CN103814024B - 作为溶血磷脂酸(lpa)受体拮抗剂的苄基哌啶化合物 - Google Patents

作为溶血磷脂酸(lpa)受体拮抗剂的苄基哌啶化合物 Download PDF

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Publication number
CN103814024B
CN103814024B CN201280046889.6A CN201280046889A CN103814024B CN 103814024 B CN103814024 B CN 103814024B CN 201280046889 A CN201280046889 A CN 201280046889A CN 103814024 B CN103814024 B CN 103814024B
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piperidin
benzyl
methyl
compound
subformula
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Chinese (zh)
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CN103814024A (zh
Inventor
K.席曼
W.施特勒
M.布施
D.维恩克
O.珀施克
C.布格尔
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Merck Patent GmbH
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Merck Patent GmbH
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02Ophthalmic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
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    • 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
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    • 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
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    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201280046889.6A 2011-09-26 2012-09-07 作为溶血磷脂酸(lpa)受体拮抗剂的苄基哌啶化合物 Expired - Fee Related CN103814024B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11007796 2011-09-26
EP11007796.3 2011-09-26
PCT/EP2012/003771 WO2013045028A1 (en) 2011-09-26 2012-09-07 Benzyl piperidine compounds as lysophosphatidic acid (lpa) receptor antagonist

Publications (2)

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CN103814024A CN103814024A (zh) 2014-05-21
CN103814024B true CN103814024B (zh) 2016-11-23

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US (1) US9527850B2 (enExample)
EP (1) EP2844648B1 (enExample)
JP (1) JP6163156B2 (enExample)
CN (1) CN103814024B (enExample)
AU (1) AU2012314943B9 (enExample)
CA (1) CA2849820C (enExample)
ES (1) ES2612934T3 (enExample)
IL (1) IL231699A (enExample)
WO (1) WO2013045028A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2809671B1 (en) * 2012-01-30 2016-01-13 Cephalon, Inc. Imidazo [4, 5 - b]pyridine derivatives as alk and jak modulators for the treatment of proliferative disorders
US10913736B2 (en) * 2014-08-22 2021-02-09 University Of Washington Specific inhibitors of methionyl-tRNA synthetase
JP7054529B2 (ja) 2016-06-21 2022-04-14 エックス4 ファーマシューティカルズ, インコーポレイテッド Cxcr4阻害剤およびその使用
WO2017223243A1 (en) * 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
WO2018016523A1 (ja) * 2016-07-20 2018-01-25 国立大学法人 長崎大学 新規放射線防護剤
WO2020007964A1 (en) * 2018-07-05 2020-01-09 Idorsia Pharmaceuticals Ltd 2-(2-azabicyclo[3.1.0]hexan-1-yl)-1h-benzimidazole derivatives
CN113461640B (zh) * 2021-06-17 2023-08-11 中央民族大学 Lpar1抑制剂、医药用途及其制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1695955A1 (en) * 2003-12-19 2006-08-30 Ono Pharmaceutical Co., Ltd. Compounds having lysophosphatidic acid receptor antagonism and uses thereof
US20090005416A1 (en) * 2007-06-29 2009-01-01 Pfizer Inc. Benzimidazole derivatives
WO2009102574A1 (en) * 2008-02-13 2009-08-20 Merck & Co., Inc. Quinolizidinone m1 receptor positive allosteric modulators
WO2010063352A1 (en) * 2008-12-01 2010-06-10 Merck Patent Gmbh 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer
WO2010115491A2 (en) * 2009-04-02 2010-10-14 Merck Patent Gmbh Piperidine and piperazine derivatives as autotaxin inhibitors

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
GB804786A (en) * 1955-12-16 1958-11-26 Rhone Poulenc Sa New indole derivatives and process for their preparation
FR2666582B1 (fr) * 1990-09-07 1994-09-02 Synthelabo Derives de benzimidazole, leur preparation et leur application en therapeutique.
ES2048109B1 (es) * 1992-07-20 1994-12-16 Espanola Prod Quimicos Procedimiento de preparacion de nuevos derivados piperidicos del bencimidazol.
US20090062268A1 (en) * 2007-08-27 2009-03-05 Lead Therapeutics, Inc. Novel inhibitors of poly(adp-ribose)polymerase (parp)

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1695955A1 (en) * 2003-12-19 2006-08-30 Ono Pharmaceutical Co., Ltd. Compounds having lysophosphatidic acid receptor antagonism and uses thereof
US20090005416A1 (en) * 2007-06-29 2009-01-01 Pfizer Inc. Benzimidazole derivatives
WO2009102574A1 (en) * 2008-02-13 2009-08-20 Merck & Co., Inc. Quinolizidinone m1 receptor positive allosteric modulators
WO2010063352A1 (en) * 2008-12-01 2010-06-10 Merck Patent Gmbh 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer
WO2010115491A2 (en) * 2009-04-02 2010-10-14 Merck Patent Gmbh Piperidine and piperazine derivatives as autotaxin inhibitors

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AU2012314943A1 (en) 2014-05-15
WO2013045028A9 (en) 2014-12-24
IL231699A (en) 2016-09-29
JP6163156B2 (ja) 2017-07-12
AU2012314943B2 (en) 2017-02-02
US9527850B2 (en) 2016-12-27
ES2612934T3 (es) 2017-05-19
WO2013045028A1 (en) 2013-04-04
CA2849820A1 (en) 2013-04-04
EP2844648B1 (en) 2016-11-09
CN103814024A (zh) 2014-05-21
JP2014526526A (ja) 2014-10-06
US20150011557A1 (en) 2015-01-08
AU2012314943B9 (en) 2017-06-08
CA2849820C (en) 2019-08-27
EP2844648A1 (en) 2015-03-11
IL231699A0 (en) 2014-05-28

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