TWI520945B - 環丙基苯甲醯胺衍生物之新穎結晶形式 - Google Patents

環丙基苯甲醯胺衍生物之新穎結晶形式 Download PDF

Info

Publication number
TWI520945B
TWI520945B TW100105296A TW100105296A TWI520945B TW I520945 B TWI520945 B TW I520945B TW 100105296 A TW100105296 A TW 100105296A TW 100105296 A TW100105296 A TW 100105296A TW I520945 B TWI520945 B TW I520945B
Authority
TW
Taiwan
Prior art keywords
crystalline form
compound
pain
wavelength
measured
Prior art date
Application number
TW100105296A
Other languages
English (en)
Chinese (zh)
Other versions
TW201136897A (en
Inventor
麥可Ａ 烏辛斯基
Original Assignee
阿斯特捷利康公司
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=TWI520945(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 阿斯特捷利康公司 filed Critical 阿斯特捷利康公司
Publication of TW201136897A publication Critical patent/TW201136897A/zh
Application granted granted Critical
Publication of TWI520945B publication Critical patent/TWI520945B/zh

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)
  • Hematology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Anesthesiology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Epoxy Compounds (AREA)
TW100105296A 2010-02-18 2011-02-17 環丙基苯甲醯胺衍生物之新穎結晶形式 TWI520945B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US30558310P 2010-02-18 2010-02-18

Publications (2)

Publication Number Publication Date
TW201136897A TW201136897A (en) 2011-11-01
TWI520945B true TWI520945B (zh) 2016-02-11

Family

ID=44370080

Family Applications (2)

Application Number Title Priority Date Filing Date
TW100105296A TWI520945B (zh) 2010-02-18 2011-02-17 環丙基苯甲醯胺衍生物之新穎結晶形式
TW100105300A TWI494301B (zh) 2010-02-18 2011-02-17 製備環丙基醯胺衍生物之方法及相關中間物

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW100105300A TWI494301B (zh) 2010-02-18 2011-02-17 製備環丙基醯胺衍生物之方法及相關中間物

Country Status (19)

Country Link
US (2) US9012452B2 (enExample)
EP (2) EP2536702A4 (enExample)
JP (3) JP2013520414A (enExample)
KR (2) KR20130002316A (enExample)
CN (2) CN103168027B (enExample)
AR (2) AR080204A1 (enExample)
AU (2) AU2011218491C1 (enExample)
BR (2) BR112012020629A2 (enExample)
CA (2) CA2790040A1 (enExample)
CL (2) CL2012002259A1 (enExample)
CO (1) CO6592109A2 (enExample)
ES (1) ES2541857T3 (enExample)
IL (1) IL221431A (enExample)
MX (2) MX336333B (enExample)
NZ (2) NZ601920A (enExample)
RU (2) RU2012136148A (enExample)
SG (3) SG182732A1 (enExample)
TW (2) TWI520945B (enExample)
WO (2) WO2011102795A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20140047T1 (en) 2007-08-22 2014-02-14 Astrazeneca Ab Cycloptopyl amide derivatives
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
CA2790040A1 (en) * 2010-02-18 2011-08-25 Astrazeneca Ab Processes for making cyclopropyl amide derivatives and intermediates associated therewith
NZ602108A (en) * 2010-02-18 2014-09-26 Astrazeneca Ab Solid forms comprising a cyclopropyl amide derivative
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
CN105073709A (zh) * 2013-03-22 2015-11-18 默克专利有限公司 用于制备有机电致发光器件用材料的合成结构单元
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

