CN103168027B - 制备环丙基酰胺衍生物的方法及其相关中间体 - Google Patents

制备环丙基酰胺衍生物的方法及其相关中间体 Download PDF

Info

Publication number
CN103168027B
CN103168027B CN201180019632.7A CN201180019632A CN103168027B CN 103168027 B CN103168027 B CN 103168027B CN 201180019632 A CN201180019632 A CN 201180019632A CN 103168027 B CN103168027 B CN 103168027B
Authority
CN
China
Prior art keywords
compound
formula
jacket
ester group
preparation formula
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
CN201180019632.7A
Other languages
English (en)
Chinese (zh)
Other versions
CN103168027A (zh
Inventor
R.斯特兰恩
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.)
AstraZeneca AB
Original Assignee
AstraZeneca AB
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44370080&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN103168027(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by AstraZeneca AB filed Critical AstraZeneca AB
Publication of CN103168027A publication Critical patent/CN103168027A/zh
Application granted granted Critical
Publication of CN103168027B publication Critical patent/CN103168027B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/65—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/06—Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/14—Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/84—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Epoxy Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201180019632.7A 2010-02-18 2011-02-17 制备环丙基酰胺衍生物的方法及其相关中间体 Expired - Fee Related CN103168027B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30558310P 2010-02-18 2010-02-18
US61/305,583 2010-02-18
PCT/SE2011/050171 WO2011102794A1 (en) 2010-02-18 2011-02-17 Processes for making cyclopropyl amide derivatives and intermediates associated therewith

Publications (2)

Publication Number Publication Date
CN103168027A CN103168027A (zh) 2013-06-19
CN103168027B true CN103168027B (zh) 2015-08-26

Family

ID=44370080

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201180019632.7A Expired - Fee Related CN103168027B (zh) 2010-02-18 2011-02-17 制备环丙基酰胺衍生物的方法及其相关中间体
CN2011800196365A Pending CN102869651A (zh) 2010-02-18 2011-02-17 环丙基苯甲酰胺衍生物的新结晶形式

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2011800196365A Pending CN102869651A (zh) 2010-02-18 2011-02-17 环丙基苯甲酰胺衍生物的新结晶形式

Country Status (19)

Country Link
US (2) US20110201623A1 (https=)
EP (2) EP2536702A4 (https=)
JP (3) JP2013520413A (https=)
KR (2) KR20130002316A (https=)
CN (2) CN103168027B (https=)
AR (2) AR080204A1 (https=)
AU (2) AU2011218491C1 (https=)
BR (2) BR112012020782A2 (https=)
CA (2) CA2788444A1 (https=)
CL (2) CL2012002259A1 (https=)
CO (1) CO6592109A2 (https=)
ES (1) ES2541857T3 (https=)
IL (1) IL221431A (https=)
MX (2) MX336333B (https=)
NZ (2) NZ602110A (https=)
RU (2) RU2012139082A (https=)
SG (3) SG10201501226VA (https=)
TW (2) TWI520945B (https=)
WO (2) WO2011102795A1 (https=)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SA08290520B1 (ar) 2007-08-22 2012-02-22 استرازينيكا ايه بي مشتقات سيكلو بروبيل أميد وتركيبات صيدلية تحتوي عليها لعلاج حالة مرضية سببها مستقبلات هيستامين h3
TW201039825A (en) * 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
JP5746718B2 (ja) * 2010-02-18 2015-07-08 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ シクロプロピルアミド誘導体からなる固体形態
RU2012139082A (ru) * 2010-02-18 2014-03-27 Астразенека Аб Способы получения производных циклопропиламида и связанных с ними промежуточных соединений
FR3003466B1 (fr) * 2013-03-22 2015-08-07 Servier Lab Utilisation du 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1h)-yl]propoxy}benzamide pour le traitement des douleurs neuropathiques
EP2976322B1 (de) * 2013-03-22 2019-11-20 Merck Patent GmbH Synthesebausteine für die herstellung von materialien für organische elektrolumineszenzvorrichtungen
CN103342655A (zh) * 2013-07-02 2013-10-09 扬州大学 取代乙二酮双苯胺希夫碱合成取代酰胺的新方法
JP2026000886A (ja) 2024-06-18 2026-01-06 イーライ リリー アンド カンパニー Ｇｉｐ受容体アゴニスト化合物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006087169A1 (en) * 2005-02-15 2006-08-24 Glaxo Group Limited Compounds which potentiate glutamate receptor and uses thereof in medicine
WO2007011065A2 (en) * 2005-07-22 2007-01-25 Mitsubishi Tanabe Pharma Corporation Intermediate compound for synthesizing pharmaceutical agent and production method thereof
WO2008075068A2 (en) * 2006-12-21 2008-06-26 Astrazeneca Ab Acylaminopyrazoles as fgfr inhibitors
CN101462980A (zh) * 2009-01-05 2009-06-24 扬州天辰精细化工有限公司 2，6—二氟苯甲酰胺的工业化生产方法
WO2009135842A1 (en) * 2008-05-08 2009-11-12 Evotec Neurosciences Gmbh Azetidines and cyclobutanes as histamine h3 receptor antagonists

