ES2548913T3 - Derivados heterocíclicos como inhibidores de glutaminil ciclasa - Google Patents

Derivados heterocíclicos como inhibidores de glutaminil ciclasa Download PDF

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Publication number
ES2548913T3
ES2548913T3 ES10751952.2T ES10751952T ES2548913T3 ES 2548913 T3 ES2548913 T3 ES 2548913T3 ES 10751952 T ES10751952 T ES 10751952T ES 2548913 T3 ES2548913 T3 ES 2548913T3
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Prior art keywords
phenyl
alkyl
benzo
substituted
imidazol
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ES10751952.2T
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English (en)
Spanish (es)
Inventor
Ulrich Heiser
Robert Sommer
Daniel Ramsbeck
Antje Meyer
Torsten Hoffmann
Livia Boehme
Hans-Ulrich Demuth
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Vivoryon Therapeutics AG
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Probiodrug AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • A—HUMAN NECESSITIES
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    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D471/04—Ortho-condensed systems

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ES10751952.2T 2009-09-11 2010-09-13 Derivados heterocíclicos como inhibidores de glutaminil ciclasa Active ES2548913T3 (es)

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Application Number Priority Date Filing Date Title
US24143209P 2009-09-11 2009-09-11
US241432P 2009-09-11
PCT/EP2010/063341 WO2011029920A1 (en) 2009-09-11 2010-09-13 Heterocylcic derivatives as inhibitors of glutaminyl cyclase

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ES2548913T3 true ES2548913T3 (es) 2015-10-21

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EP (1) EP2475428B1 (OSRAM)
JP (1) JP5934645B2 (OSRAM)
KR (1) KR101755737B1 (OSRAM)
CN (1) CN102695546B (OSRAM)
AU (1) AU2010294214B2 (OSRAM)
BR (1) BR112012008346B1 (OSRAM)
CA (1) CA2772488C (OSRAM)
DK (1) DK2475428T3 (OSRAM)
EA (1) EA022007B1 (OSRAM)
ES (1) ES2548913T3 (OSRAM)
IL (1) IL218259A (OSRAM)
MX (1) MX2012002993A (OSRAM)
NZ (1) NZ598685A (OSRAM)
PL (1) PL2475428T3 (OSRAM)
SG (1) SG178953A1 (OSRAM)
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Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
SG10201604304RA (en) * 2011-05-27 2016-07-28 Probiodrug Ag Radiolabelled glutaminyl cyclase inhibitors
JP6454651B2 (ja) * 2013-03-15 2019-01-23 プロビオドルグ エージー 新規阻害剤
FI2968346T3 (fi) 2013-03-15 2024-05-06 Cancer Research Tech Llc Menetelmiä ja koostumuksia gamma-glutamyylisyklin muokkaamiseksi
TWI477479B (zh) * 2013-07-18 2015-03-21 Daxin Materials Corp 二胺苯化合物、聚合物、配向膜用組成物、配向膜以及液晶顯示元件
DE102015011780A1 (de) * 2015-09-16 2017-03-16 Hochschule Anhalt Neue Glutaminylcyclase-lnhibitoren
GB201705263D0 (en) 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
DK3658141T3 (da) 2017-07-24 2023-02-06 Stichting Het Nederlands Kanker Inst Antoni Van Leeuwenhoek Ziekenhuis Behandling af patologiske tilstande ved direkte og indirekte målretning af Sirpalpha-CD47-interaktion
EP3461819B1 (en) * 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase
MX2020003546A (es) 2017-10-10 2020-08-03 Douglas Pharmaceuticals Ltd Formulacion farmaceutica de liberacion prolongada y metodos de tratamiento.
US10869838B2 (en) 2017-10-10 2020-12-22 Douglas Pharmaceuticals, Ltd. Extended release pharmaceutical formulation
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
JP2021512960A (ja) * 2018-02-06 2021-05-20 シャンハイ ハイファ ファーマシューティカル カンパニー，リミティッド Ｂｅｔ阻害活性を有する化合物並びにその製造方法及び使用
AU2019223215B2 (en) * 2018-02-23 2022-09-15 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Novel inhibitors of bacterial glutaminyl cyclases for use in the treatment of periodontal and related diseases
TWI715156B (zh) * 2018-08-31 2021-01-01 財團法人國家衛生研究院 苯并咪唑化合物及其用於治療阿茲海默症或亨丁頓氏症之用途
WO2020047360A1 (en) * 2018-08-31 2020-03-05 National Health Research Institutes Benzimidazole compounds and use thereof for treating alzheimer's disease or huntington's disease
GB201918410D0 (en) * 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of alpha1-antitrypsin deficiency
AU2022298746A1 (en) 2021-06-24 2023-11-30 Insilico Medicine Ip Limited Beta-lactam derivatives for the treatment of diseases
AU2022203580A1 (en) * 2021-09-17 2023-04-06 Academia Sinica Methods of Increasing Cell Phagocytosis
CN115448892B (zh) * 2022-09-19 2023-07-07 郑州铁路职业技术学院 一种苯并噻二唑杂环化合物的合成方法
EP4455142A1 (en) 2023-04-26 2024-10-30 Scenic Immunology B.V. Novel inhibitor of qpctl and/or qc
US20250026738A1 (en) 2023-06-16 2025-01-23 Vivoryon Therapeutics N.V. Crystalline pharmaceutically acceptable salt and polymorphic form of the glutaminyl cyclase inhibitor varoglutamstat
WO2025021012A1 (en) * 2023-07-21 2025-01-30 Insilico Medicine Ip Limited Crystalline beta-lactam derivatives and uses thereof
WO2025224179A1 (en) 2024-04-23 2025-10-30 Vivoryon Therapeutics N.V. Glutaminyl cyclase inhbitors for use in the treatment of kidney disease
WO2025224169A1 (en) 2024-04-23 2025-10-30 Vivoryon Therapeutics N.V. Dose regimens for the glutaminyl cyclase inhibitor varoglutamstat

Family Cites Families (596)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JPS6172439A (ja) 1984-09-18 1986-04-14 Sanyo Electric Co Ltd デ−タ転送方式
DE3684633D1 (de) 1985-04-16 1992-05-07 Suntory Ltd Dipeptid-derivate von fettsaeure, verfahren zu ihrer herstellung, heilmittel, das sie enthaelt und anwendung.
