JP4319245B2 - ヒスタミン−３受容体拮抗薬 - Google Patents

ヒスタミン−３受容体拮抗薬 Download PDF

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JP4319245B2
JP4319245B2 JP2008537213A JP2008537213A JP4319245B2 JP 4319245 B2 JP4319245 B2 JP 4319245B2 JP 2008537213 A JP2008537213 A JP 2008537213A JP 2008537213 A JP2008537213 A JP 2008537213A JP 4319245 B2 JP4319245 B2 JP 4319245B2
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pyrrolidin
fluoro
ylmethyl
phenyl
cyclobutanecarboxylic acid
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JP2009513619A (ja
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ティ． ワガー トラヴィス
イェグナ チャンドラセカラン ラマラクシュミ
ウィリアム バトラ− トッド
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ファイザー・プロダクツ・インク
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    • 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
    • C07D295/04—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
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    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/58—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than 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
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
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  • Anesthesiology (AREA)
  • Nutrition Science (AREA)
  • Rheumatology (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
JP2008537213A 2005-10-27 2006-10-16 ヒスタミン−３受容体拮抗薬 Expired - Fee Related JP4319245B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US73099605P 2005-10-27 2005-10-27
PCT/IB2006/002977 WO2007049123A1 (en) 2005-10-27 2006-10-16 Histamine-3 receptor antagonists

Related Child Applications (1)

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JP2009055839A Division JP5064427B2 (ja) 2005-10-27 2009-03-10 ヒスタミン−３受容体拮抗薬

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JP2009513619A JP2009513619A (ja) 2009-04-02
JP4319245B2 true JP4319245B2 (ja) 2009-08-26

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JP2009055839A Expired - Fee Related JP5064427B2 (ja) 2005-10-27 2009-03-10 ヒスタミン−３受容体拮抗薬

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US (2) US8158673B2 (enExample)
EP (1) EP1951660B1 (enExample)
JP (2) JP4319245B2 (enExample)
KR (1) KR101025358B1 (enExample)
CN (1) CN101296898B (enExample)
AP (1) AP2403A (enExample)
AR (1) AR056879A1 (enExample)
AU (1) AU2006307645B2 (enExample)
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CA (1) CA2621323C (enExample)
CR (1) CR9910A (enExample)
CU (1) CU23806B7 (enExample)
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DO (1) DOP2006000239A (enExample)
EA (1) EA013602B1 (enExample)
EC (1) ECSP088373A (enExample)
ES (1) ES2444370T3 (enExample)
GE (1) GEP20104937B (enExample)
GT (1) GT200600471A (enExample)
HN (1) HN2006036385A (enExample)
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MA (1) MA29888B1 (enExample)
MY (1) MY145001A (enExample)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010516749A (ja) * 2007-01-22 2010-05-20 ファイザー・プロダクツ・インク 治療用化合物のトシル酸塩およびその医薬組成物

