CN103415506B - 作为用于治疗糖尿病的hsl抑制剂的仲-羟基环己基衍生物 - Google Patents

作为用于治疗糖尿病的hsl抑制剂的仲-羟基环己基衍生物 Download PDF

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Publication number
CN103415506B
CN103415506B CN201280012084.XA CN201280012084A CN103415506B CN 103415506 B CN103415506 B CN 103415506B CN 201280012084 A CN201280012084 A CN 201280012084A CN 103415506 B CN103415506 B CN 103415506B
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China
Prior art keywords
phenyl
hydroxy
alkyl
compound
trifluoro
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Expired - Fee Related
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CN201280012084.XA
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English (en)
Chinese (zh)
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CN103415506A (zh
Inventor
丹尼尔·洪齐格
维尔纳·奈德哈特
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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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
    • C07D209/54—Spiro-condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/402—1-aryl substituted, e.g. piretanide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
CN201280012084.XA 2011-03-16 2012-03-13 作为用于治疗糖尿病的hsl抑制剂的仲-羟基环己基衍生物 Expired - Fee Related CN103415506B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11158386 2011-03-16
EP11158386.0 2011-03-16
PCT/EP2012/054307 WO2012123432A1 (en) 2011-03-16 2012-03-13 Sec-hydroxycyclohexyl derivatives as hsl inhibitors for the treatment diabetes

Publications (2)

Publication Number Publication Date
CN103415506A CN103415506A (zh) 2013-11-27
CN103415506B true CN103415506B (zh) 2015-08-05

Family

ID=45812793

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CN201280012084.XA Expired - Fee Related CN103415506B (zh) 2011-03-16 2012-03-13 作为用于治疗糖尿病的hsl抑制剂的仲-羟基环己基衍生物

Country Status (10)

Country Link
US (1) US8722721B2 (enExample)
EP (1) EP2686299A1 (enExample)
JP (1) JP6117709B2 (enExample)
KR (1) KR20140022840A (enExample)
CN (1) CN103415506B (enExample)
BR (1) BR112013022416A2 (enExample)
CA (1) CA2830126A1 (enExample)
MX (1) MX339513B (enExample)
RU (1) RU2013142647A (enExample)
WO (1) WO2012123432A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8097634B2 (en) * 2010-04-15 2012-01-17 Hoffmann-La Roche Inc. Azacyclic derivatives
US8809384B2 (en) * 2011-03-25 2014-08-19 Hoffmann-La Roche Inc. Azaspirodecanone compounds
UY36060A (es) 2014-04-02 2015-10-30 Bayer Pharma AG Compuestos de azol sustituidos con amida
CN104788360B (zh) * 2015-03-30 2017-07-25 曲阜师范大学 3‑砜基螺环三烯酮类化合物及其制备方法
CN117551046B (zh) * 2023-11-17 2025-10-28 广东药科大学附属第一医院 二氨基脲类hsl抑制剂、制备方法及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101432265A (zh) * 2006-04-25 2009-05-13 伊莱利利公司 11-β-羟类固醇脱氢酶1的抑制剂
CN102858743A (zh) * 2009-10-15 2013-01-02 霍夫曼-拉罗奇有限公司 作为可用于治疗糖尿病的hsl抑制剂的螺环-稠合的环己烷衍生物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10247680B4 (de) * 2002-10-12 2005-09-01 Aventis Pharma Deutschland Gmbh Neue bicyclische Inhibitoren der Hormon Sensitiven Lipase
EP1529528A1 (en) * 2003-11-07 2005-05-11 Universitätsklinikum Freiburg 2-pyrrolidone derivatives and their use in protecting mammalian cells against oxidation stress
WO2007103719A2 (en) * 2006-03-03 2007-09-13 Incyte Corporation MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
US8329904B2 (en) * 2009-05-12 2012-12-11 Hoffmann-La Roche Inc. Azacyclic derivatives
TW201118069A (en) * 2009-10-28 2011-06-01 Lundbeck & Co As H Spirolactam derivatives and uses of same
US8389539B2 (en) * 2009-12-01 2013-03-05 Hoffman-La Roche Inc. Azacyclic derivatives
US8097634B2 (en) * 2010-04-15 2012-01-17 Hoffmann-La Roche Inc. Azacyclic derivatives
AR081384A1 (es) 2010-05-11 2012-08-29 Sanofi Aventis N- fenil espirolactama bipirrolidinas sustituidas, preparacion y uso terapeutico de las mismas

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101432265A (zh) * 2006-04-25 2009-05-13 伊莱利利公司 11-β-羟类固醇脱氢酶1的抑制剂
CN102858743A (zh) * 2009-10-15 2013-01-02 霍夫曼-拉罗奇有限公司 作为可用于治疗糖尿病的hsl抑制剂的螺环-稠合的环己烷衍生物

Also Published As

Publication number Publication date
EP2686299A1 (en) 2014-01-22
BR112013022416A2 (pt) 2016-12-13
WO2012123432A1 (en) 2012-09-20
US20120238613A1 (en) 2012-09-20
US8722721B2 (en) 2014-05-13
CA2830126A1 (en) 2012-09-20
HK1190706A1 (en) 2014-07-11
MX2013010006A (es) 2013-12-06
KR20140022840A (ko) 2014-02-25
MX339513B (es) 2016-05-30
JP6117709B2 (ja) 2017-04-19
CN103415506A (zh) 2013-11-27
RU2013142647A (ru) 2015-04-27
JP2014508178A (ja) 2014-04-03

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