KR101451487B1 - 이환형 헤테로환 및 ccr2 수용체 길항제로서의 이의 용도 - Google Patents

이환형 헤테로환 및 ccr2 수용체 길항제로서의 이의 용도 Download PDF

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KR101451487B1
KR101451487B1 KR1020127008883A KR20127008883A KR101451487B1 KR 101451487 B1 KR101451487 B1 KR 101451487B1 KR 1020127008883 A KR1020127008883 A KR 1020127008883A KR 20127008883 A KR20127008883 A KR 20127008883A KR 101451487 B1 KR101451487 B1 KR 101451487B1
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alkyl
hydroxy
methyl
oxo
carboxylic acid
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KR20120051090A (ko
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요한네스 애비
알프레드 빙겔리
루크 그린
귀도 하르트만
한스 피 매르키
파트리지오 맛타이
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에프. 호프만-라 로슈 아게
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020127008883A 2009-10-07 2010-10-05 이환형 헤테로환 및 ccr2 수용체 길항제로서의 이의 용도 Expired - Fee Related KR101451487B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09172408.8 2009-10-07
EP09172408 2009-10-07
PCT/EP2010/064770 WO2011042399A1 (en) 2009-10-07 2010-10-05 Bicyclic heterocycles and their use as ccr2 receptor antagonists

Publications (2)

Publication Number Publication Date
KR20120051090A KR20120051090A (ko) 2012-05-21
KR101451487B1 true KR101451487B1 (ko) 2014-10-15

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KR1020127008883A Expired - Fee Related KR101451487B1 (ko) 2009-10-07 2010-10-05 이환형 헤테로환 및 ccr2 수용체 길항제로서의 이의 용도

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US (1) US8471004B2 (enExample)
EP (1) EP2486042B1 (enExample)
JP (1) JP5559336B2 (enExample)
KR (1) KR101451487B1 (enExample)
CN (1) CN102574858B (enExample)
AU (1) AU2010305495A1 (enExample)
BR (1) BR112012008221A2 (enExample)
CA (1) CA2774215A1 (enExample)
ES (1) ES2455266T3 (enExample)
IL (1) IL217965A0 (enExample)
IN (1) IN2012DN00764A (enExample)
MX (1) MX2012002390A (enExample)
WO (1) WO2011042399A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2852160A1 (en) 2011-10-28 2013-05-02 Galderma Research & Development New leukocyte infiltrate markers for rosacea and uses thereof
DK3050574T3 (da) 2015-01-28 2020-01-20 Univ Bordeaux Anvendelse af plerixafor til behandling og/eller forebyggelse af akutte forværringer af kronisk obstruktiv lungesygdom
WO2020033791A1 (en) 2018-08-09 2020-02-13 Verseau Therapeutics, Inc. Oligonucleotide compositions for targeting ccr2 and csf1r and uses thereof
CN111423454B (zh) * 2020-04-24 2021-06-22 苏州大学 哌嗪类化合物及其在制备趋化因子受体ccr2拮抗剂中的应用
CN113979889A (zh) * 2021-11-09 2022-01-28 西安康福诺生物科技有限公司 一种双官能化聚乙二醇基胺的合成方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3740256A1 (de) 1987-05-14 1988-12-08 Bayer Ag Thiazolo-hydantoine
WO2002070523A1 (en) * 2001-03-07 2002-09-12 Pfizer Products Inc. Modulators of chemokine receptor activity
CA2516705A1 (en) * 2003-02-24 2004-09-10 Merck & Co., Inc. Aminocyclopentyl fused heterotricylicamide modulators of chemokine receptor activity
EP1756089B1 (en) * 2004-05-26 2008-10-22 Janssen Pharmaceutica N.V. Mercaptoimidazoles as ccr2 receptor antagonists
EP1858515A2 (en) * 2005-03-04 2007-11-28 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for the treatment and/or prevention of anxiety disorders
KR101176697B1 (ko) * 2006-04-20 2012-08-23 에프. 호프만-라 로슈 아게 케모카인 수용체의 다이아제판 유도체 조절자
CA2695998A1 (en) 2007-07-19 2009-01-22 F. Hoffmann-La Roche Ag Novel heterocyclyl compounds
MX2010003621A (es) 2007-10-01 2010-04-14 Hoffmann La Roche N-heterociclil biaril carboxamidas como antagonistas del receptor ccr.

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
IL Farmaco Edizione. Scientifica, 1973, vol.28(6), pp.463-477 *
IL Farmaco Edizione. Scientifica, 1973, vol.28(6), pp.463-477*

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JP5559336B2 (ja) 2014-07-23
EP2486042B1 (en) 2014-01-22
IN2012DN00764A (enExample) 2015-06-26
ES2455266T3 (es) 2014-04-15
US20110082294A1 (en) 2011-04-07
US8471004B2 (en) 2013-06-25
IL217965A0 (en) 2012-03-29
AU2010305495A1 (en) 2012-03-15
MX2012002390A (es) 2012-04-02
EP2486042A1 (en) 2012-08-15
BR112012008221A2 (pt) 2016-03-08
CN102574858B (zh) 2015-06-24
KR20120051090A (ko) 2012-05-21
CN102574858A (zh) 2012-07-11
WO2011042399A1 (en) 2011-04-14
JP2013506701A (ja) 2013-02-28
CA2774215A1 (en) 2011-04-14

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