JPH0623190B2 (ja) 1985-04-16 1994-03-30 サントリー株式会社 インヒビタ−活性を有するｎ−アシルピロリジン誘導体及びその製法並びに用途
US4873342A (en) 1985-04-16 1989-10-10 Suntory Limited 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
CA1334092C (en) 1986-07-11 1995-01-24 David John Carini Angiotensin ii receptor blocking imidazoles
US5223482A (en) 1986-11-17 1993-06-29 Scios Nova Inc. Recombinant Alzheimer's protease inhibitory amyloid protein and method of use
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
DE3786229T2 (de) 1986-11-20 1993-10-07 Ono Pharmaceutical Co 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
EP0277588B1 (en) 1987-02-04 1993-03-24 Ono Pharmaceutical Co., Ltd. Prolinal derivatives
JP2528343B2 (ja) 1987-02-04 1996-08-28 小野薬品工業株式会社 新規なプロリナ―ル誘導体
DE3875361T2 (de) 1987-02-23 1993-03-25 Ono Pharmaceutical Co 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
CA1339014C (en) 1987-10-08 1997-03-25 Ronald E. Majocha Antibodies to a4 amyloid peptide
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
EP0419683A4 (en) 1989-04-13 1992-03-11 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
AU5525090A (en) 1989-04-14 1990-11-16 Research Foundation For Mental Hygiene, Inc. Monoclonal antibody to amyloid peptide
AU5439790A (en) 1989-04-14 1990-11-16 Research Foundation For Mental Hygiene, Inc. Cerebrovascular amyloid protein-specific monoclonal antibody sv17-6e10
ATE190051T1 (de) 1989-06-14 2000-03-15 Smithkline Beecham Corp Imidazoalkensäure
JPH082791B2 (ja) 1989-07-24 1996-01-17 キッセイ薬品工業株式会社 健忘症治療剤
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
DE122010000024I1 (de) 1990-02-19 2010-07-08 Novartis Ag Acylverbindungen
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
PT97078B (pt) 1990-03-20 1997-07-31 Sanofi Sa Processo para a preparacao de derivados heterociclicos n-substituidos e de composicoes farmaceuticas que os contem
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
US5196444A (en) 1990-04-27 1993-03-23 Takeda Chemical Industries, Ltd. 1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and compositions and methods of pharmaceutical use thereof
JPH049367A (ja) 1990-04-26 1992-01-14 Zeria Pharmaceut Co Ltd アリールアルカノイル誘導体，該化合物の製造中間体及びそれらを含有する医薬
EP0536163A1 (en) 1990-06-04 1993-04-14 Pfizer Inc. Aromatic pyrrolidine and thiazolidine amides
US5407950A (en) 1990-06-07 1995-04-18 Zeria Pharmaceutical Co., Ltd. Arylalkanoylamine derivative and drug containing the same
JPH07108897B2 (ja) 1990-07-27 1995-11-22 日本たばこ産業株式会社 新規なプロリン誘導体
EP0468469A2 (en) 1990-07-27 1992-01-29 Japan Tobacco Inc. Proline derivatives
JPH05186498A (ja) 1991-12-27 1993-07-27 Japan Tobacco Inc プロリン誘導体
US5506256A (en) 1990-07-27 1996-04-09 Yoshitomi Pharmaceutical Industries, Ltd. Proline derivatives possessing prolyl endopeptidase-inhibitory activity
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
IE920540A1 (en) 1991-02-21 1992-08-26 Sankyo Co 1-biphenylmethylimidazole derivatives, their preparation and¹their therapetuic use
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
ATE157988T1 (de) 1991-06-20 1997-09-15 Snow Brand Milk Products Co Ltd Neuartige prolyl-endopeptidase-inhibitoren sna- 115 und sna-115t, ihre herstellung, und hierbei verwendete stämme
DE4121975A1 (de) 1991-07-03 1993-01-07 Basf Ag Thermoplastische formmassen auf der basis von polycarbonaten, styrol/acrylnitril-polymerisaten und polyolefinen
JP3010795B2 (ja) 1991-07-04 2000-02-21 不二製油株式会社 ペプチドの苦味除去方法
CA2113115A1 (en) 1991-07-29 1993-02-18 Vlad E. Gregor Quinazoline derivatives as acetylcholinesterase inhibitors
TW226375B (OSRAM) 1991-10-24 1994-07-11 American Home Prod
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
PT664291E (pt) 1992-10-05 2000-11-30 Ube Industries Composto de pirimidina
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
WO1994017197A1 (fr) 1993-01-25 1994-08-04 Takeda Chemical Industries, Ltd. ANTICORPS DIRIGE CONTRE LE β-AMYLOIDE OU UN DERIVE DE CE DERNIER ET SON UTILISATION
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
WO1994020476A1 (fr) 1993-03-02 1994-09-15 Fujisawa Pharmaceutical Co., Ltd. Nouveau compose heterocyclique
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
AU6983894A (en) 1993-06-30 1995-01-24 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.
EP0709373B1 (en) 1993-07-23 2001-10-17 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Pyrrolidine derivative
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.
EP0731788B1 (en) 1993-12-02 2002-09-11 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.
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 .
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.
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
IL115613A0 (en) 1994-10-20 1996-01-19 Lilly Co Eli Bicyclic neuropeptide y receptor antagonists
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
US5786180A (en) 1995-02-14 1998-07-28 Bayer Corporation Monoclonal antibody 369.2B specific for β A4 peptide
US5552411A (en) 1995-05-26 1996-09-03 Warner-Lambert Company Sulfonylquinolines as central nervous system and cardiovascular agents
IL117997A0 (en) 1995-06-07 1996-10-31 Pfizer Neuropeptide Y1 specific ligands
US5668151A (en) 1995-06-07 1997-09-16 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: piperidine derivatives
US5635503A (en) 1995-06-07 1997-06-03 Bristol-Myers Squibb Company Dihydropyridine npy antagonists: piperazine derivatives
US5554621A (en) 1995-06-07 1996-09-10 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: nitrogen heterocyclic 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
WO1997012613A1 (en) 1995-10-05 1997-04-10 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
DE19544686A1 (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
WO1997020821A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
WO1997020820A1 (en) 1995-12-01 1997-06-12 Novartis 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
AU7692896A (en) 1995-12-01 1997-06-27 Novartis Ag Quinazolin-2,4-diazirines as NPY receptor antagonist
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
PT892796E (pt) 1996-04-12 2002-03-28 Aventis Pharma Inc Derivados de isatina como inibidores de acetilcolinesterase e analgesicos
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)
ES2184111T3 (es) 1996-07-05 2003-04-01 Wwk Trust Composiciones para el tratamiento de neuropatias perifericas que contienen antidepresivos y/o inhibidores de la monoaminoxidasa y/o vitamina b12 y/o precursores o inductores de un neurotransmisor.
