999-09-17 2000-08-24 Amine derivatives of benzo-4,5-thieno-2,3-d pyrimidines
JP2001524996A JP2003509511A (en) 1999-09-17 2000-08-24 Amine derivative
NO20021310A NO20021310D0 (en) 1999-09-17 2002-03-15 amine derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19944604A DE19944604A1 (en) 1999-09-17 1999-09-17 Amine derivatives
DE19944604.0 1999-09-17

Publications (2)

Publication Number Publication Date
WO2001021620A2 WO2001021620A2 (en) 2001-03-29
WO2001021620A3 true WO2001021620A3 (en) 2001-11-01

Family

ID=7922374

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/008256 Ceased WO2001021620A2 (en) 1999-09-17 2000-08-24 Amine derivatives of benzo-4,5-thieno-2,3-d pyrimidines

Country Status (11)

Country Link
EP (1) EP1212329A2 (en)
JP (1) JP2003509511A (en)
KR (1) KR20020027652A (en)
AU (1) AU7412700A (en)
BR (1) BR0014052A (en)
CA (1) CA2387520A1 (en)
CZ (1) CZ2002817A3 (en)
DE (1) DE19944604A1 (en)
NO (1) NO20021310D0 (en)
PL (1) PL353319A1 (en)
WO (1) WO2001021620A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10148883A1 (en) 2001-10-04 2003-04-10 Merck Patent Gmbh New fused bi- or tricyclic pyrimidine derivatives, are phosphodiesterase V inhibitors useful e.g. for treating impotence, cardiovascular disorders, inflammation or tumors
WO2003035653A1 (en) * 2001-10-26 2003-05-01 Nippon Soda Co.,Ltd. Pyridothienopyrimidine compound and salt thereof
AR059901A1 (en) 2006-03-20 2008-05-07 Bayer Pharmaceuticals Corp USEFUL TETRAHYDROPIRIDOTIENOPIRIMIDINE COMPOUNDS TO TREAT OR PREVENT CELLULAR PROLIFERATIVE DISORDERS.

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1603313A (en) * 1964-01-15 1971-04-05 Thieno 3 2-d pyrimidines
EP0728759A1 (en) * 1995-02-24 1996-08-28 Ono Pharmaceutical Co., Ltd. Heterocyclic compounds
WO1998017668A1 (en) * 1996-10-24 1998-04-30 Merck Patent Gmbh Thienopyrimidine with phosphodiesterase v inhibiting effect
US5948911A (en) * 1998-11-20 1999-09-07 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure to thienopyrimidine derivatives
WO1999055708A1 (en) * 1998-04-29 1999-11-04 Merck Patent Gmbh Condensed thienopyrimidines with phosphodiesterase-v inhibiting action
WO2000059912A1 (en) * 1999-03-30 2000-10-12 Nippon Soda Co., Ltd. Thienopyrimidine compounds and salts thereof and process for the preparation of the same
WO2000078767A1 (en) * 1999-06-19 2000-12-28 Merck Patent Gmbh Thienopyrimidines as phosphodiesterase inhibitors

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1603313A (en) * 1964-01-15 1971-04-05 Thieno 3 2-d pyrimidines
EP0728759A1 (en) * 1995-02-24 1996-08-28 Ono Pharmaceutical Co., Ltd. Heterocyclic compounds
WO1998017668A1 (en) * 1996-10-24 1998-04-30 Merck Patent Gmbh Thienopyrimidine with phosphodiesterase v inhibiting effect
WO1999055708A1 (en) * 1998-04-29 1999-11-04 Merck Patent Gmbh Condensed thienopyrimidines with phosphodiesterase-v inhibiting action
US5948911A (en) * 1998-11-20 1999-09-07 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure to thienopyrimidine derivatives
WO2000059912A1 (en) * 1999-03-30 2000-10-12 Nippon Soda Co., Ltd. Thienopyrimidine compounds and salts thereof and process for the preparation of the same
WO2000078767A1 (en) * 1999-06-19 2000-12-28 Merck Patent Gmbh Thienopyrimidines as phosphodiesterase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MOLINA, PEDRO ET AL: "Iminophosphorane-mediated bispyrido annulation onto five-membered rings. X-ray crystal structure of 6,7-dibenzylamino-13-methoxymethyl- 13H-diquino[4,3-b:3',4'-d]pyrrole.acetonitrile complex", TETRAHEDRON (1995), 51(44), 12127-42, XP002164407 *

Also Published As

Publication number Publication date
NO20021310L (en) 2002-03-15
PL353319A1 (en) 2003-11-17
JP2003509511A (en) 2003-03-11
AU7412700A (en) 2001-04-24
DE19944604A1 (en) 2001-03-22
NO20021310D0 (en) 2002-03-15
WO2001021620A2 (en) 2001-03-29
KR20020027652A (en) 2002-04-13
EP1212329A2 (en) 2002-06-12
BR0014052A (en) 2002-05-21
CZ2002817A3 (en) 2002-06-12
CA2387520A1 (en) 2001-03-29

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