ATE554085T1 - Neue inhibitoren von glutaminylcyclase - Google Patents

Neue inhibitoren von glutaminylcyclase

Info

Publication number
ATE554085T1
ATE554085T1 AT07847471T AT07847471T ATE554085T1 AT E554085 T1 ATE554085 T1 AT E554085T1 AT 07847471 T AT07847471 T AT 07847471T AT 07847471 T AT07847471 T AT 07847471T AT E554085 T1 ATE554085 T1 AT E554085T1
Authority
AT
Austria
Prior art keywords
alkyl
carbocyclyl
heteroaryl
glutaminyl cyclase
new inhibitors
Prior art date
Application number
AT07847471T
Other languages
English (en)
Inventor
Mirko Buchholz
Andre J Niestroj
Ulrich Heiser
Daniel Ramsbeck
Stephan Schilling
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
Application granted granted Critical
Publication of ATE554085T1 publication Critical patent/ATE554085T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
AT07847471T 2006-11-30 2007-11-28 Neue inhibitoren von glutaminylcyclase ATE554085T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US86784506P 2006-11-30 2006-11-30
PCT/EP2007/062953 WO2008065141A1 (en) 2006-11-30 2007-11-28 Novel inhibitors of glutaminyl cyclase

Publications (1)

Publication Number Publication Date
ATE554085T1 true ATE554085T1 (de) 2012-05-15

Family

ID=39133797

Family Applications (1)

Application Number Title Priority Date Filing Date
AT07847471T ATE554085T1 (de) 2006-11-30 2007-11-28 Neue inhibitoren von glutaminylcyclase

Country Status (7)

Country Link
US (1) US9126987B2 (de)
EP (1) EP2091948B1 (de)
JP (1) JP5523107B2 (de)
AT (1) ATE554085T1 (de)
DK (1) DK2091948T3 (de)
SI (1) SI2091948T1 (de)
WO (1) WO2008065141A1 (de)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008055950A1 (en) * 2006-11-09 2008-05-15 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
WO2008055945A1 (en) * 2006-11-09 2008-05-15 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
US8420684B2 (en) * 2006-11-09 2013-04-16 Probiodrug Ag Inhibitors of glutaminyl cyclase
JP5612860B2 (ja) * 2007-03-09 2014-10-22 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イミダゾ［１，５−ａ］ピリジン誘導体
WO2008128986A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Urea derivatives as glutaminyl cyclase inhibitors
EP2142515B1 (de) * 2007-04-18 2014-03-26 Probiodrug AG Nitrovinyl-diamin derivate als glutaminyl cyclase hemmer
DK2142513T3 (da) * 2007-04-18 2014-06-10 Probiodrug Ag Nitrovinyl-diamin-derivater som glutaminyl-cyclase-inhibitorer
DK2142514T3 (da) * 2007-04-18 2015-03-23 Probiodrug Ag Thioureaderivater som glutaminylcyclase-inhibitorer
WO2008128982A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Thioxoquinazolinone derivatives as glutaminyl cyclase inhibitors
DK2160380T3 (da) * 2007-04-18 2014-06-30 Probiodrug Ag Cyano-guanidin derivater som glutaminyl cyclase inhibitorer
EP2142536B1 (de) * 2007-04-20 2015-10-21 Probiodrug AG Aminopyrimidinderivate als glutaminylcyclaseinhibitoren
WO2009034158A2 (en) * 2007-09-12 2009-03-19 Probiodrug Ag Transgenic mice
NZ586665A (en) * 2008-01-14 2011-12-22 Probiodrug Ag MOUSE MODELS CARRYING A KNOCK-OUT MUTATION OF THE GLUTAMINYL CYCLASE GENE (Qpct)
AU2009273387B9 (en) 2008-07-21 2015-06-11 Vivoryon Therapeutics N.V. Diagnostic antibody assay
CN102203124A (zh) * 2008-07-25 2011-09-28 雅培制药有限公司 淀粉状蛋白β肽类似物，其寡聚物，用于制备的方法以及包括所述类似物或寡聚物的组合物，及其用途
AU2010294214B2 (en) 2009-09-11 2015-05-07 Vivoryon Therapeutics N.V. Heterocylcic derivatives as inhibitors of glutaminyl cyclase
WO2011076854A1 (en) 2009-12-22 2011-06-30 Probiodrug Ag CLEAVAGE OF β-AMYLOID PRECURSOR PROTEIN
JP2013519891A (ja) 2010-02-18 2013-05-30 プロビオドルグ エージー ピログルタミン酸修飾ｍｃｐ−１を決定することにより炎症性疾患を診断する方法及びグルタミニルシクラーゼの阻害剤のスクリーニング方法
JP6026284B2 (ja) * 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
AU2011226074B2 (en) 2010-03-10 2015-01-22 Vivoryon Therapeutics N.V. Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5)
EP2560953B1 (de) 2010-04-21 2016-01-06 Probiodrug AG Hemmer der glutaminylzyklase
CN101914094B (zh) * 2010-07-29 2012-08-22 南京大学 1,3,4-噁二唑衍生物及其制法与在制备抗肿瘤药物中的应用
WO2012022804A1 (en) 2010-08-19 2012-02-23 Probiodrug Ag Crystal structure of glutaminyl cyclase
JP6050264B2 (ja) 2011-03-16 2016-12-21 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
JP6220675B2 (ja) 2011-03-16 2017-11-01 プロビオドルグ エージー 診断用抗体アッセイ
US20170363645A1 (en) 2014-12-19 2017-12-21 Probiodrug Ag Novel Method for the Detection of pGlu-Abeta Peptides
CN105384692B (zh) * 2015-10-26 2018-06-29 深圳大学 一种谷氨酰胺酰基环化酶抑制剂
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
EP3521308B1 (de) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanisierte und deimmunisierte antikörper
CN111320617A (zh) * 2018-12-17 2020-06-23 华中科技大学 苯基噁二唑类衍生物及其制备方法与应用
CN111362930B (zh) * 2020-04-15 2023-02-03 安徽医科大学 一种1，2，4-噁二唑-吡啶类化合物及其应用

Family Cites Families (466)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5736816A (ja) 1980-08-14 1982-02-27 Toshiba Corp Chodendokoirunoseizohoho
JPS57192573A (en) 1981-05-25 1982-11-26 Hochiki Co Fire fighting agent
JPS60165712A (ja) 1984-02-08 1985-08-28 パイオニア株式会社 可変調整部品の自動調整方法
JPS6126111A (ja) 1984-07-16 1986-02-05 Shin Meiwa Ind Co Ltd 産業用ロボツト
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
JPS6152021A (ja) 1984-08-22 1986-03-14 Fujitsu Ltd スケルチ回路
JPS6172439A (ja) 1984-09-18 1986-04-14 Sanyo Electric Co Ltd デ−タ転送方式
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
EP0201743B1 (de) 1985-04-16 1992-04-01 Suntory Limited Dipeptid-Derivate von Fettsäure, Verfahren zu ihrer Herstellung, Heilmittel, das sie enthält und Anwendung
CA1309805C (en) 1985-04-16 1992-11-03 Naoki Higuchi Dipeptide derivative and synthesis and use thereof
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
JPS6386485A (ja) 1986-09-30 1988-04-16 Agency Of Ind Science & Technol トンネル型ジヨセフソン接合素子
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
EP0268190B1 (de) 1986-11-20 1993-06-16 Ono Pharmaceutical Co., Ltd. Prolinalderivate
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
ATE84787T1 (de) 1986-12-29 1993-02-15 Ono Pharmaceutical Co Prolin-derivate.
