CN101277949A - 二肽基肽酶-ⅳ抑制剂 - Google Patents

二肽基肽酶-ⅳ抑制剂 Download PDF

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Publication number
CN101277949A
CN101277949A CNA2006800134175A CN200680013417A CN101277949A CN 101277949 A CN101277949 A CN 101277949A CN A2006800134175 A CNA2006800134175 A CN A2006800134175A CN 200680013417 A CN200680013417 A CN 200680013417A CN 101277949 A CN101277949 A CN 101277949A
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China
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alkyl
heterocyclylalkyl
compound
aryl
heteroaryl
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Chinese (zh)
Inventor
H·克罗特
T·福伊尔施泰因
F·里希特
J·伯尔
M·埃塞尔斯
B·诺尔特
M·施奈德
M·霍赫居特尔
F-F·弗里克尔
A·塔韦拉斯
C·施滕内克
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Alantos Pharmaceuticals Holding Inc
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Alantos Pharmaceuticals Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36694223&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN101277949(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Alantos Pharmaceuticals Inc filed Critical Alantos Pharmaceuticals Inc
Publication of CN101277949A publication Critical patent/CN101277949A/zh
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    • 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
    • C07D207/10—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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CNA2006800134175A 2005-04-22 2006-04-21 二肽基肽酶-ⅳ抑制剂 Pending CN101277949A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US67415105P 2005-04-22 2005-04-22
US60/674,151 2005-04-22

Publications (1)

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CN101277949A true CN101277949A (zh) 2008-10-01

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CNA2006800134175A Pending CN101277949A (zh) 2005-04-22 2006-04-21 二肽基肽酶-ⅳ抑制剂

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US (3) US7553861B2 (enExample)
EP (1) EP1888562B1 (enExample)
JP (2) JP4568361B2 (enExample)
KR (1) KR20080000665A (enExample)
CN (1) CN101277949A (enExample)
AP (1) AP2007004234A0 (enExample)
AU (2) AU2006239929B2 (enExample)
BR (1) BRPI0608469A2 (enExample)
CA (1) CA2599419A1 (enExample)
CR (1) CR9462A (enExample)
EA (1) EA200702208A1 (enExample)
ES (1) ES2477868T3 (enExample)
IL (1) IL186607A0 (enExample)
MA (1) MA29387B1 (enExample)
MX (1) MX2007011453A (enExample)
NO (1) NO20075973L (enExample)
TN (1) TNSN07244A1 (enExample)
WO (1) WO2006116157A2 (enExample)
ZA (1) ZA200708179B (enExample)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104356046A (zh) * 2014-11-02 2015-02-18 浙江医药高等专科学校 环烷基取代的环己烷羧酸酰胺类衍生物及其用途
CN104356048A (zh) * 2014-11-02 2015-02-18 浙江医药高等专科学校 环己烷羧酸酰胺类衍生物、其制备方法和用途
CN105330579A (zh) * 2014-08-08 2016-02-17 杭州雷索药业有限公司 依泽替米贝及其衍生物在治疗或预防癫痫中的应用
CN105343093A (zh) * 2015-12-14 2016-02-24 上海壹志医药科技有限公司 环丙沙星的药物用途
CN108290881A (zh) * 2015-09-28 2018-07-17 健泰科生物技术公司 治疗性化合物和其使用方法
CN113040090A (zh) * 2021-04-13 2021-06-29 南京医科大学 构建孤独症的动物模型的方法及相应应用

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
JP4568361B2 (ja) * 2005-04-22 2010-10-27 アラントス・ファーマシューティカルズ・ホールディング・インコーポレーテッド ジペプチジルペプチダーゼ−ｉｖ阻害剤
WO2007050485A2 (en) * 2005-10-25 2007-05-03 Merck & Co., Inc. Combination of a dipeptidyl peptidase-4 inhibitor and an anti-hypertensive agent for the treatment of diabetes and hypertension
CA2633167A1 (en) * 2005-12-16 2007-07-12 Merck & Co., Inc. Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
MX2008014024A (es) 2006-05-04 2008-11-14 Boehringer Ingelheim Int Formas poliformas.
