JP6050264B2 - グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体 - Google Patents

グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体 Download PDF

Info

Publication number
JP6050264B2
JP6050264B2 JP2013558454A JP2013558454A JP6050264B2 JP 6050264 B2 JP6050264 B2 JP 6050264B2 JP 2013558454 A JP2013558454 A JP 2013558454A JP 2013558454 A JP2013558454 A JP 2013558454A JP 6050264 B2 JP6050264 B2 JP 6050264B2
Authority
JP
Japan
Prior art keywords
phenyl
substituted
cycloalkyl
alkyl
heterocyclyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2013558454A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014508184A (ja
JP2014508184A5 (enExample
Inventor
ヘイセル ウルリクフ
ヘイセル ウルリクフ
ラムスベクク ダニエル
ラムスベクク ダニエル
Original Assignee
プロビオドルグ エージー
プロビオドルグ エージー
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 プロビオドルグ エージー, プロビオドルグ エージー filed Critical プロビオドルグ エージー
Publication of JP2014508184A publication Critical patent/JP2014508184A/ja
Publication of JP2014508184A5 publication Critical patent/JP2014508184A5/ja
Application granted granted Critical
Publication of JP6050264B2 publication Critical patent/JP6050264B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19—Cytokines; Lymphokines; Interferons
    • A61K38/20—Interleukins [IL]
    • A61K38/2026—IL-4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19—Cytokines; Lymphokines; Interferons
    • A61K38/21—Interferons [IFN]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
JP2013558454A 2011-03-16 2012-03-16 グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体 Active JP6050264B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161453333P 2011-03-16 2011-03-16
US61/453,333 2011-03-16
PCT/EP2012/054631 WO2012123563A1 (en) 2011-03-16 2012-03-16 Benz imidazole derivatives as inhibitors of glutaminyl cyclase

Publications (3)

Publication Number Publication Date
JP2014508184A JP2014508184A (ja) 2014-04-03
JP2014508184A5 JP2014508184A5 (enExample) 2015-05-07
JP6050264B2 true JP6050264B2 (ja) 2016-12-21

Family

ID=45852540

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013558454A Active JP6050264B2 (ja) 2011-03-16 2012-03-16 グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体

Country Status (6)

Country Link
US (1) US8530670B2 (enExample)
EP (1) EP2686313B1 (enExample)
JP (1) JP6050264B2 (enExample)
DK (1) DK2686313T3 (enExample)
ES (1) ES2570167T3 (enExample)
WO (1) WO2012123563A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX376945B (es) * 2013-07-19 2025-03-04 Syngenta Participations Ag Proceso novedoso para la preparación de pirrolidina-dionas espiroheterocíclicas.
US20170363645A1 (en) 2014-12-19 2017-12-21 Probiodrug Ag Novel Method for the Detection of pGlu-Abeta Peptides
DE102015011780A1 (de) * 2015-09-16 2017-03-16 Hochschule Anhalt Neue Glutaminylcyclase-lnhibitoren
CN116462666B (zh) * 2017-01-10 2025-07-15 瑞士苏黎世联邦理工学院 细胞保护性化合物及其用途
US10702495B2 (en) 2017-02-20 2020-07-07 Nexien Biopharma, Inc. Method and compositions for treating dystrophies and myotonia
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
EP3543231A1 (en) * 2018-03-19 2019-09-25 ETH Zurich Compounds for treating cns- and neurodegenerative diseases
CN108611370A (zh) * 2018-05-10 2018-10-02 江苏天瑞精准医疗科技有限公司 一种pimt表达质粒、扩增引物、构建方法及应用
EP3750528A1 (en) 2019-06-11 2020-12-16 Nexien Biopharma, Inc. Compositions for treating dystrophies and myotonia
CN118019737A (zh) * 2021-06-24 2024-05-10 英矽智能科技知识产权有限公司 用于治疗疾病的β-内酰胺衍生物

Family Cites Families (551)