Family Cites Families (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE637271A (https=) 1963-04-04 1900-01-01
NL128365C (https=) 1963-11-05
US3449427A (en) 1965-06-03 1969-06-10 Smithkline Corp Aminocyclopropane derivatives of 5h-dibenzo(a,d)cycloheptenes
US3697506A (en) 1970-08-07 1972-10-10 Pfizer Crystalline alkali metal salts of {60 -carboxybenzylpenicillin and process therefor
US3686335A (en) 1970-12-21 1972-08-22 Smith Kline French Lab 5-vinyl-5h-di benzo(a,d)cycloheptenes
US4432987A (en) * 1982-04-23 1984-02-21 Pfizer Inc. Crystalline benzenesulfonate salts of sultamicillin
US4547505A (en) 1983-03-25 1985-10-15 Degussa Aktiengesellschaft N-Phenyl-N-'-cycloalkylalkanoylpiperazine useful as analgetics and process for its production
CS244821B2 (en) 1983-06-16 1986-08-14 Boehringer Ingelheim Ltd Production method of new substituted phenylalkyl(piperazinyl or homopiperazinyle)-prpylureas or thioureas
DE3418167A1 (de) 1984-05-16 1985-11-21 Bayer Ag, 5090 Leverkusen Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen heteroaryloxyacetamiden
DE3600288A1 (de) 1986-01-08 1987-07-16 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonylharnstoff-derivaten
DE3618004A1 (de) 1986-05-28 1987-12-03 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonyliso(thio)-harnstoff-derivaten
EP0507863A4 (en) 1989-12-28 1993-07-07 Virginia Commonwealth University Sigma receptor ligands and the use thereof
EP0435320B1 (en) 1989-12-29 1994-10-05 Banyu Pharmaceutical Co., Ltd. 2(2-Cyclopropylpyrrolidin-4-ylthio)-carbapenem derivatives
AU2505392A (en) 1991-08-22 1993-03-16 Monsanto Company Safening herbicidal pyrazolylsulfonylureas
DE4131139A1 (de) 1991-09-19 1993-03-25 Bayer Ag Verfahren zur herstellung von 1-fluor-cyclopropan-1-carbonsaeure
US5721359A (en) 1993-03-12 1998-02-24 Pharmacia & Upjohn Company Crystalline ceftiofur free acid
AU4368996A (en) 1994-11-23 1996-06-17 Neurogen Corporation Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands
US5604253A (en) 1995-05-22 1997-02-18 Merck Frosst Canada, Inc. N-benzylindol-3-yl propanoic acid derivatives as cyclooxygenase inhibitors
US5859246A (en) 1997-01-30 1999-01-12 Neurogen Corporation 1-phenyl-4-benzylpiperazines: dopamine receptor subtype specific ligands
US6124299A (en) 1997-02-24 2000-09-26 Zymogenetics, Inc. Calcitonin mimetics
US6160134A (en) 1997-12-24 2000-12-12 Bristol-Myers Squibb Co. Process for preparing chiral cyclopropane carboxylic acids and acyl guanidines
TR200002182T2 (tr) 1998-01-27 2000-12-21 Aventis Pharmaceuticals Products Inc. İkame edilmiş aksozaherosayklil faktör xa inhibitörleri
US6268367B1 (en) 1998-02-23 2001-07-31 Zymogenetics, Inc. Piperazine derivatives for treating bone deficit conditions