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
WO2008011518A2 (en) * 2006-07-19 2008-01-24 Diakine Therapeutics, Inc. Encapsulation system
AU2008210988B2 (en) * 2007-02-01 2012-09-06 Allocure, Inc. Potentiation of stem cell homing and treatment of organ dysfunction or organ failure
CN101652147B (zh) 2007-04-03 2013-07-24 田边三菱制药株式会社 二肽基肽酶iv抑制化合物和甜味剂的并用
CA2696579C (en) * 2007-08-17 2017-01-24 Boehringer Ingelheim International Gmbh Purine derivatives for use in the treatment of fab-related diseases
GB2465132B (en) 2007-09-21 2012-06-06 Lupin Ltd Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors
CL2008003653A1 (es) * 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
WO2009099172A1 (ja) * 2008-02-07 2009-08-13 Takeda Pharmaceutical Company Limited 医薬
PE20091730A1 (es) 2008-04-03 2009-12-10 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
US20090264476A1 (en) * 2008-04-18 2009-10-22 Mckelvey Craig CB-1 receptor modulator formulations
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
MY164581A (en) 2008-08-15 2018-01-15 Boehringer Ingelheim Int Purin derivatives for use in the treatment of fab-related diseases
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
EP2382216A1 (en) 2008-12-23 2011-11-02 Boehringer Ingelheim International GmbH Salt forms of organic compound
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
TWI466672B (zh) 2009-01-29 2015-01-01 Boehringer Ingelheim Int 小兒科病人糖尿病之治療
EA029759B1 (ru) 2009-02-13 2018-05-31 Бёрингер Ингельхайм Интернациональ Гмбх Антидиабетические лекарственные средства, содержащие ингибитор dpp-4 (линаглиптин) необязательно в комбинации с другими антидиабетическими средствами
WO2010146597A1 (en) 2009-06-18 2010-12-23 Lupin Limited 2-amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent dpp-iv inhibitors
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
EP3646859A1 (en) 2009-11-27 2020-05-06 Boehringer Ingelheim International GmbH Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
US20130109703A1 (en) 2010-03-18 2013-05-02 Boehringer Ingelheim International Gmbh Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions
JP2013523819A (ja) 2010-04-06 2013-06-17 アリーナ ファーマシューティカルズ， インコーポレイテッド Ｇｐｒ１１９レセプターのモジュレーターおよびそれに関連する障害の処置
AU2011249722B2 (en) 2010-05-05 2015-09-17 Boehringer Ingelheim International Gmbh Combination therapy
CN106975074A (zh) 2010-06-24 2017-07-25 勃林格殷格翰国际有限公司 糖尿病治疗
PH12013500547A1 (en) 2010-09-22 2013-06-10 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
SG10201600912SA (en) 2011-03-04 2016-03-30 Intrexon Corp Vectors conditionally expressing protein
US20140018371A1 (en) 2011-04-01 2014-01-16 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145603A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
PH12014500137A1 (en) 2011-07-15 2017-08-18 Boehringer Ingelheim Int Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
CA2844985A1 (en) 2011-08-16 2013-02-21 Mt. Sinai School Of Medicine Tricyclic compounds as anticancer agents
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
US20130303554A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in sirs and/or sepsis
WO2013171167A1 (en) 2012-05-14 2013-11-21 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
SG11201506450RA (en) 2013-02-19 2015-09-29 Icahn School Med Mount Sinai Tricyclic heterocycles as anticancer agents
CN105188706A (zh) * 2013-03-15 2015-12-23 勃林格殷格翰国际有限公司 利格列汀在心脏和肾脏保护性抗糖尿病治疗中的用途
EP3110449B1 (en) 2014-02-28 2023-06-28 Boehringer Ingelheim International GmbH Medical use of a dpp-4 inhibitor
WO2015138496A1 (en) 2014-03-11 2015-09-17 Icahn School Of Medicine At Mount Sinai Constrained tricyclic sulfonamides
WO2015138500A1 (en) 2014-03-11 2015-09-17 Icahn School Of Medicine At Mount Sinai Sulfonamides derived from tricyclyl-2-aminocycloalkanols as anticancer agents
MX386778B (es) 2015-03-09 2025-03-19 Intekrin Therapeutics Inc Métodos para el tratamiento de enfermedad de hígado graso no alcohólico y/o lipodistrofia.
JP6955485B2 (ja) 2015-09-09 2021-10-27 アイカーン スクール オブ メディスン アット マウント サイナイＩｃａｈｎ Ｓｃｈｏｏｌ ｏｆ Ｍｅｄｉｃｉｎｅ ａｔ Ｍｔ． Ｓｉｎａｉ 抗がん剤としての複素環式の限定された三環系スルホンアミド
JP6966425B2 (ja) 2015-09-09 2021-11-17 アイカーン スクール オブ メディスン アット マウント サイナイIcahn School of Medicine at Mt. Sinai 抗がん剤としての複素環式の限定された三環系スルホンアミド
WO2017211979A1 (en) 2016-06-10 2017-12-14 Boehringer Ingelheim International Gmbh Combinations of linagliptin and metformin
US10918647B2 (en) 2016-07-26 2021-02-16 University Of Southern California Selective bromodomain inhibition of fungal Bdf1
WO2018049014A1 (en) 2016-09-07 2018-03-15 Trustees Of Tufts College Dash inhibitors, and uses related thereto
WO2018093144A1 (ko) * 2016-11-15 2018-05-24 주식회사 엘지화학 제2형 당뇨병 및 당뇨성 이상지질혈증 치료용 복합제제
CA3058806A1 (en) 2017-04-03 2018-10-11 Coherus Biosciences Inc. Ppar.gamma. agonist for treatment of progressive supranuclear palsy
US11559537B2 (en) 2017-04-07 2023-01-24 Trustees Of Tufts College Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists
KR101983298B1 (ko) * 2018-06-11 2019-05-29 연세대학교 산학협력단 인플라마좀 매개 염증성 질환의 예방 또는 치료용 약학 조성물
AU2019348194B2 (en) * 2018-09-28 2025-04-03 Griffith University Agents and methods for modulating pathogen activity
WO2022003405A1 (en) * 2020-07-03 2022-01-06 Savoi Guilherme One-pot process to obtain a pyrrolidine-2-carbonitrile intermediate compound and industrial scale telescopic process to prepare (2s)-1-[n-(3-hydroxyadamantan-1-yl)glycyl]-2-pyrrolidinecarbonitrile (vildagliptin) using same
IL305835A (en) 2021-03-15 2023-11-01 Maze Therapeutics Inc Glycogen synthase 1 (GYS1) inhibitors and methods of using them
JP7055517B1 (ja) 2021-12-22 2022-04-18 株式会社ブンリ 分離装置

Family Cites Families (248)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3297709A (en) * 1965-11-19 1967-01-10 American Home Prod Certain substituted tetrazole derivatives
DE3607194A1 (de) * 1986-03-05 1987-09-10 Merck Patent Gmbh Carbamoylphenothiazine
DE3633485A1 (de) 1986-10-02 1988-04-07 Bayer Ag Substituierte 2-pyri(mi)dyl-2'-pyridyl-(thio)-ether
FR2643371B1 (fr) 1989-02-17 1993-11-05 Roussel Uclaf Nouveaux derives de l'acide 2-amino pentanedioique, leur procede de preparation et leur application comme medicaments
US5118811A (en) 1989-04-13 1992-06-02 Japan Tobacco Inc. Amino acid derivatives possessing prolyl endopeptidase-inhibitory activities
IT1232350B (it) 1989-08-04 1992-01-28 Poli Ind Chimica Spa Nuovi ergolinici derivati dalla prolina e strutture correlate con attivita' dopaminergica.
