CN102639497A - 乳酸脱氢酶(ldh)的化合物抑制剂以及包含这些化合物的药学组合物 - Google Patents

乳酸脱氢酶(ldh)的化合物抑制剂以及包含这些化合物的药学组合物 Download PDF

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Publication number
CN102639497A
CN102639497A CN2010800516087A CN201080051608A CN102639497A CN 102639497 A CN102639497 A CN 102639497A CN 2010800516087 A CN2010800516087 A CN 2010800516087A CN 201080051608 A CN201080051608 A CN 201080051608A CN 102639497 A CN102639497 A CN 102639497A
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CN
China
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alkyl
hydroxy
indole
carboxylic acid
phenyl
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Pending
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CN2010800516087A
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Chinese (zh)
Inventor
F·米努托洛
M·马基亚
C·格朗茨
S·罗伊
G·詹纳西尼
A·卢卡茨尼
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Universita di Pisa
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Universita di Pisa
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
CN2010800516087A 2009-11-09 2010-11-05 乳酸脱氢酶(ldh)的化合物抑制剂以及包含这些化合物的药学组合物 Pending CN102639497A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IT000140A ITPI20090140A1 (it) 2009-11-09 2009-11-09 Composto inibitore dell'enzima lattato deidrogenasi (ldh) e composizione farmaceutica che comprende tale composto
ITPI2009A000140 2009-11-09
PCT/EP2010/006740 WO2011054525A1 (en) 2009-11-09 2010-11-05 Compounds inhibitors of enzyme lactate dehydrogenase (ldh) and pharmaceutical compositions containing these compounds

Publications (1)

Publication Number Publication Date
CN102639497A true CN102639497A (zh) 2012-08-15

Family

ID=42244578

Family Applications (1)

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CN2010800516087A Pending CN102639497A (zh) 2009-11-09 2010-11-05 乳酸脱氢酶(ldh)的化合物抑制剂以及包含这些化合物的药学组合物

Country Status (11)

Country Link
US (1) US20120309794A1 (https=)
EP (1) EP2499114A1 (https=)
JP (1) JP2013510106A (https=)
CN (1) CN102639497A (https=)
AU (1) AU2010314367A1 (https=)
BR (1) BR112012010868A2 (https=)
CA (1) CA2780136A1 (https=)
EA (1) EA201290316A1 (https=)
IT (1) ITPI20090140A1 (https=)
WO (1) WO2011054525A1 (https=)
ZA (1) ZA201203993B (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ITPI20110143A1 (it) * 2011-12-20 2013-06-21 Univ Pisa Agenti terapeutici in grado di ridurre la produzione cellulare di acido lattico e composizioni farmaceutiche che comprendono tali composti
WO2014115764A1 (ja) * 2013-01-25 2014-07-31 国立大学法人岡山大学 乳酸脱水素酵素阻害剤およびそれを含有する医薬品
US9750761B2 (en) 2014-05-21 2017-09-05 University Of Rochester LDH inhibitors as treatment for fibrosis and fibrotic-related disorders
FR3030516B1 (fr) * 2014-12-19 2019-12-27 Galderma Research & Development Derives sulfonamides bicycles en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t)
CN107249583B (zh) * 2015-02-09 2021-05-07 国立大学法人冈山大学 乳酸脱氢酶抑制剂以及含有该抑制剂的抗癫痫剂
AU2017290233A1 (en) * 2016-06-29 2019-01-24 The Trustees Of The University Of Pennsylvania 1 H-pyrazol-1 -YL-thiazoles as inhibitors of lactate dehydrogenase and methods of use thereof
EP4306108A1 (en) * 2022-07-11 2024-01-17 Theodossis Theodossiou 5-aminolevulinic acid, or an ester thereof for use in treatment of cancer based on the inhibition of lactate dehydrogenase

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4950602A (en) * 1987-02-20 1990-08-21 Cornell Research Foundation, Inc. Inhibition of lactate production by pyruvate adducts

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1923481A1 (de) * 1969-05-08 1970-11-12 Hoechst Ag Verfahren zur Herstellung von Amiden und Estern der 1-Hydroxy-benzimidazol-2-carbonsaeure
DE2060199A1 (de) * 1970-12-08 1972-07-06 Bayer Ag 1-Hydroxy-2-carbonamido-benzimidazol-3-oxide sowie deren Alkalisalze
GB2065098A (en) * 1979-12-07 1981-06-24 Erba Farmitalia N-substituted Thiazolyl Derivatives of 7-amino- cephalosporanic Acid
US4762870A (en) * 1987-04-13 1988-08-09 The Firestone Tire & Rubber Company Rubber compositions modified with hydroxy-benz-imidazole oxides
JPH0331257A (ja) * 1989-06-28 1991-02-12 Kissei Pharmaceut Co Ltd インドール誘導体の製造方法
JPH0525140A (ja) * 1991-07-22 1993-02-02 Sankyo Co Ltd ベンズイミダゾール誘導体
US6169107B1 (en) * 1993-04-28 2001-01-02 Sumitomo Pharmaceutical Co., Ltd. Indoloylguanidine derivatives
EP0717984B1 (en) 1994-12-20 2004-11-03 Unilever Plc Lactate dehydrogenase inhibitors in cosmetic compositions
JP2935102B2 (ja) * 1996-07-04 1999-08-16 大塚化学株式会社 インドール−２−カルボン酸エステル誘導体及び該誘導体を有効成分とする農園芸用殺菌剤
WO1998036774A1 (en) 1996-12-18 1998-08-27 The Johns Hopkins University School Of Medicine Method of treating a lactate dehydrogenase-a (ldh-a)-associated disorder
EP1742637A4 (en) * 2004-04-23 2011-06-08 Paratek Pharm Innc TRANSCRIPTION FACTOR MODULATION COMPOUNDS AND METHODS OF USE
WO2006017494A2 (en) 2004-08-02 2006-02-16 Elizabeth Mazzio Inhibition of anaerobic glucose metabolism
JP2009020453A (ja) * 2007-07-13 2009-01-29 Fujifilm Corp 感光性組成物、硬化性組成物、カラーフィルタ用硬化性組成物、カラーフィルタ及びその製造方法、並びに、平版印刷版原版
US8278436B2 (en) 2008-07-30 2012-10-02 Wisconsin Alumni Research Foundation Glycosylated warfarin analogs and uses thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4950602A (en) * 1987-02-20 1990-08-21 Cornell Research Foundation, Inc. Inhibition of lactate production by pyruvate adducts

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
R.M.ACHESON ET AL: "The tautomerism and bromination of some 1-hydroxyindole-2-carboxylic acid derivatives", 《JOURNAL OF THE CHEMICAL SOCIETY SECTION C》 *

Also Published As

Publication number Publication date
EA201290316A1 (ru) 2012-10-30
EP2499114A1 (en) 2012-09-19
US20120309794A1 (en) 2012-12-06
AU2010314367A1 (en) 2012-05-31
CA2780136A1 (en) 2011-05-12
BR112012010868A2 (pt) 2017-02-21
ITPI20090140A1 (it) 2011-05-10
JP2013510106A (ja) 2013-03-21
WO2011054525A1 (en) 2011-05-12
ZA201203993B (en) 2014-11-26

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