WO2002018350A1 - Grk inhibitor - Google Patents

Grk inhibitor Download PDF

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Publication number
WO2002018350A1
WO2002018350A1 PCT/JP2001/007397 JP0107397W WO0218350A1 WO 2002018350 A1 WO2002018350 A1 WO 2002018350A1 JP 0107397 W JP0107397 W JP 0107397W WO 0218350 A1 WO0218350 A1 WO 0218350A1
Authority
WO
WIPO (PCT)
Prior art keywords
ring
grk inhibitor
represents optionally
grk
inhibitor
Prior art date
Application number
PCT/JP2001/007397
Other languages
French (fr)
Japanese (ja)
Inventor
Shoji Fukumoto
Toshifumi Watanabe
Shota Ikeda
Original Assignee
Takeda Chemical Industries, Ltd.
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 Takeda Chemical Industries, Ltd. filed Critical Takeda Chemical Industries, Ltd.
Priority to AU2001282520A priority Critical patent/AU2001282520A1/en
Publication of WO2002018350A1 publication Critical patent/WO2002018350A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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

Abstract

A novel GRK inhibitor which contains a compound represented by the formula, a salt thereof, or a prodrug comprising either of these: wherein ring A represents optionally further substituted nitrogen-containing heterocycle; R?1 and R2¿ each represents optionally substituted amino; and X represents a spacer comprising a linear part constituted of one to four atoms, provided that R1 may be bonded to R2 or/and X to form a ring. It is useful as a preventive/remedy for cardiac failure, etc.
PCT/JP2001/007397 2000-08-29 2001-08-29 Grk inhibitor WO2002018350A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001282520A AU2001282520A1 (en) 2000-08-29 2001-08-29 Grk inhibitor

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2000264499 2000-08-29
JP2000-264499 2000-08-29

Publications (1)

Publication Number Publication Date
WO2002018350A1 true WO2002018350A1 (en) 2002-03-07

Family

ID=18751904

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2001/007397 WO2002018350A1 (en) 2000-08-29 2001-08-29 Grk inhibitor

Country Status (2)

Country Link
AU (1) AU2001282520A1 (en)
WO (1) WO2002018350A1 (en)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005037271A2 (en) * 2003-10-17 2005-04-28 Tanabe Seiyaku Co., Ltd. Large conductance calcium-activated k channel opener
WO2008001883A1 (en) 2006-06-29 2008-01-03 Nissan Chemical Industries, Ltd. α-AMINO ACID DERIVATIVE AND PHARMACEUTICAL COMPRISING THE SAME AS ACTIVE INGREDIENT
US7482350B2 (en) 2004-05-08 2009-01-27 Neurogen Corporation 4,5-disubstituted-2-aryl pyrimidines
US8748442B2 (en) 2010-06-30 2014-06-10 Ironwood Pharmaceuticals, Inc. sGC stimulators
US9061030B2 (en) 2010-11-09 2015-06-23 Ironwood Pharmaceuticals, Inc. sGC stimulators
US9139564B2 (en) 2011-12-27 2015-09-22 Ironwood Pharmaceuticals, Inc. 2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63126868A (en) * 1986-10-18 1988-05-30 ザ　ウエルカム　フアウンデーシヨン　リミテツド Compound or salt thereof, pharmaceutical preparation containing the same, remedy or prevention of tumor breeding of animal, production of said compound and novel chemical intermediate
JPH029869A (en) * 1988-04-15 1990-01-12 Wellcome Found Ltd:The Novel compound

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63126868A (en) * 1986-10-18 1988-05-30 ザ　ウエルカム　フアウンデーシヨン　リミテツド Compound or salt thereof, pharmaceutical preparation containing the same, remedy or prevention of tumor breeding of animal, production of said compound and novel chemical intermediate
JPH029869A (en) * 1988-04-15 1990-01-12 Wellcome Found Ltd:The Novel compound