DE69116692T2 (de) * 1990-06-07 1996-09-05 Zeria Pharm Co Ltd Neue arylalkanoylaminderivate und diese enthaltendes arzneimittel
JP2518965B2 (ja) 1990-09-21 1996-07-31 三井東圧化学株式会社 新規ピリジン誘導体及びそれを有効成分として含有する制癌剤効果増強剤
IL100428A0 (en) 1990-12-21 1992-09-06 Ciba Geigy Pyrimidinyl-and triazinyl-salicylamides,their preparation and their use as herbicides and plant growth regulants
JPH05155771A (ja) 1991-12-05 1993-06-22 Zeria Pharmaceut Co Ltd アリールアルカノイル誘導体を含有する後天性免疫不全症候群予防治療剤
DE4141399A1 (de) 1991-12-16 1993-06-17 Bayer Ag 4-(substituierte)amino-3-arylpyrrolinon-derivate
PH31294A (en) * 1992-02-13 1998-07-06 Thomae Gmbh Dr K Benzimidazolyl derivatives, pharmaceutical compositions containing these compounds and process for preparing them.
DE4206041A1 (de) 1992-02-27 1993-09-02 Bayer Ag Sulfonylbenzyl-substituierte imidazolylpropensaeurederivate
DE4206045A1 (de) 1992-02-27 1993-09-02 Bayer Ag Sulfonylbenzyl substituierte pyridone
US5569662A (en) 1992-03-23 1996-10-29 Pfizer Inc. Quinuclidine derivatives as substance P antagonists
US5254453A (en) * 1992-04-16 1993-10-19 Eastman Kodak Company Process for preparing narrow size distribution small tabular grains
AU4321693A (en) * 1992-06-17 1994-01-04 Ciba-Geigy Ag Pyrimidinyl-and triazinyl compounds with herbicidal activity
WO1994000421A1 (en) 1992-06-19 1994-01-06 James Black Foundation Limited Bicyclooctane and bicycloheptane derivatives
JP2655754B2 (ja) * 1992-07-01 1997-09-24 フアイザー・インコーポレイテツド コレシストキニンレセプター拮抗剤としてのベンゾチアゼピン及びベンゾオキサゼピンの誘導体
DE4301105A1 (de) 1993-01-18 1994-07-21 Agfa Gevaert Ag Farbfotografisches Aufzeichnungsmaterial
DE4301106A1 (de) 1993-01-18 1994-07-21 Agfa Gevaert Ag Farbfotografisches Aufzeichnungsmaterial
CA2166975C (en) 1993-07-16 2005-04-05 Mark G. Bock Benzoxazinone and benzopyrimidinone piperidinyl tocolytic oxytocin receptor antagonists
FR2711992A1 (fr) 1993-11-03 1995-05-12 Lipha Nouveaux dérivé hétérocycliques, procédé de préparation et composition pharmaceutique les contenant.
US5492920A (en) * 1993-12-10 1996-02-20 Merck & Co., Inc. Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone
US5494919A (en) * 1993-11-09 1996-02-27 Merck & Co., Inc. 2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
US5492916A (en) * 1993-12-23 1996-02-20 Merck & Co., Inc. Di- and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
IL111785A0 (en) * 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
JPH07228529A (ja) * 1994-02-17 1995-08-29 Zeria Pharmaceut Co Ltd コリンエステラーゼ賦活剤
US5804560A (en) 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
JP4036470B2 (ja) * 1995-02-13 2008-01-23 バイエル・アクチエンゲゼルシヤフト 除草剤および有害生物防除剤としての２−フェニル置換複素環式１，３−ケトエノール
JP3599403B2 (ja) 1995-02-24 2004-12-08 山之内製薬株式会社 ベンズアゼピン誘導体の新規製造法
US5795894A (en) 1995-05-02 1998-08-18 Schering Corporation Piperazino derivatives as neurokinn antagonists
BR9608229A (pt) * 1995-05-09 1998-12-29 Bayer Ag Cetoenóis alquil-dihalogenofenil-substituídos
US5514505A (en) * 1995-05-15 1996-05-07 Xerox Corporation Method for obtaining improved image contrast in migration imaging members
US5563014A (en) 1995-05-15 1996-10-08 Xerox Corporation Migration imaging members
HUT76640A (en) * 1995-08-17 1997-10-28 Chinoin Gyogyszer Es Vegyeszet Compounds of pharmaceutical activity cyclic amide derivatives, pharmaceutical compositions containing them, process for producing them and their use
PT862562E (pt) 1995-09-13 2001-11-30 Takeda Chemical Industries Ltd Compostos de benzoxazepina sua producao e utilizacao como agentes para reducao dos niveis de lipidos
US6057314A (en) * 1995-12-21 2000-05-02 Biochem Pharma Inc. Low molecular weight bicyclic thrombin inhibitors
ES2218660T3 (es) 1996-01-16 2004-11-16 Bristol-Myers Squibb Company Inhibidores aromaticos conformacionalmente restringidos de la proteina de transferencia de trigliceridos microsomales y procedimiento.