Family Cites Families (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL297170A (enExample) * 1963-04-04 1900-01-01
NL128365C (enExample) 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
WO1991009594A1 (en) 1989-12-28 1991-07-11 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
EP0531271A1 (en) 1991-08-22 1993-03-10 Monsanto Company Safening herbicidal pyrazolysulfonylureas
DE4131139A1 (de) * 1991-09-19 1993-03-25 Bayer Ag Verfahren zur herstellung von 1-fluor-cyclopropan-1-carbonsaeure
DK0690864T3 (da) * 1993-03-12 2001-09-17 Upjohn Co Krystallinsk ceftiofur på fri syreform
CA2205998C (en) 1994-11-23 2002-07-16 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
WO1998037077A1 (en) 1997-02-24 1998-08-27 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
DE69934093T2 (de) 1998-01-27 2007-06-21 Aventis Pharmaceuticals Inc. SUBSTITUIERTE OXOAZAHETEROCYCLYL FAKTOR Xa HEMMER
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
WO2000076993A1 (en) 1999-06-16 2000-12-21 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
NZ519984A (en) * 2000-01-07 2004-03-26 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
CA2415606A1 (en) 2000-07-20 2002-01-31 Neurogen Corporation Capsaicin receptor ligands
KR20030062447A (ko) 2000-12-25 2003-07-25 아지노모토 가부시키가이샤 광학 활성 할로하이드린 화합물의 제조방법
ATE324371T1 (de) 2001-02-23 2006-05-15 Merck & Co Inc N-substituierte heterocyclische nichtaryl- nmda/nr2b-antagonisten
DE60234453D1 (de) 2001-07-02 2009-12-31 High Point Pharmaceuticals Llc Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren
EP1422228A1 (en) 2001-08-08 2004-05-26 Takeda Chemical Industries, Ltd. BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
WO2003026572A2 (en) * 2001-09-26 2003-04-03 Merck & Co., Inc. Crystalline forms of ertapenem sodium
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
CN1642947A (zh) * 2002-03-22 2005-07-20 株式会社Lg生命科学 ( 2 S )－N－5－[氨基(亚氨基)甲基]－2－噻吩基甲基－1－( 2 R ) －2－[(羧甲基) 氨基]－3 ,3－二苯基丙酰－2－吡咯烷甲酰胺·nH2O的新晶形
WO2003103666A2 (en) 2002-06-07 2003-12-18 Altana Pharma Ag Novel 4,5-dihydro-imidazo[4,5,1-ij]quinolin-6-ones
US20040077618A1 (en) * 2002-10-22 2004-04-22 Bennani Youssef L. Cycloalkylamides and their therapeutic applications
US20040209858A1 (en) * 2002-10-22 2004-10-21 Bennani Youssef L. Cycloalkylamides and their therapeutic applications
AU2003284402A1 (en) 2002-11-15 2004-06-15 Yamanouchi Pharmaceutical Co., Ltd. Antagonist to melanin-concentrating hormone receptor
AU2003296993A1 (en) 2002-12-13 2004-07-09 Smithkline Beecham Corporation Cyclopropyl compounds as ccr5 antagonists
HRP20080541T3 (en) * 2003-04-23 2008-12-31 Glaxo Group Limited Piperazine derivatives and their use for the treatment of neurological and psychiatric diseases
PL1618092T3 (pl) 2003-05-01 2011-02-28 Bristol Myers Squibb Co Związki amidopirazolowe z podstawnikami arylowymi jako inhibitory kinazy
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
EP1694410B1 (en) 2003-12-15 2010-04-14 Japan Tobacco, Inc. Cyclopropane derivatives and pharmaceutical use thereof
CN1997371A (zh) 2004-07-06 2007-07-11 泽农医药公司 烟酰胺衍生物及其作为治疗剂的用途
TW200621760A (en) 2004-09-09 2006-07-01 Mitsubishi Pharma Corp 2-morpholino-4-pyrimidone compound
CN101048397A (zh) 2004-09-29 2007-10-03 三菱制药株式会社 作为τ蛋白激酶1抑制剂的6－（吡啶基）－4－嘧啶酮衍生物
DE602005005080T2 (de) 2004-10-15 2009-02-26 Glaxo Group Ltd., Greenford Pyrrolidinderivate als histaminrezeptor-liganden
CA2591003A1 (en) 2004-12-27 2006-07-06 Astrazeneca Ab Pyrazolone compounds as metabotropic glutamate receptor agonists for the treatment of neurological and psychiatric disorders
EP1844052A1 (en) * 2005-01-26 2007-10-17 Pharmacia & Upjohn Company LLC Thieno[2,3-d]pyrimidine compounds as inhibitors of adp-mediated platelets aggregation
US7790758B2 (en) 2005-02-15 2010-09-07 Glaxo Group Limited Compounds which potentiate glutamate receptor and uses thereof in medicine
TW200640864A (en) 2005-02-17 2006-12-01 Astellas Pharma Inc Pyridyl non-aromatic nitrogenated heterocyclic-1-carboxylate ester derivative
