DK2091948T3 - Nye inhibitorer af glutaminylcyclase - Google Patents

Nye inhibitorer af glutaminylcyclase

Info

Publication number
DK2091948T3
DK2091948T3 DK07847471.5T DK07847471T DK2091948T3 DK 2091948 T3 DK2091948 T3 DK 2091948T3 DK 07847471 T DK07847471 T DK 07847471T DK 2091948 T3 DK2091948 T3 DK 2091948T3
Authority
DK
Denmark
Prior art keywords
alkyl
carbocyclyl
heteroaryl
novel inhibitors
glutaminyl cyclase
Prior art date
Application number
DK07847471.5T
Other languages
Danish (da)
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 DK2091948T3 publication Critical patent/DK2091948T3/da

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
DK07847471.5T 2006-11-30 2007-11-28 Nye inhibitorer af glutaminylcyclase DK2091948T3 (da)

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
DK2091948T3 true DK2091948T3 (da) 2012-07-23

Family

ID=39133797

Family Applications (1)

Application Number Title Priority Date Filing Date
DK07847471.5T DK2091948T3 (da) 2006-11-30 2007-11-28 Nye inhibitorer af glutaminylcyclase

Country Status (7)

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

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2481442T3 (es) * 2006-11-09 2014-07-30 Probiodrug Ag Inhibidores novedosos de glutaminil ciclasa
JP5379692B2 (ja) * 2006-11-09 2013-12-25 プロビオドルグ エージー 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての3−ヒドロキシ−1,5−ジヒドロ−ピロール−2−オン誘導体
US8420684B2 (en) * 2006-11-09 2013-04-16 Probiodrug Ag Inhibitors of glutaminyl cyclase
EP2118101B1 (en) * 2007-03-09 2012-09-26 Probiodrug AG Imidazo [1,5-a] pyridine derivatives as inhibitors of glutaminyl cyclase
JP5675342B2 (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シアノグアニジン誘導体
US9512082B2 (en) * 2007-04-18 2016-12-06 Probiodrug Ag Inhibitors of glutaminyl cyclase
US8202897B2 (en) * 2007-04-18 2012-06-19 Probiodrug Ag Inhibitors of glutaminyl cyclases
JP5667440B2 (ja) * 2007-04-18 2015-02-12 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チオ尿素誘導体
JP5675341B2 (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チオキソキナゾリノン誘導体
DK2142513T3 (da) * 2007-04-18 2014-06-10 Probiodrug Ag Nitrovinyl-diamin-derivater som glutaminyl-cyclase-inhibitorer
EP2142536B1 (en) * 2007-04-20 2015-10-21 Probiodrug AG Aminopyrimidine derivatives as glutaminyl cyclase inhibitors
JP2011501652A (ja) * 2007-09-12 2011-01-13 プロビオドルグ エージー トランスジェニックマウス
EP2238252B1 (en) * 2008-01-14 2013-07-31 Probiodrug AG Mouse models carrying a knock-out mutation of the glutaminyl cyclase gene
AU2009273387B9 (en) * 2008-07-21 2015-06-11 Vivoryon Therapeutics N.V. Diagnostic antibody assay
US20110092445A1 (en) * 2008-07-25 2011-04-21 Abbott Laboratories Amyloid ß peptide analogues, oligomers thereof, processes for preparing and composi-tions comprising said analogues or oligomers, and their uses
NZ598685A (en) 2009-09-11 2013-05-31 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
US20110152341A1 (en) 2009-12-22 2011-06-23 Probiodrug Ag Cleavage of b-amyloid precursor protein
US20110212853A1 (en) 2010-02-18 2011-09-01 Probiodrug Ag Novel diagnostic method
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
DK2545047T3 (da) 2010-03-10 2014-07-28 Probiodrug Ag Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5)
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
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
SG192805A1 (en) 2011-03-16 2013-09-30 Probiodrug Ag Diagnostic antibody assay
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
JP2018501482A (ja) 2014-12-19 2018-01-18 プロビオドルグ エージー pGlu−Abetaペプチドの検出のための新規の方法
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
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
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
CA1309805C (en) 1985-04-16 1992-11-03 Naoki Higuchi Dipeptide derivative and synthesis and use thereof
CA1298033C (en) 1985-04-16 1992-03-24 Takaharu Tanaka Dipeptide derivative of fatty acid
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
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
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
US5262431A (en) 1986-12-29 1993-11-16 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
EP0275482B1 (en) 1986-12-29 1993-01-20 Ono Pharmaceutical Co., Ltd. Proline derivatives
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
ES2054712T3 (es) 1987-02-04 1994-08-16 Ono Pharmaceutical Co Un procedimiento para la preparacion de los derivados de prolinal.
EP0280956B1 (en) 1987-02-23 1992-10-21 Ono Pharmaceutical Co., Ltd. Thiazolidine derivatives
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
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
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
US5118811A (en) 1989-04-13 1992-06-02 Japan Tobacco Inc. Amino acid derivatives possessing prolyl endopeptidase-inhibitory activities