US5767097A (en) * 1996-01-23 1998-06-16 Icn Pharmaceuticals, Inc. Specific modulation of Th1/Th2 cytokine expression by ribavirin in activated T-lymphocytes
DE19613329A1 (de) * 1996-04-03 1997-10-09 Hoechst Schering Agrevo Gmbh Substituierte Pyridine/Pyrimidine, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel
TW397821B (en) 1996-04-19 2000-07-11 American Home Produits Corp 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof
US20020006899A1 (en) * 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
US6537987B1 (en) * 1996-06-20 2003-03-25 Pfizer Inc. 4,1-benzoxazepines or 4,1-benzothiazepines and their use as squalene synthetase inhibitors
AU3359697A (en) 1996-07-08 1998-02-02 Yamanouchi Pharmaceutical Co., Ltd. Bone resorption inhibitors
US5968929A (en) * 1996-10-30 1999-10-19 Schering Corporation Piperazino derivatives as neurokinin antagonists
US6011155A (en) * 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
HU227487B1 (en) * 1996-12-19 2011-07-28 Isagro Spa Fungicidal compositions based on (n-phenylacetyl-n-2,6-xylyl)methyl alaninate (benalaxyl), use thereof
US6180698B1 (en) * 1997-02-28 2001-01-30 Candescent Technologies Corporation Polycarbonate-containing liquid chemical formulation and method for making polycarbonate film
US6500885B1 (en) 1997-02-28 2002-12-31 Candescent Technologies Corporation Polycarbonate-containing liquid chemical formulation and methods for making and using polycarbonate film
US5914150A (en) * 1997-02-28 1999-06-22 Candescent Technologies Corporation Formation of polycarbonate film with apertures determined by etching charged-particle tracks
US6319902B1 (en) 1997-08-22 2001-11-20 Shionogi & Co., Ltd. Peptide derivatives having thiazolyl-alanine residue
WO1999014998A2 (en) 1997-09-24 1999-04-01 Amgen Inc. Method for preventing and treating hearing loss using sensorineurotrophic compounds
DE04029691T1 (de) 1998-02-02 2007-11-08 Trustees Of Tufts College, Medford Verwendung von Dipetidylpeptidasehemmer zur Regulierung des Glukosemetabolismus
US6583170B1 (en) 1998-05-15 2003-06-24 Wyeth 2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol and estrogen formulations
HUP0102923A3 (en) 1998-06-03 2002-01-28 Gpi Nil Holdings Inc Wilmingto Aza-heterocyclic compounds used to treat neurological disorders and hair loss and pharmaceutical compositions containing them
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
EA200001144A1 (ru) * 1998-06-03 2001-10-22 Джи-Пи-Ай Эн-Ай-Эл Холдингз, Инк. Аза-гетероциклические соединения, применяемые для лечения неврологических расстройств и выпадения волос
HUP0102935A3 (en) * 1998-06-03 2002-01-28 Gpi Nil Holdings Inc Wilmingto N-linked sulfonamides of n-heterocyclic carboxylic acids or carboxylic acid isosteres and pharmaceutical compositions containing them
DE19826972A1 (de) 1998-06-18 1999-12-23 Univ Magdeburg Tech Verwendung von Enzyminhibitoren und pharmazeutische Zubereitung zur Therapie von dermatologischen Erkrankungen mit follikulären und epidermalen Hyperkeratosen und einer verstärkten Keratinozytenproliferation
US6337340B1 (en) * 1998-08-14 2002-01-08 Gpi Nil Holdings, Inc. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders
US20030176357A1 (en) 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
DE19959916A1 (de) * 1998-12-30 2000-07-20 Henkel Chile Sa Füllstoffhaltige Polymerdispersion, Verfahren zu deren Herstellung und deren Verwendung
HK1039108A1 (zh) 1999-03-15 2002-04-12 Axys Pharmaceuticals, Inc. 以n-氰甲基酰胺作为蛋白酶抑制剂
GB9906715D0 (en) * 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
WO2000061556A1 (en) 1999-04-09 2000-10-19 Meiji Seika Kaisha, Ltd. Nitrogen-containing heterocyclic compounds and benamide compounds and drugs containing the same
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
GB2355457A (en) * 1999-09-30 2001-04-25 Merck & Co Inc Novel spirotricyclic substituted azacycloalkane derivatives useful as alpha 1a adrenoceptor antagonists
CO5271670A1 (es) 1999-10-29 2003-04-30 Pfizer Prod Inc Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas
US20040152745A1 (en) 1999-11-12 2004-08-05 Guilford Pharmaceuticals, Inc. Dipeptidyl peptidase IV inhibitors and methods of making and using dipeptidyl peptidase IV inhibitors
GB9928330D0 (en) * 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
US6380398B2 (en) * 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
ES2275654T5 (es) 2000-01-21 2012-06-07 Novartis Ag Combinaciones que contienen inhibidores de la dipeptidilpeptidasa-IV y agentes antidiabéticos
US7064145B2 (en) 2000-02-25 2006-06-20 Novo Nordisk A/S Inhibition of beta cell degeneration
US20030073701A1 (en) * 2001-03-31 2003-04-17 Thompson Lorin A. Succinoylamino heterocycles as inhibitors of a beta protein production
CZ20023234A3 (cs) 2000-03-31 2003-01-15 Probiodrug Ag Léčivo proti diabetu
GB0010188D0 (en) * 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
CA2407597A1 (en) * 2000-05-01 2001-11-08 Dupont Pharmaceuticals Company Tricyclic fused pyridine and pyrimidine derivatives as crf receptor antagonists
DE10025464A1 (de) * 2000-05-23 2001-12-06 Inst Medizintechnologie Magdeb Kombinierte Verwendung von Enzyminhibitoren zur Therapie von Autoimmunerkrankungen, bei Transplantationen und Tumorerkrankungen sowie Kombinationen von Enzyminhibitoren umfassende pharmazeutische Zubereitungen