EP0915860A1 (en) 1996-07-23 1999-05-19 Neurogen Corporation Certain substituted benzylamine derivatives; a new class of neuropeptide-y1 specific ligands
EP0915859B1 (en) 1996-07-23 2003-01-02 Neurogen Corporation Certain substituted benzylamine derivatives; a new class of neuropeptide y1 specific ligands
DK0918761T3 (da) 1996-07-23 2003-08-25 Neurogen Corp Visse amido- og aminosubstituerede benzylaminderivater, en ny klasse af neuropeptid Y1-specifikke ligander
WO1998005337A1 (en) 1996-08-01 1998-02-12 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
PT984778E (pt) 1996-08-23 2002-09-30 Agouron Pharma Ligandos do neuropeptido 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
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
US20030068316A1 (en) 1997-02-05 2003-04-10 Klein William L. Anti-ADDL antibodies and uses thereof
JP2894445B2 (ja) 1997-02-12 1999-05-24 日本たばこ産業株式会社 Ｃｅｔｐ活性阻害剤として有効な化合物
CA2284001A1 (en) 1997-03-13 1998-09-17 Keith Tipton Cytoprotective agents comprising monoamine oxidase inhibitors
NZ337765A (en) 1997-04-09 2001-09-28 Mindset Biopharmaceuticals Usa Recombinant antibodies having specificity for beta-amyloid N-terminus and C-terminus and use in treating Alzheimer's Disease
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
WO1998046559A1 (en) 1997-04-16 1998-10-22 Arqule, Inc. SYNTHESIS AND USE OF α-KETOAMIDE DERIVATIVES AND ARRAYS
WO1998050075A1 (en) 1997-05-07 1998-11-12 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
EP0980247A1 (en) 1997-05-07 2000-02-23 Algos Pharmaceutical Corporation Composition and method combining an antidepressant with an nmda receptor antagonist, for treating neuropathic pain
JP3963488B2 (ja) 1997-06-30 2007-08-22 メルツ ファーマ ゲゼルシャフト ミット ベシュレンクテル ハフツンク ウント コンパニー コマンディゲゼルシャフト アウフ アクチェン １−アミノ−アルキルシクロヘキサンｎｍｄａ受容体拮抗薬
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
US7179892B2 (en) 2000-12-06 2007-02-20 Neuralab Limited Humanized antibodies that recognize beta amyloid peptide
US7964192B1 (en) 1997-12-02 2011-06-21 Janssen Alzheimer Immunotherapy Prevention and treatment of amyloidgenic disease
TWI239847B (en) 1997-12-02 2005-09-21 Elan Pharm Inc N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease
WO1999038501A2 (en) 1998-02-02 1999-08-05 Trustees Of Tufts College Method of regulating glucose metabolism, and reagents related thereto
AU3034299A (en) 1998-03-09 1999-09-27 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
WO1999057120A1 (en) 1998-05-04 1999-11-11 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
DK1078005T3 (da) 1998-05-21 2010-08-09 Univ Tennessee Res Foundation Fremgangsmåder til amyloidfjernelse ved anvendelse af anti-amyloidantistoffer
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
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
IT1304904B1 (it) 1998-09-11 2001-04-05 Eisai Co Ltd Derivati anticolinesterasici per il trattamento delle sindromidolorose funzionali e/o organiche
AU1408699A (en) 1998-11-12 2000-06-05 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
WO2000030674A1 (en) 1998-11-26 2000-06-02 Ferring Bv Neuropeptide y y4 agents in the treatment of reproductive disorders
GB9902459D0 (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
GB9902452D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902453D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
WO2000056711A1 (en) 1999-03-23 2000-09-28 Sumitomo Pharmaceuticals Co., Ltd. Tricyclic indole-2-carboxylic acid compound used as nmda receptor antagonist
CA2363984A1 (en) 1999-04-15 2000-10-26 Merck Frosst Canada & Co. Antibodies that recognize app cleaved by caspases and methods of use
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
WO2000077178A1 (en) 1999-06-16 2000-12-21 Boston Biomedical Research Institute IMMUNOLOGICAL CONTROL OF β-AMYLOID LEVELS IN VIVO
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
WO2001000215A1 (en) 1999-06-25 2001-01-04 Wake Forest University Compositions for treating or preventing neurodegeneration and cognitive decline
US6316449B1 (en) 1999-07-08 2001-11-13 Millennium Pharmaceuticals, Inc. Chemokine receptor antagonists
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
JP2003507013A (ja) 1999-08-13 2003-02-25 ザ・トラスティーズ・オブ・コランビア・ユニバーシティー・イン・ザ・シティー・オブ・ニューヨーク βシートフィブリルのＲＡＧＥへの結合を阻害する方法及びその結果
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
AU1916401A (en) 1999-11-12 2001-06-06 Guilford Pharmaceuticals Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
US20020094335A1 (en) 1999-11-29 2002-07-18 Robert Chalifour Vaccine for the prevention and treatment of alzheimer's and amyloid related diseases
GB9928330D0 (en) 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
AU2001228309A1 (en) 2000-01-24 2001-08-07 Novo-Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
AU779875B2 (en) 2000-01-24 2005-02-17 Merck Sharp & Dohme Limited Gamma-secretase inhibitors
CA2399080C (en) 2000-02-03 2013-05-21 Millennium Pharmaceuticals, Inc. Humanized anti-ccr2 antibodies and methods of use therefor
SI1257584T2 (sl) 2000-02-24 2013-07-31 Washington University St. Louis Humanizirana protitelesa, ki veĹľejo amiloidni peptid beta
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
JP2003528071A (ja) 2000-03-23 2003-09-24 エラン ファーマスーティカルズ インコーポレイテッド アルツハイマー病治療用組成物および方法
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
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
ATE337292T1 (de) 2000-04-26 2006-09-15 Warner Lambert Co Trans-n- 4-(4-hydroxyphenyl)cyclohexylö-3- phenylpropionamid als subtyp-selektiver nmda rezeptor antagonist
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
CA2410660A1 (en) 2000-06-01 2001-12-06 Warner-Lambert Company Cyclohexylamine derivatives as subtype selective nmda receptor antagonists
MXPA02010503A (es) 2000-06-06 2003-03-10 Warner Lambert Co Ciclohexilaminas biciclicas y su uso como antagonistas del receptor nmda.
EP1299374B1 (en) 2000-06-22 2006-12-27 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
US6686449B2 (en) 2000-06-30 2004-02-03 Pharmacia & Upjohn Company Mutant presenilin 1 polypeptides
ATE302751T1 (de) 2000-06-30 2005-09-15 Elan Pharm Inc Verbindungen zur behandlung der alzheimerischen krankheit
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
US7179912B2 (en) * 2000-09-01 2007-02-20 Icos Corporation Materials and methods to potentiate cancer treatment
US6556971B1 (en) 2000-09-01 2003-04-29 Snap-On Technologies, Inc. Computer-implemented speech recognition system training
WO2002027418A2 (en) 2000-09-25 2002-04-04 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
AU1074702A (en) 2000-11-02 2002-05-15 Merck Sharp & Dohme Sulfamides as gamma-secretase inhibitors
US20020150948A1 (en) 2000-11-03 2002-10-17 Gerardo Castillo Antibody PTI-HS7 for treatment of alzheimer's disease and other amyloidoses and parkinson's disease
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
TWI255272B (en) 2000-12-06 2006-05-21 Guriq Basi Humanized antibodies that recognize beta amyloid peptide
US6495335B2 (en) 2000-12-07 2002-12-17 Mario Chojkier Compositions and methods for diagnosing alzheimer's disease
US6670364B2 (en) 2001-01-31 2003-12-30 Telik, Inc. Antagonists of MCP-1 function and methods of use thereof
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
US6815175B2 (en) 2001-03-16 2004-11-09 Cornell Research Foundation, Inc. Anti-amyloid peptide antibody based diagnosis and treatment of a neurological disease or disorder
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
ES2437875T3 (es) 2001-04-30 2014-01-14 Eli Lilly And Company Anticuerpos humanizados que reconocen el péptido beta-amiloide
AU2002257162A1 (en) 2001-04-30 2002-11-11 Eli Lilly And Company Humanized antibodies
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
MXPA03011046A (es) 2001-06-01 2004-06-25 Elan Pharm Inc Hidroxialquilaminas.
DE60209348T2 (de) 2001-06-20 2006-10-12 Merck & Co., Inc. Dipeptidylpeptidase-hemmer zur behandlung von diabetes
CA2450579A1 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
IL158923A0 (en) 2001-06-27 2004-05-12 Smithkline Beecham Corp Fluoropyrrolidines as dipeptidyl peptidase inhibitors
RU2299066C2 (ru) 2001-06-27 2007-05-20 Пробиодруг Аг Новые ингибиторы дипептидилпептидазы iv и их применение в качестве противораковых агентов
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
ATE380175T1 (de) 2001-06-27 2007-12-15 Smithkline Beecham Corp Pyrrolidine als dipeptidyl peptidase inhibitoren
WO2003072556A1 (en) 2001-06-27 2003-09-04 Prosidion Ltd. Glutaminyl based dpiv inhibitors
WO2003002553A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
MXPA04000140A (es) 2001-06-27 2004-06-03 Elan Pharm Inc Derivados de beta-hidroxiamina utiles en el tratamiento de enfermedad de alzheimer.
ATE388951T1 (de) 2001-07-03 2008-03-15 Novo Nordisk As 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
MXPA04000737A (es) 2001-07-24 2004-07-08 Richter Gedeon Vegyeszet Derivados de piperidina como antagonistas receptores de nmda.