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
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
WO1991018891A1 (en) 1990-06-04 1991-12-12 Pfizer Inc. Aromatic pyrrolidine and thiazolidine amides
ATE133407T1 (de) 1990-06-07 1996-02-15 Zeria Pharm Co Ltd Neue arylalkanoylaminderivate und diese enthaltendes arzneimittel
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
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
WO1993000361A1 (en) 1991-06-20 1993-01-07 Snow Brand Milk Products Co., Ltd. Novel prolyl endopeptidase inhibitors sna-115 and sna-115t, production thereof, and strain which produces said inhibitors
HUT66324A (en) 1991-07-29 1994-11-28 Warner Lambert Co Quinazoline derivatives as acetylcholinesterase inhibitors and pharmaceutical compositions containing them
CA2126212A1 (en) 1991-12-19 1993-07-08 Albert Tseng 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
ES2149213T3 (es) 1992-10-05 2000-11-01 Ube Industries Compuesto de pirimidina.
US5260286A (en) 1992-10-16 1993-11-09 Japan Tobacco, Inc. 2-piperidinecarboxylic acid derivatives useful as NMDA receptor antagonists
US5536737A (en) 1992-11-20 1996-07-16 Japan Tobacco Inc. 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 (en) 1993-02-16 1994-08-24 Merrell Dow Pharmaceuticals Inc. Silylated acetylcholinesterase inhibitors
AU4982293A (en) 1993-03-02 1994-09-26 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 (en) 1993-06-04 1994-12-07 Merrell Dow Pharmaceuticals Inc. Aromatic acetylcholinesterase inhibitors
CA2165200A1 (en) 1993-06-18 1995-01-05 Ambikaipakan Balasubramaniam Neuropeptide y antagonists and agonists
WO1995001352A1 (en) 1993-06-30 1995-01-12 Zeria Pharmaceutical Co., Ltd. Thiazolidine derivative and medicine containing the same
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.
DE69428703T2 (de) 1993-07-23 2002-05-29 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Tokio/Tokyo 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
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 .
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 .
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
US5663192A (en) 1994-10-20 1997-09-02 Eli Lilly And Company Heterocyclic neuropeptide Y receptor antagonists
WO1996012489A1 (en) 1994-10-20 1996-05-02 Eli Lilly And Company Bicyclic 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
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
AU717422B2 (en) 1995-09-01 2000-03-23 Eli Lilly And Company 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.
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
WO1997020820A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl compounds
AU7692696A (en) 1995-12-01 1997-06-27 Novartis Ag Heteroaryl derivatives
AU7692996A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Receptor antagonists
WO1997020822A1 (en) 1995-12-01 1997-06-12 Novartis Ag Quinazolin-2,4-diazirines as npy receptor antagonist
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
JPH09157253A (ja) 1995-12-12 1997-06-17 Yamanouchi Pharmaceut Co Ltd 新規アミノ酸誘導体
ZA9610741B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Substituted piperidine analogs and their use as subtype selective nmda receptor antagonists
ZA9610745B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Subsituted 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
EP0871442A1 (en) 1996-01-09 1998-10-21 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)
AU3451797A (en) 1996-07-05 1998-02-02 Andrew Peter Worsley 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
US5985873A (en) 1996-07-23 1999-11-16 Neurogen Corporation Certain substituted benzylamine derivatives a new class of Neuropeptide-Y1 specific ligands
DK0915859T3 (da) 1996-07-23 2003-03-03 Neurogen Corp Visse substituerede benzylaminderivater; en ny klasse af Neuropeptid Y1-specifikke ligander
JP2000515527A (ja) 1996-07-23 2000-11-21 ニューロジェン・コーポレーション 特定のアミド―およびアミノ―置換ベンジルアミン誘導体;新種の神経ペプチドy1特異的リガンド
WO1998005337A1 (en) 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
EP0927167A1 (en) 1996-08-14 1999-07-07 Warner-Lambert Company 2-phenyl benzimidazole derivatives as mcp-1 antagonists
US6849733B1 (en) 1996-08-23 2005-02-01 Agouron Pharmaceuticals, Inc. Neuropeptide-Y ligands
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
WO1998010757A2 (en) 1996-09-11 1998-03-19 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services 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
EP0975366A1 (en) 1997-03-13 2000-02-02 The Provost, Fellows And Scholars Of The College Of The Holy And Undivided Trinity Of Queen Elizabeth Near Dublin Cytoprotective agents comprising monoamine oxidase inhibitors
CA2286660A1 (en) 1997-04-16 1998-10-22 Arqule, Inc. Synthesis and use of .alpha.-ketoamide derivatives and arrays
