ZA200508439B - Medical use of inhibitors of glutaminyl and glutamate cyclases - Google Patents

Medical use of inhibitors of glutaminyl and glutamate cyclases

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Publication number
ZA200508439B
ZA200508439B ZA200508439A ZA200508439A ZA200508439B ZA 200508439 B ZA200508439 B ZA 200508439B ZA 200508439 A ZA200508439 A ZA 200508439A ZA 200508439 A ZA200508439 A ZA 200508439A ZA 200508439 B ZA200508439 B ZA 200508439B
Authority
ZA
South Africa
Prior art keywords
impaired
inhibitors
sleep
regulation
glutaminyl
Prior art date
Application number
ZA200508439A
Other languages
English (en)
Inventor
Demuth Hans-Ulrich
Hoffmann Torsten
Andru J Niestroj
Schilling Stephan
Heiser Ulrich
Original Assignee
Probiodrug Ag
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 Probiodrug Ag filed Critical Probiodrug Ag
Publication of ZA200508439B publication Critical patent/ZA200508439B/xx

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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
    • C07D207/08—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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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ZA200508439A 2003-05-05 2004-05-05 Medical use of inhibitors of glutaminyl and glutamate cyclases ZA200508439B (en)

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Families Citing this family (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1608317B1 (en) 2003-03-25 2012-09-26 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
KR20110059664A (ko) * 2003-05-05 2011-06-02 프로비오드룩 아게 글루타미닐 및 글루타메이트 사이클라제의 이펙터의 용도
US8338120B2 (en) * 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
US7732162B2 (en) * 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
DE602004026289D1 (de) 2003-05-05 2010-05-12 Probiodrug Ag Glutaminylcyclase-hemmer
WO2005016911A1 (en) 2003-08-13 2005-02-24 Takeda Pharmaceutical Company Limited 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors
JP2007505121A (ja) 2003-09-08 2007-03-08 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
KR20120007079A (ko) 2003-10-15 2012-01-19 프로비오드룩 아게 글루타미닐 및 글루타메이트 사이클라제 이펙터의 용도
US20100099721A1 (en) * 2003-11-03 2010-04-22 Probiodrug Ag Novel compounds for the treatment of neurological disorders
US7667044B2 (en) 2003-11-03 2010-02-23 Probiodrug Ag Compounds for the treatment of neurological disorders
US20050137142A1 (en) * 2003-11-03 2005-06-23 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US20050171112A1 (en) * 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
EP1713780B1 (en) * 2004-02-05 2012-01-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
ATE541835T1 (de) * 2004-02-05 2012-02-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
KR20060124712A (ko) * 2004-02-20 2006-12-05 노파르티스 아게 신경퇴행 및 인지 장애를 치료하기 위한 ｄｐｐ ⅳ 억제제
CN102127053A (zh) * 2004-03-15 2011-07-20 武田药品工业株式会社 二肽基肽酶抑制剂
PL1765327T3 (pl) * 2004-06-17 2015-01-30 Cytokinetics Inc Związki, kompozycje i sposoby
FR2873368B1 (fr) * 2004-07-26 2008-01-04 Merck Sante Soc Par Actions Si Derives de guanidine et leurs utilisations en therapeutique
EP1828192B1 (en) 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DOP2006000008A (es) * 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
ES2477868T3 (es) 2005-04-22 2014-07-18 Alantos Pharmaceuticals Holding, Inc. Inhibidores de dipeptidil peptidasa-IV
CN101443357A (zh) * 2005-08-12 2009-05-27 先灵公司 Mcp1融合物
EP1942898B2 (en) 2005-09-14 2014-05-14 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors for treating diabetes
KR101368988B1 (ko) 2005-09-16 2014-02-28 다케다 야쿠힌 고교 가부시키가이샤 디펩티딜 펩티다제 억제제
ES2419007T3 (es) 2005-12-15 2013-08-19 Cytokinetics, Inc. Ciertas entidades químicas, composiciones y procedimientos
US7825120B2 (en) * 2005-12-15 2010-11-02 Cytokinetics, Inc. Certain substituted ((piperazin-1-ylmethyl)benzyl)ureas
JP2007169167A (ja) * 2005-12-19 2007-07-05 Shiseido Co Ltd Ｃｅ形成・成熟化剤、不全角化阻害剤、皮膚バリアー機能回復促進剤およびスキンケア用皮膚外用組成物