DE10029077A1 (de) 2000-06-13 2001-12-20 Bayer Ag Thiazolylsubstituierte Heterocyclen
US6432969B1 (en) 2000-06-13 2002-08-13 Novartis Ag N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US7078397B2 (en) 2000-06-19 2006-07-18 Smithkline Beecham Corporation Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus
CA2414111A1 (en) * 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for increasing nitric oxide synthase activity
US6509332B2 (en) * 2000-07-06 2003-01-21 Wyeth Methods of treating excessive intraocular pressure
US6369051B1 (en) * 2000-07-06 2002-04-09 American Home Products Corporation Combinations of SSRI and estrogenic agents
US20020019373A1 (en) * 2000-07-06 2002-02-14 American Home Products Corporation Combinations of bisphosphonates and estrogenic agents
AR029539A1 (es) * 2000-07-06 2003-07-02 Wyeth Corp Combinaciones de estatinas y agentes estrogenicos
US6455568B2 (en) * 2000-07-06 2002-09-24 Wyeth Combination therapy for inhibiting sphincter incontinence
US20020028800A1 (en) * 2000-07-06 2002-03-07 American Home Products Corporation Combination therapy for prosthesis-related bone degeneration
US6358991B2 (en) * 2000-07-06 2002-03-19 American Home Products Corporation Methods of treating neuropeptide Y-related conditions
US6376486B1 (en) * 2000-07-06 2002-04-23 American Home Products Corporation Methods of inhibiting sphincter incontinence
US20020025952A1 (en) * 2000-07-06 2002-02-28 American Home Products Corporation Combinations of statins, estrogens and estrogenic agents
AU2001271706A1 (en) * 2000-07-06 2002-01-21 American Home Products Corporation Use of substituted indole compounds for treating breast disorders
US20020028792A1 (en) * 2000-07-06 2002-03-07 American Home Products Corporation Combinations of bisphosphonates, estrogens and estrogenic agents
JP4812225B2 (ja) 2000-07-11 2011-11-09 塩野義製薬株式会社 生理活性ペプチド含有腸溶性製剤
CA2418656C (en) 2000-08-10 2011-02-01 Mitsubishi Pharma Corporation Proline derivatives and use thereof as drugs
US6559163B2 (en) * 2000-08-16 2003-05-06 Neurogen Corporation 2,4-substituted quinoline derivatives
AU2001294196B2 (en) 2000-10-06 2005-11-17 Tanabe Seiyaku Co., Ltd. Nitrogenous five-membered ring compounds
US6518299B1 (en) * 2000-10-20 2003-02-11 Biocryst Pharmaceuticals, Inc. Substituted pyrrolidine compounds useful as neuraminidase inhibitors
TWI243162B (en) * 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
JPWO2002051836A1 (ja) 2000-12-27 2004-04-22 協和醗酵工業株式会社 ジペプチジルペプチダーゼ−ｉｖ阻害剤
WO2002053170A2 (de) 2001-01-02 2002-07-11 Institut Für Medizintechnologie Magdeburg Gmbh (Imtm) Kombinierte verwendung von enzyminhibitoren und pharmazeutischen zubereitungen daraus zur therapie und prophylaxe der arteriosklerose, zur therapie und prävention allergischer reaktionen von typ i nach gell und coombs und zur therapie und prävention dermatologischer erkrankungen mit follikulären und epidermalen hyperkeratos
DE10100053A1 (de) 2001-01-02 2002-08-22 Keyneurotek Ag I G Verwendung von Enzyminhibitoren der Dipeptidylpeptidase IV sowie der Aminopeptidase N und pharmazeutischen Zubereitungen daraus zur Prävention und/oder Therapie Ischämie-bedingter akuter und chronischer neurodegenerativer Prozesse und Erkrankungen
SK10802003A3 (sk) * 2001-02-02 2004-05-04 Takeda Chemical Industries, Ltd. Kondenzovaná heterocyklická zlúčenina, jej použitie a jej farmaceutický prípravok
MXPA03007349A (es) * 2001-02-24 2003-12-04 Boehringer Ingelheim Pharma Derivados de xantina, su preparacion y su empleo como medicamentos.
EP1370211A4 (en) * 2001-03-02 2005-02-09 Bristol Myers Squibb Co SIMULTANEOUS ADMINISTRATION OF MELANOCORTIN RECEPTOR AGONISTS AND A PHOSPHODIESTERASE HEMMER FOR THE TREATMENT OF DISEASES RELATED TO CYCLIC AMP
CA2437594A1 (en) * 2001-03-02 2002-09-12 Graham S. Poindexter Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same
JP2002265439A (ja) 2001-03-08 2002-09-18 Mitsubishi Pharma Corp シアノピロリジン誘導体およびその医薬用途
FR2822826B1 (fr) * 2001-03-28 2003-05-09 Servier Lab Nouveaux derives sulfonyles d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US20030032625A1 (en) * 2001-03-29 2003-02-13 Topo Target Aps Succinimide and maleimide derivatives and their use as topoisomerase II catalytic inhibitors
GB0109146D0 (en) 2001-04-11 2001-05-30 Ferring Bv Treatment of type 2 diabetes
JP2004536047A (ja) * 2001-04-11 2004-12-02 ブリストル−マイヤーズ　スクイブ　カンパニー 糖尿病処置用ｃ−アリールグルコシドのアミノ酸複合体および方法
FR2824825B1 (fr) * 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
MXPA03011095A (es) 2001-05-29 2005-04-28 Guilford Pharm Inc Metodo para tratar una lesion nerviosa causada por cirugia.
FR2825717B1 (fr) 2001-06-08 2005-02-18 Rhodia Chimie Sa Preparation stereoselective de l-acides amines cycliques
DE60224189T2 (de) 2001-06-20 2008-12-11 Merck & Co., Inc. Dipeptidylpeptidase-hemmer zur behandlung von diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
US7368421B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
ES2296979T3 (es) 2001-06-27 2008-05-01 Smithkline Beecham Corporation Fluoropirrolidinas como inhibidores de dipeptidil peptidasa.