WO2003012141A1 (en) 2001-07-31 2003-02-13 Takeda Chemical Industries, Ltd. Method of screening alzheimer’s disease-associated gene
EP1420032B2 (en) 2001-08-03 2015-12-16 Medical & Biological Laboratories Co., Ltd. Antibody recognizing gm1 ganglioside-bound amyloid beta-protein and dna encoding the antibody
BR0211698A (pt) 2001-08-03 2004-11-09 Schering Corp Inibidores de gama-secretase
WO2003013527A1 (en) 2001-08-03 2003-02-20 Schering Corporation Sulfonamide derivatives as gamma secretase inhibitors
US20040192898A1 (en) 2001-08-17 2004-09-30 Jia Audrey Yunhua Anti-abeta antibodies
AU2002324468A1 (en) 2001-08-17 2003-03-03 Eli Lilly And Company Rapid improvement of cognition in conditions related to abeta
EP1423127A1 (en) 2001-08-30 2004-06-02 Ortho-Mcneil Pharmaceutical, Inc. Treatment of dementia and memory disorders with anticonvulsants and acetylcholinesterase inhibitors
JPWO2003024942A1 (ja) 2001-09-14 2004-12-24 三菱ウェルファーマ株式会社 チアゾリジン誘導体およびその医薬用途
JP2005509603A (ja) 2001-09-19 2005-04-14 ノボ　ノルディスク　アクティーゼルスカブ Ｄｐｐ−ｉｖ酵素の阻害剤であるヘテロ環化合物
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
EP1448218A4 (en) 2001-10-23 2009-01-14 Oklahoma Med Res Found BETA SECRETASE INHIBITORS AND METHODS OF USE
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
CN100488982C (zh) 2001-11-02 2009-05-20 迪尔基因国际有限公司 与β-淀粉样蛋白结合并引起蛋白质构象转变的单克隆抗体的制备方法
EP1447095B1 (en) 2001-11-02 2012-06-13 Kensuke Egashira Preventives and/or remedies for post-transplant arteriosclerosis as rejection of organ transplant
WO2003040183A2 (en) 2001-11-09 2003-05-15 The Genetics Company, Inc Compounds for the diagnosis/prevention/treatment of alzheimer's disease
RS54204A (sr) 2001-11-19 2006-12-15 Elan Pharmaceuticals Inc. 3,4-disupstituisani, 3,5-disupstituisani i 3,4,5- supstituisani piperidini i piperazini
EP1572894B1 (en) 2001-11-21 2016-04-13 New York University Synthetic immunogenic but non-deposit-forming polypeptides and peptides homologous to amyloid beta, prion protein, amylin, alpha synuclein, or polyglutamine repeats for induction of an immune response thereto
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
AU2002354433A1 (en) 2001-12-06 2003-06-17 Japan As Represented By Secretary Of Chubu National Hospital Alzheimer's disease-associated gene and protein and use thereof
WO2003051374A2 (en) 2001-12-17 2003-06-26 New York State Office Of Mental Health SEQUESTRATION OF Aβ IN THE PERIPHERY IN THE ABSENCE OF IMMUNOMODULATING AGENT AS A THERAPEUTIC APPROACH FOR THE TREATMENT OR PREVENTION OF BETA-AMYLOID RELATED DISEASES
BR0215240A (pt) 2001-12-19 2004-10-26 Atherogenics Inc Derivados de calcona e seu uso no tratamento de doenças
AU2002357359B2 (en) 2001-12-21 2009-01-08 Csl Limited Compositions comprising immunoreactive reagents and saponins, and methods of use thereof
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
AU2003235799A1 (en) 2002-01-08 2003-07-24 Nordic Bioscience A/S Modulation of iamt (pimt or pcmt) in immune system
CA2473441A1 (en) 2002-01-18 2003-07-24 The Genetics Company Inc. Beta-secretase inhibitors
US20070021345A1 (en) 2003-06-30 2007-01-25 Ehud Gazit Peptides antibodies directed thereagainst and methods using same for diagnosing and treating amyloid-associated diseases
KR20040081165A (ko) 2002-01-31 2004-09-20 텔 아비브 유니버시티 퓨쳐 테크놀로지 디벨롭먼트 엘.피. 펩타이드 항체 및 이를 이용한 아밀로이드-관련 질환의진단 및 치료 방법
US20040171614A1 (en) 2002-02-06 2004-09-02 Schering-Plough Corporation Novel gamma secretase inhibitors
TW200302717A (en) 2002-02-06 2003-08-16 Schering Corp Novel gamma secretase inhibitors
ATE309988T1 (de) 2002-02-13 2005-12-15 Hoffmann La Roche Neue pyridin- und quinolin-derivate
ES2345096T3 (es) 2002-02-13 2010-09-15 F. Hoffmann-La Roche Ag Nuevos derivados de piridina y pirimidina.
AR038568A1 (es) 2002-02-20 2005-01-19 Hoffmann La Roche Anticuerpos anti-a beta y su uso
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
MY139983A (en) 2002-03-12 2009-11-30 Janssen Alzheimer Immunotherap Humanized antibodies that recognize beta amyloid peptide
AU2003225916A1 (en) 2002-03-25 2003-10-13 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP4405811B2 (ja) 2002-03-29 2010-01-27 エーザイ・アール・アンド・ディー・マネジメント株式会社 （１−インダノン）−（１，２，３，６−テトラヒドロピリジン）誘導体
AU2003226356A1 (en) 2002-04-12 2003-10-27 Ramot At Tel Aviv University Ltd. Prevention of brain inflammation as a result of induced autoimmune response
JP4662719B2 (ja) 2002-04-19 2011-03-30 ザ ガバニング カウンシル オブ ザ ユニバーシティ オブ トロント アルツハイマー病の処置のための免疫学的方法および組成物
JP4404643B2 (ja) 2002-04-24 2010-01-27 啓 森 ガンマセクレターゼ阻害剤
CN1649845A (zh) 2002-04-26 2005-08-03 先灵公司 蝇蕈碱拮抗剂
US7205336B2 (en) 2002-05-17 2007-04-17 Merck & Co., Inc. β-secretase inhibitors
AU2003227516B2 (en) 2002-05-31 2008-03-20 H. Lundbeck A/S A combination of an NMDA-antagonist and acetylcholine esterase inhibitors for the treatment of alzheimer's disease
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
PL374007A1 (en) 2002-06-06 2005-09-19 Eisai Co, Ltd. Novel fused imidazole derivative
ATE357487T1 (de) 2002-06-19 2007-04-15 Cytec Surface Specialties Sa Halb-glänzende pulverbeschichtungszusammensetzungen
AU2003248259A1 (en) 2002-07-10 2004-02-02 Yamanouchi Pharmaceutical Co., Ltd. Novel azetidine derivative or salt thereof
JP4530852B2 (ja) 2002-07-15 2010-08-25 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病治療のためのピペリジノピリミジンジペプチジルペプチダーゼ阻害剤
EP1523309A2 (en) 2002-07-19 2005-04-20 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
KR101150449B1 (ko) 2002-08-21 2012-06-01 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 8-［3-아미노-피페리딘-1-일］-크산틴, 이의 제조방법 및 이를 포함하는 약제학적 조성물
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
ES2201929B1 (es) 2002-09-12 2005-05-16 Araclon Biotech, S.L. Anticuerpos policlonales, metodo de preparacion y uso de los mismos.
