CN102056922B - 作为tafia抑制剂的大环脲和磺酰胺衍生物 - Google Patents

作为tafia抑制剂的大环脲和磺酰胺衍生物 Download PDF

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Publication number
CN102056922B
CN102056922B CN2009801210767A CN200980121076A CN102056922B CN 102056922 B CN102056922 B CN 102056922B CN 2009801210767 A CN2009801210767 A CN 2009801210767A CN 200980121076 A CN200980121076 A CN 200980121076A CN 102056922 B CN102056922 B CN 102056922B
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formula
compound
oxo
amino
dioxa
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CN102056922A (zh
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克里斯托弗·卡勒斯
马克·不伦斯特拉普
安德烈亚斯·埃弗尔斯
安贾·格洛比希
赫尔曼·施鲁德
迈克尔·瓦格纳
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Sanofi Aventis France
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/01—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having one nitrogen atom
    • 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
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
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    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN2009801210767A 2008-06-06 2009-05-22 作为tafia抑制剂的大环脲和磺酰胺衍生物 Expired - Fee Related CN102056922B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08290520.9 2008-06-06
EP08290520 2008-06-06
PCT/EP2009/003650 WO2009146802A1 (de) 2008-06-06 2009-05-22 Makrocyclische harnstoff- und sulfamidderivate als inhibitoren von tafia

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CN102056922A CN102056922A (zh) 2011-05-11
CN102056922B true CN102056922B (zh) 2013-11-20

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CN2009801210767A Expired - Fee Related CN102056922B (zh) 2008-06-06 2009-05-22 作为tafia抑制剂的大环脲和磺酰胺衍生物

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US (5) US8580777B2 (cg-RX-API-DMAC7.html)
EP (1) EP2300462B1 (cg-RX-API-DMAC7.html)
JP (1) JP5531011B2 (cg-RX-API-DMAC7.html)
KR (1) KR101673886B1 (cg-RX-API-DMAC7.html)
CN (1) CN102056922B (cg-RX-API-DMAC7.html)
AR (1) AR072007A1 (cg-RX-API-DMAC7.html)
AU (1) AU2009254257B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0913349A2 (cg-RX-API-DMAC7.html)
CA (1) CA2726554C (cg-RX-API-DMAC7.html)
CL (1) CL2009001358A1 (cg-RX-API-DMAC7.html)
CO (1) CO6321271A2 (cg-RX-API-DMAC7.html)
CR (1) CR11807A (cg-RX-API-DMAC7.html)
CY (1) CY1115604T1 (cg-RX-API-DMAC7.html)
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DO (1) DOP2010000363A (cg-RX-API-DMAC7.html)
EC (1) ECSP10010655A (cg-RX-API-DMAC7.html)
ES (1) ES2494390T3 (cg-RX-API-DMAC7.html)
HN (1) HN2010002558A (cg-RX-API-DMAC7.html)
HR (1) HRP20140787T1 (cg-RX-API-DMAC7.html)
IL (1) IL209772A (cg-RX-API-DMAC7.html)
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Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2494390T3 (es) 2008-06-06 2014-09-15 Sanofi Derivados macrocíclicos de urea y de sulfamida como inhibidores de TAFIa
AU2009263076B2 (en) 2008-06-23 2012-07-26 Astrazeneca Ab New heterocyclic carboxamides for use as thrombin inhibitors
US8354444B2 (en) 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
ME02630B (me) * 2012-03-06 2017-06-20 Pfizer Makrociklički derivati, namijenjeni liječenju proliferativnih bolesti
EP3027611B1 (en) * 2013-06-10 2017-07-26 Sanofi Macrocyclic urea derivatives as inhibitors of tafi a, their preparation and their use as pharmaceuticals
UY35809A (es) * 2013-11-05 2015-05-29 Bayer Pharma AG (aza)piridopirazolopirimidinonas e indazolopirimidinonas y sus usos
CN103755852B (zh) * 2013-12-18 2015-12-09 湖北大学 线型聚苯乙烯支载(4s)-(4’-氧苄基)-2-正丁基环磺酰胺及其制备方法和用途
CN106631832A (zh) * 2016-10-08 2017-05-10 帕潘纳(北京)科技有限公司 一种氨基醚类化合物的制备方法
US10411291B2 (en) * 2017-03-22 2019-09-10 Nanotek Instruments, Inc. Multivalent metal ion battery having a cathode layer of protected graphitic carbon and manufacturing method