WO2007078839A2 (en) * 2005-12-19 2007-07-12 Cytokinetics, Inc. Compounds, compositions and methods
US7572614B2 (en) 2006-02-24 2009-08-11 Academia Sinica Crystal structure of soluble glutaminyl cyclase
SI1971862T1 (sl) 2006-04-11 2011-02-28 Arena Pharm Inc Postopki uporabe GPR119 receptorja za identificiranje spojin, uporabnih za povečanje kostne mase pri posamezniku
PE20071221A1 (es) 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
EA200802054A1 (ru) 2006-04-12 2009-04-28 Пробиодруг Аг Ингибиторы фермента
DK2073810T3 (da) * 2006-09-13 2011-10-31 Takeda Pharmaceutical Anvendelse af 2-6-(3-aminio-piperidin-l-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-l-ylmethyl-4-fluor-benzonitril til behandling af diabetes, cancer, autoimmune sygdomme og HIV infektion
US8324383B2 (en) * 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
US8889709B2 (en) 2006-09-21 2014-11-18 Probiodrug Ag Use of isoQC inhibitors in the treatment and prevention of inflammatory diseases or conditions
US9277737B2 (en) 2006-09-21 2016-03-08 Probiodrug Ag Mouse models carrying a knock-out mutation of the QPCTL-gene
EP2581449B1 (en) 2006-09-21 2016-09-14 Probiodrug AG Novel genes related to glutaminyl cyclase
DK2091945T3 (da) * 2006-11-09 2014-04-22 Probiodrug Ag Nye inhibitorer af glutaminylcyclase
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
WO2008055950A1 (en) * 2006-11-09 2008-05-15 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US8420684B2 (en) * 2006-11-09 2013-04-16 Probiodrug Ag Inhibitors of glutaminyl cyclase
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
US20080200567A1 (en) * 2007-01-19 2008-08-21 Probiodrug Ag In vivo screening models for treatment of alzheimer's disease and other qpct-related disorders
AU2008220785B2 (en) * 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
GB2447017A (en) * 2007-03-01 2008-09-03 Probiodrug Ag New use for inhibitors of glutaminyl peptide cyclotransferinase
EA201400366A1 (ru) * 2007-03-01 2014-08-29 Пробиодруг Аг Новое применение ингибиторов глутаминилциклазы
US7803810B2 (en) * 2007-03-09 2010-09-28 Probiodrug Ag Inhibitors
US8093236B2 (en) * 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
DK2160389T3 (da) * 2007-04-18 2014-06-23 Probiodrug Ag Thioxoquinazolinonderivater som glutaminylcyclaseinhibitorer
WO2008128985A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
JP5675343B2 (ja) * 2007-04-18 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としての尿素誘導体
DK2142515T3 (da) * 2007-04-18 2014-06-23 Probiodrug Ag Nitrovinyl-diaminderivater som glutaminyl-cyclase-inhibitorer
WO2008128983A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Cyano-guanidine derivatives as glutaminyl cyclase inhibitors
WO2008128981A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Nitrovinyl-diamine derivatives as glutaminyl cyclase inhibitors
EP2142536B1 (en) * 2007-04-20 2015-10-21 Probiodrug AG Aminopyrimidine derivatives as glutaminyl cyclase inhibitors
AU2008297070A1 (en) * 2007-09-12 2009-03-19 Probiodrug Ag Transgenic mice
CA2710494A1 (en) * 2008-01-14 2009-07-23 Probiodrug Ag Mouse models carrying a knock-out mutation of the glutaminyl cyclase gene
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
CA2731044C (en) * 2008-07-21 2020-07-14 Probiodrug Ag Diagnostic antibody assay
WO2010026209A1 (en) * 2008-09-04 2010-03-11 Probiodrug Ag Use of isoQC inhibitors
EP2344157B1 (en) * 2008-09-04 2016-05-25 Probiodrug AG Novel inhibitors
US20100144140A1 (en) * 2008-12-10 2010-06-10 Novellus Systems, Inc. Methods for depositing tungsten films having low resistivity for gapfill applications
US8486940B2 (en) 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
CA2789091A1 (en) 2010-02-18 2011-08-25 Probiodrug Ag Methods of diagnosing inflammatory diseases by determining pyroglutamate-modified mcp-1 and screening methods for inhibitors of glutaminyl cyclase
ES2586231T3 (es) 2010-03-03 2016-10-13 Probiodrug Ag Inhibidores de glutaminil ciclasa
CN102791704B (zh) 2010-03-10 2015-11-25 前体生物药物股份公司 谷氨酰胺酰环化酶(qc, ec 2.3.2.5)的杂环抑制剂
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
US8524217B2 (en) 2010-05-11 2013-09-03 Merck Sharp & Dohme Corp. MCP1-Ig fusion variants
WO2012022804A1 (en) 2010-08-19 2012-02-23 Probiodrug Ag Crystal structure of glutaminyl cyclase
EP2635675B1 (en) * 2010-11-02 2016-01-06 Probiodrug AG Crystal structure of isoglutaminyl cyclase
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
AU2013292519B2 (en) 2012-07-19 2017-12-07 Drexel University Sigma receptor ligands for modulating cellular protein homeostasis
CN107141266B (zh) * 2017-06-28 2019-04-09 佳木斯大学附属第一医院 一种用于治疗阿尔茨海默病的杂环化合物及其制备方法
DK3658141T3 (da) 2017-07-24 2023-02-06 Stichting Het Nederlands Kanker Inst Antoni Van Leeuwenhoek Ziekenhuis Behandling af patologiske tilstande ved direkte og indirekte målretning af Sirpalpha-CD47-interaktion
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
US11117870B2 (en) 2017-11-01 2021-09-14 Drexel University Compounds, compositions, and methods for treating diseases
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CN110590801B (zh) * 2019-09-05 2020-11-03 中国药科大学 谷氨酰胺酶小分子荧光探针及其制备方法和用途
CN118019737A (zh) 2021-06-24 2024-05-10 英矽智能科技知识产权有限公司 用于治疗疾病的β-内酰胺衍生物

Family Cites Families (233)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2961377A (en) 1957-08-05 1960-11-22 Us Vitamin Pharm Corp Oral anti-diabetic compositions and methods
US3174901A (en) 1963-01-31 1965-03-23 Jan Marcel Didier Aron Samuel Process for the oral treatment of diabetes
DE2009743A1 (de) 1970-03-03 1971-09-16 Farbenfabriken Bayer Ag, 5090 Leverkusen Substituierte Biguanide mit antihyperglykämischer Wirkung
US3879541A (en) 1970-03-03 1975-04-22 Bayer Ag Antihyperglycemic methods and compositions
US3960949A (en) 1971-04-02 1976-06-01 Schering Aktiengesellschaft 1,2-Biguanides
CH602612A5 (hr) 1974-10-11 1978-07-31 Hoffmann La Roche
JPS605593B2 (ja) 1981-03-20 1985-02-12 北興化学工業株式会社 イミダゾ−ル誘導体および農園芸用殺菌剤
JPS6137764A (ja) 1984-07-31 1986-02-22 Suntory Ltd 抗プロリルエンドペプチダ−ゼ活性を有する新規生理活性化合物
CA1309805C (en) 1985-04-16 1992-11-03 Naoki Higuchi Dipeptide derivative and synthesis and use thereof
DE3684633D1 (de) 1985-04-16 1992-05-07 Suntory Ltd Dipeptid-derivate von fettsaeure, verfahren zu ihrer herstellung, heilmittel, das sie enthaelt und anwendung.
JPH0623190B2 (ja) 1985-04-16 1994-03-30 サントリー株式会社 インヒビタ−活性を有するｎ−アシルピロリジン誘導体及びその製法並びに用途
JPS62114957A (ja) 1985-11-13 1987-05-26 Suntory Ltd プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジン誘導体およびその製法並びに用途
JPH0714878B2 (ja) 1985-11-14 1995-02-22 サントリー株式会社 ピロリジンアミドを有効成分とするプロリルエンドペプチダーゼ阻害剤
JPH0764834B2 (ja) 1985-11-29 1995-07-12 サントリー株式会社 プロリルエンドペプチダーゼ阻害活性を有する新規ピロリジンアミド誘導体およびその製法並びに用途
CA1320734C (en) 1986-02-04 1993-07-27 Suntory Limited Pyrrolidineamide derivative of acylamino acid and pharmaceutical composition containing the same
US5198458A (en) 1986-02-04 1993-03-30 Suntory Limited Pyrrolidineamide derivatives of acylamino acid and pharmaceutical composition containing the same
JPH08806B2 (ja) 1986-11-18 1996-01-10 サントリー株式会社 プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジンアミド誘導体
US5254550A (en) 1986-11-20 1993-10-19 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
ES2058089T3 (es) 1986-11-20 1994-11-01 Ono Pharmaceutical Co Un procedimiento para la preparacion de un nuevo derivado de prolinal.
JPS63162672A (ja) 1986-12-25 1988-07-06 Ono Pharmaceut Co Ltd 新規なプロリナ−ル誘導体、それらの製造方法およびそれらを含有する抗健忘症剤
JPH089591B2 (ja) 1986-12-29 1996-01-31 小野薬品工業株式会社 新規なプロリナール誘導体
ES2046195T3 (es) 1986-12-29 1994-02-01 Ono Pharmaceutical Co., Ltd. Un procedimiento para la preparacion de los derivados de prolinal.
US5262431A (en) 1986-12-29 1993-11-16 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
JP2528343B2 (ja) 1987-02-04 1996-08-28 小野薬品工業株式会社 新規なプロリナ―ル誘導体
EP0277588B1 (en) 1987-02-04 1993-03-24 Ono Pharmaceutical Co., Ltd. Prolinal derivatives
ES2052619T3 (es) 1987-02-23 1994-07-16 Ono Pharmaceutical Co Un procedimiento para la preparacion de los nuevos derivados de tiazolidina.
DE3712365A1 (de) 1987-04-11 1988-10-27 Hoechst Ag Neue 2-acylpyrrolidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel sowie deren verwendung
JPS6442465A (en) 1987-08-07 1989-02-14 Wakunaga Pharma Co Ltd N-acylprolylpyrrolidine derivative, production and use thereof
US4857524A (en) 1987-08-08 1989-08-15 Kissei Pharmaceutical Co., Ltd. Thiazolidine compounds and therapeutic method
JP2649237B2 (ja) 1988-03-07 1997-09-03 キッセイ薬品工業 株式会社 チアゾリジン誘導体
JP2515558B2 (ja) 1987-09-10 1996-07-10 株式会社ヤクルト本社 新規なペプチドおよびそれを有効成分とする抗健忘症剤
US4935493A (en) 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
JPH0742309B2 (ja) 1987-11-30 1995-05-10 キッセイ薬品工業株式会社 チアゾリジン誘導体
JPH01250370A (ja) 1987-12-23 1989-10-05 Zeria Pharmaceut Co Ltd 新規アミノ酸イミド誘導体、製法ならびに用途
US5053414A (en) 1988-04-08 1991-10-01 Ono Pharmaceutical Co., Ltd. Heterocyclic compounds
US5328899A (en) 1988-07-15 1994-07-12 The Salk Institute For Biological Studies NPY peptide analogs
ZA896374B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y antagonists
ZA896376B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y agonists
JP2531989B2 (ja) 1988-09-14 1996-09-04 吉富製薬株式会社 ピリジン化合物
CA2004028C (en) 1988-12-08 1998-09-22 Motoki Torizuka Condensed benzene derivative
US5433955A (en) 1989-01-23 1995-07-18 Akzo N.V. Site specific in vivo activation of therapeutic drugs
JPH02207070A (ja) 1989-02-07 1990-08-16 Zeria Pharmaceut Co Ltd アミノ酸イミド誘導体、それを含有する医薬及び該化合物の製造中間体
JP2691442B2 (ja) 1989-02-20 1997-12-17 株式会社ヤクルト本社 新規なプロリン誘導体
EP0419683A4 (en) 1989-04-13 1992-03-11 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
JPH0331298A (ja) 1989-06-28 1991-02-12 Ajinomoto Co Inc プロリルエンドペプチターゼ阻害ペプチド
JPH0776211B2 (ja) 1989-07-24 1995-08-16 キッセイ薬品工業株式会社 ピログルタミン酸誘導体
JPH082791B2 (ja) 1989-07-24 1996-01-17 キッセイ薬品工業株式会社 健忘症治療剤
JPH082869B2 (ja) 1989-07-24 1996-01-17 キッセイ薬品工業株式会社 健忘症治療剤およびプロリン誘導体
JPH07103101B2 (ja) 1989-07-24 1995-11-08 キッセイ薬品工業株式会社 ピログルタミン酸誘導体
DD296075A5 (de) 1989-08-07 1991-11-21 Martin-Luther-Universitaet Halle-Wittenberg,De Verfahren zur herstellung neuer inhibitoren der dipeptidyl peptidase iv
DE3939797A1 (de) 1989-12-01 1991-06-06 Basf Ag Neue vom neuropeptid y abgeleitete peptide
EP0512042B1 (en) 1990-01-24 1998-04-08 BUCKLEY, Douglas I. Glp-1 analogs useful for diabetes treatment
JPH04211648A (ja) 1990-07-27 1992-08-03 Nippon Kayaku Co Ltd ケト酸アミド誘導体
JPH03255080A (ja) 1990-03-05 1991-11-13 Yoshitomi Pharmaceut Ind Ltd ベンゼン化合物
US5073549A (en) 1990-03-22 1991-12-17 Bristol-Myers Squibb Company BU-4164E - A and B, prolyl endopeptidase inhibitors and their methods of use
US4999349A (en) 1990-03-22 1991-03-12 Bristol-Myers Squibb Co. BU-4164E - A and B, prolyl endopeptidase inhibitors
US5462928A (en) 1990-04-14 1995-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
DE69124371T2 (de) 1990-04-14 1997-06-12 New England Medical Center Inc Typ-iv-dipeptidyl-aminopeptidase-inhibitoren
JPH049367A (ja) 1990-04-26 1992-01-14 Zeria Pharmaceut Co Ltd アリールアルカノイル誘導体，該化合物の製造中間体及びそれらを含有する医薬
US5077409A (en) * 1990-05-04 1991-12-31 American Cyanamid Company Method of preparing bis-aryl amide and urea antagonists of platelet activating factor
US6517824B1 (en) 1990-05-14 2003-02-11 University Of Medicine & Denistry Of New Jersey Polymer compositions comprising antifibrotic agents, and methods of treatment, pharmaceutical compositions, and methods of preparation therefor
WO1991017767A1 (en) 1990-05-21 1991-11-28 New England Medical Center Hospitals, Inc. Method of treating inhibition of dipeptidyl aminopeptidase type iv
EP0536163A1 (en) 1990-06-04 1993-04-14 Pfizer Inc. Aromatic pyrrolidine and thiazolidine amides
WO1991018877A1 (fr) 1990-06-07 1991-12-12 Zeria Pharmaceutical Co., Ltd. Nouveau derive d'arylalcanoylamine et medicament contenant ce derive
JPH07108897B2 (ja) 1990-07-27 1995-11-22 日本たばこ産業株式会社 新規なプロリン誘導体
EP0468469A2 (en) 1990-07-27 1992-01-29 Japan Tobacco Inc. Proline derivatives
US5506256A (en) 1990-07-27 1996-04-09 Yoshitomi Pharmaceutical Industries, Ltd. Proline derivatives possessing prolyl endopeptidase-inhibitory activity
JPH05186498A (ja) 1991-12-27 1993-07-27 Japan Tobacco Inc プロリン誘導体
JPH04235162A (ja) 1990-08-09 1992-08-24 Zeria Pharmaceut Co Ltd 新規コハク酸アミド誘導体およびそれを含有する医薬
JPH04208299A (ja) 1990-11-30 1992-07-29 Ajinomoto Co Inc プロリルエンドペプチターゼ阻害ペプチド
JPH0819154B2 (ja) 1991-03-14 1996-02-28 江崎グリコ株式会社 ジペプチジルカルボキシペプチダーゼを阻害するペプチド
JPH04334357A (ja) 1991-05-02 1992-11-20 Fujirebio Inc 酵素阻害作用を有するアシル誘導体
EP0553357B1 (en) 1991-06-20 1997-09-10 Snow Brand Milk Products Co., Ltd. Novel prolyl endopeptidase inhibitors sna-115 and sna-115t, production thereof, and strain which produces said inhibitors
JP3010795B2 (ja) 1991-07-04 2000-02-21 不二製油株式会社 ペプチドの苦味除去方法
GB9115740D0 (en) * 1991-07-20 1991-09-04 Smithkline Beecham Plc Medicaments
CA2121369C (en) 1991-10-22 2003-04-29 William W. Bachovchin Inhibitors of dipeptidyl-aminopeptidase type iv
EP0672054A4 (en) 1991-12-19 1996-02-07 Garvan Inst Med Res NEW MOLECULE INHIBITING THE BIOLOGICAL FUNCTION OF THE TYROSINE NEUROPEPTIDE.
JPH05301826A (ja) 1991-12-24 1993-11-16 Snow Brand Milk Prod Co Ltd プロリルエンドペプチダーゼ阻害剤
JPH05201970A (ja) 1992-01-24 1993-08-10 Japan Tobacco Inc 新規プロリン誘導体
EP0633882A1 (en) 1992-04-01 1995-01-18 The University Of Toledo 4- 4'-piperidinyl or 3'-pirrolidinyl] substituted imidazoles as h3-receptor antagonists and therapeutic uses thereof
JP3318622B2 (ja) 1992-05-27 2002-08-26 独立行政法人産業技術総合研究所 プロリルエンドペプチダーゼ阻害剤
GB9213215D0 (en) 1992-06-20 1992-08-05 Wellcome Found Peptides
IL106998A0 (en) 1992-09-17 1993-12-28 Univ Florida Brain-enhanced delivery of neuroactive peptides by sequential metabolism
JPH06116284A (ja) 1992-10-02 1994-04-26 Yamanouchi Pharmaceut Co Ltd 新規ペプチド
FR2696740B1 (fr) 1992-10-13 1994-12-30 Dospharma Sa Dérivés prodrogués de la diméthylbiguanide et applications comme médicaments.
EP0670309A1 (en) 1992-11-20 1995-09-06 Japan Tobacco Inc. Compound with prolyl endopeptidase inhibitor activity and pharmaceutical use thereof
JPH06192298A (ja) 1992-12-24 1994-07-12 Mitsui Toatsu Chem Inc 新規機能性ペプチド
DE4326465A1 (de) 1993-01-20 1995-02-09 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JPH06234693A (ja) 1993-02-09 1994-08-23 Snow Brand Milk Prod Co Ltd 新規イソテトラセノン系物質及びその製造法
FR2701480B1 (fr) 1993-02-15 1995-05-24 Sanofi Elf Composés à groupe sulfamoyle et amidino, leur procédé de préparation et les compositions pharmaceutiques les contenant.
FR2703050B1 (fr) 1993-03-24 1995-04-28 Adir Nouveaux dérivés bicycliques azotés, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
JPH11501281A (ja) 1993-06-18 1999-02-02 ユニバーシティ オブ シンシナティ 神経ペプチドｙアンタゴニスト及びアゴニスト
WO1995001352A1 (fr) 1993-06-30 1995-01-12 Zeria Pharmaceutical Co., Ltd. Derive de thiazolidine et medicament le contenant
WO1995003277A1 (fr) 1993-07-23 1995-02-02 Zaidan Hojin Biseibutsu Kagaku Kenkyukai Nouveau derive de pyrrolidine
WO1995011689A1 (en) 1993-10-29 1995-05-04 Trustees Of Tufts College Use of inhibitors of dipeptidyl-aminopeptidase to block entry of hiv into cells
HUT74687A (en) 1993-12-02 1997-01-28 Merrell Pharma Inc Pyrrole and thiazolidine derivatives of prolyl endopeptidase inhibitor activity and pharmaceutical compositions containing the same
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
CA2137206A1 (en) 1993-12-09 1995-06-10 John A. Galloway Glucagon-like insulinotropic peptides, compositions and methods
US5705483A (en) 1993-12-09 1998-01-06 Eli Lilly And Company Glucagon-like insulinotropic peptides, compositions and methods
AU1891295A (en) 1994-02-22 1995-09-04 Knoll Aktiengesellschaft Use of 1-(arylalkylaminoalkyl) imidazoles for treating neurological damage
JPH07267988A (ja) 1994-03-31 1995-10-17 Yamanouchi Pharmaceut Co Ltd 新規ペプチド
US5435493A (en) * 1994-04-21 1995-07-25 J. Houle Et Fils Inc. Manure distributor with atop discharge pipes and manure spreader incorporating the same
US5543396A (en) 1994-04-28 1996-08-06 Georgia Tech Research Corp. Proline phosphonate derivatives
US5552426A (en) 1994-04-29 1996-09-03 Eli Lilly And Company Methods for treating a physiological disorder associated with β-amyloid peptide
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
US5663192A (en) 1994-10-20 1997-09-02 Eli Lilly And Company Heterocyclic neuropeptide Y receptor antagonists
US6562862B1 (en) 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
EP0895781A3 (en) 1994-10-20 1999-07-07 Eli Lilly And Company Use of benzofurans, benzothiophenes or indoles for the manufacture of a medicament for the treatment of conditions associated with an excess of tachykinins
GB9500601D0 (en) 1995-01-12 1995-03-01 Wellcome Found Modified peptides
US5614379A (en) 1995-04-26 1997-03-25 Eli Lilly And Company Process for preparing anti-obesity protein
US5552411A (en) 1995-05-26 1996-09-03 Warner-Lambert Company Sulfonylquinolines as central nervous system and cardiovascular agents
US6448282B1 (en) 1995-05-30 2002-09-10 Gliatech, Inc. 1H-4(5)-substituted imidazole derivatives
US5554621A (en) 1995-06-07 1996-09-10 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: nitrogen heterocyclic derivatives
IL117997A0 (en) 1995-06-07 1996-10-31 Pfizer Neuropeptide Y1 specific ligands
US5668151A (en) 1995-06-07 1997-09-16 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: piperidine derivatives
US5635503A (en) 1995-06-07 1997-06-03 Bristol-Myers Squibb Company Dihydropyridine npy antagonists: piperazine derivatives
JP3727383B2 (ja) 1995-07-31 2005-12-14 月桂冠株式会社 プロリルエンドペプチダーゼ阻害剤
CZ132897A3 (en) 1995-09-01 1997-11-12 Lilly Co Eli Antagonist of indolylneuropeptide y receptor
DE19544686A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19544685A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19544687A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
WO1997020822A1 (en) 1995-12-01 1997-06-12 Novartis Ag Quinazolin-2,4-diazirines as npy receptor antagonist
WO1997020821A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
AU7692996A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Receptor antagonists
WO1997020820A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl compounds
JPH09157253A (ja) 1995-12-12 1997-06-17 Yamanouchi Pharmaceut Co Ltd 新規アミノ酸誘導体
CA2242579A1 (en) 1996-01-09 1997-07-17 Eli Lilly And Company Benzimidzolyl neuropeptide y receptor antagonists
US5662723A (en) 1996-03-22 1997-09-02 Libbey Glass Inc. Apparatus and method for forming a decorative pattern on glassware having an edge
AU1940897A (en) 1996-03-28 1997-10-17 Shionogi & Co., Ltd. Lymph-absorbable imidazole derivatives
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
AU2764797A (en) 1996-05-14 1997-12-05 Novo Nordisk A/S Somatostatin agonists and antagonists
AU3224997A (en) 1996-05-29 1998-01-05 Prototek, Inc Prodrugs of thalidomide and methods for using same as modulators of t-cell function
WO1997046250A1 (en) 1996-06-04 1997-12-11 Synaptic Pharmaceutical Corporation Methods of modifying feeding behavior, compounds useful in such methods, and dna encoding a hypothalamic atypical neuropeptide y/peptide yy receptor (y5)
ES2186907T3 (es) 1996-07-23 2003-05-16 Neurogen Corp Ciertos derivados de bencilamina sustituidos; una nueva clase de ligandos especificos del neuropeptido y1.
DE69721541T2 (de) 1996-07-23 2004-03-18 Neurogen Corp., Branford Einige amido-und amino-substituierte benzylaminderivate: eine neue klasse von neuropeptid y1 spezifischen liganden
CA2260982A1 (en) 1996-07-23 1998-01-29 Neurogen Corporation Certain substituted benzylamine derivatives; a new class of neuropeptide-y1 specific ligands
JP2001502296A (ja) 1996-08-23 2001-02-20 アラネックス コーポレーション ニューロペプチド―ｙリガンド
US6006753A (en) 1996-08-30 1999-12-28 Eli Lilly And Company Use of GLP-1 or analogs to abolish catabolic changes after surgery
JP3880664B2 (ja) 1996-09-04 2007-02-14 月桂冠株式会社 プロリルエンドペプチダーゼ阻害ペプチド
US5827898A (en) 1996-10-07 1998-10-27 Shaman Pharmaceuticals, Inc. Use of bisphenolic compounds to treat type II diabetes
FR2754709B1 (fr) 1996-10-23 1999-03-05 Sanofi Sa Composition cosmetique contenant un antagoniste des recepteurs du neuropeptide gamma et alpha 2 antagonistes susceptibles d'etre incorpores dans une telle composition
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
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
AR016751A1 (es) 1996-11-22 2001-08-01 Athena Neurosciences Inc Metodo para inhibir la liberacion del peptido beta-amiloide en una celula, composicion farmaceutica y compuestos utiles en dicho metodo
SE9703414D0 (sv) 1997-09-23 1997-09-23 Astra Ab New compounds
CA2307597A1 (en) 1997-10-21 1999-04-29 Cambridge Neuroscience, Inc. Pharmaceutically active compounds and methods of use
EP2823812A1 (en) 1998-02-02 2015-01-14 Trustees Of Tufts College Dipeptidylpeptidase IV inhibitors for use in the treatment of Type II diabetes
US5994379A (en) * 1998-02-13 1999-11-30 Merck Frosst Canada, Inc. Bisaryl COX-2 inhibiting compounds, compositions and methods of use
DE59907545D1 (de) * 1998-02-13 2003-12-04 Schwabe Willmar Gmbh & Co Stabile hyperforin-salze, verfahren zu ihrer herstellung und verwendung zur therapie der alzheimerschen krankheit
EP1062222A1 (en) 1998-03-09 2000-12-27 Fondatech Benelux N.V. Serine peptidase modulators
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
EP1084129B1 (en) 1998-06-05 2003-01-22 Point Therapeutics, Inc. Cyclic boroproline compounds
JP2002517500A (ja) 1998-06-12 2002-06-18 ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス β−カルボリン化合物
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
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
WO2000001849A1 (en) 1998-07-02 2000-01-13 Invitro Diagnostics, Inc. Methods, compositions and apparatus for making nucleic acid molecules having a selected affinity to a target molecule
DE69911975T2 (de) 1998-07-31 2004-09-09 Novo Nordisk A/S In-vitro stimulation von beta zellen vermehrung
DE19834610A1 (de) 1998-07-31 2000-02-24 Probiodrug Ges Fuer Arzneim Mechanismus-orientierte Inhibitoren der Dipeptidyl Peptidase I
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
WO2000010549A1 (en) 1998-08-21 2000-03-02 Point Therapeutics, Inc. Regulation of substrate activity
WO2000030674A1 (en) 1998-11-26 2000-06-02 Ferring Bv Neuropeptide y y4 agents in the treatment of reproductive disorders
WO2000053171A1 (en) 1999-03-05 2000-09-14 Molteni L. E C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv
US6211182B1 (en) 1999-03-08 2001-04-03 Schering Corporation Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms
PT1171465E (pt) 1999-03-29 2004-12-31 Uutech Ltd Analogos de petido inibidor gastrico e sua utilizacao para o tratamento de diabetes
US6121311A (en) 1999-04-28 2000-09-19 Japan Tobacco Inc. Method for treating cocainism
EP1177172A1 (en) 1999-05-05 2002-02-06 Ortho-McNeil Pharmaceutical, Inc. 3a,4,5,9b-TETRAHYDRO-1H-BENZ e]INDOL-2-YL AMINE-DERIVED NEUROPEPTIDE Y RECEPTORS LIGANDS USEFUL IN THE TREATMENT OF OBESITY AND OTHER DISORDERS
FR2793638A1 (fr) 1999-05-12 2000-11-17 Ascom Monetel Sa Systeme d'alimentation a partir d'une ligne telephonique
JP3148739B2 (ja) 1999-05-19 2001-03-26 ドーマー株式会社 プロリルエンドペプチダーゼ阻害剤
US6172081B1 (en) 1999-06-24 2001-01-09 Novartis Ag Tetrahydroisoquinoline 3-carboxamide derivatives
US6110949A (en) 1999-06-24 2000-08-29 Novartis Ag N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6107317A (en) 1999-06-24 2000-08-22 Novartis Ag N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
GB9917909D0 (en) 1999-07-31 1999-09-29 Synphar Lab Inc Cysteine protease inhibitors
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
AU1916401A (en) 1999-11-12 2001-06-06 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
WO2001055105A1 (en) 2000-01-24 2001-08-02 Novo Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
US7064145B2 (en) 2000-02-25 2006-06-20 Novo Nordisk A/S Inhibition of beta cell degeneration
DE60042585D1 (de) 2000-02-29 2009-09-03 Univ Firenze 3-Aza-6,8-dioxabicycloÄ3.2.1Üoctane und Analoga sowie diese enthaltende kombinatorische Bibliotheken
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
PT2055302E (pt) 2000-03-31 2014-12-03 Royalty Pharma Collection Trust Processo para a melhoria da sinalização de ilhéus em diabetes mellitus e para a sua prevenção
US6605589B1 (en) 2000-03-31 2003-08-12 Parker Hughes Institute Cathepsin inhibitors in cancer treatment
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
AU2001268958B2 (en) 2000-07-04 2006-03-09 Novo Nordisk A/S Heterocyclic compounds, which are inhibitors of the enzyme dpp-iv
US6794405B2 (en) * 2000-08-17 2004-09-21 Merck & Co., Inc. Alicyclic imidazoles as H3 agents
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
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
US20030013177A1 (en) 2001-05-23 2003-01-16 Ebens Allen J. Polynucleotides encoding insect glutaminyl cyclase and uses thereof
ES2257555T3 (es) 2001-06-20 2006-08-01 MERCK & CO., INC. Inhibidores de dipeptidilpeptidasa para el tratamiento de la diabetes.
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
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
EP1399471B1 (en) 2001-06-27 2008-01-30 Probiodrug AG Use of dipeptidyl peptidase iv inhibitors as therapeutics for neurological disorders
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
DE60221983T2 (de) 2001-06-27 2008-05-15 Smithkline Beecham Corp. Fluorpyrrolidine als dipeptidyl-peptidase inhibitoren
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
EP1399420B1 (en) 2001-06-27 2007-12-05 SmithKline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
BR0210644A (pt) 2001-06-27 2004-07-20 Smithkline Beecham Corp Composto, formulação farmacêutica, método para inibir uma protease que cliva pós prolina/alanina, método para o tratamento ou profilaxia de distúrbios, e, uso do composto
JP2004530729A (ja) 2001-06-27 2004-10-07 プロバイオドラッグ アーゲー ジペプチジルペプチダーゼｉｖ触媒作用の拮抗調節に有用なペプチド構造
WO2003004496A1 (en) 2001-07-03 2003-01-16 Novo Nordisk A/S Dpp-iv-inhibiting purine derivatives for the treatment of diabetes
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
CN100341862C (zh) 2001-09-14 2007-10-10 三菱制药株式会社 噻唑烷衍生物及其医药用途
JP2005509603A (ja) 2001-09-19 2005-04-14 ノボ　ノルディスク　アクティーゼルスカブ Ｄｐｐ−ｉｖ酵素の阻害剤であるヘテロ環化合物
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
US7727964B2 (en) 2001-11-26 2010-06-01 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
WO2003057144A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
US6727261B2 (en) 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
JP4359146B2 (ja) 2002-02-13 2009-11-04 エフ．ホフマン−ラ ロシュ アーゲー 新規なピリジン−およびピリミジン−誘導体
BR0307576A (pt) 2002-02-13 2005-01-11 Hoffmann La Roche Compostos; processo para a fabricação de compostos; composições farmacêuticas; método para o tratamento e/ou profilaxia de doenças associadas com o dpp iv; e uso de compostos
US6858613B2 (en) * 2002-02-19 2005-02-22 Pfizer Inc. Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
ATE373660T1 (de) 2002-03-25 2007-10-15 Merck & Co Inc Heterocyclische beta-aminoverbindungen als inhibitoren der dipeptidylpeptidase zur behandlung bzw. prävention von diabetes
WO2003101958A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
WO2003101449A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
RU2297418C9 (ru) 2002-06-06 2009-01-27 Эйсай Ко., Лтд. Новые конденсированные производные имидазола, ингибитор дипептидилпептидазы iv, фармацевтическая композиция, способ лечения и применение на их основе
WO2004007446A1 (ja) 2002-07-10 2004-01-22 Yamanouchi Pharmaceutical Co., Ltd. 新規なアゼチジン誘導体又はその塩
CA2490818A1 (en) 2002-07-15 2004-01-22 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
PL216134B1 (pl) 2002-08-21 2014-03-31 Boehringer Ingelheim Pharma 8-[3-aminopiperydyn-1-ylo]-ksantyny, kompozycja farmaceutyczna je zawierająca, zastosowanie związków oraz sposób ich wytwarzania
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
DE10238477A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
EP1560811B9 (en) 2002-09-19 2008-03-05 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
CA2521907A1 (en) * 2003-04-10 2004-10-21 Pfizer Inc. Bicyclic compounds as nr2b receptor antagonists
DE602004026289D1 (de) 2003-05-05 2010-05-12 Probiodrug Ag Glutaminylcyclase-hemmer
WO2004099134A2 (en) 2003-05-05 2004-11-18 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
KR20120007079A (ko) 2003-10-15 2012-01-19 프로비오드룩 아게 글루타미닐 및 글루타메이트 사이클라제 이펙터의 용도
US20050137142A1 (en) 2003-11-03 2005-06-23 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US20050171112A1 (en) 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
EP1713780B1 (en) 2004-02-05 2012-01-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase

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US7655684B2 (en) 2010-02-02
US7371871B2 (en) 2008-05-13
EP1620091B1 (en) 2010-03-31
ATE462432T1 (de) 2010-04-15
US20080153892A1 (en) 2008-06-26
WO2004098591A3 (en) 2005-03-31
WO2004098591A2 (en) 2004-11-18
EP1620091A2 (en) 2006-02-01
US20040224875A1 (en) 2004-11-11
JP4806628B2 (ja) 2011-11-02
DE602004026289D1 (de) 2010-05-12

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