CA2289190A1 (en) 1997-05-07 1998-11-12 Algos Pharmaceutical Corporation Composition and method combining an antidepressant with an nmda receptor antagonist, for treating neuropathic pain
AU7472798A (en) 1997-05-07 1998-11-27 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
CA2292558C (en) 1997-06-30 2006-09-19 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane nmda receptor antagonists
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
AU7696098A (en) 1997-08-11 1999-03-01 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
EP1052994A2 (en) 1998-02-02 2000-11-22 Trustees Of Tufts College Use of dipeptidylpetidase inhibitors to regulate glucose metabolism
WO1999046272A1 (en) 1998-03-09 1999-09-16 Fondatech Benelux N.V. Serine peptidase modulators
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
AU3879899A (en) 1998-05-04 1999-11-23 Neotherapeutics, Inc. Novel dopamine-like 9-substituted hypoxanthine and methods of use
WO1999057120A1 (en) 1998-05-04 1999-11-11 Neotherapeutics, Inc. Novel serotonin-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
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
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
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
WO2000007617A1 (en) 1998-07-31 2000-02-17 Novo Nordisk A/S Use of glp-1 and analogues for preventing type ii diabetes
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
PL348107A1 (en) 1998-10-16 2002-05-06 Janssen Pharmaceutica Nv Therapy 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
CA2351347A1 (en) 1998-11-23 2000-06-02 Bonnie Davis Dosage formulations for acetylcholinesterase inhibitors
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
GB9902453D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902459D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
AU3195600A (en) 1999-03-23 2000-10-09 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
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
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
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
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
AU6053900A (en) 1999-06-25 2001-01-31 Morris Notelovitz 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 (en) 1999-08-16 2001-02-28 Sanofi-Synthelabo Use of monoamine oxydase inhibitors for the manufacture of drugs intended for the treatment of obesity
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
CA2390231A1 (en) 1999-11-12 2001-05-17 Paul Jackson 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
AU779875B2 (en) 2000-01-24 2005-02-17 Merck Sharp & Dohme Limited Gamma-secretase inhibitors
JP2003520849A (ja) 2000-01-24 2003-07-08 ノボ ノルディスク アクティーゼルスカブ 酵素dpp−ivの阻害剤であるn−置換2−シアノピロールおよび−ピロリン
MXPA02007449A (es) 2000-02-03 2003-04-14 Millennium Pharm Inc Anticuerpos anti-ccr2 humanizados y metodos para el uso de los mismos.
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
EP1265849B1 (en) 2000-03-23 2006-10-25 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
GB0008710D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic compounds
WO2001078728A1 (fr) 2000-04-13 2001-10-25 Eisai Co., Ltd. Inhibiteurs d'acetylcholinesterases contenant des sels de 1-benzyl-pyridinium
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
CN1441773A (zh) 2000-04-26 2003-09-10 沃尼尔·朗伯公司 作为亚型选择性nmda受体拮抗剂的环己胺衍生物
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
AU2001263130A1 (en) 2000-06-06 2001-12-17 Warner Lambert Company Bicyclic cyclohexylamines and their use as nmda receptor antagonists
AU783522B2 (en) 2000-06-22 2005-11-03 Pharmos Corporation Novel non-psychotropic cannabinoids
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
CA2410972A1 (en) 2000-06-30 2002-01-10 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
US6686449B2 (en) 2000-06-30 2004-02-03 Pharmacia & Upjohn Company Mutant presenilin 1 polypeptides
EP1301187B1 (en) 2000-07-04 2005-07-06 Novo Nordisk A/S Purine-2,6-diones which are inhibitors of the enzyme dipeptidyl peptidase iv (dpp-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
US20040236450A1 (en) 2000-09-25 2004-11-25 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
EP1334085B1 (en) 2000-11-02 2005-08-24 Merck Sharp & Dohme Ltd. 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
PL365027A1 (en) 2001-03-01 2004-12-27 Shionogi & Co, Ltd. Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
TWI245761B (en) 2001-03-01 2005-12-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
JP2005506292A (ja) 2001-03-08 2005-03-03 エモリー ユニバーシティ pHに依存するNMDAレセプターアンタゴニスト
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
CA2448834A1 (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
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
