EA200200590A1 - Производные пирролидина в качестве ингибиторов фосфодиэстеразы, специфичной к циклическому амф - Google Patents

Производные пирролидина в качестве ингибиторов фосфодиэстеразы, специфичной к циклическому амф

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Publication number
EA200200590A1
EA200200590A1 EA200200590A EA200200590A EA200200590A1 EA 200200590 A1 EA200200590 A1 EA 200200590A1 EA 200200590 A EA200200590 A EA 200200590A EA 200200590 A EA200200590 A EA 200200590A EA 200200590 A1 EA200200590 A1 EA 200200590A1
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EA
Eurasian Patent Office
Prior art keywords
inhibitors
phosphodyesterase
specific
cyclic amp
pyrrolidine derivatives
Prior art date
Application number
EA200200590A
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English (en)
Other versions
EA005686B1 (ru
Inventor
Тимоти Дж. Мартинс
Керри У. Фаулер
Джошуа Одинго
Эдвард А. Кесицки
Эйми Оливер
Лоренс И. Бэрджесс
Джон Дж. Годино
Закари С. Джоунс
Брэдли Дж. Ньюхаус
Стивен Шлахтер
Original Assignee
Айкос Корпорейшн
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Publication date
Application filed by Айкос Корпорейшн filed Critical Айкос Корпорейшн
Publication of EA200200590A1 publication Critical patent/EA200200590A1/ru
Publication of EA005686B1 publication Critical patent/EA005686B1/ru

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Abstract

Предложены новые соединения ряда пирролидина, которые имеют структурную формулу (II) и которые являются сильнодействующими и селективными ингибиторами PDE4, а также способы их получения. Описано также использование соединений при лечении воспалительных заболеваний и других заболеваний, включающих повышенные уровни цитокинов, а также нарушения центральной нервной системы (ЦНС).Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200200590A 1999-12-23 2000-11-28 Производные пирролидина в качестве ингибиторов фосфодиэстеразы, специфичной к циклическому амф EA005686B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/471,846 US6258833B1 (en) 1999-12-23 1999-12-23 Cyclic AMP-specific phosphodiesterase inhibitors
PCT/US2000/032401 WO2001047905A1 (en) 1999-12-23 2000-11-28 Pyrrolidine derivatives as cyclic amp-specific phosphodiesterase inhibitors

Publications (2)

Publication Number Publication Date
EA200200590A1 true EA200200590A1 (ru) 2002-12-26
EA005686B1 EA005686B1 (ru) 2005-04-28