US6383520B1 (en) 1998-06-26 2002-05-07 Chugai Seiyaku Kabushiki Kaisha Fine powder of L-α-aminoadipic acid derivative, oral solid preparations containing the same, and method for treatment of bulk powders
US6284761B1 (en) 1999-01-08 2001-09-04 Neurogen Corporation 1-phenyl-4-(1-[2-aryl]cyclopropyl)methylpiperazines: dopamine receptor ligands
JP2002534421A (ja) 1999-01-08 2002-10-15 ニューロゲン コーポレイション １−フェニル−４−（１−［２−アリール］シクロプロピル）メチルピペラジン：ドーパミン受容体リガンド
GB9913083D0 (en) * 1999-06-04 1999-08-04 Novartis Ag Organic compounds
AU5426500A (en) 1999-06-16 2001-01-02 Takeda Chemical Industries Ltd. Benzazepine derivatives, process for the preparation of the same and uses thereof
WO2001022963A1 (en) 1999-09-27 2001-04-05 Merck & Co., Inc. Method of preventing osteoporosis
WO2001051919A2 (en) 2000-01-07 2001-07-19 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
US6521619B2 (en) 2000-06-29 2003-02-18 Icos Corporation Aryl phenylcyclopropyl sulfide derivatives and their use as cell adhesion inhibiting anti-inflammatory and immune suppressive agents
AU2001268724B2 (en) 2000-06-29 2005-06-16 Abbott Laboratories Aryl phenycyclopropyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
JP2004525071A (ja) 2000-07-20 2004-08-19 ニューロジェン コーポレイション カプサイシン受容体リガンド
WO2002051781A1 (fr) 2000-12-25 2002-07-04 Ajinomoto Co., Inc. Procede permettant de preparer un compose d'halohydrine optiquement actif
PL364625A1 (en) * 2001-02-23 2004-12-13 Merck & Co, Inc. N-substituted nonaryl-heterocyclic nmda/nr2b antagonists
EP1421071B1 (en) 2001-07-02 2009-11-18 High Point Pharmaceuticals, LLC Substituted piperazine and diazepane derivaives as histamine h3 receptor modulators
US7262185B2 (en) 2001-08-08 2007-08-28 Takeda Chemical Industries Ltd. Benzazepine derivative, process for producing the same, and use
US7145002B2 (en) 2001-09-26 2006-12-05 Merck & Co. Inc. Crystalline forms of carbapenem antibiotics and methods of preparation
AU2002363236A1 (en) * 2001-10-30 2003-05-12 Millennium Pharmaceuticals, Inc. Compounds, pharmaceutical compositions and methods of use therefor
US6861432B2 (en) * 2001-11-23 2005-03-01 Schering Aktiengesellschaft Piperazine derivatives that destabilize androgen receptors
JP2005526800A (ja) 2002-03-22 2005-09-08 エルジー・ライフ・サイエンシーズ・リミテッド （２Ｓ）−Ｎ−５−［アミノ（イミノ）メチル］−２−チエニルメチル−１−（２Ｒ）−２−［（カルボキシルメチル）アミノ］−３，３−ジフェニルプロパノイル−２−ピロリジンカルボキサミド・ｎＨ２Ｏの新しい結晶形
AU2003236686A1 (en) 2002-06-07 2003-12-22 Altana Pharma Ag 4,5-dihydro-imidazo(4,5,1-j) quinolin-6-ones as parp inhibitors
US20040209858A1 (en) 2002-10-22 2004-10-21 Bennani Youssef L. Cycloalkylamides and their therapeutic applications
US20040077618A1 (en) 2002-10-22 2004-04-22 Bennani Youssef L. Cycloalkylamides and their therapeutic applications
JPWO2004046110A1 (ja) 2002-11-15 2006-03-16 アステラス製薬株式会社 メラニン凝集ホルモン受容体拮抗剤
US7569579B2 (en) 2002-12-13 2009-08-04 Smithkline Beecham Corporation Cyclopropyl compounds as ccr5 antagonists