JP4426449B2 (ja) 2002-09-12 2010-03-03 財団法人化学及血清療法研究所 ヒト抗ヒトｍｃｐ−１抗体及び該抗体フラグメント
WO2010012004A2 (en) 2008-07-25 2010-01-28 The Regents Of The University Of California Monoclonal antibodies specific for pathological amyoid aggregates common to amyloids formed from proteins of differing sequence
US9535076B2 (en) 2002-09-12 2017-01-03 The Regents Of The University Of California Methods and compositions for eliciting an amyloid-selective immune response
US8871447B2 (en) 2002-09-12 2014-10-28 The Regents Of The University Of California Immunogens and corresponding antibodies specific for high molecular weight aggregation intermediates common to amyloids formed from proteins of differing sequence
CA2497725C (en) 2002-09-19 2012-04-10 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
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
WO2004029629A1 (en) 2002-09-27 2004-04-08 Janssen Pharmaceutica N.V. N-11 truncated amyloid-beta nomoclonal antibodies, compositions, methods and uses
WO2004031400A2 (en) 2002-10-01 2004-04-15 Northwestern University Amyloid beta-derived diffusible ligands (addls), addl-surrogates, addl-binding molecules, and uses thereof
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
JP4491346B2 (ja) 2002-10-07 2010-06-30 メルク・シャープ・エンド・ドーム・コーポレイション 抗糖尿病ベータアミノ複素環ジペプチジルペプチダーゼ阻害剤
WO2004033455A2 (en) 2002-10-08 2004-04-22 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
BR0315157A (pt) 2002-10-09 2005-08-09 Rinat Neuroscience Corp Métodos de tratar doença de alzheimer empregando-se anticorpos direcionados contra peptìdeo beta amilóide e composições deste
GB0223494D0 (en) 2002-10-09 2002-11-13 Neuropharma Sa Dual binding site acetylcholinesterase inhibitors for the treatment of alzheimer's disease
EP1556362B1 (en) 2002-10-18 2008-03-26 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2003274353B2 (en) 2002-10-24 2007-04-05 Merz Pharma Gmbh & Co. Kgaa Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase inhibitors
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
AU2003285296A1 (en) 2002-10-30 2004-05-25 Nordic Bioscience A/S Coumpounds modulating the activity of gapdh and/or iamt
AU2003286776A1 (en) 2002-10-30 2004-06-07 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
US7452911B2 (en) 2002-10-31 2008-11-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
GB0225474D0 (en) 2002-11-01 2002-12-11 Merck Sharp & Dohme Therapeutic agents
FR2846667B1 (fr) 2002-11-06 2004-12-31 Pasteur Institut Fragments variables d'anticorps de camelides a chaine unique diriges contre le peptide beta-amyloide 1-42 et leurs applications pour le diagnostic et le traitement des maladies neuroagregatives
AU2003290577B2 (en) 2002-11-07 2008-12-11 Merck Sharp & Dohme Corp. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
ATE443043T1 (de) 2002-11-12 2009-10-15 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
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
WO2004056727A2 (en) 2002-12-19 2004-07-08 Atherogenics, Inc. Process of making chalcone derivatives
WO2004058266A1 (en) 2002-12-20 2004-07-15 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CA2512111A1 (en) 2003-01-07 2004-07-29 Merck And Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease
EP1589969A4 (en) 2003-01-17 2008-08-13 Merck & Co Inc 3-AMINO-4-PHENYLBUTANEAN DERIVATEALS DIPEPTIDYLPEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
EP1592689A4 (en) 2003-01-31 2008-12-24 Merck & Co Inc 3-AMINO-4-PHENYLBUTANEAN DERIVATIVES AS DIPEPTIDYLPEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
DE10303974A1 (de) 2003-01-31 2004-08-05 Abbott Gmbh & Co. Kg Amyloid-β(1-42)-Oligomere, Verfahren zu deren Herstellung und deren Verwendung
PL378571A1 (pl) 2003-02-01 2006-05-02 Neuralab Limited Czynna immunizacja dla wytworzenia przeciwciał przeciw rozpuszczalnemu A-ß
PL378405A1 (pl) 2003-02-04 2006-04-03 F. Hoffmann-La Roche Ag Pochodne malonoamidu jako inhibitory <$Egamma> - sekretazy
WO2004071408A2 (en) 2003-02-10 2004-08-26 Applied Molecular Evolution, Inc. Aβ BINDING MOLECULES
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
CN1777436A (zh) 2003-02-18 2006-05-24 罗斯坎普研究有限责任公司 β和γ分泌酶抑制剂的抗血管生成和抗肿瘤性
US8663650B2 (en) 2003-02-21 2014-03-04 Ac Immune Sa Methods and compositions comprising supramolecular constructs
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
KR20060054174A (ko) 2003-03-28 2006-05-22 센토코 인코포레이티드 항-아밀로이드 항체, 조성물, 방법 및 용도
EP1611144B1 (en) 2003-04-09 2010-09-15 Wyeth LLC Derivatives of 2-(8,9-dioxo-2,6-diazabicyclo(5.2.0)non-1(7)-en-2-yl)alkyl phosphonic acid and their use as n-methyl-d-aspartate (nmda) recetor antagonists
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
CN1784220B (zh) 2003-05-05 2011-08-03 前体生物药物股份公司 谷氨酰胺酰基和谷氨酸环化酶效应物的应用
ZA200508439B (en) 2003-05-05 2007-03-28 Probiodrug Ag Medical use of inhibitors of glutaminyl and glutamate cyclases
WO2004099134A2 (en) 2003-05-05 2004-11-18 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
ES2246178B1 (es) 2003-05-08 2007-03-01 Universidad De Zaragoza. Uso de anticuerpos para el tratamiento de enfermedades amiloideas.
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
WO2004101562A2 (en) 2003-05-13 2004-11-25 Schering Corporation Bridged n-arylsulfonylpiperidines as gamma-secretase inhibitors
US7560455B2 (en) 2003-05-14 2009-07-14 Merck & Co., Inc. 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2007511467A (ja) 2003-05-14 2007-05-10 タケダ サン ディエゴ インコーポレイテッド ジペプチジルペプチダーゼインヒビター
EP1644346A1 (en) 2003-05-16 2006-04-12 MERCK SHARP &amp; DOHME LTD. Cyclic sulfonamides for inhibition of gamma-secretase
EA010430B1 (ru) 2003-05-27 2008-08-29 Форест Лэборэтериз, Инк. Сочетание антагониста nmda-рецептора и селективного ингибитора обратного захвата серотонина для лечения депрессии и других психических расстройств
TWI374893B (en) 2003-05-30 2012-10-21 Janssen Alzheimer Immunotherap Humanized antibodies that recognize beta amyloid peptide
AU2003902828A0 (en) 2003-06-05 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
EP1635818B1 (en) 2003-06-06 2010-04-07 Merck Sharp & Dohme Corp. 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
WO2004112701A2 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2005000846A1 (en) 2003-06-20 2005-01-06 F.Hoffmann-La Roche Ag Hexahydropyridoisoqinolines as dpp-iv inhibitors
MXPA05013904A (es) 2003-06-20 2006-02-24 Hoffmann La Roche Derivados de pirido[2,1-a] isoquinolinas como inhibidores de dipeptidil-peptidasa iv(dpp-iv).