US20030135023A1 (en) 2001-06-27 2003-07-17 Hans-Ulrich Demuth Peptide structures useful for competitive modulation of dipeptidyl peptidase IV catalysis
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
US7183290B2 (en) 2001-06-27 2007-02-27 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US7196201B2 (en) 2001-06-27 2007-03-27 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
FI20011466A0 (fi) * 2001-07-04 2001-07-04 Orion Corp Prolyylioligopeptidaasia inhiboivaa aktiivisuutta omaavia yhdisteitä, niiden valmistusmenetelmiä ja käyttö
WO2003015768A2 (en) 2001-08-16 2003-02-27 Probiodrug Ag Use of inhibitors of proline endopeptidase to modulate inositol (1,4,5) triphosphate concentration dependent on intracellular signal cascades
JP4337138B2 (ja) 2001-08-31 2009-09-30 味の素株式会社 新規ジアリールアルケン誘導体及び新規ジアリールアルカン誘導体
TWI246510B (en) 2001-09-14 2006-01-01 Mitsubishi Pharma Corp Thiazolidine derivatives and pharmaceutical uses thereof
GB0125446D0 (en) * 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
GB0125445D0 (en) * 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
US6861440B2 (en) * 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
CA2464995A1 (en) * 2001-10-31 2003-05-08 Novartis Ag Methods to treat diabetes and related conditions based on polymorphisms in the tcf1 gene
EP1442028A4 (en) 2001-11-06 2009-11-04 Bristol Myers Squibb Co SUBSTITUTED ACID DERIVATIVES, WHICH APPRECIATE AS ANTIDIBILICS AND AGENTS AGAINST OBESITAS, AND METHODS
US20030125304A1 (en) 2001-11-09 2003-07-03 Hans-Ulrich Demuth Substituted amino ketone compounds
US20050101638A1 (en) * 2002-11-08 2005-05-12 Webb Randy L. Combination of organic compounds
US20030114389A1 (en) 2001-11-13 2003-06-19 Webb Randy Lee Combination of organic compounds
AU2002357767C1 (en) 2001-11-26 2009-03-19 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
WO2003048125A1 (en) 2001-12-03 2003-06-12 F. Hoffmann-La Roche Ag Aminotetralin derivatives as muscarinic receptor antagonists
GB0129988D0 (en) 2001-12-14 2002-02-06 Ferring Bv Imidazolidineacetic acid derivatives
WO2003054228A2 (en) 2001-12-21 2003-07-03 Axxima Pharmaceuticals Ag Human cellular enzymes as targets against hepatitis c virus infections
WO2003057144A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
EP1513522A2 (en) 2002-01-18 2005-03-16 Sri International Methods of treating conditions associated with an edg receptor
AU2003218969A1 (en) 2002-02-01 2003-09-02 Probiodrug Ag Modulation of t lymphocytes using dp iv inhibitors
DE60217186T2 (de) 2002-02-28 2007-09-27 Prosidion Ltd. Dpiv-inhibitoren auf glutaminbasis
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
DE10211555A1 (de) 2002-03-15 2003-10-02 Imtm Inst Fuer Medizintechnolo Verwendung der Inhibitoren von Enzymen mit Aktivitäten der Aminopeptidase N und/oder der Dipeptidylpeptidase IV und pharmazeutischen Zubereitungen daraus zur Therapie und Prävention dermatologischer Erkrankungen mit sebozytärer Hyperproliferation und veränderten Differenzierungszuständen
TW200810743A (en) * 2002-03-22 2008-03-01 Novartis Ag Combination of organic compounds
AU2003220896A1 (en) 2002-03-28 2003-11-10 Sumitomo Pharmaceuticals Co., Ltd. Novel heteroaryl compounds
JP4329381B2 (ja) * 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
JP4329382B2 (ja) 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
RU2004132719A (ru) * 2002-04-08 2005-08-27 Торрент Фармасьютикалз Лтд. (In) Тиазолидин-4-карбонитрилы и их аналоги, применение указанных соединений в качестве ингибиторов дипептидилпептидаз
US20040106802A1 (en) 2002-04-08 2004-06-03 Torrent Pharmaceuticals Ltd. Novel compounds and therapeutic uses thereof
AU2003235913A1 (en) 2002-05-09 2003-11-11 Taisho Pharmaceutical Co., Ltd. Cyanopyrrolidine derivatives
JP2004026820A (ja) 2002-05-09 2004-01-29 Taisho Pharmaceut Co Ltd ジペプチジルペプチダーゼｉｖ阻害剤
US7057046B2 (en) * 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
GB0212412D0 (en) 2002-05-29 2002-07-10 Novartis Ag Combination of organic compounds
PT1513519E (pt) 2002-06-03 2009-05-06 Novartis Ag Uso de cianopirrolidinas substituídas e preparações de combinações que as contêm para tratar hiperlipidemia e doenças associadas
AU2003239919A1 (en) 2002-06-03 2003-12-19 Activbiotics, Inc. Intravenous rifalazil formulation and methods of use thereof
HUP0202001A2 (hu) 2002-06-14 2005-08-29 Sanofi-Aventis DDP-IV gátló hatású azabiciklooktán- és nonánszármazékok
IL166156A0 (en) 2002-07-09 2006-01-15 Point Therapeutics Inc Boroproline compound combination therapy
TW200401635A (en) 2002-07-23 2004-02-01 Yamanouchi Pharma Co Ltd 2-Cyano-4-fluoropyrrolidine derivative or salt thereof
GB0217786D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
GB0217783D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