PL1615909T3 (pl) 2003-04-23 2009-01-30 Glaxo Group Ltd Pochodne piperazyny i ich zastosowanie w leczeniu chorób neurologicznych i psychicznych
DK1618092T3 (da) 2003-05-01 2011-01-31 Bristol Myers Squibb Co Aryl-substituerede pyrazol-amidforbindelser, der er anvendelige som kinasehæmmere
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
JP2007516982A (ja) 2003-12-15 2007-06-28 日本たばこ産業株式会社 シクロプロパン化合物及びその医薬用途
CA2573198A1 (en) 2004-07-06 2006-02-09 Xenon Pharmaceuticals Inc. Nicotinamide derivatives and their use as therapeutic agents
AR050865A1 (es) 2004-09-09 2006-11-29 Sanofi Aventis Derivados de 2- morfolino-4-pirimidona
PT1805164E (pt) 2004-09-29 2011-04-11 Sanofi Aventis Derivados de 6-(piridinil)-4-pirimidona como inibidores de proteína-cinase tau 1
EP1802307B1 (en) 2004-10-15 2008-02-27 Glaxo Group Limited Pyrrolidine derivatives as histamine receptors ligands
KR20070106690A (ko) 2004-12-27 2007-11-05 아스트라제네카 아베 피라졸론 화합물 및 대사성 글루타메이트 수용체길항제로서 그들의 용도
CA2595882A1 (en) * 2005-01-26 2006-08-03 Pharmacia & Upjohn Company Llc Thieno [2,3-d] pyrimidine compounds as inhibitors of adp-mediated platelets aggregation
ES2528674T3 (es) 2005-02-17 2015-02-11 Astellas Pharma Inc. Piperidina y carboxilatos de piperacina como inhibidores de FAAH
EP1874780A1 (en) 2005-03-25 2008-01-09 Pharmacia & Upjohn Company LLC 4-piperazinylthieno[2,3-d]pyrimidine compounds as platelet aggregation inhibitors
EP1869051A1 (en) 2005-03-28 2007-12-26 Pharmacia & Upjohn Company LLC 4-piperazinylthieno ý2,3-d¨pyrimidine compounds as platelet aggregation inhibitors
CA2603041A1 (en) 2005-03-28 2006-10-05 Pharmacia & Upjohn Company Llc 4-piperazinylthieno [2, 3-d] pyrimidine compounds as platelet aggregation inhibitors
JP2008534573A (ja) 2005-03-28 2008-08-28 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー 血小板凝集阻害剤としての４−ピペラジノチエノ［２，３−ｄ］ピリミジン化合物
WO2007011623A1 (en) 2005-07-15 2007-01-25 Schering Corporation Quinazoline derivatives useful in cancer treatment
US7851474B2 (en) 2005-08-02 2010-12-14 Neurogen Corporation Dipiperazinyl ketones and related analogues
KR101336106B1 (ko) 2005-09-16 2013-12-05 얀센 파마슈티카 엔.브이. 히스타민 ｈ3 수용체의 조절제로서 사이클로프로필 아민
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
MX367916B (es) 2005-10-31 2019-09-11 Janssen Pharmaceutica N V Star Procedimientos para la preparacion de derivados de ciclopropilamida.
NZ593074A (en) 2005-12-21 2012-04-27 Vertex Pharma sulfonamide-pyrrolidone derivatives as Modulators of Ion Channels
US8119668B2 (en) 2005-12-23 2012-02-21 Nelson Erik B Treatment methods employing histamine H3 receptor antagonists, including betahistine
AU2007204426A1 (en) 2006-01-13 2007-07-19 F. Hoffmann-La Roche Ag Cyclohexyl piperazinyl methanone derivatives and their use as histamine H3 receptor modulators