AU2004255183A1 (en) 2003-06-30 2005-01-20 Merck & Co., Inc. N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
CN1909897A (zh) 2003-07-01 2007-02-07 默克公司 用于治疗阿尔茨海默病的苯基羧化物β－分泌酶抑制剂
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
DE602004027048D1 (de) 2003-07-16 2010-06-17 Resverlogix Inc Verbindungen und methoden für das downregulating der effekte von tgf-beta
EP1671129A1 (en) 2003-07-21 2006-06-21 Angiogenetics Sweden AB Compounds and methods for promoting angiogenesis by using a gamma-secretase inhibitor or inhibiting the gamma-secretase pathway
WO2005014041A2 (en) 2003-07-24 2005-02-17 Novartis Ag Use of an amyloid beta dna vaccine for the treatment and/or prevention of amyloid diseases
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
US7259160B2 (en) 2003-07-31 2007-08-21 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2005011599A2 (en) 2003-08-01 2005-02-10 Northwestern University Antibodies specific for toxic amyloid beta protein oligomers
GB0318447D0 (en) 2003-08-05 2003-09-10 Merck Sharp & Dohme Therapeutic agents
WO2005016911A1 (en) 2003-08-13 2005-02-24 Takeda Pharmaceutical Company Limited 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors
JP2007502278A (ja) 2003-08-14 2007-02-08 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大員環β−セクレターゼ阻害剤
WO2005018424A2 (en) 2003-08-18 2005-03-03 Research Foundation For Mental Hygiene, Inc. Antibodies specific for fibrillar amyloid and a procedure to detect fibrillar amyloid deposits
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)
WO2005023858A1 (en) 2003-09-05 2005-03-17 Cellzome Ag Protein complexes associated with app-processing
JP2007513058A (ja) 2003-09-08 2007-05-24 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
EP1699777B1 (en) 2003-09-08 2012-12-12 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CA2538220A1 (en) 2003-09-09 2005-03-24 Takeda Pharmaceutical Company Limited Use of antibody
PE20050948A1 (es) 2003-09-09 2005-12-16 Japan Tobacco Inc Compuestos de carbamoil-amina como inhibidores de la dipeptidil peptidasa iv
JP2007527865A (ja) 2003-09-12 2007-10-04 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 種々の配列を有するタンパク質から形成されたアミロイドに共通の高分子量凝集中間体に特異的なモノクローナル抗体
GB0322140D0 (en) 2003-09-22 2003-10-22 Pfizer Ltd Combinations
EP1667984B1 (en) 2003-09-24 2011-05-18 Merck Sharp & Dohme Ltd. Gamma-secretase inhibitors
ATE396973T1 (de) 2003-10-03 2008-06-15 Merck & Co Inc Benzylether- und benzylamino-beta-sekretase- hemmer zur behandlung von alzheimer-krankheit
CN1839131A (zh) 2003-10-06 2006-09-27 托伦脱药品有限公司 吡咯烷甲腈类化合物及其作为dpp－iv抑制剂的应用
PL1673347T3 (pl) 2003-10-06 2016-01-29 Hoffmann La Roche Podstawione pochodne dibenzo-azepiny i benzo-diazepiny użyteczne jako inhibitory gamma-sekretazy
WO2005035522A1 (en) 2003-10-08 2005-04-21 Pfizer Japan, Inc. 1-‘2-(4-hydroxyphenyl)-2-hydroxyethyl!-piperidin-4-ol compounds as nmda receptor antagonists
CN102302781A (zh) 2003-10-15 2012-01-04 前体生物药物股份公司 谷氨酰胺酰基环化酶效应物和谷氨酸环化酶效应物的应用
MXPA06003762A (es) 2003-10-16 2006-06-14 Boehringer Ingelheim Int Composicion farmaceutica que comprende un inhibidor de recaptacion de neurotransmisor monoamina y un inhibidor de acetilcolinesterasa.
GB0324236D0 (en) 2003-10-16 2003-11-19 Astrazeneca Ab Chemical compounds
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
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
US7674913B2 (en) 2003-11-12 2010-03-09 Phenomix Corporation Heterocyclic boronic acid compounds
JP4576386B2 (ja) 2003-11-24 2010-11-04 メルク・シャープ・エンド・ドーム・コーポレイション アルツハイマー病治療用のベンジルエーテルおよびベンジルアミノ系β−セクレターゼ阻害薬
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
EP1697308B1 (en) 2003-12-19 2014-03-19 Merck Sharp & Dohme Corp. Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease
AU2005205882A1 (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
CA2554959A1 (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
EP1713780B1 (en) 2004-02-05 2012-01-18 Probiodrug AG Novel 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
EP1758905B1 (de) 2004-02-18 2009-04-29 Boehringer Ingelheim International GmbH 8-[3-amino-piperidin-1-yl]-xanthine, deren herstellung und deren verwendung als dpp-iv hemmer
WO2005080435A1 (ja) 2004-02-20 2005-09-01 Immuno-Biological Laboratories Co., Ltd. モノクローナル抗体およびその利用
KR101292707B1 (ko) 2004-02-23 2013-08-02 트러스티즈 오브 터프츠 칼리지 디펩티딜펩티다아제 ⅳ의 억제제
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
UA85871C2 (uk) 2004-03-15 2009-03-10 Такеда Фармасьютікал Компані Лімітед Інгібітори дипептидилпептидази
US20070213388A1 (en) 2004-03-19 2007-09-13 Bruinsma Gosse B Acetylcholinesterase Inhibitors and N-Methyl-D-Aspartate Antagonists Useful in the Treatment of of Cognitive Disorders
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
AU2005230681B2 (en) 2004-04-05 2009-07-30 Schering Corporation Novel gamma secretase inhibitors
EP1740581B1 (en) 2004-04-20 2012-08-22 Merck Sharp & Dohme Corp. 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
CA2564432A1 (en) 2004-04-27 2005-11-10 Juridical Foundation The Chemo-Sero-Therapeutic Research Institute Human anti-amyloid .beta. peptide antibody and fragment of said antibody
JP2007536234A (ja) 2004-05-04 2007-12-13 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としての１，２，４−オキサジアゾール誘導体
HRP20090471T1 (hr) 2004-05-12 2009-10-31 Pfizer Products Inc. Derivati prolina i njihova upotreba kao inhibitori dipeptidil-peptidaze iv
US7449599B2 (en) 2004-05-13 2008-11-11 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 (en) 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1753730A1 (en) 2004-06-04 2007-02-21 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DE602005022871D1 (de) 2004-06-07 2010-09-23 Univ Ramot Verfahren zur passiven immunisierung gegen eine durch amyloidaggregation gekennzeichnete krankheit oder erkrankung mit vermindertem nervenentzündungsrisiko
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
EP1604989A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1604980A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1758854B1 (en) 2004-06-15 2014-07-16 Merck Sharp & Dohme Corp. 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
AU2005265148B2 (en) 2004-06-21 2011-01-20 Merck Sharp & Dohme Corp. Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
SE0401601D0 (sv) 2004-06-21 2004-06-21 Bioarctic Neuroscience Ab Protofibril specific antibodies and uses thereof
CA2572289A1 (en) 2004-06-30 2006-08-17 Centocor, Inc. Anti-mcp-1 antibodies, compositions, methods and uses
CA2570183A1 (en) 2004-06-30 2006-01-12 Schering Corporation Substituted n-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
WO2006014478A1 (en) 2004-07-02 2006-02-09 Northwestern University MONOLOCAL ANTIBODIES THAT TARGET PATHOLOGICAL ASSEMBLIES OF AMYLOID β (ABETA)
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
US20080038192A1 (en) 2004-07-19 2008-02-14 Neurochem Inc. Diagnostic Methods Of Multiple Organ Amyloidosis
WO2006014638A2 (en) 2004-07-19 2006-02-09 The General Hospital Corporation ANTIBODIES TO CROSS-LINKED AMYLOID β OLIGOMERS
AR049726A1 (es) 2004-07-22 2006-08-30 Schering Corp Amidas sustituidas inhibidoras de beta secretasa
ATE396990T1 (de) 2004-07-28 2008-06-15 Schering Corp Makrocyclische inhibitoren der beta-sekretase
HUP0401523A3 (en) 2004-07-29 2007-05-02 Richter Gedeon Vegyeszet Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them
MX2007000998A (es) 2004-07-30 2007-07-11 Rinat Neuroscience Corp Anticuerpos dirigidos peptido beta-amiloide y procedimientos que usan los mismos.