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
ATE370943T1 (de) 2001-06-27 2007-09-15 Smithkline Beecham Corp Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
CN1471538A (zh) 2001-06-27 2004-01-28 前体生物药物股份有限公司 用于竞争性调节二肽基肽酶iv催化的肽结构
HUP0400321A2 (hu) 2001-06-27 2004-08-30 Smithkline Beecham Corp. Fluorpirrolidin-származékok mint dipeptidil-dipeptidáz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
WO2003002596A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Use of dipeptidyl peptidase iv inhibitors as therapeutics for neurological disorders
BR0210721A (pt) 2001-06-27 2004-07-20 Elan Pharm Inc Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição
EP1399420B1 (en) 2001-06-27 2007-12-05 SmithKline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
EP1404675B1 (en) 2001-07-03 2008-03-12 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
US6948038B2 (en) * 2001-07-24 2005-09-20 Microsoft Corporation System and method for backing up and restoring data
SK287726B6 (en) 2001-07-24 2011-07-06 Richter Gedeon Vegyeszet Carboxylic acid amide derivatives, their preparation, pharmaceutical compositions containing them and process for preparing pharmaceutical compositions
MXPA04001016A (es) 2001-08-03 2004-05-27 Schering Corp Derivados de sulfonamida como inhibidores de la gamma secretasa.
MXPA04001014A (es) 2001-08-03 2004-05-27 Schering Corp Novedosos inhibidores de la gama secretasa.
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
EP1426366A4 (en) 2001-09-14 2004-12-08 Mitsubishi Pharma Corp THIAZOLIDE DERIVATIVES AND THEIR MEDICAL USE
AU2002331311A1 (en) 2001-09-19 2003-04-01 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
AU2002359301B2 (en) 2001-10-23 2008-07-03 Comentis, Inc. Beta-secretase inhibitors and methods of use
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
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
AU2002360403A1 (en) 2001-11-19 2003-06-10 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
WO2003053368A2 (en) 2001-12-19 2003-07-03 Atherogenics, Inc. Chalcone derivatives and their use to treat diseases
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
WO2003059346A1 (en) 2002-01-18 2003-07-24 The Genetics Company Inc. Beta-secretase inhibitors
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
CA2474578C (en) 2002-02-13 2009-08-25 F. Hoffmann-La Roche Ag Novel pyridin- and pyrimidin-derivatives
EP1476429B1 (en) 2002-02-13 2005-11-16 F. Hoffmann-La Roche Ag Novel pyridine- and quinoline-derivatives
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
US7307164B2 (en) 2002-03-25 2007-12-11 Merck & Co., Inc. β-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE60318306T2 (de) 2002-03-29 2008-12-11 Eisai R&D Management Co., Ltd. (1-indanon)-(1,2,3,6-tetrahydropyridin)derivat
US6996738B2 (en) 2002-04-15 2006-02-07 Broadcom Corporation Robust and scalable de-skew method for data path skew control
BR0304562A (pt) 2002-04-24 2004-07-20 Hiroshi Mori Inibidor de gama-secretase
ATE413388T1 (de) 2002-04-26 2008-11-15 Schering Corp Muskarin antagonisten
WO2003099202A2 (en) 2002-05-17 2003-12-04 Merck & Co., Inc. Beta-secretase inhibitors
PT1509232E (pt) 2002-05-31 2009-01-07 Lundbeck & Co As H Uma combinação de um antagonista de nmda e inibidores da acetilcolina esterase para o tratamento da doença de alzheimer
EP1513808A2 (en) 2002-06-04 2005-03-16 Pfizer Products Inc. Fluorinated cyclic amides as dipeptidyl peptidase iv inhibitors
AU2003233010A1 (en) 2002-06-04 2003-12-19 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
US20050171300A1 (en) 2002-06-19 2005-08-04 Luc Moens Semi-gloss powder coating compositions
AU2003248259A1 (en) 2002-07-10 2004-02-02 Yamanouchi Pharmaceutical Co., Ltd. Novel azetidine derivative or salt thereof
AU2003251869A1 (en) 2002-07-15 2004-02-02 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
TW200410672A (en) 2002-07-19 2004-07-01 Merz Pharma Gmbh & Co Kgaa 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
SI1532149T1 (sl) 2002-08-21 2010-05-31 Boehringer Ingelheim Pharma amino piperidin il ksantini njihova priprava in njihova uporaba kot zdravila
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
KR20050042801A (ko) 2002-09-12 2005-05-10 자이단호진 가가쿠오요비겟세이료호겐쿠쇼 인간형 항인간 mcp-1 항체 및 그의 항체 단편
CA2497725C (en) 2002-09-19 2012-04-10 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
EP1539725A1 (en) 2002-09-20 2005-06-15 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
EP1554280B1 (en) 2002-10-07 2007-08-15 Merck & Co., Inc. Antidiabetic beta-amino heterocyclic dipeptidyl peptidase inhibitors
WO2004033455A2 (en) 2002-10-08 2004-04-22 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
CA2502269C (en) 2002-10-18 2009-12-22 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