CN101384581B (zh) * 2006-02-17 2013-09-18 弗·哈夫曼-拉罗切有限公司 作为5ht2/d3调节剂的苯甲酰基-哌啶衍生物
JP2009528240A (ja) 2006-03-01 2009-08-06 セメンテク・ピーティーワイ・リミテッド メーソンリー部材用マトリックス及びその製造方法
JP2009132621A (ja) 2006-03-13 2009-06-18 Ajinomoto Co Inc シクロプロピルアミド化合物の製造方法
JP2009530390A (ja) 2006-03-23 2009-08-27 アムゲン インコーポレイティッド １−フェニルスルホニル−ジアザ複素環アミド化合物およびヒドロキシステロイドデヒドロゲナーゼ調節因子としてのその使用
WO2007138928A1 (ja) 2006-05-26 2007-12-06 Kaneka Corporation 光学活性３－アミノ－２－ヒドロキシプロピオン酸シクロプロピルアミド誘導体およびその塩の製造方法
CN103382174A (zh) 2006-06-23 2013-11-06 雅培制药有限公司 作为组胺h3受体调节物的环丙胺衍生物
US9108948B2 (en) 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
US20100016293A1 (en) 2006-07-03 2010-01-21 Rogier Adriaan Smits Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use
GB0615620D0 (en) * 2006-08-05 2006-09-13 Astrazeneca Ab A process for the preparation of optically active intermediates
EP2056828A4 (en) * 2006-08-21 2010-06-23 Merck Sharp & Dohme SULFONYLATED PIPERAZINES AS CANNABINOID-1 RECEPTOR MODULATORS
TW200828371A (en) * 2006-09-21 2008-07-01 Matsushita Electric Industrial Co Ltd Chip-type filter
DE102006056526A1 (de) * 2006-11-30 2008-06-05 Archimica Gmbh Verfahren zur stereoselektiven Synthese von chiralen Epoxiden durch ADH-Reduktion von alpha-Abgangsgruppen-substituierten Ketonen und Cyclisierung
WO2008147864A2 (en) 2007-05-22 2008-12-04 Xenon Pharmaceuticals Inc. Methods of using piperazine compounds in treating sodium channel-mediated diseases or conditions
WO2008150364A1 (en) 2007-05-23 2008-12-11 Merck & Co., Inc. Cyclopropyl pyrrolidine orexin receptor antagonists
JP2010529157A (ja) 2007-06-11 2010-08-26 エフ．ホフマン−ラ ロシュ アーゲー シクロヘキシル誘導体
SA08290520B1 (ar) * 2007-08-22 2012-02-22 استرازينيكا ايه بي مشتقات سيكلو بروبيل أميد وتركيبات صيدلية تحتوي عليها لعلاج حالة مرضية سببها مستقبلات هيستامين h3
MX2010003155A (es) * 2007-10-04 2010-04-01 Hoffmann La Roche Derivados de ciclopropil aril amida y uso de los mismos.
PE20091313A1 (es) 2008-01-15 2009-09-03 Lilly Co Eli (r)-2-(4-ciclopropansulfonil-fenil)-n-pirazin-2-il-3-(tetrahidropiran-4-il)-propionamida cristalina
DE102008049371A1 (de) 2008-03-06 2009-09-10 Mühlbauer Ag Einrichtung mit einem RFID-Transponder in einem elektrisch leitfähigen Gegenstand und Herstellungsverfahren hierfür
NZ588634A (en) * 2008-03-20 2012-03-30 Forest Lab Holdings Ltd Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase
US8586607B2 (en) 2008-07-28 2013-11-19 Syddansk Universitet Compounds for the treatment of metabolic diseases
TW201039825A (en) * 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
JP5746718B2 (ja) 2010-02-18 2015-07-08 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ シクロプロピルアミド誘導体からなる固体形態
RU2012139082A (ru) 2010-02-18 2014-03-27 Астразенека Аб Способы получения производных циклопропиламида и связанных с ними промежуточных соединений