EP1623983A1 (en) 2004-08-05 2006-02-08 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Heterocyclic compounds useful as DPP-IV inhibitors
JP4820757B2 (ja) 2004-08-11 2011-11-24 国立大学法人京都大学 抗体及びその利用
EP1784188B1 (en) 2004-08-23 2010-07-14 Merck Sharp & Dohme Corp. Fused triazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
CA2577987A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
US20070293486A1 (en) 2004-08-25 2007-12-20 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
US7335491B2 (en) 2004-08-27 2008-02-26 Wyeth Research Ireland Limited Production of anti-abeta
JP2008513364A (ja) 2004-09-14 2008-05-01 ザ ジェネティクス カンパニー，インコーポレイテッド ヒドラゾン誘導体およびβ−セクレターゼインヒビターとしてのその使用
CA2580265A1 (en) 2004-09-17 2006-03-30 Comentis, Inc. Amino-containing compounds which inhibit memapsin 2 beta-secretase activity and methods of use thereof
EP1797052A1 (en) 2004-09-17 2007-06-20 Comentis, Inc. Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
US20060246075A1 (en) 2004-09-29 2006-11-02 Marc Mercken Anti-amyloid antibodies, compositions, methods and uses
CA2582447C (en) 2004-10-01 2012-04-17 Merck & Co., Inc. 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
RU2007116869A (ru) 2004-10-08 2008-11-20 Новартис АГ (CH) Комбинация органических соединений
EP2008660A1 (en) 2004-10-12 2008-12-31 Ernir Snorrason Inhibitors of acetylcholinesterase for treating skin diseases
JP2008515989A (ja) 2004-10-13 2008-05-15 メルク エンド カムパニー インコーポレーテッド アルツハイマー病を治療するためのβ−セクレターゼ阻害薬として有用なスピロピペリジン化合物
CA2626049A1 (en) 2004-10-15 2006-04-20 Biopharmacopae Design International Inc. Methods and therapeutic compositions comprising plant extracts for the treatment of cancer
AU2005299808B2 (en) 2004-10-25 2009-08-20 Novartis Ag Combination of DPP-IV inhibitor, PPAR antidiabetic and metformin
NZ554725A (en) 2004-10-25 2009-10-30 Merck & Co Inc Anti-ADDL antibodies and uses thereof
RU2007119535A (ru) 2004-10-28 2008-12-10 ЭЙСАЙ Р энд Д МЕНЕДЖМЕНТ КО. Способ тестирования болезни альцгеймера и диагностический реагент
US7932275B2 (en) 2004-10-29 2011-04-26 Merck, Sharp & Dohme Corp. 2-aminopyridine compounds useful as β-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
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
AU2005309601A1 (en) 2004-11-23 2006-06-01 Neuromolecular Pharmaceuticals, Inc. Composition comprising a sustained release coating or matrix and an NMDA receptor antagonist, method for administration such NMDA antagonist to a subject
CN101061119A (zh) 2004-11-23 2007-10-24 默克公司 治疗阿尔茨海默氏病的大环氨基吡啶β－分泌酶抑制剂
EP1845968A2 (en) 2004-11-24 2007-10-24 Neuromolecular Pharmaceuticals, Inc Composition comprising an nmda receptor antagonist and levodopa and use thereof for treating neurological disease
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
EP1851216A2 (en) 2004-11-30 2007-11-07 F.Hoffmann-La Roche Ag Substituted benzoquinolizines as dpp-iv inhibitors for the treatment of diabetes
US20080139458A1 (en) 2004-12-03 2008-06-12 Jay Gregory D Methods of Treatment For Injured or Diseased Joints
US20060240486A1 (en) 2004-12-15 2006-10-26 Johnson-Wood Kelly L Immunoprecipitation-based assay for predicting in vivo efficacy of beta-amyloid antibodies
WO2006066049A2 (en) 2004-12-15 2006-06-22 Neuralab Limited Humanized antibodies that recognize beta amyloid peptide
EP1838349A1 (en) 2004-12-15 2007-10-03 Neuralab, Ltd. Amyloid beta antibodies for use in improving cognition
TW200635607A (en) 2004-12-15 2006-10-16 Elan Pharm Inc Humanized Aβ antibodies for use in improving cognition
AU2005318597A1 (en) 2004-12-20 2006-06-29 F. Hoffmann-La Roche Ag 4-aminopiperidine derivatives
US7411093B2 (en) 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
JP2008524331A (ja) 2004-12-21 2008-07-10 武田薬品工業株式会社 ジペプチジルペプチダーゼ阻害剤
EP2425846A1 (en) 2004-12-23 2012-03-07 Voyager 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
JP2008526861A (ja) 2005-01-06 2008-07-24 メルク エンド カムパニー インコーポレーテッド 炎症性障害を治療するための薬剤併用療法および医薬組成物
WO2006078576A2 (en) 2005-01-19 2006-07-27 Merck & Co., Inc. Aminomethyl beta-secretase inhibitors for the treatment of alzheimer's disease
EP1841455A1 (en) 2005-01-24 2007-10-10 Amgen Inc. Humanized anti-amyloid antibody
TW200640529A (en) 2005-02-28 2006-12-01 Thomas Christian Lines Composition for treating mental health disorders
EP1858501A1 (en) 2005-03-07 2007-11-28 Michael Hermanussen Nmda receptor antagonists in the medical intervention of metabolic disorders
ES2259270B1 (es) 2005-03-09 2007-11-01 Consejo Superior De Investigaciones Cientificas Metodo de diagnostico in vitro de la enfermedad de alzheimer mediante un anticuerpo monoclonal.
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
ES2318918B1 (es) 2005-04-01 2010-02-16 Biotherapix Molecular Medicines, S.L.U. Anticuerpos humanos con capacidad de union al peptido beta-amiloide y sus aplicaciones.