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Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6455571B1 (en) * 1998-04-23 2002-09-24 Abbott Laboratories Inhibitors of neuraminidases
US6258833B1 (en) * 1999-12-23 2001-07-10 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
US20010049368A1 (en) * 2000-02-29 2001-12-06 Reines Scott A. Method for treating or preventing depression
WO2002002500A1 (en) * 2000-07-03 2002-01-10 Speedel Pharma Ag Preparation of (r)-2-alkyl-3-phenylpropionic acids
US6953774B2 (en) * 2000-08-11 2005-10-11 Applied Research Systems Ars Holding N.V. Methods of inducing ovulation
WO2002047540A2 (en) * 2000-12-15 2002-06-20 The General Hospital Corporation Methods for inhibiting fibrosis
US20040014099A1 (en) * 2001-03-19 2004-01-22 Decode Genetics Ehf. Susceptibility gene for human stroke; methods of treatment
US20030073711A1 (en) * 2001-08-23 2003-04-17 Whitehead Clark M. Methods for treatment of scleroderma
US6479493B1 (en) 2001-08-23 2002-11-12 Cell Pathways, Inc. Methods for treatment of type I diabetes
KR100951218B1 (ko) 2001-10-16 2010-04-05 메모리 파마슈티칼스 코포레이션 신경계 증후군의 치료를 위한 ｐｄｅ-4 억제제로서의4-(4-알콕시-3-히드록시페닐)-2-피롤리돈 유도체
KR101056916B1 (ko) 2001-12-14 2011-08-12 라보라토리스 세로노 에스.에이. 비폴리펩티드 고리에이엠피 레벨 모듈레이터를 이용한 배란유도 방법
MY140561A (en) * 2002-02-20 2009-12-31 Nycomed Gmbh Dosage form containing pde 4 inhibitor as active ingredient
DE10228132A1 (de) * 2002-06-24 2004-01-22 Arzneimittelwerk Dresden Gmbh Amide cyclischer Aminosäuren als PDE 4 Inhibitoren
PL1606261T3 (pl) 2003-03-10 2010-04-30 Astrazeneca Ab Nowy sposób przygotowania roflumilastu
CN1805929A (zh) * 2003-04-16 2006-07-19 记忆药物公司 磷酸二酯酶4抑制剂
AU2004232973A1 (en) * 2003-04-18 2004-11-04 Memory Pharmaceuticals Corporation Pyrazole derivatives as phosphodiesterase 4 inhibitors
WO2005000247A2 (en) * 2003-06-25 2005-01-06 Smithkline Beecham Corporation 4-carboxamido quinoline derivatives for use as nk-2 and nk-3
EP1670476A4 (en) * 2003-09-30 2009-05-27 Merck & Co Inc ANTAGONISTS OF TACHYKININ RECEPTOR BASED ON PHENYL PYRROLIDINE ETHER
US20050201989A1 (en) * 2004-02-19 2005-09-15 St. Camillus Medical, Inc. Compositions and methods for ex vivo preservation of blood vessels for vascular grafts using inhibitors of tumor necrosis factor-alpha
ES2317223T3 (es) * 2004-04-08 2009-04-16 Wyeth Derivados de tioamida como moduladores del receptor de progesterona.
US7432266B2 (en) * 2004-10-15 2008-10-07 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors
US7585882B2 (en) * 2004-10-20 2009-09-08 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors
ES2421916T3 (es) * 2005-03-16 2013-09-06 Nycomed Gmbh Forma farmacéutica de sabor enmascarado que contiene roflumilast
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
EP2377530A3 (en) 2005-10-21 2012-06-20 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
WO2007053596A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
CN101355876B (zh) 2005-11-09 2012-09-05 康宾纳特克斯公司 一种适用于眼部给药的组合物
AU2007223036A1 (en) * 2006-03-08 2007-09-13 Braincells, Inc. Modulation of neurogenesis by nootropic agents
US20100216734A1 (en) * 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2026813A2 (en) * 2006-05-09 2009-02-25 Braincells, Inc. 5 ht receptor mediated neurogenesis
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
JP2009536669A (ja) 2006-05-09 2009-10-15 ブレインセルス，インコーポレイティド アンジオテンシン調節による神経新生
KR20090064418A (ko) 2006-09-08 2009-06-18 브레인셀즈 인코퍼레이션 4-아실아미노피리딘 유도체 포함 조합물
CA2663347A1 (en) * 2006-09-19 2008-03-27 Braincells, Inc. Ppar mediated modulation of neurogenesis
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
US20100210633A1 (en) * 2006-10-12 2010-08-19 Epix Delaware, Inc. Carboxamide compounds and their use
DK2176220T3 (da) 2007-08-07 2013-06-10 Takeda Pharmaceutical Pyrrolidin-2-on-derivater som androgenreceptormodulatorer.
JP2011506466A (ja) 2007-12-11 2011-03-03 株式会社サイトパスファインダー カルボキサミド化合物ならびにケモカイン受容体アゴニストとしてのそれらの使用
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CN102603623A (zh) * 2011-12-26 2012-07-25 北京赛林泰医药技术有限公司 制备高纯度罗氟司特的方法
US20150119399A1 (en) 2012-01-10 2015-04-30 President And Fellows Of Harvard College Beta-cell replication promoting compounds and methods of their use
JO3264B1 (ar) * 2013-03-13 2018-09-16 Lilly Co Eli مركبات ازيتيدينيل أوكسي فينيل بيروليدين
ES2733552T3 (es) * 2014-01-24 2019-11-29 Celgene Corp Procedimientos para el tratamiento de la obesidad mediante apremilast
HUE052714T2 (hu) * 2014-05-29 2021-05-28 Mitsubishi Tanabe Pharma Corp Új pirrolidin vegyület és alkalmazás melanokortin receptor agonistaként
WO2016033776A1 (en) * 2014-09-04 2016-03-10 Eli Lilly And Company Crystalline (2s) -3- [ (3s, 4s) -3- [ (1r) -1-hydroxyethyl] -4- (4-methoxy-3- { [1- (5-methylpyridin-2-yl) azetidin-3-yl] oxy} phenyl) -3-methylpyrrolidin-1-yl] -3-oxopropane-1, 2-diol
AR101696A1 (es) 2014-09-12 2017-01-04 Lilly Co Eli Compuestos de azetidiniloxifenilpirrolidina
WO2017072796A1 (en) 2015-10-30 2017-05-04 Council Of Scientific & Industrial Research 2-pyridone based compounds useful as potential phosphodiesterase3a (pde3a)inhibitors and a process for the preparation thereof
JP6392297B2 (ja) * 2015-11-27 2018-09-19 田辺三菱製薬株式会社 医薬組成物
CN111094270B (zh) 2017-09-29 2023-09-22 田边三菱制药株式会社 光学活性吡咯烷化合物及其制造方法
CA3123995C (en) * 2018-12-18 2023-05-23 Wuhan Humanwell Innovative Drug Research and Development Center Limited Company Phenylpyrrolidine compound and use thereof
CN112409333A (zh) * 2019-08-23 2021-02-26 湖北生物医药产业技术研究院有限公司 苯基吡咯烷类化合物
TW202146385A (zh) * 2020-04-29 2021-12-16 大陸商廣東東陽光藥業有限公司 取代的吡咯烷類化合物及其在藥物中的應用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5821622B2 (ja) * 1973-02-28 1983-05-02 ウェルファイド株式会社 ピロリジンメタノ−ル ノ セイゾウホウ
JPS50108258A (ru) * 1974-02-08 1975-08-26
US5665754A (en) * 1993-09-20 1997-09-09 Glaxo Wellcome Inc. Substituted pyrrolidines
JPH07300455A (ja) * 1994-03-08 1995-11-14 Mitsubishi Chem Corp ３−フェニルピロリジン誘導体
CA2143143A1 (en) * 1994-03-08 1995-09-09 Toshihiko Tanaka 3-phenylpyrrolidine derivatives
US5998428A (en) 1995-05-31 1999-12-07 Smithkline Beecham Corporation Compounds and methods for treating PDE IV-related diseases
US5856103A (en) * 1994-10-07 1999-01-05 Board Of Regents The University Of Texas Method for selectively ranking sequences for antisense targeting
DE19601938A1 (de) * 1996-01-12 1997-07-17 Schering Ag Neue Phosphodiesteraseinhibitoren
ID22781A (id) * 1997-04-04 1999-12-09 Pfizer Prod Inc Turunan-turunan nikotinamida
US6258833B1 (en) * 1999-12-23 2001-07-10 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors

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