GB0217780D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
AR040726A1 (es) 2002-07-31 2005-04-20 Smithkline Beecham Corp Compuesto de 2- fenilpiridin-4-il-heterociclico, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento
TW200404796A (en) 2002-08-19 2004-04-01 Ono Pharmaceutical Co Nitrogen-containing compound
UA78104C2 (en) 2002-08-29 2007-02-15 Taisho Pharmaceutical Co Ltd Benzenesulfonate salts of 4-fluoro-2-cyanopyrrolidine derivatives
AU2003293311A1 (en) 2002-09-18 2004-04-23 Prosidion Ltd. Secondary binding site of dipeptidyl peptidase iv (dp iv)
US20040058876A1 (en) * 2002-09-18 2004-03-25 Torsten Hoffmann Secondary binding site of dipeptidyl peptidase IV (DP IV)
US7262207B2 (en) 2002-09-19 2007-08-28 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
US7238724B2 (en) 2002-09-19 2007-07-03 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
US20040121964A1 (en) 2002-09-19 2004-06-24 Madar David J. Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
US6995180B2 (en) 2002-10-23 2006-02-07 Bristol Myers Squibb Company Glycinenitrile-based inhibitors of dipeptidyl peptidase IV and methods
WO2004042533A2 (en) 2002-11-01 2004-05-21 Prominence Networks, Inc. End-to-end qos internet protocol
EP1562925B1 (en) 2002-11-07 2007-01-03 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
DE10254304A1 (de) 2002-11-21 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
EP1422293A1 (en) 2002-11-25 2004-05-26 F. Hoffmann-La Roche Ag Crystal structure of dipeptidyl peptidase IV
AU2002952946A0 (en) 2002-11-27 2002-12-12 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
CA2508487A1 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CN100348189C (zh) 2002-12-10 2007-11-14 诺瓦提斯公司 DPP－IV抑制剂与PPAR－α化合物的组合
US20040192680A1 (en) 2002-12-20 2004-09-30 Anderson Steven N. Novel amides that activate soluble guanylate cyclase
US20040121994A1 (en) 2002-12-20 2004-06-24 Anderson Steven N. Novel amides that activate soluble guanylate cyclase
JP2004244412A (ja) 2003-01-20 2004-09-02 Kotobuki Seiyaku Kk ４位に置換基を有する２−シアノピロリジン誘導体及びその製造方法並びにそれを含有する薬剤
DK1595866T3 (en) 2003-01-31 2016-08-22 Sanwa Kagaku Kenkyusho Co Cyanopyrrolidines suitable for the treatment of inter alia metabolism syndrome
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
AU2003207881A1 (en) * 2003-02-28 2004-09-17 Aic Dipeptidyl peptidase inhibitors
DE10309005A1 (de) 2003-03-01 2004-09-09 Morphochem Aktiengesellschaft für kombinatorische Chemie Neue Verbindungen, die Dipetidyl Peptidase (DPPIV) und Neurale Endopeptidase (NEP) inhibieren
JP2006519846A (ja) 2003-03-10 2006-08-31 シェーリング　コーポレイション 複素環式キナーゼインヒビター：使用および合成の方法
WO2004092128A1 (en) 2003-04-10 2004-10-28 Smithkline Beecham Corporation Anhydrous crystalline forms of (2s, 4s)-1-{(2r)-2-amino-3-‘4-methoxybenzyl)sulfonyl!-3-methylbutanoyl}-4-fluoropyrrolindine-2-carbonitrile
WO2004089362A1 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S 2-cyanopyrroles and their analogues as ddp-iv inhibitors
AR044019A1 (es) 2003-04-16 2005-08-24 Novartis Ag Proceso para la preparacion de 2-cianopirrolidinas n-sustituidas
US20050014747A1 (en) * 2003-04-18 2005-01-20 Emily Reinhard Dihydrothiazine prodrugs of thiazolium agents
US7381537B2 (en) * 2003-05-05 2008-06-03 Probiodrug Ag Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease
WO2004098591A2 (en) 2003-05-05 2004-11-18 Probiodrug Ag Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases
WO2004099157A1 (en) 2003-05-07 2004-11-18 Pfizer Products Inc. Cannabinoid receptor ligands and uses thereof
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
EP1627870A1 (en) 2003-05-15 2006-02-22 Taisho Pharmaceutical Co., Ltd Cyanofluoropyrrolidine derivative
CN1798556A (zh) * 2003-06-06 2006-07-05 麦克公司 作为治疗或者预防糖尿病的二肽基肽酶抑制剂的稠合吲哚
US7235662B2 (en) 2003-06-11 2007-06-26 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
JP4579239B2 (ja) 2003-06-17 2010-11-10 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療または予防するためのジペプチジルペプチダーゼ阻害剤としてのシクロヘキシルグリシン誘導体
US20040259887A1 (en) 2003-06-18 2004-12-23 Pfizer Inc Cannabinoid receptor ligands and uses thereof
DK1638970T3 (da) 2003-06-20 2011-01-03 Hoffmann La Roche Pyrid (2, 1-A)-isoquinolinderivater som DPP-IV-inhibitorer
JP2005023038A (ja) 2003-07-04 2005-01-27 Taisho Pharmaceut Co Ltd 慢性腎疾患治療薬
DE10330842A1 (de) 2003-07-08 2005-02-10 Institut für Medizintechnologie Magdeburg GmbH, IMTM Verwendung der Inhibitoren von Enzymen mit Aktivitäten der Aminopeptidase N und/oder der Dipeptidylpeptidase IV und pharmazeutischen Zubereitungen daraus zur Therapie und Prävention dermatologischer Erkrankungen mit Hyperproliferation und veränderten Differenzierungszuständen von Fibroblasten
CN1852893A (zh) 2003-07-21 2006-10-25 史密丝克莱恩比彻姆公司 (2S,4S)－4－氟－1－[4－氟－β－(4－氟苯基)－L－苯基丙氨酰基]－2－吡咯烷甲腈对甲苯磺酸盐及其无水晶体形式