AU2006241219A1 (en) 2005-04-27 2006-11-02 Novartis Ag Methods of treating atherosclerosis
MY148086A (en) 2005-04-29 2013-02-28 Rinat Neuroscience Corp Antibodies directed against amyloid-beta peptide and methods using same
TW200716174A (en) 2005-05-19 2007-05-01 Centocor Inc Anti-MCP-1 antibodies, compositions, methods and uses
EP1912966A2 (en) 2005-06-01 2008-04-23 Ucb, S.A. 2-oxo-1-pyrrolidine derivatives and their therapeutic use on the central nervous system
EP1921137A4 (en) 2005-06-21 2011-01-26 Med & Biological Lab Co Ltd ANTIBODIES WITH INHIBITOR EFFECT ON THE FORMATION OF AMYLOID FIBRILLES
WO2007011810A1 (en) 2005-07-18 2007-01-25 Merck & Co., Inc. Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
WO2007019078A2 (en) 2005-08-03 2007-02-15 Merck & Co., Inc. Tricyclic beta-secretase inhibitors for the treatment of alzheimer's disease
US20090182021A1 (en) 2005-08-03 2009-07-16 Nanternet Philippe G Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
US7338974B2 (en) 2005-08-12 2008-03-04 Bristol-Myers Squibb Company Macrocyclic diaminopropanes as beta-secretase inhibitors
EP1937720B1 (en) 2005-08-18 2014-04-09 Ramot at Tel-Aviv University Ltd. Single chain antibodies against beta-amyloid peptide
US20080227806A1 (en) 2005-09-28 2008-09-18 American Life Science Pharmaceuticals Novel Drugs for Dementia
WO2007051333A1 (en) 2005-11-02 2007-05-10 Oncalis Ag Triazine beta-secretase inhibitors
MY181173A (en) 2005-12-12 2020-12-21 Ac Immune Sa Therapeutic vaccine
ES2454253T3 (es) 2005-12-12 2014-04-10 Ac Immune S.A. Anticuerpos monoclonales específicos de beta A 1-42 con propiedades terapéuticas
PE20071321A1 (es) 2006-01-20 2007-12-29 Schering Corp Bencensulfonil-cromano, tiocromano, tetrahidronaftaleno e inhibidores de gamma secretasa relacionados
JP5097695B2 (ja) 2006-02-22 2012-12-12 株式会社林原 抗アミロイドβペプチド抗体産生誘導用のペプチドワクチン
GB0704100D0 (en) 2006-03-17 2007-04-11 Vodafone Plc Improvements in an ehspa architecture
DE602007003703D1 (de) 2006-03-30 2010-01-21 Glaxo Group Ltd Gegen amyloid-beta peptid gerichtete antikörper
KR101605207B1 (ko) 2006-07-14 2016-03-22 에이씨 이뮨 에스.에이. 아밀로이드 베타에 대해 인간화된 항체
SI2074145T1 (sl) 2006-10-02 2017-12-29 Ac Immune S.A. Humanizirano protitelo proti amiloid beta
JP2010508272A (ja) 2006-10-30 2010-03-18 メルク エンド カムパニー インコーポレーテッド アルツハイマー病を治療するためのスピロピペリジンβセクレターゼ阻害剤
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
DK2091945T3 (da) * 2006-11-09 2014-04-22 Probiodrug Ag Nye inhibitorer af glutaminylcyclase
EP2086960B1 (en) 2006-11-09 2014-03-05 Probiodrug AG Novel inhibitors of glutaminyl cyclase
SI2091948T1 (sl) 2006-11-30 2012-07-31 Probiodrug Ag Novi inhibitorji glutaminil ciklaze
US20100216875A1 (en) 2006-12-20 2010-08-26 Gregory Hook Methods of treating alzheimer's disease
CN101679409B (zh) * 2006-12-22 2014-11-26 Astex治疗学有限公司 双环杂环衍生化合物、其医药组合物和其用途
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
EP2865670B1 (en) 2007-04-18 2017-01-11 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
DK2142513T3 (da) 2007-04-18 2014-06-10 Probiodrug Ag Nitrovinyl-diamin-derivater som glutaminyl-cyclase-inhibitorer
DK2160380T3 (da) 2007-04-18 2014-06-30 Probiodrug Ag Cyano-guanidin derivater som glutaminyl cyclase inhibitorer
ES2478673T3 (es) 2007-04-18 2014-07-22 Probiodrug Ag Derivados de tioxoquinazolinona como inhibidores de la glutaminil ciclasa
JP5675343B2 (ja) 2007-04-18 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としての尿素誘導体
DK2142515T3 (da) 2007-04-18 2014-06-23 Probiodrug Ag Nitrovinyl-diaminderivater som glutaminyl-cyclase-inhibitorer
EP2142536B1 (en) 2007-04-20 2015-10-21 Probiodrug AG Aminopyrimidine derivatives as glutaminyl cyclase inhibitors
JP5400032B2 (ja) * 2007-04-20 2014-01-29 ザ リサーチ ファウンデーション オブ ザ ステイト ユニヴァーシティ オブ ニューヨーク ベンズイミダゾール及びその医薬組成物
MX2009012525A (es) 2007-05-25 2009-12-09 Elan Pharm Inc Pirazol-pirrolidinas como inhibidores de gamma secretasa.
AR066987A1 (es) 2007-06-12 2009-09-23 Ac Immune Sa Anticuerpo monoclonal contra proteina beta-amiloide
WO2008151927A2 (en) 2007-06-15 2008-12-18 Nycomed Gmbh 6-n-substituted benz imidazole derivatives as acid pump antagonists
US8664411B2 (en) 2007-07-05 2014-03-04 Merck Sharp & Dohme Corp. Tetrahydropyranochromene gamma secretase inhibitors
PE20090447A1 (es) 2007-07-17 2009-04-18 Schering Corp Bencensulfonil-cromano, tiocromano, tetrahidronaftaleno e inhibidores relacionados de la gamma secretasa
EA026787B1 (ru) 2007-08-27 2017-05-31 Общество С Ограниченной Ответственностью "Ниармедик Плюс" Конструкция нуклеиновой кислоты и ее применение для лечения, предотвращения и сдерживания болезни альцгеймера
EP2527369A3 (en) 2007-09-13 2012-12-19 University Of Zurich Prorektorat Forschung Monoclonal amyloid beta (abeta)-specific antibody and uses thereof
US8299267B2 (en) 2007-09-24 2012-10-30 Comentis, Inc. (3-hydroxy-4-amino-butan-2-yl) -3- (2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating
WO2009042907A1 (en) 2007-09-27 2009-04-02 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Isoindoline compounds for the treatment of spinal muscular atrophy and other uses
GB0720912D0 (en) 2007-10-25 2007-12-05 Univ Cardiff Monoclonal Anitbody for APP
EP2226081A4 (en) 2007-10-25 2011-10-12 Univ Kagoshima PEPTIDE VACCINE WITH A MIMIC MOLECULE OF AMYLOID PEPTIDE
MX2010004660A (es) 2007-10-29 2010-07-30 Inserm Inst Nat De La Sante De NUEVOS ANTICUERPOS ESPECIFICOS DE LOS PEPTIDOS ß-AMILOIDES Y SUS USOS COMO AGENTES DE DIAGNOSTICO Y DROGAS.
KR101581733B1 (ko) 2007-11-16 2015-12-31 더 락커펠러 유니버시티 원섬유 형태의 베타­아밀로이드 단백질에 대해 특이적인 항체
US9345753B2 (en) 2008-01-16 2016-05-24 Yeda Research And Development Co. Ltd. At The Weizmann Institute Of Science Vaccine for alzheimer's disease
ITNA20080006A1 (it) 2008-01-28 2009-07-29 Consiglio Nazionale Ricerche Proteine chimeriche capaci di formare particelle virus-like, che contengono sequenze peptidiche del beta-amiloide e la componente e2 della alfachetoacido deidrogenasi di "geobacillus stearothermophilus", utili per l'induzione di una risposta anticorp
AU2009217518A1 (en) 2008-02-28 2009-09-03 Merck Sharp & Dohme Corp. 2-aminoimidazole beta-secretase inhibitors for the treatment of Alzheimer's disease
PT2294066E (pt) 2008-04-28 2014-11-21 Janssen Pharmaceutica Nv Benzoimidazoles como inibidores da prolil-hidroxilase
CA2729965A1 (en) * 2008-07-14 2010-01-21 Gilead Sciences, Inc. Fused heterocyclyc inhibitor compounds
EP2303920A4 (en) 2008-07-25 2011-11-09 Abbott Lab SS-AMYLOID PEPTIDE ANALOGUES, OLIGOMERS THEREOF, PREPARATION METHODS AND COMPOSITIONS COMPRISING THE SAME OR OLIGOMERIC ANALOGUES, AND USES THEREOF
WO2010016912A2 (en) 2008-08-07 2010-02-11 Mercia Pharma, Llc Immunotherapeutic compositions for the treatment of alzheimer's disease
WO2010021680A2 (en) 2008-08-19 2010-02-25 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
JP5707327B2 (ja) 2008-09-04 2015-04-30 プロビオドルグ エージー 新規の阻害剤
EP2348042B1 (en) 2008-10-16 2017-07-05 The Chemo-Sero-Therapeutic Research Institute Modified amyloid beta peptide
NZ592823A (en) 2008-11-23 2012-12-21 Pfizer Spirocyclic lactams for treating neurodegenerative and/or neurological disorders
US8609897B2 (en) 2009-02-06 2013-12-17 Merck Sharp & Dohme Corp. Trifluoromethylsulfonamide gamma secretase inhibitor
US8865701B2 (en) 2009-02-20 2014-10-21 Merck Sharp & Dohme Corp. Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer'S disease

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