BR0016693A - Derivados de pirrolidina como inibidores de fosfodiesterase especìfico amp cìclico - Google Patents

Derivados de pirrolidina como inibidores de fosfodiesterase especìfico amp cìclico

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Publication number
BR0016693A
BR0016693A BR0016693-6A BR0016693A BR0016693A BR 0016693 A BR0016693 A BR 0016693A BR 0016693 A BR0016693 A BR 0016693A BR 0016693 A BR0016693 A BR 0016693A
Authority
BR
Brazil
Prior art keywords
phosphodiesterase inhibitors
specific phosphodiesterase
cyclic amp
pyrrolidine derivatives
discovered
Prior art date
Application number
BR0016693-6A
Other languages
English (en)
Other versions
BRPI0016693B1 (pt
Inventor
Timothy J Martins
Kerry W Fowler
Joshua Odingo
Laurence E Burgess
Edward A Kesicki
Amy Oliver
John J Gaudino
Zachary S Jones
Bradley J Newhouse
Stephen Schlachter
Original Assignee
Icos Corp
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 Icos Corp filed Critical Icos Corp
Publication of BR0016693A publication Critical patent/BR0016693A/pt
Publication of BRPI0016693B1 publication Critical patent/BRPI0016693B1/pt

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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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Abstract

"DERIVADOS DE PIRROLIDINA COMO INIBIDORES DE FOSFODIESTERASE ESPECìFICO AMP CìCLICO". São descobertos novos compostos de pirrolidina contendo a fórmula estrutural (II) que são inibidores potentes e específicos da PDE4, assim como métodos para fabricação dos mesmos. Também são descobertos os usos desses compostos no tratamento de doenças inflamatórias e outras desordens envolvendo elevados níveis de citoquinas, bem como desordens do sistema nervoso central (SNC).
BRPI0016693-6A 1999-12-23 2000-11-28 Derivados de pirrolidina como inibidores de fosfodiesterase específico amp cíclico BRPI0016693B1 (pt)

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
BR0016693A true BR0016693A (pt) 2003-03-11
BRPI0016693B1 BRPI0016693B1 (pt) 2015-09-01

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BRPI0016693-6A BRPI0016693B1 (pt) 1999-12-23 2000-11-28 Derivados de pirrolidina como inibidores de fosfodiesterase específico amp cíclico