* 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
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
US4873342A (en) 1985-04-16 1989-10-10 Suntory Limited Dipeptide derivative and synthesis and use thereof
US4772587A (en) 1985-04-16 1988-09-20 Suntory Limited 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
CA1334092C (en) 1986-07-11 1995-01-24 David John Carini Angiotensin ii receptor blocking imidazoles
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
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
EP0268190B1 (en) 1986-11-20 1993-06-16 Ono Pharmaceutical Co., Ltd. Prolinal derivatives
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
US5262431A (en) 1986-12-29 1993-11-16 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
DE3783754T2 (de) 1986-12-29 1993-08-05 Ono Pharmaceutical Co Prolin-derivate.
DE3879522T2 (de) 1987-02-04 1993-09-02 Ono Pharmaceutical Co Prolinalderivate.
EP0461677B1 (en) 1987-02-23 1997-04-16 Ono Pharmaceutical Co., Ltd. Novel thiazolidine derivatives
JPS6442465A (en) 1987-08-07 1989-02-14 Wakunaga Pharma Co Ltd N-acylprolylpyrrolidine derivative, production and use thereof
US4857524A (en) 1987-08-08 1989-08-15 Kissei Pharmaceutical Co., Ltd. Thiazolidine compounds and therapeutic method
JP2649237B2 (ja) 1988-03-07 1997-09-03 キッセイ薬品工業 株式会社 チアゾリジン誘導体
JP2515558B2 (ja) 1987-09-10 1996-07-10 株式会社ヤクルト本社 新規なペプチドおよびそれを有効成分とする抗健忘症剤
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
ZA896376B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y agonists
ZA896374B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y antagonists
JP2531989B2 (ja) 1988-09-14 1996-09-04 吉富製薬株式会社 ピリジン化合物
CA2004028C (en) 1988-12-08 1998-09-22 Motoki Torizuka Condensed benzene derivative
JPH02207070A (ja) 1989-02-07 1990-08-16 Zeria Pharmaceut Co Ltd アミノ酸イミド誘導体、それを含有する医薬及び該化合物の製造中間体
WO1990012005A1 (fr) 1989-04-13 1990-10-18 Japan Tobacco Inc. Nouveaux derives aminoacides possedant une activite d'inhibiteur de la prolylendopeptidase
WO1990012871A1 (en) 1989-04-14 1990-11-01 Research Foundation For Mental Hygiene, Inc. Cerebrovascular amyloid protein-specific monoclonal antibody sv17-6e10
AU5525090A (en) 1989-04-14 1990-11-16 Research Foundation For Mental Hygiene, Inc. Monoclonal antibody to amyloid peptide
DK0403159T3 (da) 1989-06-14 2000-08-14 Smithkline Beecham Corp Imidazolylalkensyrer
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
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
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
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
WO1991018891A1 (en) 1990-06-04 1991-12-12 Pfizer Inc. Aromatic pyrrolidine and thiazolidine amides
CA2084204A1 (en) 1990-06-07 1991-12-08 Akihiro Okubo Arylalkanoylamine derivative and drug containing the same
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
CA2229000C (en) 1991-02-21 2002-04-09 Sankyo Company, Limited 1-biphenylimidazole derivatives, their preparation and their therapeutic 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
DE69222142T2 (de) 1991-06-20 1998-04-09 Snow Brand Milk Products Co., Ltd., Sapporo, Hokkaido 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
CA2113115A1 (en) 1991-07-29 1993-02-18 Vlad E. Gregor Quinazoline derivatives as acetylcholinesterase inhibitors
TW226375B (enExample) 1991-10-24 1994-07-11 American Home Prod
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
WO1994007890A1 (fr) 1992-10-05 1994-04-14 Ube Industries, Ltd. Compose pyrimidine
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
EP0683234B2 (en) 1993-01-25 2007-06-06 Takeda Chemical Industries, Ltd. Antibody against beta-amyloid or their derivative and use thereof
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
JPH11501281A (ja) 1993-06-18 1999-02-02 ユニバーシティ オブ シンシナティ 神経ペプチドｙアンタゴニスト及びアゴニスト
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.
DK0731788T3 (da) 1993-12-02 2003-01-20 Merrell Pharma Inc Prolylendopeptidaseinhibitorer
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 .
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 .
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.
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
EP0716854A3 (en) 1994-10-20 1996-08-28 Lilly Co Eli Compositions for inhibiting neuropeptide Y
US5663192A (en) 1994-10-20 1997-09-02 Eli Lilly And Company Heterocyclic 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
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
US5668151A (en) 1995-06-07 1997-09-16 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: piperidine 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.
DE19544687A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19544686A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19544685A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
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
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
WO1997020821A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
AU7626496A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Heteroaryl compounds
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
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
EP0892796B1 (en) 1996-04-12 2001-10-24 Aventis Pharmaceuticals Inc. Isatin derivatives as acetylcholinesterase inhibitors and analgesics
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
EP1007073A4 (en) 1996-06-04 2002-03-27 Synaptic Pharma Corp METHODS OF MODIFYING FOOD BEHAVIOR, COMPOUNDS USEFUL IN SAID METHODS, AND DNA ENCODING A HYPOTHALAMIC NEUROPEPTIDE Y / PEPTIDE YY Y5 RECEPTOR
DE69715899T2 (de) 1996-07-05 2003-05-28 The Wwk Trust, Kent Zusammensetzungen zur behandlung der peripheren neuropathie, die antidepressiven verbindungen und/oder monoamino-oxidaseinhibitoren und/oder vitamin b12 und/oder neurotransmitter-vorläufer oder induktoren enthalten
US5985873A (en) 1996-07-23 1999-11-16 Neurogen Corporation Certain substituted benzylamine derivatives a new class of Neuropeptide-Y1 specific ligands
EP0918761B1 (en) 1996-07-23 2003-05-02 Neurogen Corporation Certain amido- and amino-substituted benzylamine derivatives; a new class of neuropeptite 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
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