WO2006100591A1 (en) 2005-03-25 2006-09-28 Pharmacia & Upjohn Company Llc 4-piperazinnylthieno [2,3-d] pyrimidine compounds as platelet aggregation inhibitors
CA2602538A1 (en) 2005-03-28 2006-10-05 Pharmacia & Upjohn Company Llc 4-piperazinothieno [2, 3-d] pyrimidine compounds as platelet aggregation inhibitors
WO2006103544A2 (en) 2005-03-28 2006-10-05 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
EP1924568A1 (en) 2005-07-15 2008-05-28 Schering Corporation Quinazoline derivatives useful in cancer treatment
TW200740779A (en) * 2005-07-22 2007-11-01 Mitsubishi Pharma Corp Intermediate compound for synthesizing pharmaceutical agent and production method thereof
EP1909797A4 (en) 2005-08-02 2013-02-27 Neurogen Corp DIPIPERAZINYL KETONE AND RELATED ANALOG
CA2622760C (en) * 2005-09-16 2012-12-04 Janssen Pharmaceutica N.V. Cyclopropyl amines as modulators of the histamine h3 receptor
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
ES2395049T3 (es) 2005-10-31 2013-02-07 Janssen Pharmaceutica Nv Procedimiento para la preparación de derivados de ciclopropilamida
KR20080081178A (ko) 2005-12-21 2008-09-08 버텍스 파마슈티칼스 인코포레이티드 이온 채널 조절인자로서의 헤테로사이클릭 유도체
WO2007076140A2 (en) 2005-12-23 2007-07-05 University Of Cincinnati Treatment methods employing histamine h3 receptor antagonists, including betahistine
EP1976840A1 (en) * 2006-01-13 2008-10-08 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
MX2008011133A (es) 2006-03-01 2008-12-18 Cementech Pty Ltd Matriz para elementos de albañileria y metodo de fabricacion de la misma.
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
US7524848B2 (en) 2006-03-23 2009-04-28 Amgen Inc. Diaza heterocyclic amide compounds and their uses
US7834190B2 (en) 2006-05-26 2010-11-16 Kaneka Corporation Process for production of optically active-3-amino-2-hydroxypropionic cyclopropylamide derivatives and salts thereof
US9108948B2 (en) * 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
JP5203360B2 (ja) * 2006-06-23 2013-06-05 アボット・ラボラトリーズ ヒスタミンｈ３受容体調節剤としてのシクロプロピルアミン誘導体
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
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
WO2008147864A2 (en) 2007-05-22 2008-12-04 Xenon Pharmaceuticals Inc. Methods of using piperazine compounds in treating sodium channel-mediated diseases or conditions
CA2687230A1 (en) 2007-05-23 2008-12-11 Merck & Co., Inc. Cyclopropyl pyrrolidine orexin receptor antagonists
ES2350511T3 (es) 2007-06-11 2011-01-24 F. Hoffmann-La Roche Ag Derivados ciclohexilo.
HRP20140047T1 (en) * 2007-08-22 2014-02-14 Astrazeneca Ab Cycloptopyl amide derivatives
JP5362729B2 (ja) * 2007-10-04 2013-12-11 エフ．ホフマン−ラ ロシュ アーゲー シクロプロピルアリールアミド誘導体及びその使用
AR070107A1 (es) 2008-01-15 2010-03-17 Lilly Co Eli R-2-(4-ciclopropansulfonil-fenil)-n-pirazin-2-il-3-(tetrahidropiran-4-il)-propionamida en forma cristalina, composicion farmaceutica que la comprende y su uso para la manufactura de un medicamento util para la prevencion o tratamiento de hiperglicemia
DE102008049371A1 (de) 2008-03-06 2009-09-10 Mühlbauer Ag Einrichtung mit einem RFID-Transponder in einem elektrisch leitfähigen Gegenstand und Herstellungsverfahren hierfür
WO2009117659A1 (en) * 2008-03-20 2009-09-24 Forest Laboratories Holdings Limited Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase
WO2009135842A1 (en) * 2008-05-08 2009-11-12 Evotec Neurosciences Gmbh Azetidines and cyclobutanes as histamine h3 receptor antagonists
WO2010012650A1 (en) 2008-07-28 2010-02-04 Syddansk Universitet Compounds for the treatment of metabolic diseases
CN101462980B (zh) * 2009-01-05 2013-01-09 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
TW201039825A (en) * 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
CA2790040A1 (en) 2010-02-18 2011-08-25 Astrazeneca Ab Processes for making cyclopropyl amide derivatives and intermediates associated therewith
NZ602108A (en) * 2010-02-18 2014-09-26 Astrazeneca Ab Solid forms comprising a cyclopropyl amide derivative