UA83645C2 (ru) 2002-10-24 2008-08-11 Мерц Фарма Гмбх Унд Ко. Кгаа Фармацевтический продукт, который содержит производное 1-аминоциклогексана и ингибитор ацетилхолинестеразы, его применение
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
AU2003285296A1 (en) 2002-10-30 2004-05-25 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
WO2004043940A1 (en) 2002-11-07 2004-05-27 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CA2505098A1 (en) 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
AU2002952946A0 (en) 2002-11-27 2002-12-12 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
AU2003297564A1 (en) 2002-12-04 2004-06-23 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
WO2004052280A2 (en) 2002-12-10 2004-06-24 Imclone Systems Incorporated Anti-angiogenic compounds and their use in cancer treatment
US20040181075A1 (en) 2002-12-19 2004-09-16 Weingarten M. David 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
WO2004062625A2 (en) 2003-01-07 2004-07-29 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease
WO2004064778A2 (en) 2003-01-17 2004-08-05 Merck & Co. Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2006516573A (ja) 2003-01-31 2006-07-06 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
EP1592684B1 (en) 2003-02-04 2008-07-30 F. Hoffmann-La Roche Ag Malonamide derivatives as gamma-secretase inhibitors
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
US20040229816A1 (en) 2003-02-18 2004-11-18 Daniel Paris Anti-angiogenic and anti-tumoral properties of beta and gamma secretase inhibitors
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
WO2004076433A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
EP1454627A1 (en) 2003-03-06 2004-09-08 MyoContract Ltd. Alpha-Keto carbonyl calpain inhibitors
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
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CA2520125A1 (en) 2003-03-28 2004-10-14 Acadia Pharmaceuticals Inc. Muscarinic m1 receptor agonists for pain management
CN1863810B (zh) 2003-04-09 2010-12-01 惠氏公司 [2-(8,9-二氧代-2,6-二氮杂二环[5.2.0]壬-1(7)-烯-2-基)烷基]膦酸衍生物及其作为n-甲基-d-天冬氨酸(nmda)受体拮抗剂的应用
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
US7732162B2 (en) * 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
ZA200508439B (en) * 2003-05-05 2007-03-28 Probiodrug Ag Medical use of inhibitors of glutaminyl and glutamate cyclases
US8338120B2 (en) * 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
US20040229848A1 (en) 2003-05-05 2004-11-18 Hans-Ulrich Demuth Glutaminyl based DP IV-inhibitors
NZ568459A (en) * 2003-05-05 2009-06-26 Probiodrug Ag Use of effectors of glutaminyl and glutamate cyclases
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
PE20050555A1 (es) 2003-05-13 2005-07-19 Schering Corp Compuestos con puente n-arilsulfonilpiperidina como inhibidores de la gamma-secretasa
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
AU2004240563A1 (en) 2003-05-14 2004-12-02 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
NZ542797A (en) 2003-05-16 2007-12-21 Merck Sharp & Dohme Cyclohexyl sulfones comprising an additional fused ring cyclic sulfonamide group suitable for inhibition of gamma-secretase
US20050014743A1 (en) 2003-05-27 2005-01-20 Forest Laboratories, Inc. 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
CN1798556A (zh) 2003-06-06 2006-07-05 麦克公司 作为治疗或者预防糖尿病的二肽基肽酶抑制剂的稠合吲哚
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
CN1809544A (zh) 2003-06-17 2006-07-26 麦克公司 作为二肽基肽酶抑制剂用于治疗或预防糖尿病的环己基甘氨酸衍生物
BRPI0411509A (pt) 2003-06-20 2006-07-25 Hoffmann La Roche compostos, processo para a sua manufatura, composições farmacêuticas que compreendem os mesmos, método para tratamento e/ou profilaxia de enfermidades que estão associadas com dpp-iv e sua utilização
WO2005000848A1 (en) 2003-06-20 2005-01-06 F. Hoffmann-La Roche Ag Pyrido` 2, 1-a - isoquinoline derivatives as dpp-iv inhibitors
US7291620B2 (en) 2003-06-30 2007-11-06 Merck + Co., Inc. N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
EP1643986A4 (en) 2003-07-01 2009-04-08 Merck & Co Inc PHENYL ACARBOXYLATE BETA SECRETASE INHIBITORS FOR THE TREATMENT OF MORBUS ALZHEIMER
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
WO2005007199A1 (en) 2003-07-16 2005-01-27 Rvx Therapeutics, Inc. COMPOUNDS AND METHODS FOR DOWNREGULATING THE EFFECTS OF TGF-β
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
CA2529674A1 (en) 2003-07-28 2005-02-03 Merz Pharma Gmbh & Co. Kgaa The use of 1-amino-alkylcyclohexane compounds in the treatment of pain hypersensitivity
CA2533893A1 (en) 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
GB0318447D0 (en) 2003-08-05 2003-09-10 Merck Sharp & Dohme Therapeutic agents
ZA200602051B (en) 2003-08-13 2007-10-31 Takeda Pharmaceutical 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors
US7329746B2 (en) 2003-08-14 2008-02-12 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)