ES2176776T3 (es) 1996-08-23 2002-12-01 Agouron Pharma Ligandos del 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
US6011155A (en) 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
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
AU6417198A (en) 1997-03-13 1998-09-29 Bioresearch Ireland a division of Eolas - The Irish Science and Technology Agency Cytoprotective agents comprising monoamine oxidase inhibitors
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
WO1998044955A1 (en) 1997-04-09 1998-10-15 Mindset Ltd. Recombinant antibodies specific for beta-amyloid ends, dna encoding and methods of use thereof
EP0975584B1 (en) 1997-04-16 2002-09-25 Arqule, Inc. Synthesis and use of alpha-ketoamide derivatives and arrays
JP2001527554A (ja) 1997-05-07 2001-12-25 アルゴス ファーマシューティカル コーポレーション 抗うつ薬とｎｍｄａレセプター拮抗薬とを組み合わせる神経障害痛の治療用組成物及び治療方法
WO1998050075A1 (en) 1997-05-07 1998-11-12 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
JP3255080B2 (ja) 1997-05-28 2002-02-12 日新電機株式会社 ガス絶縁開閉装置
JP3031298B2 (ja) 1997-06-18 2000-04-10 日本電気株式会社 電流検出型センスアンプ
UA61962C2 (uk) 1997-06-30 2003-12-15 Мерц Фарма Гмбх Унд Ко. Кгаа Сполука 1-аміноалкілциклогексану, фармацевтична композиція на її основі та спосіб лікування
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
EP2823812A1 (en) 1998-02-02 2015-01-14 Trustees Of Tufts College Dipeptidylpeptidase IV inhibitors for use in the treatment of Type II diabetes
EP1062222A1 (en) 1998-03-09 2000-12-27 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
AU3786299A (en) 1998-05-04 1999-11-23 Neotherapeutics, Inc. Novel serotonin-like 9-substituted hypoxanthine and methods of use
WO1999057119A1 (en) 1998-05-04 1999-11-11 Neotherapeutics, Inc. Novel dopamine-like 9-substituted hypoxanthine and methods of use
MXPA00011348A (es) 1998-05-21 2003-04-22 Univ Tennesse Res Corp Metodos para la remocion de material amiloide utilizando anticuerpos anti-amiloide.
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
PE20000728A1 (es) 1998-06-26 2000-08-21 Cocensys Inc Heterociclos 4-bencil piperidina alquilsulfoxido y su uso como antagonistas receptores subtipo-selectivo nmda
US6262081B1 (en) 1998-07-10 2001-07-17 Dupont Pharmaceuticals Company Composition for and method of treating neurological disorders
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
AU5027299A (en) 1998-07-31 2000-02-28 Novo Nordisk A/S Use of glp-1 and analogues for preventing type ii diabetes
JP4009367B2 (ja) 1998-08-04 2007-11-14 株式会社ディスコ スピン洗浄・乾燥方法
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
JP4208299B2 (ja) 1998-08-19 2009-01-14 東レ株式会社 金属板貼合わせ成形加工用ポリエステルフィルム
IT1304904B1 (it) 1998-09-11 2001-04-05 Eisai Co Ltd Derivati anticolinesterasici per il trattamento delle sindromidolorose funzionali e/o organiche
IL142588A0 (en) 1998-10-16 2002-03-10 Janssen Pharmaceutica Nv Therapy for improving cognition
CA2351224A1 (en) 1998-11-12 2000-05-25 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
AU1738800A (en) 1998-11-23 2000-06-13 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
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
GB9902452D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
EP1163220A1 (en) 1999-03-23 2001-12-19 Sumitomo Pharmaceuticals Company, Limited Tricyclic indole-2-carboxylic acid compound used as nmda receptor antagonist
WO2000063250A1 (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
HK1041263A1 (zh) 1999-05-05 2002-07-05 Ortho-Mcneil Pharmaceutical, Inc. 可用於治疗肥胖和其他疾病的3a，4，5，9b-四氢-1h-苯并[e]吲-2-基胺衍生的神经肽y受体配体
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
JP3056486B1 (ja) 1999-06-15 2000-06-26 株式会社東京機械製作所 印刷機用インキレ―ル
ES2312348T3 (es) 1999-06-16 2009-03-01 Boston Biomedical Research Institute Control inmunologico de niveles de beta-amiloide in vivo.
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
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
US6524616B1 (en) 1999-06-25 2003-02-25 Wake Forest University Health Services Compositions and methods for treating or preventing neurodegeneration and cognitive decline and dysfunction associated with alzheimer's disease, aging, other dementia related disorders and estrogen deficiency related conditions
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
EP1307219A4 (en) 1999-08-13 2005-04-06 Univ Columbia METHODS OF INHIBITING BETA FIBRILLE BINDING BETA TO RAGE RECEPTOR, AND CONSEQUENCES THEREOF
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
GB9928330D0 (en) 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
WO2001053255A1 (en) 2000-01-24 2001-07-26 Merck Sharp & Dohme Limited Gamma-secretase inhibitors
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
IL151378A0 (en) 2000-02-24 2003-04-10 Univ Washington Humanized antibodies that sequester amyloid beta peptide
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
AU2001255620A1 (en) 2000-04-26 2001-11-07 Warner-Lambert Company Cyclohexylamine derivative as subtype selective NMDA receptor antagonists
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
US20010036949A1 (en) 2000-05-09 2001-11-01 Coe Jotham Wadsworth Pharmaceutical composition and method of treatment of diseases of cognitive dysfunction in a mammal
AU2001261487A1 (en) 2000-06-01 2001-12-11 Warner Lambert Company Cyclohexylamine derivatives as subtype selective nmda receptor antagonists
BR0111267A (pt) 2000-06-06 2003-12-16 Warner Lambert Co Cicloexilaminas bicìclicas e seu uso como antagonistas do receptor de nmda
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
JP2004502665A (ja) 2000-06-30 2004-01-29 イーラン　ファーマスーティカルズ、インコーポレイテッド アルツハイマー病を治療する化合物
US6686449B2 (en) 2000-06-30 2004-02-03 Pharmacia & Upjohn Company Mutant presenilin 1 polypeptides
AU6895801A (en) 2000-07-04 2002-01-14 Novo Nordisk As Heterocyclic compounds, which are inhibitors of the enzyme 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
ES2248397T3 (es) 2000-11-02 2006-03-16 MERCK SHARP & DOHME LTD. Sulfamidas como inhibidores de la gamma-secretasa.
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
WO2002072542A2 (en) 2001-03-08 2002-09-19 Emory University Ph-dependent nmda receptor antagonists
US6649196B2 (en) 2001-03-12 2003-11-18 Mayo Foundation For Medical Education And Research Methods of reducing β-amyloid polypeptides