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8158673B2 (en) * 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
EP2123644B1 (en) 2007-03-07 2014-12-17 Takeda Pharmaceutical Company Limited Benzoxazepine derivatives and use thereof
BRPI0815591B8 (pt) 2007-08-22 2021-05-25 Astrazeneca Ab composto, composição farmacêutica, e, uso de um composto.
CN101939306A (zh) * 2007-12-07 2011-01-05 美国辉瑞有限公司 反式-n-异丁基-3-氟-3-[3-氟-4-(吡咯烷-1-基-甲基)-苯基]环丁烷甲酰胺的甲苯磺酸盐
CA2721303C (en) * 2008-05-08 2016-06-28 Evotec Ag Azetidines and cyclobutanes as histamine h3 receptor antagonists
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
AU2011218492B2 (en) 2010-02-18 2014-11-13 Astrazeneca Ab New crystalline form of a cyclopropyl benzamide derivative
WO2012131539A1 (en) 2011-03-31 2012-10-04 Pfizer Inc. Novel bicyclic pyridinones
WO2012172449A1 (en) 2011-06-13 2012-12-20 Pfizer Inc. Lactams as beta secretase inhibitors
WO2013030713A1 (en) 2011-08-31 2013-03-07 Pfizer Inc. Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
CA2872154C (en) 2012-05-04 2016-08-23 Pfizer Inc. Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin-2-amine compounds as inhibitors of app, bace1 and bace2
MD20140130A2 (ro) 2012-06-29 2015-04-30 Pfizer Inc. 4-(amino-substituite)-7H-pirolo[2,3-d]pirimidine noi ca inhibitori de LRRK2
WO2014045162A1 (en) 2012-09-20 2014-03-27 Pfizer Inc. ALKYL-SUBSTITUTED HEXAHYDROPYRANO[3,4-d] [1,3]THIAZIN-2-ANIME COMPOUNDS
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
WO2014078568A1 (en) 2012-11-14 2014-05-22 The Johns Hopkins University Methods and compositions for treating schizophrenia
EP2931731A1 (en) 2012-12-11 2015-10-21 Pfizer Inc. Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1
JP6162820B2 (ja) 2012-12-19 2017-07-12 ファイザー・インク 炭素環式および複素環式置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
WO2014125394A1 (en) 2013-02-13 2014-08-21 Pfizer Inc. HETEROARYL-SUBSTITUTED HEXAHYDROPYRANO [3,4-d][1,3] THIAZIN-2-AMINE COMPOUNDS
US9233981B1 (en) 2013-02-15 2016-01-12 Pfizer Inc. Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
EA201591360A1 (ru) 2013-02-19 2016-03-31 Пфайзер Инк. Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств
JP6425717B2 (ja) 2013-10-04 2018-11-21 ファイザー・インク ガンマセクレターゼモジュレーターとしての新規二環式ピリジノン
WO2015092592A1 (en) 2013-12-17 2015-06-25 Pfizer Inc. Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors
CR20160454A (es) 2014-04-01 2016-12-06 Pfizer CROMENO Y 1,1 a,2,7b—TETRAHIDROCICLOPROPA[C]CROMENO PIRIDOPIRAZINADIONAS NOVEDOSAS
AU2015245260A1 (en) 2014-04-10 2016-10-06 Pfizer Inc. 2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides
EP3172210B1 (en) 2014-07-24 2020-01-15 Pfizer Inc Pyrazolopyrimidine compounds
AU2015298378B2 (en) 2014-08-06 2018-08-02 Pfizer Inc. Imidazopyridazine compounds
DK3253755T3 (da) 2015-02-03 2020-09-28 Pfizer Hidtil ukendte cyclopropabenzofuranyl-pyridopyrazindioner
TN2017000485A1 (en) 2015-06-17 2019-04-12 Pfizer Tricyclic compounds and their use as phosphodiesterase inhibitors
RU2722149C1 (ru) 2015-09-14 2020-05-27 Пфайзер Инк. Новые производные имидазо[4,5-c] хинолинов и имидазо[4,5-c][1,5] нафтиридинов в качестве ингибиторов LRRK2
AU2016325665A1 (en) 2015-09-24 2018-03-08 Pfizer Inc. N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3] thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl] amides
JP2018531924A (ja) 2015-09-24 2018-11-01 ファイザー・インク テトラヒドロピラノ［３，４−ｄ］［１，３］オキサジン誘導体、およびｂａｃｅ阻害剤としてのその使用
EP3353174A1 (en) 2015-09-24 2018-08-01 Pfizer Inc N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl]amides useful as bace inhibitors
CN108699080B (zh) 2016-02-23 2021-05-14 辉瑞公司 6,7-二氢-5H-吡唑并[5,1-b][1,3]噁嗪-2-甲酰胺化合物
SG11201811712QA (en) 2016-07-01 2019-01-30 Pfizer 5,7-dihydro-pyrrolo-pyridine derivatives for treating neurological and neurodegenerative diseases
EP3592740B1 (en) 2017-03-10 2022-02-09 Pfizer Inc. Cyclic substituted imidazo[4,5-c]quinoline derivatives
EP3592741B1 (en) 2017-03-10 2023-02-15 Pfizer Inc. Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors
US20230137562A1 (en) 2017-06-07 2023-05-04 Adrx, Inc. Tau aggregation inhibitors
FI3642202T3 (fi) 2017-06-22 2023-03-01 Dihydro-pyrrolo-pyridiinijohdannaisia
US11453701B2 (en) 2017-08-18 2022-09-27 Adrx, Inc. Tau aggregation peptide inhibitors
WO2019183636A1 (en) 2018-03-23 2019-09-26 Pfizer Inc. Piperazine azaspiro derivaves
WO2022182658A1 (en) 2021-02-23 2022-09-01 Hoth Therapeutics, Inc. Use of aprepitant for treating alzheimer's disease
CN116514645A (zh) * 2023-04-08 2023-08-01 绍兴上虞华伦化工有限公司 二氟-4溴苯甲醛及其制备工艺
WO2025145091A1 (en) 2023-12-29 2025-07-03 Pfizer Inc. Crystalline forms of a muscarinic m4 receptor modulator and methods of treating diseases

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6559140B2 (en) 2000-03-09 2003-05-06 Abbott Laboratories Cyclic and bicyclic diamino histamine-3 receptor antagonists
AU2002254114A1 (en) 2001-03-23 2002-10-08 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
US7671047B2 (en) 2002-06-19 2010-03-02 Sanofi-Aventis Deutschland Gmbh Cationically substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
JP2004131497A (ja) * 2002-09-18 2004-04-30 Satoshi Shuto シスシクロプロパン誘導体
DK1651615T3 (da) * 2003-07-29 2010-05-25 High Point Pharmaceuticals Llc Pyridazinyl-piperaziner og anvendelse deraf som histamin-H3-receptorligander
CA2551037A1 (en) * 2003-09-22 2005-03-31 Banyu Pharmaceutical Co., Ltd. Novel piperidine derivative
WO2005080361A1 (en) 2004-02-02 2005-09-01 Pfizer Products Inc. Histamine-3 receptor modulators
CA2561628C (en) * 2004-04-01 2012-05-08 Eli Lilly And Company Histamine h3 receptor agents, preparation and therapeutic uses
US7456164B2 (en) 2004-05-07 2008-11-25 Pfizer, Inc 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands
EP1595881A1 (en) 2004-05-12 2005-11-16 Pfizer Limited Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
ES2354569T3 (es) 2005-06-22 2011-03-16 Pfizer Products Inc. Antagonistas del receptor de histamina-3.
US8158673B2 (en) * 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
KR101108109B1 (ko) * 2007-01-22 2012-02-06 화이자 프로덕츠 인코포레이티드 치료 화합물의 토실레이트 염 및 이의 약학 조성물

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010516749A (ja) * 2007-01-22 2010-05-20 ファイザー・プロダクツ・インク 治療用化合物のトシル酸塩およびその医薬組成物

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