US20050065144A1 (en) 2003-09-08 2005-03-24 Syrrx, Inc. Dipeptidyl peptidase inhibitors
EP1699777B1 (en) 2003-09-08 2012-12-12 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
TW200530157A (en) 2003-09-09 2005-09-16 Japan Tobacco Inc Dipeptidyl peptidase iv inhibitor
GB0322140D0 (en) 2003-09-22 2003-10-22 Pfizer Ltd Combinations
ATE509917T1 (de) 2003-09-24 2011-06-15 Merck Sharp & Dohme Gamma-secretase-inhibitoren
CN1859904A (zh) 2003-10-03 2006-11-08 默克公司 用于治疗阿尔茨海默氏病的苄醚和苄氨基β-分泌酶抑制剂
AU2003269307A1 (en) 2003-10-06 2005-04-21 Torrent Pharmaceuticals Ltd. Azolidinecarbonitriles and their use as dpp-iv inhibitors
RU2356895C2 (ru) 2003-10-06 2009-05-27 Ф.Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ЗАМЕЩЕННОГО ДИБЕНЗОАЗЕПИНА И БЕНЗОДИАЗЕПИНА, ПОЛЕЗНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ γ-СЕКРЕТАЗЫ
EP1673366A1 (en) 2003-10-08 2006-06-28 Pfizer, Inc. 1-"2-(4-hydroxyphenyl)-2-hydroxyethyl]-piperidin-4-ol compounds as nmda receptor antagonists
NZ546322A (en) 2003-10-15 2008-11-28 Probiodrug Ag Use of effectors of glutaminyl and glutamate cyclases
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
JP2007509165A (ja) 2003-10-22 2007-04-12 メルツ・ファルマ・ゲゼルシヤフト・ミト・ベシュレンクテル・ハフツング・ウント・コンパニー・コマンデイトゲゼルシヤフト・アウフ・アクティーン アミロイドパシーにおいて、フィブリロジェニックAβペプチドの沈着を改変するために、1−アミノシクロヘキサン誘導体を使用する方法
EP1824846A2 (en) 2003-11-03 2007-08-29 Probiodrug AG Novel compounds for the treatment of neurological disorders
US20050171112A1 (en) * 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US7667044B2 (en) * 2003-11-03 2010-02-23 Probiodrug Ag Compounds for the treatment of neurological disorders
EP1680120A2 (en) * 2003-11-03 2006-07-19 Probiodrug AG Combinations useful for the treatment of neuronal disorders
WO2005044195A2 (en) 2003-11-04 2005-05-19 Merck & Co., Inc. Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
BRPI0416450A (pt) 2003-11-11 2007-03-06 Hoffmann La Roche derivados de ácido fosfìnico, inibidores de beta - secretase para o tratamento de mal de alzheimer
EP1997533B8 (en) 2003-11-12 2014-10-29 Sino-Med International Alliance, Inc. Heterocyclic boronic acid compounds, dipeptidyl peptidase IV inhibitors
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
EP1541148A1 (en) 2003-12-09 2005-06-15 Graffinity Pharmaceuticals Aktiengesellschaft Dpp-iv inhibitors
EP1541143A1 (en) 2003-12-09 2005-06-15 Graffinity Pharmaceuticals Aktiengesellschaft Dpp-iv inhibitors
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
CN100537523C (zh) 2003-12-19 2009-09-09 默克公司 用于治疗阿尔茨海默病的苯基酰胺和吡啶基酰胺类β-分泌酶抑制剂
CA2554617A1 (en) 2004-01-22 2005-08-04 Boehringer Ingelheim International Gmbh 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
CA2554809C (en) 2004-02-05 2014-04-29 Probiodrug Ag Novel n-alkyl thiourea- and thioamide-substituted imidazolyl inhibitors of glutaminyl cyclase
AU2005215775B2 (en) 2004-02-13 2011-02-03 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
DE502005007196D1 (de) 2004-02-18 2009-06-10 Boehringer Ingelheim Pharma 8-ä3-amino-piperidin-1-ylü-xanthine, deren herstellung und deren verwendung als dpp-iv hemmer
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 (en) 2004-03-05 2005-11-09 Graffinity Pharmaceuticals AG DPP-IV inhibitors
CA2559611C (en) 2004-03-09 2012-01-17 National Health Research Institutes Pyrrolidine compounds
BRPI0418639B8 (pt) 2004-03-15 2021-05-25 Takeda Pharmaceutical compostos inibidores de dipeptidil peptidase, assim como composição farmacêutica contendo os mesmos
JP2007529556A (ja) 2004-03-19 2007-10-25 アクソニクス インコーポレイテッド 認知障害の処置に有用なアセチルコリンエステラーゼ阻害剤およびn−メチル−d−アスパラギン酸拮抗剤
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
KR20070010144A (ko) 2004-04-05 2007-01-22 쉐링 코포레이션 신규한 감마 세크레타제 억제제
CA2563615A1 (en) 2004-04-20 2005-11-03 Merck & Co., Inc. 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
JP4764418B2 (ja) 2004-04-20 2011-09-07 メルク・シャープ・エンド・ドーム・コーポレイション アルツハイマー病の治療のためのβ−セクレターゼ阻害剤として有用な2,4,6−置換ピリジル誘導体化合物
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
US7687492B2 (en) 2004-05-04 2010-03-30 Merck Sharp & Dohme Corp. 1,2,4-Oxadiazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2005116014A1 (en) 2004-05-12 2005-12-08 Pfizer Products Inc. Proline derivatives and their use as dipeptidyl peptidase iv inhibitors
CA2566053A1 (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
CN1960990A (zh) 2004-05-18 2007-05-09 默克公司 作为用于治疗或预防糖尿病的二肽基肽酶-ⅳ抑制剂的环己基丙氨酸衍生物
EP1598341A1 (en) 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
EP1604989A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1604662A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft 1-[(3R)-Amino-4-(2-fluoro-phenyl)-butyl]-pyrrolidine-(2R)-carboxylic acid benzyl amine derivatives and related compounds as dipeptidyl peptidase IV (DPP-IV) inhibitors for the treatment of type 2 diabetes mellitus