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
US6677365B2 (en) 2001-04-03 2004-01-13 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
ES2312569T3 (es) 2001-04-30 2009-03-01 Eli Lilly And Company Anticuerpos humanizados.
ES2318006T3 (es) 2001-04-30 2009-05-01 Eli Lilly And Company Anticuerpos humanizados que reconocen el peptido beta-amiloide.
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
US20030013177A1 (en) 2001-05-23 2003-01-16 Ebens Allen J. Polynucleotides encoding insect glutaminyl cyclase and uses thereof
US6562783B2 (en) 2001-05-30 2003-05-13 Neurologic, Inc. Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
WO2002098849A2 (en) 2001-06-01 2002-12-12 Elan Pharmaceuticals, Inc. Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer’s disease and similar diseases
EP1406872B1 (en) 2001-06-20 2007-12-19 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
DE60209348T2 (de) 2001-06-20 2006-10-12 Merck & Co., Inc. Dipeptidylpeptidase-hemmer zur behandlung von 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
WO2003002530A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
WO2003002122A1 (en) 2001-06-27 2003-01-09 Elan Pharmaceuticals, Inc. Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease
CN1723196A (zh) 2001-06-27 2006-01-18 史密丝克莱恩比彻姆公司 作为二肽酶抑制剂的氟代吡咯烷
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
WO2003002593A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
ATE385238T1 (de) 2001-06-27 2008-02-15 Probiodrug Ag Verwendung von dpiv-inhibitoren als therapeutika für krankhafte neurologische zustände
ATE370943T1 (de) 2001-06-27 2007-09-15 Smithkline Beecham Corp Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren
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
ATE408611T1 (de) 2001-07-24 2008-10-15 Richter Gedeon Nyrt Piperidine als nmda-rezeptorantagonisten
US20040234990A1 (en) 2001-07-31 2004-11-25 Hiroto Komano Method of screening alzheimer's disease-associated gene
CN1780621A (zh) 2001-08-03 2006-05-31 先灵公司 作为γ分泌酶抑制剂的磺酰胺衍生物
JP4729717B2 (ja) 2001-08-03 2011-07-20 株式会社医学生物学研究所 ＧＭ１ガングリオシド結合型アミロイドβタンパク質を認識する抗体、及び該抗体をコードするＤＮＡ
CN1304390C (zh) 2001-08-03 2007-03-14 先灵公司 新颖的γ—分泌酶抑制剂
WO2003015691A2 (en) 2001-08-17 2003-02-27 Eli Lilly And Company RAPID IMPROVEMENT OF COGNITION IN CONDITIONS RELATED TO A$g(b)
CA2451998A1 (en) 2001-08-17 2003-02-27 Eli Lilly And Company Anti-a.beta. antibodies
WO2003020289A1 (en) 2001-08-30 2003-03-13 Ortho-Mcneil Pharmaceutical, Inc. Treatment of dementia and memory disorders with anticonvulsants and acetylcholinesterase inhibitors
EP1426366A4 (en) 2001-09-14 2004-12-08 Mitsubishi Pharma Corp THIAZOLIDE DERIVATIVES AND THEIR MEDICAL USE
EP1463727A2 (en) 2001-09-19 2004-10-06 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
CA2464736A1 (en) 2001-10-23 2003-05-15 Oklahoma Medical Research Foundation Beta-secretase inhibitors and methods of use
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
WO2003039467A2 (en) 2001-11-02 2003-05-15 Diagenics International Corporation Monoclonal antibodies specific for beta-amyloid.
US7304040B2 (en) 2001-11-02 2007-12-04 Kensuke Egashira Suppression of post-transplant arteriosclerosis
WO2003040183A2 (en) 2001-11-09 2003-05-15 The Genetics Company, Inc Compounds for the diagnosis/prevention/treatment of alzheimer's disease
JP2005514362A (ja) 2001-11-19 2005-05-19 イーラン ファーマスーティカルズ、インコーポレイテッド ３，４二置換、３，５二置換、及び３，４，５置換ピペリジン及びピペラジン
CA2466841A1 (en) 2001-11-21 2003-06-05 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
EP2316470A3 (en) 2001-11-26 2011-08-24 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
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
IL162533A0 (en) 2001-12-19 2005-11-20 Atherogenics Inc Chalcone derivatives and their use to treat diseases
US20060210555A1 (en) 2001-12-21 2006-09-21 Antigenics, Inc. 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
WO2003057204A2 (en) 2002-01-08 2003-07-17 Nordic Bioscience A/S Modulation of iamt (pimt or pcmt) in immune system
JP2005516967A (ja) 2002-01-18 2005-06-09 ザ ジェネティクス カンパニー インコーポレーティッド β−セクレターゼインヒビター
WO2003063760A2 (en) 2002-01-31 2003-08-07 Tel Aviv University Future Technology Development L.P. Peptides antibodies directed thereagainst and methods using same for diagnosing and treating amyloid-associated diseases
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
CN1308311C (zh) 2002-02-13 2007-04-04 霍夫曼-拉罗奇有限公司 新型吡啶－和喹啉－衍生物
ATE472536T1 (de) 2002-02-13 2010-07-15 Hoffmann La Roche Pyridin- und pyrimidin-derivate
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
EP1490335B1 (en) 2002-03-25 2007-09-19 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2003082820A1 (en) 2002-03-29 2003-10-09 Eisai Co., Ltd. (1-indanone)-(1,2,3,6-tetrahydropyridine) derivative
US20070134247A9 (en) 2002-04-12 2007-06-14 Ramot At Tel Aviv University Ltd. Prevention of brain inflammation as a result of induced autoimmune response
CN100360555C (zh) 2002-04-19 2008-01-09 多伦多大学董事局 治疗阿尔茨海默氏病的免疫学方法及组合物
CN1319987C (zh) 2002-04-24 2007-06-06 森启 γ－分泌酶抑制剂
ES2315494T3 (es) 2002-04-26 2009-04-01 Schering Corporation Antagonistas muscarinicos.
AU2003230392A1 (en) 2002-05-17 2003-12-12 Merck And Co., Inc. Beta-secretase inhibitors
EP1509232B1 (en) 2002-05-31 2008-11-19 H. Lundbeck A/S A combination of an nmda-antagonist and acetylcholine esterase inhibitors for the treatment of alzheimer's disease
MXPA04011958A (es) 2002-06-04 2005-03-31 Pfizer Prod Inc Amidas ciclicas fluoradas como inhibidores de la dipeptidil peptidasa iv.
AU2003233010A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
US20060100199A1 (en) 2002-06-06 2006-05-11 Seiji Yoshikawa Novel condensed imidazole derivatives
US20050171300A1 (en) 2002-06-19 2005-08-04 Luc Moens Semi-gloss powder coating compositions
JPWO2004007446A1 (ja) 2002-07-10 2005-11-10 アステラス製薬株式会社 新規なアゼチジン誘導体又はその塩
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
CN102964347B (zh) 2002-08-21 2015-11-18 勃林格殷格翰制药两合公司 8-[3-氨基-哌啶-1-基]-黄嘌呤化合物，其制备方法及作为药物制剂的用途
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
WO2006039807A1 (en) 2004-10-15 2006-04-20 Biopharmacopae Design International Inc. Methods and therapeutic compositions comprising plant extracts for the treatment of cancer
ES2201929B1 (es) 2002-09-12 2005-05-16 Araclon Biotech, S.L. Anticuerpos policlonales, metodo de preparacion y uso de los mismos.
CN1681926A (zh) 2002-09-12 2005-10-12 财团法人化学及血清疗法研究所 人的抗人mcp－1抗体和该抗体的片段
ATE506072T1 (de) 2002-09-12 2011-05-15 Univ California Immunogene und entsprechende antikörper, die spezifisch sind für häufige hochmolekulare aggregations-zwischenprodukte von amyloiden aus proteinen unterschiedlicher sequenz
AU2003282800B2 (en) 2002-09-19 2009-10-29 Abbvie Inc. 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
EP1545582A4 (en) 2002-10-01 2008-09-17 Univ Northwestern DIFFUSIBLE DERIVATIVES DERIVED FROM AMYLOID BETA (ADDL), ADDL SUBSTITUTE, ADDL BINDING MOLECULES, AND USES THEREOF
GB0223039D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223038D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
ATE370141T1 (de) 2002-10-07 2007-09-15 Merck & Co Inc Antidiabetische heterocyclische beta- aminoverbindungen als inhibitoren von dipeptidylpeptidase
AU2003269850A1 (en) 2002-10-08 2004-05-04 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
EP1633786A4 (en) 2002-10-09 2007-07-25 Rinat Neuroscience Corp METHOD FOR TREATING ALZHEIMER DISEASE WITH ANTIBODIES TO AMYLOID BETA PEPTIDE AND COMPOSITIONS THEREOF
GB0223494D0 (en) 2002-10-09 2002-11-13 Neuropharma Sa Dual binding site acetylcholinesterase inhibitors for the treatment of alzheimer's disease
DK1556362T3 (da) 2002-10-18 2008-06-09 Merck & Co Inc Heterocykliske beta-aminodipeptidylpeptidaseinhibitorer til behandling eller forebyggelse af 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
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
MXPA05004890A (es) 2002-11-07 2005-07-22 Merck & Co Inc Derivados de fenilalanina como inhibidores de dipeptidilpeptidasa para el tratamiento o prevencion de diabetes.
EP1562897B1 (en) 2002-11-12 2009-09-16 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
WO2004056727A2 (en) 2002-12-19 2004-07-08 Atherogenics, Inc. Process of making chalcone derivatives
CA2508947A1 (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
AU2004204692B2 (en) 2003-01-07 2009-07-09 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
US7388019B2 (en) 2003-01-31 2008-06-17 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE10303974A1 (de) 2003-01-31 2004-08-05 Abbott Gmbh & Co. Kg Amyloid-β(1-42)-Oligomere, Verfahren zu deren Herstellung und deren Verwendung
MXPA05008156A (es) 2003-02-01 2005-09-30 Neuralab Ltd Inmunizacion activa para generar anticuerpos para beta-a soluble.
ATE402934T1 (de) 2003-02-04 2008-08-15 Hoffmann La Roche Malonamidderivate als gamma-secretaseinhibitoren
US7575747B2 (en) 2003-02-10 2009-08-18 Applied Molecular Evolution Aβ binding molecules
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
AU2004212965A1 (en) 2003-02-18 2004-09-02 Roskamp Research Llc Anti-angiogenic and anti-tumoral properties of beta and gamma secretase inhibitors
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
AU2003207881A1 (en) 2003-02-28 2004-09-17 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
CA2518465A1 (en) 2003-03-25 2004-10-14 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
EP1613657A2 (en) 2003-03-28 2006-01-11 Centocor, Inc. Anti-amyloid antibodies, compositions, methods and uses
JP2006521399A (ja) 2003-03-28 2006-09-21 アカディア ファーマシューティカルズ，インコーポレーテッド 疼痛管理用ムスカリンｍ１受容体アゴニスト
PT1611144E (pt) 2003-04-09 2010-11-12 Wyeth Llc Derivados do ácido 2-(8,9-dioxo-2,6-diazabiciclo(5.2.0)- non-1(7)-eno-2-il)-alquil-fosfónico e sua utilização como antagonistas do receptor n-metil-d-aspartato (nmda)
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
MXPA05011861A (es) 2003-05-05 2006-02-17 Probiodrug Ag Uso de efectores de ciclasas de glutamato y glutaminil.
US20040229848A1 (en) 2003-05-05 2004-11-18 Hans-Ulrich Demuth Glutaminyl based DP IV-inhibitors
JP4806628B2 (ja) 2003-05-05 2011-11-02 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
ES2246105B1 (es) 2003-05-08 2007-03-01 Araclon Biotech, S.L. Uso de anticuerpos para el tratamiento de enfermedades amiloideas.
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
ATE401328T1 (de) 2003-05-13 2008-08-15 Schering Corp Verbrückte n-arylsulfonylpiperidine als gamma- sekretaseinhibitoren
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
ATE447574T1 (de) 2003-05-14 2009-11-15 Merck & Co Inc 3-amino-4-phenylbutansäurederivate als dipeptidylpeptidase-hemmer zur behandlung oder vorbeugung von diabetes
KR20060013404A (ko) 2003-05-16 2006-02-09 머크 샤프 앤드 돔 리미티드 γ-세크레타제 억제용 사이클릭 설폰아미드
MXPA05012493A (es) 2003-05-27 2006-05-25 Forest Laboratories Combinacion de un antagonista del receptor de nmda y un inhibidor selectivo de reabsorcion de serotonina para el tratamiento de depresion y otros trastornos de estado de animo.
PE20050627A1 (es) 2003-05-30 2005-08-10 Wyeth Corp Anticuerpos humanizados que reconocen el peptido beta amiloideo
AU2003902828A0 (en) 2003-06-05 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
US7332520B2 (en) 2003-06-06 2008-02-19 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
AU2004249163A1 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
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
BRPI0411713B8 (pt) 2003-06-20 2021-05-25 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
JP2007516207A (ja) 2003-06-30 2007-06-21 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Ｎ−アルキルフェニルカルボキサミドβ−セクレターゼ阻害剤
CN101415724B (zh) 2003-06-30 2015-12-02 特拉维夫大学未来科技开发有限公司 肽、抗肽抗体以及用它们来诊断和治疗淀粉样蛋白相关疾病的方法
US7348448B2 (en) 2003-07-01 2008-03-25 Merck & Co., Inc. Phenylcarboxylate beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005007614A1 (en) 2003-07-03 2005-01-27 The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services 6011 Monoamine oxidase inhibitors
JP2007528862A (ja) 2003-07-16 2007-10-18 アールブイエックス セラピューティクス， インコーポレイテッド ＴＧＦ−βの効果を下方制御するための化合物および方法
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
AU2004258751C1 (en) 2003-07-28 2008-07-17 Merz Pharma Gmbh & Co. Kgaa The use of 1-amino-alkylcyclohexane compounds in the treatment of pain hypersensitivity
AU2004261186A1 (en) 2003-07-31 2005-02-10 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
KR20060041309A (ko) 2003-08-13 2006-05-11 다케다 야쿠힌 고교 가부시키가이샤 ４-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도