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US (6) US6258833B1 (pt)
EP (1) EP1242400B1 (pt)
JP (1) JP4294903B2 (pt)
KR (1) KR20020063600A (pt)
CN (1) CN1434813A (pt)
AT (1) ATE325108T1 (pt)
AU (1) AU778543B2 (pt)
BG (1) BG65892B1 (pt)
BR (1) BRPI0016693B1 (pt)
CA (1) CA2395193C (pt)
CZ (1) CZ20022188A3 (pt)
DE (1) DE60027769D1 (pt)
EA (1) EA005686B1 (pt)
EE (1) EE05087B1 (pt)
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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
BR0112146A (pt) * 2000-07-03 2003-05-06 Speedel Pharma Ag Preparação de ácidos (r)-2-alquil-3-fenilpropiÈnicos
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
CA2463469A1 (en) * 2001-10-16 2003-04-24 Memory Pharmaceuticals Corporation 4-(4-alkoxy-3-hydroxyphenyl)-2-pyrrolidone derivatives as pde-4 inhibitors for the treatment of neurological syndromes
DK1463493T3 (da) 2001-12-14 2008-02-04 Serono Lab Fremgangsmåder til at inducere æglösning ved anvendelse af en ikke polypeptid-cAMP-niveaumodulator
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
DK1606261T3 (da) 2003-03-10 2010-01-18 Nycomed Gmbh Hidtil ukendt fremgangsmåde til fremstilling af roflumilast
JP2006523710A (ja) * 2003-04-16 2006-10-19 メモリー・ファーマシューティカルズ・コーポレイション ホスホジエステラーゼ４インヒビター
KR20060005375A (ko) * 2003-04-18 2006-01-17 메모리 파마슈티칼스 코포레이션 포스포디에스테라제 4 억제제로서의 피라졸 유도체
JP2007521276A (ja) * 2003-06-25 2007-08-02 スミスクライン・ビーチャム・コーポレイション Ｎｋ−２およびｎｋ−３として用いるための４−カルボキサミドキノリン誘導体
US7468437B2 (en) * 2003-09-30 2008-12-23 Merck & Co., Inc. Phenyl pyrrolidine ether tachykinin receptor antagonists
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
CA2561014C (en) * 2004-04-08 2013-09-10 Wyeth Thioamide derivatives as progesterone receptor modulators
EP1799673A1 (en) * 2004-10-15 2007-06-27 Memory Pharmaceuticals Corporation Pyrazole derivatives as phosphodiesterase 4 inhibitors
CN101166737A (zh) * 2004-10-20 2008-04-23 记忆药物公司 磷酸二酯酶4抑制剂
AU2006224619B2 (en) * 2005-03-16 2012-06-07 Takeda Gmbh Taste masked dosage form containing roflumilast
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
US7985756B2 (en) 2005-10-21 2011-07-26 Braincells Inc. Modulation of neurogenesis by PDE inhibition
WO2007053596A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
ZA200804550B (en) 2005-11-09 2009-08-26 Combinatorx Inc Methods, compositions, and kits for the treatment of medical conditions
US20100216734A1 (en) * 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
CA2643199A1 (en) * 2006-03-08 2007-09-13 Braincells, Inc. Modulation of neurogenesis by nootropic agents
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
WO2007134077A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. 5 ht receptor mediated neurogenesis
EP2068872A1 (en) 2006-09-08 2009-06-17 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
EP2066355A2 (en) * 2006-09-19 2009-06-10 Braincells, Inc. Combination comprising a peroxisome proliferator activated receptor agent and a second neurogenic agent for treating a nervous system disorder, increasing neurodifferentiation and increasing neurogenesis
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
CL2007002958A1 (es) * 2006-10-12 2008-05-09 Epix Delaware Inc Compuestos derivados de heteroaril-carboxamida, antagonistas del receptor de quimioquina; composicion farmaceutica; y uso para el tratamiento o prevencion de enfermedades tales como rechazo de transplante de organos, artritis reumatoidea, lupus, entr
AU2008284662B2 (en) 2007-08-07 2013-07-25 Takeda Pharmaceutical Company Limited Pyrrolidin-2 -one derivatives as androgen receptor modulator
KR20100102646A (ko) 2007-12-11 2010-09-24 가부시키가이샤 사이토파스파인더 카르복스아미드 화합물 및 케모카인 수용체 길항제로서의 이의 용도
WO2010099217A1 (en) 2009-02-25 2010-09-02 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
EP2804603A1 (en) 2012-01-10 2014-11-26 President and Fellows of Harvard College Beta-cell replication promoting compounds and methods of their use
TWI617553B (zh) * 2013-03-13 2018-03-11 美國禮來大藥廠 吖丁啶基氧苯基吡咯啶化合物
EP3096749B1 (en) * 2014-01-24 2019-05-15 Celgene Corporation Methods for the treatment of obesity using apremilast
MY193597A (en) * 2014-05-29 2022-10-19 Mitsubishi Tanabe Pharma Corp Novel pyrrolidine compound and application as melanocortin receptor agonist
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
EP4273141A1 (en) 2017-09-29 2023-11-08 Mitsubishi Tanabe Pharma Corporation Optically active pyrrolidine compound and method for producing same
KR20210093320A (ko) * 2018-12-18 2021-07-27 우한 휴먼웰 이노베이티브 드러그 리서치 앤드 디벨롭먼트 센터 리미티드 컴퍼니 페닐피롤리딘계 화합물 및 그의 용도
WO2021036953A1 (zh) * 2019-08-23 2021-03-04 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
TWI877358B (zh) * 2020-04-29 2025-03-21 大陸商廣東東陽光藥業股份有限公司 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 (pt) * 1974-02-08 1975-08-26
US5665754A (en) * 1993-09-20 1997-09-09 Glaxo Wellcome Inc. Substituted pyrrolidines
CA2143143A1 (en) * 1994-03-08 1995-09-09 Toshihiko Tanaka 3-phenylpyrrolidine derivatives
JPH07300455A (ja) * 1994-03-08 1995-11-14 Mitsubishi Chem Corp ３−フェニルピロリジン誘導体
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
SK132899A3 (en) * 1997-04-04 2000-09-12 Pfizer Prod Inc NICOTINAMIDE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONì (54) COMPRISING THEM
US6258833B1 (en) * 1999-12-23 2001-07-10 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors

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