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006087169A1 (en) * 2005-02-15 2006-08-24 Glaxo Group Limited Compounds which potentiate glutamate receptor and uses thereof in medicine
WO2007011065A2 (en) * 2005-07-22 2007-01-25 Mitsubishi Tanabe Pharma Corporation Intermediate compound for synthesizing pharmaceutical agent and production method thereof
WO2008075068A2 (en) * 2006-12-21 2008-06-26 Astrazeneca Ab Acylaminopyrazoles as fgfr inhibitors
WO2009135842A1 (en) * 2008-05-08 2009-11-12 Evotec Neurosciences Gmbh Azetidines and cyclobutanes as histamine h3 receptor antagonists
CN101462980A (zh) * 2009-01-05 2009-06-24 扬州天辰精细化工有限公司 2，6—二氟苯甲酰胺的工业化生产方法

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
5-Hydroxyindole-2-carboxylic Acid Amides: Novel Histamine-3 Receptor Inverse Agonists for the Treatment of Obesity;Pascale David Pierson等;《J. Med. Chem.》;20090520;第52卷(第13期);第3855-3868页 *
trans-1-[(2-phenylcyclopropyl)methyl]-4-arylpiperazines: Mixed dopamine D2/D4 receptor Antagonist as Potential Antipsychotic Agents;Xiaoyan Zhang等;《J. Med. Chem.》;20000930;第43卷(第21期);第3923-3932页 *
从组胺H_3受体的配体开发新药的展望;嵇汝运;《药学服务与研究》;20040930;第4卷(第3期);第183-187页 *
组胺H_3受体及其与神经系统疾病关系的研究进展;罗雄等;《遵义医学院学报》;20051230;第28卷(第6期);第569-571页 *
组胺H_3受体配体研究进展;吴俊等;《中国药学杂志》;20070322;第42卷(第6期);第404-409页 *