CA2535337A1 (en) 2003-08-14 2005-03-03 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for the treatment of alzheimer's disease
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
JP2007505121A (ja) 2003-09-08 2007-03-08 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
WO2005030751A2 (en) 2003-09-08 2005-04-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005025616A1 (ja) 2003-09-09 2005-03-24 Takeda Pharmaceutical Company Limited 抗体の用途
AR046330A1 (es) 2003-09-09 2005-12-07 Japan Tobacco Inc Inhibidor de dipeptidilpeptidasa iv
AU2004272112A1 (en) 2003-09-12 2005-03-24 The Regents Of The University Of California Monoclonal antibodies specific for conformational epitopes of prefibrillar aggregates
GB0322140D0 (en) 2003-09-22 2003-10-22 Pfizer Ltd Combinations
WO2005030731A1 (en) 2003-09-24 2005-04-07 Merck Sharp & Dohme Limited Gamma-secretase inhibitors
AU2004277981B2 (en) 2003-10-03 2009-10-01 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease
PT1673347E (pt) 2003-10-06 2015-11-02 Hoffmann La Roche Derivados de dibenzo-azepina e benzo-diazepina substituídos, úteis como inibidores de secretase gama
JP2007516154A (ja) 2003-10-06 2007-06-21 トレント・ファーマシューティカルズ・リミテッド アゾリジンカーボニトリル類及びそれらのｄｐｐ−ｉｖ阻害剤としての用途
BRPI0415109A (pt) 2003-10-08 2006-11-28 Pfizer compostos de 1-[2-(4-hidroxifenil)-2-hidroxietil]-piperidin-4-ol como antagonistas de receptor de nmda
CA2542419C (en) 2003-10-15 2013-06-04 Probiodrug Ag Use of glutamyl cyclase inhibitors in the treatment of familial british dementia and familial danish dementia
EP2269608A3 (en) 2003-10-16 2011-02-16 NeuroSearch AS Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an acetylcholinesterase inhibitor
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
US20050113458A1 (en) 2003-10-22 2005-05-26 Forest Laboratories, Inc. Use of 1-aminocyclohexane derivatives to modify deposition of fibrillogenic a-beta peptides in amyloidopathies
EP1824846A2 (en) 2003-11-03 2007-08-29 Probiodrug AG Novel compounds for the treatment of neurological 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
JP4451449B2 (ja) 2003-11-11 2010-04-14 エフ．ホフマン−ラ ロシュ アーゲー ホスフィン酸誘導体、アルツハイマー病の処置のためのベータセクレターゼインヒビタ
EP1689757B1 (en) 2003-11-12 2014-08-27 Phenomix Corporation Heterocyclic boronic acid compounds
WO2005051914A1 (en) 2003-11-24 2005-06-09 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
WO2005065195A2 (en) 2003-12-19 2005-07-21 Merck & Co., Inc. Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005070429A1 (en) 2004-01-22 2005-08-04 Neurosearch A/S Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an n-methyl-d-aspartate (nmda) receptors antagonist
WO2005072705A1 (en) 2004-01-29 2005-08-11 Neuromolecular, Inc. Combination of a nmda receptor antagonist and a mao-inhibitor or a gadpf-inhibitor for the treatment of central nervous system-related conditions
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
KR101099206B1 (ko) 2004-02-05 2011-12-27 프로비오드룩 아게 신규한 글루타미닐 시클라제 저해제
EP1734920A2 (en) 2004-02-13 2006-12-27 Neuromolecular Inc. Combination of a nmda receptor antagonist and an 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
CA2555050C (en) 2004-02-18 2017-11-28 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthine derivatives, the production thereof and the use in the form of a dpp-iv inhibitor
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
EP1729774A4 (en) 2004-03-09 2009-05-06 Nat Health Research Institutes PYRROLIDINE CONNECTIONS
EA013427B1 (ru) 2004-03-15 2010-04-30 Такеда Фармасьютикал Компани Лимитед Ингибиторы дипептидилпептидазы
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
JP4211648B2 (ja) 2004-03-22 2009-01-21 日本電気株式会社 ソフトウェアインストール方法およびシステム
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
AU2005236063A1 (en) 2004-04-20 2005-11-03 Merck & Co., Inc. 2, 4, 6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
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
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
US7763249B2 (en) 2004-04-27 2010-07-27 Juridical Foundation The Chemo-Sero-Therapeutic Research Institute Human anti-amyloid β peptide antibody and fragment of said antibody
CA2564264A1 (en) 2004-05-04 2005-11-17 Merck & Co., Inc. 1,2,4-oxadiazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
EP1753748B1 (en) 2004-05-12 2009-07-29 Pfizer Products Inc. Proline derivatives and their use as dipeptidyl peptidase iv inhibitors
AU2005245376A1 (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
JP2007538079A (ja) 2004-05-18 2007-12-27 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阻害剤としてのシクロヘキシルアラニン誘導体
EP1598341A1 (en) 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
JP2008501714A (ja) 2004-06-04 2008-01-24 武田薬品工業株式会社 ジペプチジルペプチダーゼインヒビター
EP1766396B1 (en) 2004-06-07 2010-08-11 Ramot at Tel-Aviv University Ltd. Method of passive immunization against disease or disorder characterized by amyloid aggregation with diminished risk of neuroinflammation
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
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
SE0401601D0 (sv) 2004-06-21 2004-06-21 Bioarctic Neuroscience Ab Protofibril specific antibodies and uses thereof
CN101602741A (zh) 2004-06-30 2009-12-16 先灵公司 作为γ-分泌酶抑制剂的取代的N-芳基磺酰基杂环胺
US7371825B2 (en) 2004-06-30 2008-05-13 Centocor, Inc. Anti-MCP-1 antibodies, compositions, methods and uses
EP1769002A1 (en) 2004-07-02 2007-04-04 Northwestern University Monolocal antibodies that target pathological assemblies of amyloid beta; (abeta)
CA2573848A1 (en) 2004-07-12 2006-02-16 Phenomix Corporation Constrained cyano compounds
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006008661A2 (en) 2004-07-19 2006-01-26 Neurochem (International) Limited 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
ATE491693T1 (de) 2004-07-22 2011-01-15 Schering Corp Substituierte amide als inhibitoren der beta- sekretase
WO2006014944A1 (en) 2004-07-28 2006-02-09 Schering Corporation Macrocyclic beta-secretase inhibitors
HUP0401523A3 (en) 2004-07-29 2007-05-02 Richter Gedeon Vegyeszet Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them
GEP20115195B (en) 2004-07-30 2011-04-11 Rinat Neuroscience Corp Antibodies directed against amyloid-beta peptide and use thereof