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WO1997030080A1 (en) * 1996-02-20 1997-08-21 Ortho Pharmaceutical Corporation Macrocyclic peptides useful in the treatment of thrombin related disorders
WO2005105781A1 (de) * 2004-04-22 2005-11-10 Sanofi-Aventis Deutschland Gmbh Imidazol-derivate als tafia-inhibitoren

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AU667995B2 (en) 1993-02-15 1996-04-18 Bayer Aktiengesellschaft New pseudopeptides having an antiviral action
TW394760B (en) 1993-09-07 2000-06-21 Hoffmann La Roche Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same
CA2298601A1 (en) 1997-08-28 1999-03-11 Pharmacia & Upjohn Company Inhibitors of protein tyrosine phosphatase
US6124278A (en) * 1998-04-03 2000-09-26 The Regents Of The University Of California Acylbenzoxazines for enhancing synaptic response
US6482921B1 (en) 1999-01-28 2002-11-19 Essential Therapeutics, Inc. Uridyl peptide antibiotic (UPA) derivatives, their synthesis and use
DE60042585D1 (de) * 2000-02-29 2009-09-03 Univ Firenze 3-Aza-6,8-dioxabicycloÄ3.2.1Üoctane und Analoga sowie diese enthaltende kombinatorische Bibliotheken
AU2007327959B2 (en) 2006-12-06 2013-08-01 Sanofi-Aventis Urea and sulfamide derivatives as tafia inhibitors
ES2494390T3 (es) 2008-06-06 2014-09-15 Sanofi Derivados macrocíclicos de urea y de sulfamida como inhibidores de TAFIa

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997030080A1 (en) * 1996-02-20 1997-08-21 Ortho Pharmaceutical Corporation Macrocyclic peptides useful in the treatment of thrombin related disorders
WO2005105781A1 (de) * 2004-04-22 2005-11-10 Sanofi-Aventis Deutschland Gmbh Imidazol-derivate als tafia-inhibitoren

Non-Patent Citations (1)

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Title
Design and synthesis of potent and selective macrocyclic thrombin inhibitors;Philippe G. Nantermet,et al.;《Bioorganic & Medicinal Chemistry Letters》;20031231;第13卷;2781-2784 *

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Publication number Publication date
MX2010012793A (es) 2010-12-14
RU2010154089A (ru) 2012-07-20
US9126955B2 (en) 2015-09-08
IL209772A0 (en) 2011-02-28
KR101673886B1 (ko) 2016-11-08
DOP2010000363A (es) 2010-12-15
AU2009254257A1 (en) 2009-12-10
CA2726554A1 (en) 2009-12-10
US20140039011A1 (en) 2014-02-06
RU2502736C2 (ru) 2013-12-27
EP2300462B1 (de) 2014-05-21
US20160251324A1 (en) 2016-09-01
ES2494390T3 (es) 2014-09-15
US9688645B2 (en) 2017-06-27
CA2726554C (en) 2015-02-24
HN2010002558A (es) 2012-08-28
EP2300462A1 (de) 2011-03-30
AR072007A1 (es) 2010-07-28
WO2009146802A1 (de) 2009-12-10
US20110178130A1 (en) 2011-07-21
US20140206760A1 (en) 2014-07-24
US8580777B2 (en) 2013-11-12
KR20110020795A (ko) 2011-03-03
PL2300462T3 (pl) 2014-10-31
JP5531011B2 (ja) 2014-06-25
IL209772A (en) 2016-04-21
ZA201007719B (en) 2011-07-27
SI2300462T1 (sl) 2014-09-30
NZ589671A (en) 2012-03-30
TWI455928B (zh) 2014-10-11
UY31868A (es) 2010-01-05
JP2011521981A (ja) 2011-07-28
UA104002C2 (ru) 2013-12-25
ECSP10010655A (es) 2011-01-31
US20160024033A1 (en) 2016-01-28
HK1152936A1 (en) 2012-03-16
CN102056922A (zh) 2011-05-11
NI201000203A (es) 2011-09-29
CO6321271A2 (es) 2011-09-20
MA32322B1 (fr) 2011-05-02
CY1115604T1 (el) 2017-01-04
SV2010003747A (es) 2011-03-15
PT2300462E (pt) 2014-08-05
AU2009254257B2 (en) 2013-11-21
TW201008917A (en) 2010-03-01
HRP20140787T1 (hr) 2014-11-21
US8722655B2 (en) 2014-05-13
US9309207B2 (en) 2016-04-12
CL2009001358A1 (es) 2009-11-27
DK2300462T3 (da) 2014-08-18
CR11807A (es) 2011-02-16
BRPI0913349A2 (pt) 2015-11-24

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