EP1604980A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
US7714021B2 (en) 2004-06-15 2010-05-11 Merck & Co., Inc. Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
GB0413389D0 (en) 2004-06-16 2004-07-21 Astrazeneca Ab Chemical compounds
WO2006009886A1 (en) 2004-06-21 2006-01-26 Merck & Co., Inc. Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
CA2572289A1 (en) 2004-06-30 2006-08-17 Centocor, Inc. Anti-mcp-1 antibodies, compositions, methods and uses
WO2006004880A2 (en) 2004-06-30 2006-01-12 Schering Corporation Substituted n-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
EP1778220A1 (en) 2004-07-12 2007-05-02 Phenomix Corporation Constrained cyano compounds
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
MX2007000760A (es) 2004-07-22 2007-04-09 Schering Corp Amida sustituida inhibidora de b secretasa.
AR050184A1 (es) 2004-07-28 2006-10-04 Schering Corp 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 (en) 2004-08-05 2006-02-08 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Heterocyclic compounds useful as DPP-IV inhibitors
CN101005877A (zh) 2004-08-23 2007-07-25 默克公司 作为用于治疗或预防糖尿病的二肽基肽酶-ⅳ抑制剂的稠合三唑衍生物
AU2005276635A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
EP1781687A1 (en) 2004-08-25 2007-05-09 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
WO2006029850A1 (en) 2004-09-14 2006-03-23 The Genetics Company, Inc. Hydrazone derivatives and their use as beta secretase inhibitors
US7659289B2 (en) 2004-09-17 2010-02-09 Comentis, Inc. Hydroxyethylene-based β-secretase inhibitors and use thereof
AU2005286844A1 (en) 2004-09-17 2006-03-30 Comentis, Inc Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
ATE481969T1 (de) 2004-10-01 2010-10-15 Merck Sharp & Dohme Aminopiperidine als dipeptidylpeptidase-iv- inhibitoren zur behandlung oder prävention von diabetes
WO2006042103A2 (en) 2004-10-05 2006-04-20 Axys Pharmaceuticals, Inc. Reversible inhibitors of cathepsin b
EP1802308A1 (en) 2004-10-08 2007-07-04 Novartis AG Combination of organic compounds
EP1807087A2 (en) 2004-10-12 2007-07-18 Ernir Snorrason Inhibitors of acetylcholinesterase for treating skin diseases
AU2005295814A1 (en) 2004-10-13 2006-04-27 Merck & Co., Inc. Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of Alzhermer's disease
CA2626049A1 (en) 2004-10-15 2006-04-20 Biopharmacopae Design International Inc. Methods and therapeutic compositions comprising plant extracts for the treatment of cancer
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.
CA2585279A1 (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
US7678783B2 (en) 2004-11-17 2010-03-16 Merck Sharp & Dohme Corp. Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
ATE512147T1 (de) 2004-11-23 2011-06-15 Merck Sharp & Dohme Makrozyklische aminiopyridyl-beta-sekretase- hemmer zur behandlung von morbus alzheimer
JP2008520718A (ja) 2004-11-23 2008-06-19 メルク エンド カムパニー インコーポレーテッド アルツハイマー病の治療のためのβ−セクレターゼ阻害剤として有用な2,3,4,6−置換ピリジル誘導体化合物
KR101301429B1 (ko) 2004-11-23 2013-08-30 아다마스 파마슈티칼스, 인코포레이티드 서방성 코팅 또는 매트릭스 및 nmda 수용체 길항제를포함하는 조성물, 대상에 대한 상기 nmda 길항제의투여 방법
US8389578B2 (en) 2004-11-24 2013-03-05 Adamas Pharmaceuticals, Inc Composition and method for treating neurological disease
EP1819674B1 (en) 2004-11-29 2011-10-05 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
KR20070087096A (ko) * 2004-12-14 2007-08-27 아스트라제네카 아베 Dgat 억제제로서의 옥사디아졸 유도체
WO2006064375A2 (en) * 2004-12-16 2006-06-22 Ab Science Aminoaryl substituted five-membered ring heterocyclic compounds for the treatment of diseases
BRPI0519585A2 (pt) 2004-12-20 2009-02-25 Hoffmann La Roche compostos de fàrmula i; processo para a fabricaÇço de compostos de fàrmula i; composiÇÕes farmacÊuticas; mÉtodo para o tratamento e/ou profilaxia de doenÇas que estço associadas com a dpp-iv e usos destes compostos
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 (en) 2004-12-23 2012-08-22 Curaxis Pharmaceutical Corporation Acetylcholinesterase Inhibitors and leuprolide acetate for the treatment of Alzheimer's disease
EP1831172B1 (en) 2004-12-28 2009-02-18 Council of Scientific and Industrial Research Substituted carbamic acid quinolin-6-yl esters useful as acetylcholinesterase inhibitors
AU2006204038A1 (en) 2005-01-06 2006-07-13 Merck & Co., Inc. Drug combination therapy and pharmaceutical compositions for treating inflammatory disorders
EP1855679B1 (en) 2005-01-19 2016-06-29 Merck Sharp & Dohme Corp. Aminomethyl beta-secretase inhibitors for the treatment of alzheimer's disease
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
WO2006099352A1 (en) 2005-03-10 2006-09-21 Bristol-Myers Squibb Company Novel 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
EP2082041B1 (en) * 2006-09-21 2018-03-14 Probiodrug AG Novel genes related to glutaminyl cyclase