EP1623983A1 (en) 2004-08-05 2006-02-08 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Heterocyclic compounds useful as DPP-IV inhibitors
US8168188B1 (en) 2004-08-11 2012-05-01 Kyoto University Antibody and utilization of the same
CA2576465A1 (en) 2004-08-23 2006-03-02 Merck & Co., Inc. Fused triazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
AU2005276635A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
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
TWI374935B (en) 2004-08-27 2012-10-21 Pfizer Ireland Pharmaceuticals Production of α-abeta
WO2006029850A1 (en) 2004-09-14 2006-03-23 The Genetics Company, Inc. Hydrazone derivatives and their use as beta secretase inhibitors
WO2006034277A1 (en) 2004-09-17 2006-03-30 Comentis, Inc. Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
US7659289B2 (en) 2004-09-17 2010-02-09 Comentis, Inc. Hydroxyethylene-based β-secretase inhibitors and use thereof
EP1799260A4 (en) 2004-09-29 2011-09-28 Centocor Inc ANTI-AMYLOID ANTIBODIES, COMPOSITIONS, TECHNIQUES AND USES
EP1796669B1 (en) 2004-10-01 2010-09-22 Merck Sharp & Dohme Corp. Aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006042103A2 (en) 2004-10-05 2006-04-20 Axys Pharmaceuticals, Inc. Reversible inhibitors of cathepsin b
AU2005294320A1 (en) 2004-10-08 2006-04-20 Novartis Ag Combination of organic compounds
US9186345B2 (en) 2004-10-12 2015-11-17 Hakon Hakonarson Method of treating skin diseases
CA2583342A1 (en) 2004-10-13 2006-04-27 Merck And Co., Inc. Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzhermer's disease
EP1807066A1 (en) 2004-10-25 2007-07-18 Novartis AG Combination of dpp-iv inhibitor, ppar antidiabetic and metformin
AU2005306997B2 (en) 2004-10-25 2012-07-05 Merck Sharp & Dohme Corp. Anti-ADDL antibodies and uses thereof
US20080199879A1 (en) 2004-10-28 2008-08-21 Sanko Junyaku Co., Ltd. Method of Assaying Alzheimer's Disease and Diagnostic Reagent
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
JP2008520670A (ja) 2004-11-17 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大環状第三アミンβ−セクレターゼ阻害剤
JP4235162B2 (ja) 2004-11-18 2009-03-11 日本電信電話株式会社 画像符号化装置，画像符号化方法，画像符号化プログラムおよびコンピュータ読み取り可能な記録媒体
CA2588295C (en) 2004-11-23 2013-10-22 Adamas Pharma, Llc Method and composition for administering an nmda receptor antagonist to a subject
WO2006057945A2 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
AU2005309708A1 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of Alzheimer's disease
CA2588296A1 (en) 2004-11-24 2006-06-01 Neuromolecular Pharmaceuticals, Inc. Composition comprising an nmda receptor antagonist and levodopa and use thereof 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
JP4842963B2 (ja) 2004-11-30 2011-12-21 エフ．ホフマン−ラ ロシュ アーゲー 糖尿病を処置するｄｐｐ−ｉｖ阻害剤としての置換ベンゾキノリジン
WO2006060473A2 (en) 2004-12-03 2006-06-08 Mucosal Therapeutics Llc Methods of treatment of injured or diseased joints with lubricin compositions
ES2396555T3 (es) 2004-12-15 2013-02-22 Janssen Alzheimer Immunotherapy Anticuerpos que reconocen péptido beta amiloide
PE20061329A1 (es) 2004-12-15 2006-12-08 Neuralab Ltd Anticuerpos ab humanizados para mejorar la cognicion
WO2006066233A1 (en) 2004-12-15 2006-06-22 Neuralab Limited An immunoprecipitation-based assay for predicting in vivo efficacy of beta-amyloid antibodies
US20060257396A1 (en) 2004-12-15 2006-11-16 Jacobsen Jack S Abeta antibodies for use in improving cognition
US7411093B2 (en) 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
CN101090888A (zh) 2004-12-20 2007-12-19 霍夫曼-拉罗奇有限公司 4－氨基哌啶衍生物
EP1828192B1 (en) 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2006071274A2 (en) 2004-12-23 2006-07-06 Voyager Pharmaceutical Corporation Leuprolide acetate and acetylcholinesterase inhibitors or nmda receptor antagonists for the treatment of alzheimer’s disease
WO2006070394A1 (en) 2004-12-28 2006-07-06 Council Of Scientific And Industrial Research Substituted carbamic acid quinolin-6-yl esters useful as acetylcholinesterase inhibitors
US20080194548A1 (en) 2005-01-06 2008-08-14 Forrest Michael J Drug Combination Therapy and Pharmaceutical Compositions for Treating Inflammatory Disorders
CA2594943A1 (en) 2005-01-19 2006-07-27 Merck & Co., Inc. Aminomethyl beta-secretase inhibitors for the treatment of alzheimer's disease
CA2589860A1 (en) 2005-01-24 2006-08-03 Amgen Inc. Humanized anti-amyloid antibody
US20060216331A1 (en) 2005-02-28 2006-09-28 Lines Thomas C Composition for treating mental health disorders
WO2006094674A1 (en) 2005-03-07 2006-09-14 Michael Hermanussen Nmda receptor antagonists in the medical intervention of metabolic disorders
WO2006095613A1 (ja) 2005-03-09 2006-09-14 Konica Minolta Medical & Graphic, Inc. 希土類賦活アルカリ土類金属フッ化ハロゲン化物輝尽性蛍光体及びそれを用いた放射線画像変換パネル
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.
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
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.
KR20080000624A (ko) 2005-04-27 2008-01-02 노파르티스 아게 아테롬성동맥경화증의 치료 방법
PE20061323A1 (es) 2005-04-29 2007-02-09 Rinat Neuroscience Corp Anticuerpos dirigidos contra el peptido amiloide beta y metodos que utilizan los mismos
PE20061444A1 (es) 2005-05-19 2007-01-15 Centocor Inc Anticuerpo anti-mcp-1, composiciones, metodos y usos
EP1921137A4 (en) 2005-06-21 2011-01-26 Med & Biological Lab Co Ltd ANTIBODIES WITH INHIBITOR EFFECT ON THE FORMATION OF AMYLOID FIBRILLES
MX2008007477A (es) 2005-12-12 2008-09-03 Ac Immune Sa Anticuerpos monoclonales especificos 1-42 beta con propiedades terapeuticas.
SG172617A1 (en) 2005-12-12 2011-07-28 Ac Immune Sa Therapeutic vaccine
GB0704100D0 (en) 2006-03-17 2007-04-11 Vodafone Plc Improvements in an ehspa architecture
NZ574188A (en) 2006-07-14 2012-05-25 Ac Immune Sa Humanized antibody against amyloid beta
EP2091945B1 (en) 2006-11-09 2014-01-15 Probiodrug AG Novel inhibitors of glutaminyl cyclase
US7741354B2 (en) 2006-11-09 2010-06-22 Probiodrug Ag Inhibitors of glutaminyl cyclase
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
JP5523107B2 (ja) 2006-11-30 2014-06-18 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
SG193828A1 (en) * 2008-09-04 2013-10-30 Probiodrug Ag Novel inhibitors
MX2012002993A (es) 2009-09-11 2012-04-19 Probiodrug Ag Derivados heterociclicos como inhibidores de ciclasa glutaminilo.
US8269019B2 (en) 2010-03-10 2012-09-18 Probiodrug Ag Inhibitors