Also Published As

Publication number Publication date
EP2536685B1 (en) 2015-04-08
EP2536702A4 (en) 2013-07-10
CO6592109A2 (es) 2013-01-02
KR20130002316A (ko) 2013-01-07
EP2536685A1 (en) 2012-12-26
US20110201623A1 (en) 2011-08-18
NZ601920A (en) 2014-08-29
JP2013520414A (ja) 2013-06-06
US9012452B2 (en) 2015-04-21
SG182732A1 (en) 2012-08-30
IL221431A (en) 2015-11-30
RU2012139082A (ru) 2014-03-27
MX2012009473A (es) 2012-09-12
MX336333B (es) 2016-01-15
AR080204A1 (es) 2012-03-21
IL221431A0 (en) 2012-10-31
KR20130004296A (ko) 2013-01-09
EP2536702A1 (en) 2012-12-26
CL2012002259A1 (es) 2012-11-30
TW201144272A (en) 2011-12-16
WO2011102795A1 (en) 2011-08-25
BR112012020782A2 (pt) 2016-05-03
AU2011218491A1 (en) 2012-10-04
US20130172560A1 (en) 2013-07-04
CA2790040A1 (en) 2011-08-25
BR112012020629A2 (pt) 2018-06-19
RU2012136148A (ru) 2014-03-27
JP2016006103A (ja) 2016-01-14
HK1178142A1 (en) 2013-09-06
AU2011218491B2 (en) 2014-11-06
NZ602110A (en) 2014-09-26
WO2011102794A1 (en) 2011-08-25
TW201136897A (en) 2011-11-01
CA2788444A1 (en) 2011-08-25
AU2011218491C1 (en) 2015-05-14
MX2012009480A (es) 2012-09-12
JP2013520413A (ja) 2013-06-06
CL2012002286A1 (es) 2013-01-25
ES2541857T3 (es) 2015-07-27
TWI520945B (zh) 2016-02-11
CN102869651A (zh) 2013-01-09
SG10201501226VA (en) 2015-04-29
CN103168027A (zh) 2013-06-19
AU2011218492B2 (en) 2014-11-13
AU2011218492A1 (en) 2012-08-23
EP2536685A4 (en) 2013-07-10
TWI494301B (zh) 2015-08-01
SG183274A1 (en) 2012-09-27
AR080205A1 (es) 2012-03-21

Similar Documents

Publication Publication Date Title
CN103168027B (zh) 制备环丙基酰胺衍生物的方法及其相关中间体
EP2381772B1 (en) Process and intermediates for the preparation of n-acylated-4-aryl beta-amino acid derivatives
US20230227459A1 (en) Method for producing 3,6-disubstituted-imidazo[1,2-b]pyridazine derivative
CN105473546A (zh) 通过新颖的中间体合成联苯丙氨醇
CN120230133A (zh) 一种3-硼-l-苯丙氨酸或其衍生物的制备方法
ES2875411T3 (es) Síntesis de trans-8-cloro-5-metil-1-[4-(piridin-2-iloxi)-ciclohexil]-5,6-dihidro-4h-2,3,5,10b-tetraaza­benzo[e]azuleno y formas cristalinas del mismo
Thaler et al. Synthesis and biological characterization of spiro [2H-(1, 3)-benzoxazine-2, 4′-piperidine] based histone deacetylase inhibitors
AU2017325870B2 (en) Tetrahydroisoquinoline kappa opioid antagonists
FR2943059A1 (fr) Derives de n-°6-aza-bicyclo°3.2.1!oct-5-yl)-aryl-methyl!- heterobenzamide,leur preparation et leur application en therapeutique
US8471016B2 (en) Process for the preparation of chiral beta amino carboxamide derivatives
CN111943945B (zh) 一种苏沃雷生中间体及其制备方法
CN103664704A (zh) 一种合成 n,n’-二取代基脲的方法
HK1178142B (en) Processes for making cyclopropyl amide derivatives and intermediates associated therewith
EP4330229B1 (en) Method for producing pyrrolidine compound
AU2021404895B2 (en) A process for the preparation of n-(bis(4-methoxyphenyl)methyl)-6-oxo-2-(pyridazin-3-yl)-1,6-dihydropyrimidine-5-carboxamide
EP3620462A1 (en) Process for the preparation of caspofungin
Nodzewska et al. Synthesis of Solid-phase Supported Chiral Amines and Investigation of Stereoselectivity of Aldol Reactions of Amine-free Tropinone Enolate
JP2020505336A (ja) キラルピロリジン−２−イル−メタノール誘導体の製造方法
EP2408763A2 (fr) Derives de n-ý(2-aza-bicycloý2.1.1¨hex-1-yl)-aryl-methyl¨-heterobenzamide, leur preparation et leur application en therapeutique
FR2944283A1 (fr) Derives de n-°(2-aza-bicyclo°2.1.1!hex-1-yl)-aryl-methyl!- heterobenzamide, leur preparation et leur application en therapeutique

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: 20150826

Termination date: 20170217

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