Also Published As

Publication number Publication date
JP2010511013A (ja) 2010-04-08
SI2091948T1 (sl) 2012-07-31
ATE554085T1 (de) 2012-05-15
JP5523107B2 (ja) 2014-06-18
US20080214620A1 (en) 2008-09-04
EP2091948A1 (en) 2009-08-26
US9126987B2 (en) 2015-09-08
EP2091948B1 (en) 2012-04-18
WO2008065141A1 (en) 2008-06-05

Similar Documents

Publication Publication Date Title
DK2091948T3 (da) Nye inhibitorer af glutaminylcyclase
BRPI1009333B8 (pt) compostos inibidores de beta-secretase, seus usos, bem como composição farmacêutica
NO20083909L (no) Bisykliske benzimidazolforbindelser, og deres anvendelse som metabotropiske glutamatreseptorforsterkere
NO20073791L (no) Pyrazolylaminopyridinderivater anvendbare som kinaseinhibitorer
ATE542813T1 (de) 6-substituierte 2- heterocyclylaminopyrazinverbindungen als chk-1- inhibitoren
EA201000113A1 (ru) Пиразольные соединения
CR10784A (es) Nuevos derivados de aminopirimidina como inhibidores de plki
EA201100189A1 (ru) Гетероарильные производные в качестве ингибиторов dgat1
ATE459622T1 (de) Tropanverbindungen
BRPI0910871A2 (pt) derivados espirocíclicos como inibidores de histona desacetilase
MX2011012627A (es) Derivados aminobutiricos sustituidos como inhibidores de nepralisina.
EA200900812A1 (ru) Производные 4-имидазолил-1,2,3,4-тетрагидрохинолина и их применение в качестве ингибиторов альдостерон/11-бета-гидроксилазы
ATE499367T1 (de) 1,3-dihydroimidazol-2-thionderivate als inhibitoren von dopamin-beta-hydroxylase
UA107784C2 (en) Inhibitor of melanin production
EA201101621A1 (ru) Производные бензоксазолона в качестве ингибиторов альдостеронсинтазы
NO20085107L (no) Spirosykliske nitriler som proteaseinhibitorer
ATE440833T1 (de) Antithrombotische diamide
EA200900090A1 (ru) Бензиламины, способ их получения и их применение в качестве противовоспалительных средств
NO20085317L (no) Imidazoazepinonforbindelser
MA33915B1 (fr) Nouveaux derives d' (heterocycle-piperidine condensee)-(piperazinyl)-1-alcanone ou d' (heterocycle-pyrrolidine condensee)-(piperazinyl)-1-alcanone et leur utilisation comme inhibiteurs de p75
EA200700360A1 (ru) Новые производные амида гетероциклической карбоновой кислоты
ATE550326T1 (de) Als modulatoren von hdl einsetzbare verbindungen
DE602007005387D1 (de) Ptors
DE502006008710D1 (de) Substituierte tetrahydroisochinoline als mmp-inhibitoren, verfahren zu ihrer herstellung und ihre verwendung als medikament
DK1723140T3 (da) Fremgangsmåde til fremstilling af tryptase-inhibitorer