Also Published As

Publication number Publication date
EP2686313B1 (en) 2016-02-03
DK2686313T3 (en) 2016-05-02
JP2014508184A (ja) 2014-04-03
US8530670B2 (en) 2013-09-10
WO2012123563A1 (en) 2012-09-20
ES2570167T3 (es) 2016-05-17
EP2686313A1 (en) 2014-01-22
US20120237475A1 (en) 2012-09-20

Similar Documents

Publication Publication Date Title
JP5688745B2 (ja) グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤
JP5612860B2 (ja) 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
JP5675340B2 (ja) 新規阻害剤
JP5523107B2 (ja) グルタミニルシクラーゼの新規阻害剤
JP5934645B2 (ja) グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
JP5707327B2 (ja) 新規の阻害剤
JP5798157B2 (ja) 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
JP6026284B2 (ja) グルタミニルシクラーゼの阻害剤
JP5667440B2 (ja) 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
JP5675343B2 (ja) グルタミニルシクラーゼ阻害剤としての尿素誘導体
JP5675342B2 (ja) 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
JP6454651B2 (ja) 新規阻害剤
JP5675344B2 (ja) グルタミニルシクラーゼ阻害剤としてのニトロビニルジアミン誘導体
DK2686313T3 (en) Benzimidazole derivatives as inhibitors of glutaminyl cyclase
JP2010509285A (ja) グルタミニルシクラーゼの新規阻害剤
JP5945532B2 (ja) グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150313

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150313

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20151112

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20151215

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160311

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160615

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160712

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161011

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20161108

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20161124

R150 Certificate of patent or registration of utility model

Ref document number: 6050264

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250