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
BIGHAM E.C.: "Multisubstrate analog inhibitors of glycinamide ribonucleotide transformylase based on 5-deazaacyclotetrahydrofolate (5-DACTHF)", HETEROCYCLES, vol. 35, no. 2, 1993, pages 1289 - 1307, XP002947298 *
BIGHAM E.C.: "Synthesis and biological activity of open-chain analogs of 5,6,7,8-tetrahydrofolic acid-potential antitumor agents", J. MED. CHEM., vol. 35, no. 8, 1992, pages 1399 - 1410, XP002947295 *
BOGER D.L.: "Multisubstrate analog based on 5,8,10-trideazafolate", BIOORG. MED. CHEM., vol. 5, no. 9, 1997, pages 1853 - 1857, XP002947299 *
HASBI A.: "Desesitization of the .delta.-opioid receptor correlates with its phosphorylation in SK-N-BE cells: Involvement of a G protein-coupled receptor kinase", J. NEUROCHEM., vol. 70, no. 5, 1998, pages 2129 - 2138, XP002947293 *
JANSEN M.: "Effect of purine synthesis inhibition on WiDr spheroids in vitro or on WiDr or colon 38 tumors in vivo. Complete growth inhibition but not regression", BIOCHEM. PHARMACOL., vol. 47, no. 6, 1994, pages 1067 - 1078, XP002947294 *
KELLY J.L.: "Synthesis and biological activity of an acyclic analog of 5,6,7,8-tetrahydrofolic acid, N-(4-((3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl)amino)benzoyl)-L-glutamic acid", J. MED. CHEM., vol. 33, no. 2, 1990, pages 561 - 567, XP002947296 *
KLEIN C.: "Towards structure-based drug design: crystal structure of a multisubstrate adduct complex of glycinamide ribonucleotide transformylase at 1.96 .ANG.resolution", J. MOL. BIOL., vol. 249, no. 1, 1995, pages 153 - 175, XP002947300 *
STYLES V.L.: "Synthesis of the pentaglutymyl derivative of N-(4-(N-(3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl)amino)benzoyl)-L-glutamic acid (5-DACTHF). An acyclic analog of tetrahydrofolic acid", J. HETEROCYCL. CHEM., vol. 27, no. 6, 1990, pages 1809 - 1813, XP002947297 *

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005037271A2 (en) * 2003-10-17 2005-04-28 Tanabe Seiyaku Co., Ltd. Large conductance calcium-activated k channel opener
WO2005037271A3 (en) * 2003-10-17 2005-09-01 Tanabe Seiyaku Co Large conductance calcium-activated k channel opener
US7482350B2 (en) 2004-05-08 2009-01-27 Neurogen Corporation 4,5-disubstituted-2-aryl pyrimidines
US8129395B2 (en) 2004-05-08 2012-03-06 Novartis International Pharmaceutical Ltd. 4,5-disubstituted-2-aryl pyrimidines
WO2008001883A1 (en) 2006-06-29 2008-01-03 Nissan Chemical Industries, Ltd. α-AMINO ACID DERIVATIVE AND PHARMACEUTICAL COMPRISING THE SAME AS ACTIVE INGREDIENT
US7879887B2 (en) 2006-06-29 2011-02-01 Nissan Chemical Industries, Ltd. α-amino acid derivatives and medicaments containing the same as an active ingredient
US8748442B2 (en) 2010-06-30 2014-06-10 Ironwood Pharmaceuticals, Inc. sGC stimulators
US10189809B2 (en) 2010-06-30 2019-01-29 Ironwood Pharmaceuticals, Inc. SGC stimulators
US9061030B2 (en) 2010-11-09 2015-06-23 Ironwood Pharmaceuticals, Inc. sGC stimulators
US9139564B2 (en) 2011-12-27 2015-09-22 Ironwood Pharmaceuticals, Inc. 2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators

Also Published As

Publication number Publication date
AU2001282520A1 (en) 2002-03-13

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