US5262431A (en) 1986-12-29 1993-11-16 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
DE3879522T2 (de) 1987-02-04 1993-09-02 Ono Pharmaceutical Co Prolinalderivate.
EP0461677B1 (de) 1987-02-23 1997-04-16 Ono Pharmaceutical Co., Ltd. Thiazolidin-Derivate
JPS6442465A (en) 1987-08-07 1989-02-14 Wakunaga Pharma Co Ltd N-acylprolylpyrrolidine derivative, production and use thereof
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
US4857524A (en) 1987-08-08 1989-08-15 Kissei Pharmaceutical Co., Ltd. Thiazolidine compounds and therapeutic method
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
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
ZA896376B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y agonists
ZA896374B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y antagonists
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
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
WO1990012005A1 (en) 1989-04-13 1990-10-18 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
DE3939797A1 (de) 1989-12-01 1991-06-06 Basf Ag Neue vom neuropeptid y abgeleitete peptide
US4985560A (en) 1990-01-12 1991-01-15 American Home Products Corporation Pyridazino(4,5-b)indolizines
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
US4999349A (en) 1990-03-22 1991-03-12 Bristol-Myers Squibb Co. BU-4164E - A and B, prolyl endopeptidase inhibitors
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
JP2511605B2 (ja) 1990-06-04 1996-07-03 ファイザー・インコーポレーテッド 芳香性ピロリジンおよびチアゾリヂンアミド類
DK0536399T3 (da) 1990-06-07 1996-06-03 Zeria Pharm Co Ltd Hidtil ukendt arylalkanonylaminderivat og lægemiddel indeholdende samme
EP0468469A2 (de) 1990-07-27 1992-01-29 Japan Tobacco Inc. Prolinderivate
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
US5104880A (en) 1991-05-01 1992-04-14 Mayo Foundation For Medical Education And Research Huperzine a analogs as acetylcholinesterase inhibitors
WO1992021333A2 (en) 1991-05-24 1992-12-10 Pharmavene, Inc. Treatment of drug withdrawal symptoms and drug craving with type b monoamine oxidase inhibitors
EP0553357B1 (de) 1991-06-20 1997-09-10 Snow Brand Milk Products Co., Ltd. Neuartige prolyl-endopeptidase-inhibitoren sna-115 und sna-115t, ihre herstellung, und hierbei verwendete stämme
WO1993003034A1 (en) 1991-07-29 1993-02-18 Warner-Lambert Company Quinazoline derivatives as acetylcholinesterase inhibitors
WO1993012139A1 (en) 1991-12-19 1993-06-24 Garvan Institute Of Medical Research A novel molecule which inhibits neuropeptide tyrosine biological function
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
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
GB9212308D0 (en) 1992-06-10 1992-07-22 Ici Plc Therapeutic compositions
GB9213215D0 (en) 1992-06-20 1992-08-05 Wellcome Found Peptides
JPH06116284A (ja) 1992-10-02 1994-04-26 Yamanouchi Pharmaceut Co Ltd 新規ペプチド
CA2146333A1 (en) 1992-10-05 1994-04-14 Tomio Kimura Pyrimidine compound
US5260286A (en) 1992-10-16 1993-11-09 Japan Tobacco, Inc. 2-piperidinecarboxylic acid derivatives useful as NMDA receptor antagonists
CA2149892C (en) 1992-11-20 1998-12-08 Koji Kobayashi Compound having prolyl endopeptidase inhibitory activity and pharmaceutical use thereof
US5354758A (en) 1992-12-16 1994-10-11 Japan Tobacco Inc. Benzomorphans useful as NMDA receptor antagonists
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.
EP0611769A1 (de) 1993-02-16 1994-08-24 Merrell Dow Pharmaceuticals Inc. Silytierte acetylcholinesterase Inhibitoren
WO1994020476A1 (en) 1993-03-02 1994-09-15 Fujisawa Pharmaceutical Co., Ltd. Novel heterocyclic compound
FR2702150B1 (fr) 1993-03-03 1995-04-07 Rhone Poulenc Rorer Sa Application de dérivés de 2H-1,2-4-benzothiadiazine-3(4H)-one-1,1-dioxyde comme antagonistes non compétitifs du récepteur NMDA.
FR2703050B1 (fr) 1993-03-24 1995-04-28 Adir Nouveaux dérivés bicycliques azotés, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
EP0627400A1 (de) 1993-06-04 1994-12-07 Merrell Dow Pharmaceuticals Inc. Aromatische Inhibitoren von Acetylcholinesterase
EP0707490A1 (de) 1993-06-18 1996-04-24 University Of Cincinnati Antagonisten und agonisten des neuropeptid y
WO1995001352A1 (fr) 1993-06-30 1995-01-12 Zeria Pharmaceutical Co., Ltd. Derive de thiazolidine et medicament le contenant
FR2707645B1 (fr) 1993-07-16 1995-08-11 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pirazine-4-one, leur préparation et les médicaments les contenant.
FR2707643B1 (fr) 1993-07-16 1995-08-11 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant.
EP0709373B1 (de) 1993-07-23 2001-10-17 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Pyrrolidin derivate
JPH0741485A (ja) 1993-07-30 1995-02-10 Katayama Seiyakushiyo:Kk セフェム誘導体およびそれを含有する抗菌剤
FR2711993B1 (fr) 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
AU684861B2 (en) 1993-12-02 1998-01-08 Merrell Pharmaceuticals Inc. Prolyl endopeptidase inhibitors
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
FR2717805B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Dérivés de 5H-indeno[1,2-b]pyrazine-2,3-dione, leur préparation et les médicaments les contenant .
FR2717812B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Indeno[1,2-e]pyrazine-4-ones, leur préparation et les médicaments les contenant.
FR2717811B1 (fr) 1994-03-28 1996-04-26 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant.
FR2717813B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, leur préparation et les médicaments les contenant .
JPH07267988A (ja) 1994-03-31 1995-10-17 Yamanouchi Pharmaceut Co Ltd 新規ペプチド
GB9410320D0 (en) 1994-05-24 1994-07-13 Fisons Corp Novel therapeutic method
GB9418443D0 (en) 1994-09-13 1994-11-02 Pfizer Ltd Therapeutic agents
US6562862B1 (en) 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
US5663192A (en) 1994-10-20 1997-09-02 Eli Lilly And Company Heterocyclic neuropeptide Y receptor antagonists
EP0716854A3 (de) 1994-10-20 1996-08-28 Lilly Co Eli Zusammensetzungen zur Inhibierung von Neuropeptid Y
FR2726275B1 (fr) 1994-11-02 1996-12-06 Rhone Poulenc Rorer Sa Spiro heterocycle-imidazo(1,2-a)indeno(1,2-e)pyrazine)-4'- ones, leur preparation et les medicaments les contenants
IL116584A0 (en) 1994-12-29 1996-03-31 Res Dev Foundation Novel flavin adenine dinucleotide analogue inhibitors of monoamine oxidase
US5691368A (en) 1995-01-11 1997-11-25 Hoechst Marion Roussel, Inc. Substituted oxazolidine calpain and/or cathepsin B inhibitors
GB9500601D0 (en) 1995-01-12 1995-03-01 Wellcome Found Modified peptides
US5552411A (en) 1995-05-26 1996-09-03 Warner-Lambert Company Sulfonylquinolines as central nervous system and cardiovascular agents
US5554621A (en) 1995-06-07 1996-09-10 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: nitrogen heterocyclic derivatives
US5668151A (en) 1995-06-07 1997-09-16 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: piperidine derivatives
IL117997A0 (en) 1995-06-07 1996-10-31 Pfizer Neuropeptide Y1 specific ligands
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
IL120724A0 (en) 1995-09-01 1997-08-14 Lilly Co Eli Indolyl neuropeptide Y receptor antagonists
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
ES2100129B1 (es) 1995-10-11 1998-02-16 Medichem Sa Nuevos compuestos aminopiridinicos policiclicos inhibidores de acetilcolinesterasa, procedimiento para su preparacion y su utilizacion.
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
DE19544686A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
AU7692896A (en) 1995-12-01 1997-06-27 Novartis Ag Quinazolin-2,4-diazirines as NPY receptor antagonist
WO1997020821A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
AU7626496A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Heteroaryl compounds
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
WO1997020823A2 (en) 1995-12-01 1997-06-12 Novartis Ag 2-amino quinazoline derivatives as npy receptor antagonists
JPH09157253A (ja) 1995-12-12 1997-06-17 Yamanouchi Pharmaceut Co Ltd 新規アミノ酸誘導体
ZA9610745B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists
ZA9610741B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Substituted piperidine analogs and their use as subtype selective nmda receptor antagonists
ZA9610736B (en) 1995-12-22 1997-06-27 Warner Lambert Co 2-Substituted piperidine analogs and their use as subtypeselective nmda receptor antagonists
CA2242579A1 (en) 1996-01-09 1997-07-17 Eli Lilly And Company Benzimidzolyl neuropeptide y receptor antagonists
GB9605027D0 (en) 1996-03-09 1996-05-08 Pfizer Ltd Quinoxalinediones
US5662723A (en) 1996-03-22 1997-09-02 Libbey Glass Inc. Apparatus and method for forming a decorative pattern on glassware having an edge
ATE207483T1 (de) 1996-04-12 2001-11-15 Aventis Pharma Inc Isatinderivate als acetylcholinesterase- inhibitoren und analgetika
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
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)
US6335323B2 (en) 1996-07-05 2002-01-01 The Wwk Trust Compositions for the treatment of peripheral neuropathies containing antidepressants and/or monoamine oxidase inhibitors and/or vitamin B12 and/or precursors or inducers of a neurotransmitter
ATE239002T1 (de) 1996-07-23 2003-05-15 Neurogen Corp 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
ATE230403T1 (de) 1996-07-23 2003-01-15 Neurogen Corp Einige amido- und ammo- substituierte benzylaminderivate: eine neue klasse von neuropeptid y1 spezifische ligande
AU3967297A (en) 1996-08-01 1998-02-25 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
JP2000516611A (ja) 1996-08-14 2000-12-12 ワーナー―ランバート・コンパニー Ｍｃｐ―１アンタゴニストとしての２―フェニルベンズイミダゾール誘導体
DE69713402T2 (de) 1996-08-23 2002-11-07 Agouron Pharma Liganden des neuropeptids y
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
AU4424697A (en) 1996-09-11 1998-04-02 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The The use of functional n-methyl-d-aspartate antagonists to ameliorate or prevent aminoglycoside-induced ototoxicity
WO1998015647A1 (en) 1996-10-08 1998-04-16 Novartis Ag Modulation of apoptosis
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
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
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
AU5716898A (en) 1997-01-08 1998-08-03 Warner-Lambert Company Acetylcholinesterase inhibitors in combination with muscarinic agonists for the treatment of alzheimer's disease
CA2284001A1 (en) 1997-03-13 1998-09-17 Keith Tipton Cytoprotective agents comprising monoamine oxidase inhibitors
EP0975584B1 (de) 1997-04-16 2002-09-25 Arqule, Inc. Herstellung und verwendung von alpha-ketoamid derivate und anordnunge
EP0980247A1 (de) 1997-05-07 2000-02-23 Algos Pharmaceutical Corporation Zusammensetzung und behandlung aus kombinationen von antidepressivamit einem nmda rezeptor antagonist, für neuropatische schmerzen
WO1998050075A1 (en) 1997-05-07 1998-11-12 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
KR100630506B1 (ko) 1997-06-30 2006-09-29 메르츠 파마 게엠베하 운트 코. 카가아 Ｎｍｄａ 수용체 길항물질로서의 1-아미노-알킬시클로헥산 화합물, 이를 함유하는 제약학적 조성물 및 이것으로 치료하는 방법
GB9716657D0 (en) 1997-08-07 1997-10-15 Zeneca Ltd Chemical compounds
GB9716879D0 (en) 1997-08-08 1997-10-15 Shire Int Licensing Bv Treatment of attention deficit disorders
WO1999007413A1 (en) 1997-08-11 1999-02-18 Algos Pharmaceutical Corporation Substance p inhibitors in combination with nmda-blockers for treating pain
SE9703376D0 (sv) 1997-09-18 1997-09-18 Astra Ab A new combination
SE9703414D0 (sv) 1997-09-23 1997-09-23 Astra Ab New compounds
AU766219B2 (en) 1998-02-02 2003-10-09 1149336 Ontario Inc. Method of regulating glucose metabolism, and reagents related thereto
JP2002506075A (ja) 1998-03-09 2002-02-26 フォンダテッヒ・ベネルクス・ナムローゼ・フェンノートシャップ セリンペプチダーゼ調節剤
US6007841A (en) 1998-03-13 1999-12-28 Algos Pharmaceutical Corporation Analgesic composition and method for treating pain
GB9805561D0 (en) 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
US6541208B1 (en) 1998-03-17 2003-04-01 University Of Maryland Biotechnology Institute Diagnostic method for distinguishing HIV-associated dementia from other forms of dementia
DE19812331A1 (de) 1998-03-20 1999-09-23 Merck Patent Gmbh Piperidinderivate
US6054451A (en) 1998-04-21 2000-04-25 Algos Pharmaceutical Corporation Analgesic composition and method for alleviating pain
AU3786299A (en) 1998-05-04 1999-11-23 Neotherapeutics, Inc. Novel serotonin-like 9-substituted hypoxanthine and methods of use
AU3879899A (en) 1998-05-04 1999-11-23 Neotherapeutics, Inc. Novel dopamine-like 9-substituted hypoxanthine and methods of use
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
PE20000728A1 (es) 1998-06-26 2000-08-21 Cocensys Inc Heterociclos 4-bencil piperidina alquilsulfoxido y su uso como antagonistas receptores subtipo-selectivo nmda
US6262081B1 (en) 1998-07-10 2001-07-17 Dupont Pharmaceuticals Company Composition for and method of treating neurological disorders
AU5027299A (en) 1998-07-31 2000-02-28 Novo Nordisk A/S Use of glp-1 and analogues for preventing type ii diabetes
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
US6218383B1 (en) 1998-08-07 2001-04-17 Targacept, Inc. Pharmaceutical compositions for the prevention and treatment of central nervous system disorders
IL125809A (en) 1998-08-17 2005-08-31 Finetech Lab Ltd Process and intermediates for production of donepezil and related compounds
IT1304904B1 (it) 1998-09-11 2001-04-05 Eisai Co Ltd Derivati anticolinesterasici per il trattamento delle sindromidolorose funzionali e/o organiche
HUP0103781A3 (en) 1998-10-16 2003-09-29 Janssen Pharmaceutica Nv Pharmaceutical compositions comprising atypical antiphsychotic agent in combination with acetylcholinesterase inhibitor for improving cognition
WO2000029023A1 (en) 1998-11-12 2000-05-25 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
JP5558648B2 (ja) 1998-11-23 2014-07-23 デイビス、ボニー アセチルコリンエステラーゼ阻害剤のための投与製剤
WO2000030674A1 (en) 1998-11-26 2000-06-02 Ferring Bv Neuropeptide y y4 agents in the treatment of reproductive disorders
ATE306264T1 (de) 1998-12-11 2005-10-15 Bonnie M Davis Verwendung von acetylcholinesterase inhibitoren zur modulierung der hypothalamus-hypophysen- gonadenachse
GB9902452D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902455D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902461D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902459D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902453D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
US6495587B1 (en) 1999-03-23 2002-12-17 Sumitomo Pharmaceuticals Company, Limited Tricyclic indole-2-carboxylic acid compound used as NMDA receptor antagonist
US6121311A (en) 1999-04-28 2000-09-19 Japan Tobacco Inc. Method for treating cocainism
MXPA01011321A (es) 1999-05-05 2003-08-01 Johnson & Johnson Neuropeptidos y ligandos de receptores 3a, 4, 5, 9b-tetrahidro-1h-benz(e)indol-2-il amino derivados utiles en el tratamiento de obesidad y otros trastornos.
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
WO2001000215A1 (en) 1999-06-25 2001-01-04 Wake Forest University Compositions for treating or preventing neurodegeneration and cognitive decline
DE19936521A1 (de) 1999-08-06 2001-02-15 Gruenenthal Gmbh Substituierte Pyrrolidin-2,3,4-trion-3-oxim-Derivate
DE19936719A1 (de) 1999-08-06 2001-02-15 Gruenenthal Gmbh Substituierte 1,5-Dihydropyrrol-2-on-Derivate
EP1078632A1 (de) 1999-08-16 2001-02-28 Sanofi-Synthelabo Verwendung von Monoamin Oxydase Inhibitoren zu Herstellung eines Medikaments zur Behandlung der Fettleibigkeit
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
TWI283577B (en) 1999-10-11 2007-07-11 Sod Conseils Rech Applic Pharmaceutical composition of imidazole derivatives acting as modulators of sodium channels and the use thereof
UA72558C2 (uk) 1999-11-01 2005-03-15 Мерц Фарма Гмбх Унд Ко. Кгаа 1-аміноалкілциклогексанові антагоністи рецептора nmda
WO2001034594A1 (en) 1999-11-12 2001-05-17 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
UA75055C2 (uk) 1999-11-30 2006-03-15 Пфайзер Продактс Інк. Похідні бензоімідазолу, що використовуються як антипроліферативний засіб, фармацевтична композиція на їх основі
EP1254113A1 (de) 2000-01-24 2002-11-06 Novo Nordisk A/S N-substituierte 2-cyanopyrrole und -pyrroline die inhibitoren des enzyms ddp-ivsind
JP2003520266A (ja) 2000-01-24 2003-07-02 メルク シャープ エンド ドーム リミテッド γ−セクレターゼ阻害薬
AU2001233277B2 (en) 2000-02-03 2004-06-03 Millennium Pharmaceuticals, Inc. Humanized anti-ccr2 antibodies and methods of use therefor
GB0005251D0 (en) 2000-03-03 2000-04-26 Merck Sharp & Dohme Therapeutic compounds
US20030144255A1 (en) 2000-03-06 2003-07-31 Bain Allen I Compositions for prevention and treatment of dementia
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
US6992081B2 (en) 2000-03-23 2006-01-31 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
ATE343562T1 (de) 2000-03-23 2006-11-15 Elan Pharm Inc Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
GB0008710D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic compounds
US6706741B2 (en) 2000-04-13 2004-03-16 Eisai Co., Ltd. Acetylcholinesterase inhibitors containing 1-benzyl-pyridinium salts
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
ES2267759T3 (es) 2000-04-26 2007-03-16 Warner-Lambert Company Llc Trans-n-4-(4-hidroxifenil) ciclohexili-3-fenilpropionamida como antagonista selectivo de subtipos de receptores nmda.
GB0010188D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
US20010036949A1 (en) 2000-05-09 2001-11-01 Coe Jotham Wadsworth Pharmaceutical composition and method of treatment of diseases of cognitive dysfunction in a mammal
AU2001261487A1 (en) 2000-06-01 2001-12-11 Warner Lambert Company Cyclohexylamine derivatives as subtype selective nmda receptor antagonists
ATE301642T1 (de) 2000-06-06 2005-08-15 Warner Lambert Co Bicyclische cyclohexylamine und ihre verwendung als nmda-rezeptor antagonisten
KR20030008153A (ko) 2000-06-22 2003-01-24 파모스 코포레이션 신규 비-향정신성 카나비노이드
GB0015488D0 (en) 2000-06-23 2000-08-16 Merck Sharp & Dohme Therapeutic agents
US6713276B2 (en) 2000-06-28 2004-03-30 Scios, Inc. Modulation of Aβ levels by β-secretase BACE2
CN1217920C (zh) 2000-06-30 2005-09-07 艾兰制药公司 治疗早老性痴呆的化合物
US6686449B2 (en) 2000-06-30 2004-02-03 Pharmacia & Upjohn Company Mutant presenilin 1 polypeptides
MXPA02012272A (es) 2000-07-04 2003-04-25 Novo Nordisk As Compuestos heterociclicos que son inhibidores de la enzima dipeptidilpeptidasa-iv.
GB0016681D0 (en) 2000-07-06 2000-08-23 Merck Sharp & Dohme Therapeutic compounds
US6556971B1 (en) 2000-09-01 2003-04-29 Snap-On Technologies, Inc. Computer-implemented speech recognition system training
AU2001293056A1 (en) 2000-09-25 2002-04-08 Motorwiz, Inc. Model-based machine diagnostics and prognostics using theory of noise and communications
US20020151591A1 (en) 2000-10-17 2002-10-17 Anabella Villalobos Combination use of acetylcholinesterase inhibitors and GABAa inverse agonists for the treatment of cognitive disorders
HU227197B1 (en) 2000-10-24 2010-10-28 Richter Gedeon Nyrt Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them
CA2427206C (en) 2000-11-02 2011-06-28 Merck Sharp & Dohme Limited Sulfamides as gamma-secretase inhibitors
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
US6670364B2 (en) 2001-01-31 2003-12-30 Telik, Inc. Antagonists of MCP-1 function and methods of use thereof
JP3616628B2 (ja) * 2001-03-01 2005-02-02 塩野義製薬株式会社 Ｈｉｖインテグラーゼ阻害活性を有する含窒素芳香族複素環化合物
TWI245761B (en) 2001-03-01 2005-12-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
CA2440284A1 (en) 2001-03-08 2002-09-19 Emory University Ph-dependent nmda receptor antagonists
US6649196B2 (en) 2001-03-12 2003-11-18 Mayo Foundation For Medical Education And Research Methods of reducing β-amyloid polypeptides
TWI236474B (en) 2001-04-03 2005-07-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
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
SI20922A (sl) 2001-05-18 2002-12-31 Krka Tovarna Zdravil, D.D., Novo Mesto Monoklonsko protitelo, ki nevtralizira aktivnost katepsina B, in njegove uporabe
US6562783B2 (en) 2001-05-30 2003-05-13 Neurologic, Inc. Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
WO2002098849A2 (en) 2001-06-01 2002-12-12 Elan Pharmaceuticals, Inc. Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer’s disease and similar diseases
CA2450579A1 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
JP2005500308A (ja) 2001-06-20 2005-01-06 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病を治療するためのジペプチジルペプチダーゼ阻害剤
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
WO2003002595A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Dipeptidyl peptidase iv inhibitors and their uses as anti-cancer agents
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
CA2419888A1 (en) 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
MXPA04000140A (es) 2001-06-27 2004-06-03 Elan Pharm Inc Derivados de beta-hidroxiamina utiles en el tratamiento de enfermedad de alzheimer.
IL158923A0 (en) 2001-06-27 2004-05-12 Smithkline Beecham Corp Fluoropyrrolidines as dipeptidyl peptidase inhibitors
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
JP4300108B2 (ja) 2001-06-27 2009-07-22 スミスクライン ビーチャム コーポレーション ジペプチジルペプチダーゼ阻害剤としてのピロリジン類
ATE370943T1 (de) 2001-06-27 2007-09-15 Smithkline Beecham Corp Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren
EP1404675B1 (de) 2001-07-03 2008-03-12 Novo Nordisk A/S Dpp-iv-inhibierende purin-derivative zur behandlung von 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
ES2312603T3 (es) 2001-07-24 2009-03-01 Richter Gedeon Nyrt Derivados de piperidina como antagonistas del receptor nmda.
US6948038B2 (en) * 2001-07-24 2005-09-20 Microsoft Corporation System and method for backing up and restoring data
KR20040019094A (ko) 2001-08-03 2004-03-04 쉐링 코포레이션 신규한 감마 세크레타제 억제제
US7122675B2 (en) 2001-08-03 2006-10-17 Schering Corporation Gamma secretase inhibitors
US20030060423A1 (en) 2001-08-30 2003-03-27 Plata-Salaman Carlos R. Co-therapy for the treatment of dementia and associated behavioral manifestations comprising anticonvulsant derivatives and acetylcholinesterase inhibitors
TWI246510B (en) 2001-09-14 2006-01-01 Mitsubishi Pharma Corp Thiazolidine derivatives and pharmaceutical uses thereof
WO2003024965A2 (en) 2001-09-19 2003-03-27 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
CA2464736A1 (en) 2001-10-23 2003-05-15 Oklahoma Medical Research Foundation Beta-secretase inhibitors and methods of use
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
WO2003037376A1 (fr) 2001-11-02 2003-05-08 Kensuke Egashira Prophylactiques et/ou remedes pour le traitement de l'arteriosclerose apres transplantation dans le cas de rejet de greffe
WO2003043987A2 (en) 2001-11-19 2003-05-30 Elan Pharmaceuticals, Inc. (4-phenyl) piperidin-3-yl-phenylcarboxylate derivatives and related compounds as beta-secretase inhibitors for the treatment of alzheimer's disease
JP4771661B2 (ja) 2001-11-26 2011-09-14 トラスティーズ オブ タフツ カレッジ Ｐｏｓｔ−プロリン開裂酵素の擬ペプチド性阻害剤
CN1596240A (zh) 2001-12-19 2005-03-16 阿特罗吉尼克斯公司 查耳酮衍生物及其治疗疾病的用途
AU2002360732A1 (en) 2001-12-26 2003-07-24 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
WO2003057204A2 (en) 2002-01-08 2003-07-17 Nordic Bioscience A/S Modulation of iamt (pimt or pcmt) in immune system
JP2005516967A (ja) 2002-01-18 2005-06-09 ザ ジェネティクス カンパニー インコーポレーティッド β−セクレターゼインヒビター
TW200302717A (en) 2002-02-06 2003-08-16 Schering Corp Novel gamma secretase inhibitors
US20040171614A1 (en) 2002-02-06 2004-09-02 Schering-Plough Corporation Novel gamma secretase inhibitors
CA2474460C (en) 2002-02-13 2009-12-22 F. Hoffmann-La Roche Ag Pyridine- and quinoline-derivatives
PL371678A1 (en) 2002-02-13 2005-06-27 F.Hoffmann-La Roche Ag Novel pyridin- and pyrimidin-derivatives
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
AU2003225916A1 (en) 2002-03-25 2003-10-13 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
ES2297141T3 (es) 2002-03-29 2008-05-01 EISAI R&D MANAGEMENT CO., LTD. Derivados de (1-indanona)-(1,2,3,6-tetrahidropiridina).
US6996738B2 (en) 2002-04-15 2006-02-07 Broadcom Corporation Robust and scalable de-skew method for data path skew control
WO2003091278A1 (fr) 2002-04-24 2003-11-06 Hiroshi Mori Inhibiteurs de gamma secretase
DE60324544D1 (de) 2002-04-26 2008-12-18 Schering Corp Muskarin antagonisten
WO2003099202A2 (en) 2002-05-17 2003-12-04 Merck & Co., Inc. Beta-secretase inhibitors
DE60324788D1 (de) 2002-05-31 2009-01-02 Lundbeck & Co As H Kombination aus einem nmda-antagonist und acetylcholinesterase-hemmern zur behandlung der alzheimer-krankheit
WO2003101449A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
WO2003101958A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
BR0311697A (pt) 2002-06-06 2005-03-22 Eisai Co Ltd Novos derivados condensados de imidazol
DE60312695T2 (de) 2002-06-19 2007-12-06 Cytec Surface Specialties, S.A. Halb-glänzende pulverbeschichtungszusammensetzungen
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
WO2004007468A1 (en) 2002-07-15 2004-01-22 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
US20040019118A1 (en) 2002-07-19 2004-01-29 Khalid Iqbal NMDA receptor antagonists and their use in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau
US7557137B2 (en) 2002-08-05 2009-07-07 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
EP2070539A1 (de) 2002-08-21 2009-06-17 Boehringer Ingelheim Pharma GmbH & Co. KG 8-[3-Amino-Piperidin-1-YL]-Xanthine, 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
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
ATE469969T1 (de) 2002-09-12 2010-06-15 Chemo Sero Therapeut Res Inst Menschlicher anti-mensch-mcp-1-antikorper sowie antikorperfragment davon
KR101072236B1 (ko) 2002-09-19 2011-10-12 아보트 러보러터리즈 디펩티딜 펩티다제-ｉｖ(ｄｐｐ-ｉｖ)의 억제제로서의약제학적 조성물
AU2003282804A1 (en) 2002-09-20 2004-04-08 Axys Pharmaceuticals, Inc. 3-(3,5-disubstituted-4-hydroxyphenyl)propionamide derivatives as cathepsin b inhibitors
US7273889B2 (en) 2002-09-25 2007-09-25 Innovative Drug Delivery Systems, Inc. NMDA receptor antagonist formulation with reduced neurotoxicity
GB0223038D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223039D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
WO2004032836A2 (en) 2002-10-07 2004-04-22 Merck & Co., Inc. Antidiabetic beta-amino heterocylcic dipeptidyl peptidase inhibitors
AU2003269850A1 (en) 2002-10-08 2004-05-04 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
GB0223494D0 (en) 2002-10-09 2002-11-13 Neuropharma Sa Dual binding site acetylcholinesterase inhibitors for the treatment of alzheimer's disease
JP4352001B2 (ja) 2002-10-18 2009-10-28 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療または予防のためのベータ−アミノ複素環式ジペプチジルペプチダーゼ阻害剤
CN100339070C (zh) 2002-10-24 2007-09-26 莫茨药物股份两合公司 包含1－氨基环己烷衍生物类和乙酰胆碱酯酶抑制剂类的药物组合物
US20040082543A1 (en) 2002-10-29 2004-04-29 Pharmacia Corporation Compositions of cyclooxygenase-2 selective inhibitors and NMDA receptor antagonists for the treatment or prevention of neuropathic pain
AU2003286776A1 (en) 2002-10-30 2004-06-07 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
WO2004039773A2 (en) 2002-10-30 2004-05-13 Nordic Bioscience A/S Coumpounds modulating the activity of gapdh and/or iamt
GB0225474D0 (en) 2002-11-01 2002-12-11 Merck Sharp & Dohme Therapeutic agents
RU2005117383A (ru) 2002-11-07 2006-01-20 Мерк энд Ко., Инк. (US) Производные фенилаланина в качестве ингибиторов дипептидилпептидазы для лечения или профилактики диабета
DE60329316D1 (de) 2002-11-12 2009-10-29 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
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
US7420079B2 (en) 2002-12-09 2008-09-02 Bristol-Myers Squibb Company Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
AU2003293376A1 (en) 2002-12-10 2004-06-30 Imclone Systems Incorporated Anti-angiogenic compounds and their use in cancer treatment
AU2003303239A1 (en) 2002-12-19 2004-07-14 Atherogenics, Inc. Process of making chalcone derivatives
JP4504924B2 (ja) 2002-12-20 2010-07-14 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての３−アミノ−４−フェニルブタン酸誘導体
AU2004204692B2 (en) 2003-01-07 2009-07-09 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of Alzheimer's disease
US7265128B2 (en) 2003-01-17 2007-09-04 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7388019B2 (en) 2003-01-31 2008-06-17 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
PL378405A1 (pl) 2003-02-04 2006-04-03 F. Hoffmann-La Roche Ag Pochodne malonoamidu jako inhibitory <$Egamma> - sekretazy
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
JP2006517979A (ja) 2003-02-18 2006-08-03 ロスカンプ リサーチ エルエルシー βセクレターゼインヒビターおよびγセクレターゼインヒビターの抗脈管形成特性および抗腫瘍特性
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
AU2003207881A1 (en) 2003-02-28 2004-09-17 Aic Dipeptidyl peptidase inhibitors
EP1454627A1 (de) 2003-03-06 2004-09-08 MyoContract Ltd. Alpha-Keto-Carbonyl-Verbindungen als Calpainhemmer
WO2004084830A2 (en) 2003-03-21 2004-10-07 Buck Institute Method for treating alzheimer’s dementia
US20040191334A1 (en) 2003-03-24 2004-09-30 Pang-Chui Shaw Use of transhinone derivates as cholinesterase inhibitors in treating related diseases
CN1894234A (zh) 2003-03-25 2007-01-10 武田药品工业株式会社 二肽基肽酶抑制剂
US20050130961A1 (en) 2003-03-28 2005-06-16 Davis Robert E. Muscarinic M1 receptor agonists for pain management
US7253153B2 (en) 2003-04-09 2007-08-07 Wyeth Derivatives of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl] phosphonic acid and methods of use thereof
GB0308318D0 (en) 2003-04-10 2003-05-14 Merck Sharp & Dohme Therapeutic agents
GB0308382D0 (en) 2003-04-10 2003-05-21 Univ Cambridge Tech Therapeutic methods and means
WO2004089362A1 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S 2-cyanopyrroles and their analogues as ddp-iv inhibitors
WO2004098591A2 (en) * 2003-05-05 2004-11-18 Probiodrug Ag Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases
EP2206496B1 (de) 2003-05-05 2014-09-17 Probiodrug AG Screening von inhibitoren der pyroglutaminsäurebildung in beta amyloid peptiden
US7732162B2 (en) 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
US8338120B2 (en) 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
WO2004099134A2 (en) 2003-05-05 2004-11-18 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
TW200510405A (en) 2003-05-13 2005-03-16 Schering Corp Bridged n-arylsulfonylpiperidines as gamma-secretase inhibitors
EP1625122A1 (de) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidylpeptidase-hemmer
CA2524531A1 (en) 2003-05-14 2004-12-02 Merck And Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7410964B2 (en) 2003-05-16 2008-08-12 Merck Sharp & Dohme Ltd. Cyclohexyl sulphones as gamma-secretase inhibitors
AU2004251636B2 (en) 2003-05-27 2006-11-09 Merz Pharma Gmbh & Co. Kgaa Combination of an NMDA receptor antagonist and a selective serotonin reuptake inhibitor for the treatment of depression and other mood disorders
AU2003902828A0 (en) 2003-06-05 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
CA2526770A1 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
CA2527806A1 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE602004030244D1 (de) 2003-06-20 2011-01-05 Hoffmann La Roche Itoren
MXPA05013734A (es) 2003-06-20 2006-03-08 Hoffmann La Roche Hexahidropiroisoquinolinas como inhibidores de dpp-iv.
CN100430377C (zh) 2003-06-30 2008-11-05 麦克公司 用于治疗阿尔茨海默病的N-烷基苯基甲酰胺β分泌酶抑制剂
WO2005004803A2 (en) 2003-07-01 2005-01-20 Merck & Co., Inc. Phenylcarboxylate beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005007614A1 (en) 2003-07-03 2005-01-27 The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services 6011 Monoamine oxidase inhibitors
ATE466595T1 (de) 2003-07-16 2010-05-15 Rvx Therapeutics Inc Verbindungen und methoden für das downregulating der effekte von tgf-beta
WO2005008250A1 (en) 2003-07-21 2005-01-27 Angiogenetics Sweden Ab Compounds and methods for promoting angiogenesis by using a gamma-secretase inhibitor or inhibiting the gamma-secretase pathway
US20070082956A1 (en) 2003-07-28 2007-04-12 Merz Pharma Gmbh & Co. Kgaa The use of 1-amino-alkylcyclohexane compounds in the treatment of pain hypersensitivity.
DE602004018503D1 (de) 2003-07-31 2009-01-29 Merck & Co Inc Hexahydrodiazepinone als inhibitoren des dipeptidylpeptidase-iv zur behandlung bzw. prävention von diabetes
GB0318447D0 (en) 2003-08-05 2003-09-10 Merck Sharp & Dohme Therapeutic agents
MXPA06001601A (es) 2003-08-13 2006-08-25 Takeda Pharmaceutical Derivados de 4-pirimidona y su uso como inhibidores de dipeptidilpeptidasa.
CA2535337A1 (en) 2003-08-14 2005-03-03 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for the treatment of alzheimer's disease
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)
WO2005026148A1 (en) 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US20050065144A1 (en) 2003-09-08 2005-03-24 Syrrx, Inc. Dipeptidyl peptidase inhibitors
WO2005025554A2 (en) 2003-09-09 2005-03-24 Japan Tobacco Inc. Dipeptidyl peptidase iv inhibitor
GB0322140D0 (en) 2003-09-22 2003-10-22 Pfizer Ltd Combinations
CA2539042A1 (en) 2003-09-24 2005-04-07 Merck Sharp & Dohme Limited Gamma-secretase inhibitors
EP1673078B1 (de) 2003-10-03 2008-05-28 Merck & Co., Inc. Benzylether- und benzylamino-beta-sekretase-hemmer zur behandlung von alzheimer-krankheit
KR100884872B1 (ko) 2003-10-06 2009-02-23 에프. 호프만-라 로슈 아게 감마-세크레타제 저해제로서 유용한 치환된다이벤조-아제핀 및 벤조-다이아제핀 유도체
AU2003269307A1 (en) 2003-10-06 2005-04-21 Torrent Pharmaceuticals Ltd. Azolidinecarbonitriles and their use as dpp-iv inhibitors
EP1673366A1 (de) 2003-10-08 2006-06-28 Pfizer, Inc. 1-[2-(4-hydroxyphenyl)-2-hydroxyethyl]-piperidin-4-olverbindungen als nmda-rezeptorantagonisten
BRPI0415409A (pt) 2003-10-15 2006-12-05 Probiodrug Ag uso de efetuadores de ciclases de glutaminila e glutamato
GB0324236D0 (en) 2003-10-16 2003-11-19 Astrazeneca Ab Chemical compounds
WO2005039580A1 (en) 2003-10-16 2005-05-06 Boehringer Ingelheim International Gmbh Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an acetylcholinesterase inhibitor
TW200519105A (en) 2003-10-20 2005-06-16 Lg Life Science Ltd Novel inhibitors of DPP-IV, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
ATE411015T1 (de) 2003-10-22 2008-10-15 Merz Pharma Gmbh & Co Kgaa Verwendung von 1-aminocyclohexan-derivaten zur modifizierung der abscheidung von fibrillogenen as peptiden in amyloidpathien
US7667044B2 (en) 2003-11-03 2010-02-23 Probiodrug Ag Compounds for the treatment of neurological disorders
EP1680120A2 (de) 2003-11-03 2006-07-19 Probiodrug AG Zusammenstellungen zur behandlung von neuronalen erkrankungen
US20050171112A1 (en) 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
WO2006058720A2 (en) 2003-11-03 2006-06-08 Probiodrug Ag Novel compounds for the treatment of neurological disorders
US7238683B2 (en) 2003-11-04 2007-07-03 Merck & Co., Inc. Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
CA2544203A1 (en) 2003-11-11 2005-05-19 F. Hoffmann-La Roche Ag Phosphinic acids derivatives, beta-secretase inhibitors for the treatment of alzheimer's disease
EP1997533B8 (de) 2003-11-12 2014-10-29 Sino-Med International Alliance, Inc. Heterocyclische Boronsäureverbindungen, Dipeptidylpeptidase IV Inhibitoren
US7354942B2 (en) 2003-11-24 2008-04-08 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease
DE10355304A1 (de) 2003-11-27 2005-06-23 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(Piperazin-1-yl)-und 8-([1,4]Diazepan-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
UY28650A1 (es) 2003-12-05 2005-02-28 Forest Laboratories Memantina para la prevencion o disminucion de la conducta suicida y para el tratamiento de la depresion mayor asociada con esta conducta
EP1541143A1 (de) 2003-12-09 2005-06-15 Graffinity Pharmaceuticals Aktiengesellschaft Dpp-iv inhibitoren
EP1541148A1 (de) 2003-12-09 2005-06-15 Graffinity Pharmaceuticals Aktiengesellschaft Dpp-iv inhibitoren
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
CA2548849A1 (en) 2003-12-19 2005-07-21 Merck & Co., Inc. Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005070429A1 (en) 2004-01-22 2005-08-04 Neurosearch A/S Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an n-methyl-d-aspartate (nmda) receptors antagonist
WO2005072705A1 (en) 2004-01-29 2005-08-11 Neuromolecular, Inc. Combination of a nmda receptor antagonist and a mao-inhibitor or a gadpf-inhibitor for the treatment of central nervous system-related conditions
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
CN1918131B (zh) 2004-02-05 2011-05-04 前体生物药物股份公司 谷氨酰胺酰基环化酶抑制剂
WO2005079756A2 (en) 2004-02-13 2005-09-01 Neuromolecular, Inc. Combination of a nmda receptor antagonist and an anti-depressive drug mao-inhibitor or a gadph-inhibitor for the treatment of psychiatric conditions
US20050182044A1 (en) 2004-02-17 2005-08-18 Bruinsma Gosse B. Combinatorial therapy with an acetylcholinesterase inhibitor and (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3,-b]indol-5-yl phenylcarbamate
PT1758905E (pt) 2004-02-18 2009-07-16 Boehringer Ingelheim Int 8-[3-amino-piperidin-1-il]-xantinas, sua preparação e sua utilização como inibidores de dpp-iv
BRPI0507972A (pt) 2004-02-23 2007-07-24 Tufts College composto ,composição farmacêutica , uso de um composto, método para inibição da atividade proteolìtica de uma enzima de clivagem pós prolina e composição farmacêutica embalada
EP1593671A1 (de) 2004-03-05 2005-11-09 Graffinity Pharmaceuticals AG DPP-IV Inhibitoren
CN1942186B (zh) 2004-03-09 2010-10-06 国家卫生研究院 吡咯烷化合物
CN102079743B (zh) 2004-03-15 2020-08-25 武田药品工业株式会社 二肽基肽酶抑制剂
EP1740172A4 (de) 2004-03-19 2007-10-10 Axonyx Inc Acetylcholinesterase-hemmer und n-methyl-d-aspartat-antagonisten zur behandlung von kognitiven störungen
WO2005095339A1 (en) 2004-03-31 2005-10-13 Pfizer Products Inc. Dicyanopyrrolidines as dipeptidyl peptidase iv inhibitors
WO2005097103A2 (en) 2004-04-01 2005-10-20 Axys Pharmaceuticals, Inc. Diabetes and metabolic syndrome therapy utilizing cathepsin b inhibitors
AR049377A1 (es) 2004-04-05 2006-07-26 Schering Corp Inhibidores de secretasa gamma
AU2005236063A1 (en) 2004-04-20 2005-11-03 Merck & Co., Inc. 2, 4, 6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
US7847100B2 (en) 2004-04-20 2010-12-07 Merck, Sharp & Dohme, Inc. 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
WO2005102390A2 (en) 2004-04-22 2005-11-03 Pfizer Japan, Inc. Combinations comprising alpha-2-delta ligands and nmda receptor antagonists
US9549895B2 (en) 2004-04-23 2017-01-24 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving the viability of photoreceptor cells
WO2005108382A1 (en) 2004-05-04 2005-11-17 Merck & Co., Inc. 1,2,4-oxadiazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
GEP20084421B (en) 2004-05-12 2008-07-10 Pfizer Prod Inc Proline derivatives and their use as dipeptidyl peptidase iv inhibitors
WO2005113484A1 (en) 2004-05-13 2005-12-01 Merck & Co., Inc. Phenyl carboxamide compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005116029A1 (en) 2004-05-18 2005-12-08 Merck & Co., Inc. Cyclohexylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
EP1598341A1 (de) 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV-Hemmer
WO2005118555A1 (en) 2004-06-04 2005-12-15 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP1604989A1 (de) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV-Hemmer
EP1604662A1 (de) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft 1-[(3R)-Amino-4-(2-fluoro-phenyl)-butyl]-pyrrolidin-(2R)-carbonsäure-benzylamine-Derivate und verwandte Verbindungen als Dipeptidyl-Peptidase IV (DPP-IV) Inhibitoren zur Behandlung von Typ 2 Diabetes Mellitus
EP1604980A1 (de) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV-Hemmer
CN1968924B (zh) 2004-06-15 2011-08-03 默沙东公司 作为β-分泌酶抑制剂用于治疗阿尔茨海默氏病的吡咯烷-3-基化合物
GB0413389D0 (en) 2004-06-16 2004-07-21 Astrazeneca Ab Chemical compounds
JP4963671B2 (ja) 2004-06-21 2012-06-27 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のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としてのアミノシクロヘキサン
US7371825B2 (en) 2004-06-30 2008-05-13 Centocor, Inc. Anti-MCP-1 antibodies, compositions, methods and uses
EP1789404B1 (de) 2004-06-30 2010-03-24 Schering Corporation Substituierte n-arylsulfonylheterocyclische amine als gamma-sekretase-hemmer
EP1778220A1 (de) 2004-07-12 2007-05-02 Phenomix Corporation Eingezwängte cyano-verbindungen
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006014762A1 (en) 2004-07-22 2006-02-09 Schering Corporation Substituted amide beta secretase inhibitors
ES2306200T3 (es) 2004-07-28 2008-11-01 Schering Corporation Inhibidores macrociclicos de beta-secretasa.
HUP0401523A3 (en) 2004-07-29 2007-05-02 Richter Gedeon Vegyeszet Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them
EP1623983A1 (de) 2004-08-05 2006-02-08 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Heterozyklische Verbindungen verwendbar als DDP-IV-Inhibitoren
AU2005277283A1 (en) 2004-08-23 2006-03-02 Merck Sharp & Dohme Corp. Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
AU2005276635A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
AU2005276631A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
US7388007B2 (en) 2004-08-26 2008-06-17 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
CA2579472A1 (en) 2004-09-14 2006-03-23 The Genetics Company, Inc. Hydrazone derivatives and their use as beta secretase inhibitors
EP1799660A2 (de) 2004-09-17 2007-06-27 Comentis, Inc. Aminohaltige verbindungen zur inhibition der aktivität von memapsin-2-beta-sekretase und verfahren zu ihrer verwendung
EP1797052A1 (de) 2004-09-17 2007-06-20 Comentis, Inc. Bizyklische verbindungen zur verhinderung der aktivität von beta-sekretase und verwendungsverfahren dafür
AU2005292134B2 (en) 2004-10-01 2010-12-23 Merck Sharp & Dohme Corp. Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2006042103A2 (en) 2004-10-05 2006-04-20 Axys Pharmaceuticals, Inc. Reversible inhibitors of cathepsin b
BRPI0516446A (pt) 2004-10-08 2008-09-02 Novartis Ag combinação de compostos orgánicos
EP1807087A2 (de) 2004-10-12 2007-07-18 Ernir Snorrason Inhibitoren von acetylcholinesterase zur behandlung von hauterkrankungen
CA2583342A1 (en) 2004-10-13 2006-04-27 Merck And Co., Inc. Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzhermer's disease
EP1816996A4 (de) 2004-10-15 2009-08-12 Biopharmacopae Design Internat Verfahren und therapeutische zusammensetzungen aus pflanzenextrakten für die krebsbehandlung
GB0423673D0 (en) 2004-10-25 2004-11-24 Glaxo Group Ltd Compounds
MX2007004934A (es) 2004-10-25 2007-06-12 Novartis Ag Combinacion de inhibidor de dpp-iv, anti-diabetico de ppar, y metformina.
AU2005310239A1 (en) 2004-10-29 2006-06-08 Merck & Co., Inc. 2-aminopyridine compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
CA2587083A1 (en) 2004-11-17 2006-05-26 Merck & Co., Inc. Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
BRPI0518483A2 (pt) 2004-11-23 2008-11-18 Neuromolecular Pharmaceuticals Inc composiÇço compreendendo uma matriz ou revestimento de liberaÇço controlada e um antagonista de receptor de nmda, mÉtodo para administraÇço de tal antagonista de nmda a um paciente
US7951949B2 (en) 2004-11-23 2011-05-31 Merck, Sharp & Dohme, Corp. Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of Alzheimer's disease
US8394837B2 (en) 2004-11-23 2013-03-12 Merck, Sharp & Dohme, Corp. 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
EP1845968A2 (de) 2004-11-24 2007-10-24 Neuromolecular Pharmaceuticals, Inc Zusammensetzung mit einem nmda-rezeptor-antagonisten und levodopa und ihre verwendung zur behandlung von neurologischen erkrankungen
AU2005309606B2 (en) 2004-11-29 2011-01-06 Merck Sharp & Dohme Corp. Fused aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
MX2007006239A (es) 2004-11-30 2007-07-20 Hoffmann La Roche Benzoquinolisinas sustituidas como inhibidores de dipeptidil peptidasa iv (dpp-iv) para tratamiento de diabetes.
US20080139458A1 (en) 2004-12-03 2008-06-12 Jay Gregory D Methods of Treatment For Injured or Diseased Joints
GB0427267D0 (en) 2004-12-13 2005-01-12 Maria Teresa De Magistris Peptide adjuvants
AU2005315430B2 (en) * 2004-12-14 2010-05-27 Astrazeneca Ab Oxadiazole derivatives as DGAT inhibitors
WO2006064375A2 (en) * 2004-12-16 2006-06-22 Ab Science Aminoaryl substituted five-membered ring heterocyclic compounds for the treatment of diseases
KR100904829B1 (ko) 2004-12-20 2009-06-25 에프. 호프만-라 로슈 아게 4-아미노피페리딘 유도체
US7411093B2 (en) 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
WO2006068978A2 (en) 2004-12-21 2006-06-29 Takeda Pharmaceutial Company Limited Dipeptidyl peptidase inhibitors
EP1827468B1 (de) 2004-12-23 2012-08-22 Curaxis Pharmaceutical Corporation Acetylcholinesterasehemmer und Leuprolidacetat zur Behandlung von Alzheimer-Krankheit
EP1831172B1 (de) 2004-12-28 2009-02-18 Council of Scientific and Industrial Research Substituierte carbaminsäurechinolin-6-ylester, die sich als acetylchinolylesteraseinhibitoren eignen
US20080194548A1 (en) 2005-01-06 2008-08-14 Forrest Michael J Drug Combination Therapy and Pharmaceutical Compositions for Treating Inflammatory Disorders
CN101106994A (zh) 2005-01-19 2008-01-16 默克公司 用于治疗阿尔茨海默氏病的氨基甲基β-分泌酶抑制剂
US20060216331A1 (en) 2005-02-28 2006-09-28 Lines Thomas C Composition for treating mental health disorders
US20080194698A1 (en) 2005-03-07 2008-08-14 Michael Hermanussen Nmda Receptor Antagonists in the Medical Intervention of Metabolic Disorders
US7745470B2 (en) 2005-03-10 2010-06-29 Bristol-Myers Squibb Company Isophthalates as beta-secretase inhibitors
FR2883285B1 (fr) 2005-03-17 2007-05-18 Sanofi Aventis Sa Sel besylate de la 7-(2-(4-(3-trifluoromethyl-phenyl) -1,2,3,6-tetrahudro-pyrid-1-yl)ethyl) isoquinoleine, sa preparation et son utilisation en therapeutique
PE20061444A1 (es) 2005-05-19 2007-01-15 Centocor Inc Anticuerpo anti-mcp-1, composiciones, metodos y usos
NZ590631A (en) 2006-09-21 2011-12-22 Probiodrug Ag Novel genes related to glutaminyl cyclase

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WO2008065141A1 (en) 2008-06-05
US20080214620A1 (en) 2008-09-04

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