JP2005047853A (ja) 2003-07-29 2005-02-24 Fuji Photo Film Co Ltd 含窒素ヘテロ環化合物の製造方法
US6995183B2 (en) * 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
DE10337074A1 (de) * 2003-08-12 2005-03-17 Keyneurotek Ag Verwendung der Inhibitoren von Enzymen mit Aktivitäten der Aminopeptidase N und/oder der Dipeptidylpeptidase IV und pharmazeutischen Zubereitungen daraus zur Therapie und Prävention von chronischen neurodegenerativen Erkrankungen
CN1839120A (zh) 2003-08-18 2006-09-27 大正制药株式会社 顺－4－氟－l－脯氨酸衍生物的制备方法
HU227684B1 (en) * 2003-08-29 2011-11-28 Sanofi Aventis Adamantane and azabicyclo-octane and nonane derivatives and their use as dpp-iv inhibitors
US7205409B2 (en) 2003-09-04 2007-04-17 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
GB0321295D0 (en) 2003-09-11 2003-10-15 Spirogen Ltd Synthesis of protected pyrrolobenzodiazepines
US7371759B2 (en) * 2003-09-25 2008-05-13 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
WO2005033099A2 (en) * 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
AU2003269307A1 (en) 2003-10-06 2005-04-21 Torrent Pharmaceuticals Ltd. Azolidinecarbonitriles and their use as dpp-iv inhibitors
US20050153885A1 (en) 2003-10-08 2005-07-14 Yun Anthony J. Treatment of conditions through modulation of the autonomic nervous system
WO2005037826A1 (en) * 2003-10-17 2005-04-28 Incyte Corporation Substituted cyclic hydroxamates as inhibitors of matrix metalloproteinases
EP1684786A4 (en) 2003-10-24 2007-12-12 Merck & Co Inc IMPROVING THE MIRROR OF THE GROWTH HORMONE WITH A DIPEPTIDYL PEPTIDASE IV INHIBITOR AND A GROWTH HORMONE SECRETAGOG
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
US20050163849A1 (en) 2003-10-31 2005-07-28 Wong Patrick S. Compositions and dosage forms for enhanced absorption of iron
US20050171112A1 (en) 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
AU2004290499C1 (en) 2003-11-03 2011-02-24 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
JP2007510651A (ja) 2003-11-04 2007-04-26 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としての縮合フェニルアラニン誘導体
JP2005139107A (ja) 2003-11-05 2005-06-02 Taisho Pharmaceut Co Ltd ジペプチジルペプチダーゼｉｖ阻害剤
KR20140089408A (ko) 2003-11-17 2014-07-14 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
US20070149451A1 (en) 2003-11-17 2007-06-28 Holmes David G Combination of a dpp IV inhibitor and an antiobesity or appetite regulating agent
AU2004293416B2 (en) 2003-11-24 2009-09-24 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease
ES2298840T3 (es) 2003-12-08 2008-05-16 F. Hoffmann-La Roche Ag Derivados de tiazol.
US7771336B2 (en) 2003-12-12 2010-08-10 Mitsubishi Heavy Industries, Ltd Folder for rotary press
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
US7326728B2 (en) 2004-01-16 2008-02-05 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κβ activity and use thereof
US7605264B2 (en) 2004-01-16 2009-10-20 Bristol-Myers Squibb Company Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
SI1715893T1 (sl) 2004-01-20 2009-12-31 Novartis Pharma Ag Direktna kompresijska formulacija in postopek
WO2005073186A1 (ja) 2004-01-29 2005-08-11 Ono Pharmaceutical Co., Ltd. ピロリジン誘導体
US7230002B2 (en) 2004-02-03 2007-06-12 Glenmark Pharmaceuticals Ltd. Dipeptidyl peptidase IV inhibitors; processes for their preparation and compositions thereof
CA2554493C (en) 2004-02-05 2012-06-26 Kyorin Pharmaceutical Co., Ltd. Bicycloester derivative
EP1713780B1 (en) 2004-02-05 2012-01-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
EP1717225A4 (en) 2004-02-18 2009-10-21 Kyorin Seiyaku Kk BICYCLIC AMIDE DERIVATIVES
AU2005215136A1 (en) 2004-02-20 2005-09-01 Novartis Ag DPP-IV inhibitors for treating neurodegeneration and cognitive disorders
EP1729774A4 (en) * 2004-03-09 2009-05-06 Nat Health Research Institutes PYRROLIDINE CONNECTIONS
JP4568361B2 (ja) * 2005-04-22 2010-10-27 アラントス・ファーマシューティカルズ・ホールディング・インコーポレーテッド ジペプチジルペプチダーゼ−ｉｖ阻害剤

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105330579A (zh) * 2014-08-08 2016-02-17 杭州雷索药业有限公司 依泽替米贝及其衍生物在治疗或预防癫痫中的应用
CN105330579B (zh) * 2014-08-08 2019-08-30 杭州雷索药业有限公司 依泽替米贝及其衍生物在治疗或预防癫痫中的应用
CN104356046A (zh) * 2014-11-02 2015-02-18 浙江医药高等专科学校 环烷基取代的环己烷羧酸酰胺类衍生物及其用途
CN104356048A (zh) * 2014-11-02 2015-02-18 浙江医药高等专科学校 环己烷羧酸酰胺类衍生物、其制备方法和用途
CN104356046B (zh) * 2014-11-02 2017-04-05 浙江医药高等专科学校 环烷基取代的环己烷羧酸酰胺类衍生物及其用途
CN108290881A (zh) * 2015-09-28 2018-07-17 健泰科生物技术公司 治疗性化合物和其使用方法
CN108290881B (zh) * 2015-09-28 2021-12-07 健泰科生物技术公司 治疗性化合物和其使用方法
CN105343093A (zh) * 2015-12-14 2016-02-24 上海壹志医药科技有限公司 环丙沙星的药物用途
CN113040090A (zh) * 2021-04-13 2021-06-29 南京医科大学 构建孤独症的动物模型的方法及相应应用

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AP2007004234A0 (en) 2007-12-31
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