CN102574858B - 双环杂环及其作为ccr2受体拮抗剂的用途 - Google Patents

双环杂环及其作为ccr2受体拮抗剂的用途 Download PDF

Info

Publication number
CN102574858B
CN102574858B CN201080044805.6A CN201080044805A CN102574858B CN 102574858 B CN102574858 B CN 102574858B CN 201080044805 A CN201080044805 A CN 201080044805A CN 102574858 B CN102574858 B CN 102574858B
Authority
CN
China
Prior art keywords
spiro
oxo
methyl
aza
phenyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN201080044805.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN102574858A (zh
Inventor
约翰尼斯.埃比
阿尔弗雷德·宾格里
卢克·格林
古伊多·哈特曼
汉斯·P·梅尔基
帕特里齐奥·马太
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CN102574858A publication Critical patent/CN102574858A/zh
Application granted granted Critical
Publication of CN102574858B publication Critical patent/CN102574858B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • 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
    • A61P9/08—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
    • 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
    • C07D417/02—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (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)
CN201080044805.6A 2009-10-07 2010-10-05 双环杂环及其作为ccr2受体拮抗剂的用途 Expired - Fee Related CN102574858B (zh)

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
CN102574858A CN102574858A (zh) 2012-07-11
CN102574858B true CN102574858B (zh) 2015-06-24

Family

ID=43105073

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080044805.6A Expired - Fee Related CN102574858B (zh) 2009-10-07 2010-10-05 双环杂环及其作为ccr2受体拮抗剂的用途

Country Status (13)

Country Link
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
EP2771484A1 (en) 2011-10-28 2014-09-03 Galderma Research & Development New leukocyte infiltrate markers for rosacea and uses thereof
ES2764840T3 (es) 2015-01-28 2020-06-04 Univ Bordeaux Uso de plerixafor para tratar y/o prevenir exacerbaciones agudas de la enfermedad pulmonar obstructiva crónica
EP3833762A4 (en) 2018-08-09 2022-09-28 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

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004529113A (ja) * 2001-03-07 2004-09-24 ファイザー・プロダクツ・インク ケモカイン受容体活性のモジュレーター
WO2004076411A3 (en) * 2003-02-24 2004-12-23 Merck & Co Inc Aminocyclopentyl fused heterotricylicamide modulators of chemokine receptor activity
US20060199805A1 (en) * 2005-03-04 2006-09-07 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for the treatment and/or prevention of anxiety disorders
CN1956976A (zh) * 2004-05-26 2007-05-02 詹森药业有限公司 作为ccr2受体拮抗剂的巯基咪唑化合物
WO2009010429A2 (en) * 2007-07-19 2009-01-22 F. Hoffmann-La Roche Ag Novel heterocyclyl compounds and their use as chemokine antagonists
WO2009043747A2 (en) * 2007-10-01 2009-04-09 F. Hoffmann-La Roche Ag N-heterocyclic biaryl carboxamides as ccr receptor antagonists

Family Cites Families (2)

* 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
WO2007122103A1 (en) * 2006-04-20 2007-11-01 F. Hoffmann-La Roche Ag Diazepan derivatives modulators of chemokine receptors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004529113A (ja) * 2001-03-07 2004-09-24 ファイザー・プロダクツ・インク ケモカイン受容体活性のモジュレーター
WO2004076411A3 (en) * 2003-02-24 2004-12-23 Merck & Co Inc Aminocyclopentyl fused heterotricylicamide modulators of chemokine receptor activity
CN1956976A (zh) * 2004-05-26 2007-05-02 詹森药业有限公司 作为ccr2受体拮抗剂的巯基咪唑化合物
US20060199805A1 (en) * 2005-03-04 2006-09-07 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for the treatment and/or prevention of anxiety disorders
WO2009010429A2 (en) * 2007-07-19 2009-01-22 F. Hoffmann-La Roche Ag Novel heterocyclyl compounds and their use as chemokine antagonists
WO2009043747A2 (en) * 2007-10-01 2009-04-09 F. Hoffmann-La Roche Ag N-heterocyclic biaryl carboxamides as ccr receptor antagonists

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Synthesis of 2,5-and 2,3,5-substituted hexahydropyrrolo[1,2-c] imidazolones;L.FONTANELLA.等;《Farmaco, Edizione Scientifica》;19731231;第28卷(第6期);第463-477页，参见第465页schema 1化合物X *

Also Published As

Publication number Publication date
IN2012DN00764A (enExample) 2015-06-26
EP2486042A1 (en) 2012-08-15
MX2012002390A (es) 2012-04-02
BR112012008221A2 (pt) 2016-03-08
US8471004B2 (en) 2013-06-25
US20110082294A1 (en) 2011-04-07
EP2486042B1 (en) 2014-01-22
ES2455266T3 (es) 2014-04-15
IL217965A0 (en) 2012-03-29
CN102574858A (zh) 2012-07-11
JP5559336B2 (ja) 2014-07-23
KR20120051090A (ko) 2012-05-21
JP2013506701A (ja) 2013-02-28
KR101451487B1 (ko) 2014-10-15
CA2774215A1 (en) 2011-04-14
WO2011042399A1 (en) 2011-04-14
AU2010305495A1 (en) 2012-03-15

Similar Documents

Publication Publication Date Title
AU2002357264B2 (en) Pyrrolidine and piperidine derivates as NK1 antagonists
JP5016666B2 (ja) ケモカイン受容体のジアゼパン誘導体モジュレーター
JP6928629B2 (ja) Ｃｎｓ疾患を治療するための縮合ジヒドロ−４ｈ−ピラゾロ［５，１−ｃ］［１，４］オキサジニル化合物およびアナログ
JP4846665B2 (ja) ピラゾロ［１，５−ａ］ピリミジン化合物
WO2007046550A1 (en) Pyrazole compounds having cannabinoid receptor (cb1) antagonizing activity
CA2885987A1 (en) Pyridine-2-amides useful as cb2 agonists
CN101754957A (zh) 新的杂环基化合物和它们作为趋化因子拮抗剂的用途
CN101421235A (zh) 5-酰氨基-2-酰胺吲哚
CN102574858B (zh) 双环杂环及其作为ccr2受体拮抗剂的用途
JP5654027B2 (ja) ケモカイン受容体のモジュレーターとしてのジアゼパン誘導体
CN104364258B (zh) 用于治疗神经变性疾病的螺四氢‑苯并噻吩衍生物
JP2021506821A (ja) バソプレシンＶ１ａ受容体拮抗薬としてのトリアゾロベンズアゼピン
AU2005279278A1 (en) Fused tricyclic derivatives for the treatment of psychotic disorders
US7354922B2 (en) Bridged ring NK1 antagonists
JPH09208582A (ja) ３−アザ及び３−オキサピペリドンタキキニン拮抗薬
JP5389917B2 (ja) ケモカインレセプターのジアゼパン及びピペラジン誘導体モデュレーター
CN102089289A (zh) 用于治疗心血管疾病的新的杂环基化合物
JP2008024693A (ja) ピラゾール化合物
RU2409582C2 (ru) Конденсированные трициклические производные для лечения психотических расстройств

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20150624

Termination date: 20161005

CF01 Termination of patent right due to non-payment of annual fee