Also Published As

Publication number Publication date
US9012452B2 (en) 2015-04-21
EP2536685B1 (en) 2015-04-08
RU2012139082A (ru) 2014-03-27
CA2788444A1 (en) 2011-08-25
TW201144272A (en) 2011-12-16
IL221431A0 (en) 2012-10-31
AU2011218492B2 (en) 2014-11-13
CN102869651A (zh) 2013-01-09
AU2011218491A1 (en) 2012-10-04
AU2011218491C1 (en) 2015-05-14
EP2536685A4 (en) 2013-07-10
NZ602110A (en) 2014-09-26
TWI494301B (zh) 2015-08-01
CN103168027A (zh) 2013-06-19
EP2536685A1 (en) 2012-12-26
CL2012002259A1 (es) 2012-11-30
JP2013520413A (ja) 2013-06-06
AU2011218492A1 (en) 2012-08-23
US20110201623A1 (en) 2011-08-18
JP2013520414A (ja) 2013-06-06
IL221431A (en) 2015-11-30
MX2012009480A (es) 2012-09-12
RU2012136148A (ru) 2014-03-27
CO6592109A2 (es) 2013-01-02
SG10201501226VA (en) 2015-04-29
CL2012002286A1 (es) 2013-01-25
BR112012020782A2 (pt) 2016-05-03
NZ601920A (en) 2014-08-29
SG183274A1 (en) 2012-09-27
EP2536702A4 (en) 2013-07-10
KR20130004296A (ko) 2013-01-09
CN103168027B (zh) 2015-08-26
MX336333B (es) 2016-01-15
JP2016006103A (ja) 2016-01-14
AR080204A1 (es) 2012-03-21
HK1178142A1 (en) 2013-09-06
TW201136897A (en) 2011-11-01
MX2012009473A (es) 2012-09-12
SG182732A1 (en) 2012-08-30
WO2011102795A1 (en) 2011-08-25
CA2790040A1 (en) 2011-08-25
EP2536702A1 (en) 2012-12-26
US20130172560A1 (en) 2013-07-04
ES2541857T3 (es) 2015-07-27
AR080205A1 (es) 2012-03-21
WO2011102794A1 (en) 2011-08-25
AU2011218491B2 (en) 2014-11-06
KR20130002316A (ko) 2013-01-07
BR112012020629A2 (pt) 2018-06-19

Similar Documents

Publication Publication Date Title
TWI520945B (zh) 環丙基苯甲醯胺衍生物之新穎結晶形式
EP2398780B1 (en) Cyclopropyl amide derivatives targeting the histamine h3 receptor
EA016687B1 (ru) Производные циклопропиламида
EP0673369A1 (de) Substituierte benzazepinone
AU2011218490B9 (en) Solid forms comprising a cyclopropyl amide derivative
JP2010509250A (ja) 新規な２−アミノ−ピリジン誘導体及びカリウムチャネルモジュレーターとしてのその使用
JP2010509249A (ja) 新規な４−アミノ−ピリジン誘導体及びカリウムチャネルモジュレーターとしてのその使用
HK1164863B (en) Cyclopropyl amide derivatives targeting the histamine h3 receptor
AU2013209365A1 (en) Cyclopropyl amide derivatives targeting the histamine h3 receptor
MXPA06009346A (en) Novel azabicyclic derivatives, preparation method thereof and pharmaceutical compositions containing same

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees