CN1658852A - 用于治疗淀粉样变性的脒衍生物 - Google Patents

用于治疗淀粉样变性的脒衍生物 Download PDF

Info

Publication number
CN1658852A
CN1658852A CN028157702A CN02815770A CN1658852A CN 1658852 A CN1658852 A CN 1658852A CN 028157702 A CN028157702 A CN 028157702A CN 02815770 A CN02815770 A CN 02815770A CN 1658852 A CN1658852 A CN 1658852A
Authority
CN
China
Prior art keywords
group
aryl
alkyl
independently
hydrogen
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.)
Pending
Application number
CN028157702A
Other languages
English (en)
Chinese (zh)
Inventor
R·J·查利福尔
孔宪起
吴新福
吕文硕
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bellus Health International Ltd
Original Assignee
Neurochem International Ltd
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 Neurochem International Ltd filed Critical Neurochem International Ltd
Publication of CN1658852A publication Critical patent/CN1658852A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P25/28—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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN028157702A 2001-08-31 2002-09-03 用于治疗淀粉样变性的脒衍生物 Pending CN1658852A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US31676101P 2001-08-31 2001-08-31
US60/316,761 2001-08-31
US38700102P 2002-06-07 2002-06-07
US60/387,001 2002-06-07

Publications (1)

Publication Number Publication Date
CN1658852A true CN1658852A (zh) 2005-08-24

Family

ID=26980581

Family Applications (1)

Application Number Title Priority Date Filing Date
CN028157702A Pending CN1658852A (zh) 2001-08-31 2002-09-03 用于治疗淀粉样变性的脒衍生物

Country Status (11)

Country Link
US (3) US20040006092A1 (https=)
EP (1) EP1420773A1 (https=)
JP (1) JP2005504053A (https=)
KR (1) KR20040036908A (https=)
CN (1) CN1658852A (https=)
BR (1) BR0212078A (https=)
CA (1) CA2455497A1 (https=)
EA (1) EA200400135A1 (https=)
IL (1) IL160208A0 (https=)
MX (1) MXPA04001153A (https=)
WO (1) WO2003017994A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103012200A (zh) * 2011-09-20 2013-04-03 北京大学 具有β-分泌酶抑制功能的化合物及其制备方法与应用
CN109553608A (zh) * 2017-09-26 2019-04-02 北京大学 一类五元六元杂环化合物及其制备方法和治疗肿瘤的用途
CN113264925A (zh) * 2020-02-14 2021-08-17 上海美悦生物科技发展有限公司 一种杂环化合物及其制备方法和用途

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL146143A0 (en) * 1999-04-28 2002-07-25 Univ Kingston Compositions and methods for treating amyloidosis
EP1237547A2 (en) * 1999-07-09 2002-09-11 Isis Innovation Limited Compounds for inhibiting diseases and preparing cells for transplantation
EP1337510A4 (en) * 2000-11-06 2005-02-23 Univ North Carolina SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF NEW DICATIONIC REVERSED AMIDINES
US6737440B2 (en) 2000-11-06 2004-05-18 The University Of North Carolina At Chapel Hill Synthesis and antimicrobial activity of novel dicationic “reversed amidines”
EP1572129A4 (en) * 2002-06-07 2007-03-28 Univ North Carolina AMIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOIDOSE
US20050020945A1 (en) * 2002-07-02 2005-01-27 Tosaya Carol A. Acoustically-aided cerebrospinal-fluid manipulation for neurodegenerative disease therapy
US20040049134A1 (en) * 2002-07-02 2004-03-11 Tosaya Carol A. System and methods for treatment of alzheimer's and other deposition-related disorders of the brain
US20070010573A1 (en) * 2003-06-23 2007-01-11 Xianqi Kong Methods and compositions for treating amyloid-related diseases
US7244764B2 (en) * 2003-06-23 2007-07-17 Neurochem (International) Limited Methods and compositions for treating amyloid-related diseases
JP2007521237A (ja) * 2003-09-05 2007-08-02 ユニバーシティ オブ ノース カロライナ アット チャペル ヒル 微生物感染症処置用の新規アミジン化合物
JP2007509176A (ja) * 2003-10-24 2007-04-12 ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル 抗原虫薬としてのジカチオン性トリアリール類似体
CA2549736A1 (en) * 2003-12-05 2005-06-23 The University Of North Carolina At Chapel Hill Cationic substituted benzofurans as antimicrobial agents
US7262223B2 (en) * 2004-01-23 2007-08-28 Neurochem (International) Limited Amidine derivatives for treating amyloidosis
WO2005079780A1 (en) * 2004-01-23 2005-09-01 Neurochem (International) Limited Amidine derivatives for treating amyloidosis
BRPI0519243A2 (pt) 2004-12-22 2009-01-06 Neurochem Int Ltd mÉtodos e composiÇÕes para tratar doenÇas relacionadas a amilàide
TW200716088A (en) * 2005-04-15 2007-05-01 Neurochem Int Ltd Formulations and methods for treating amyloidosis
AU2006201739A1 (en) * 2005-05-05 2006-11-23 The University Of North Carolina At Chapel Hill Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles
WO2007023389A2 (en) * 2005-07-21 2007-03-01 Neurochem (International) Limited Polymorphic forms of 3-amino-1-propanesulfonic acid
JP5301999B2 (ja) * 2005-10-31 2013-09-25 メルク・シャープ・アンド・ドーム・コーポレーション Ｃｅｔｐ阻害薬
MX2008008213A (es) * 2005-12-22 2008-09-03 Neurochem Int Ltd Tratamiento de trastornos renales, nefropatia diabetica y dislipidemias.
DK2089417T3 (en) 2006-10-12 2015-03-23 Bhi Ltd Partnership Methods, Compounds, Compositions and Vehicles for Delivery of 3-Amion-1-Propanesulfonic Acid
CN101730529A (zh) * 2006-12-22 2010-06-09 贝鲁斯健康(国际)有限公司 用于治疗代谢疾病和糖尿病的方法、化合物和组合物
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
EP2247558B2 (en) 2008-02-14 2024-07-03 Eli Lilly and Company Novel imaging agents for detecting neurological dysfunction
EP2116236A1 (en) * 2008-04-21 2009-11-11 Université de Mons-Hainaut Bisbenzamidine derivatives for use as antioxidant
FR2933692B1 (fr) * 2008-07-10 2022-12-02 Univ Nancy 1 Henri Poincare Nouveaux composes, leur utilisation comme medicaments, et leur procede de preparation
ES2355031B2 (es) * 2009-07-15 2011-12-26 Universidade De Santiago De Compostela Derivados de bis-benzamidinios y su uso como agentes de reconocimiento de secuencias de adn.
ES2368276B2 (es) * 2010-04-27 2012-06-28 Universidad De Santiago De Compostela Compuestos derivados de bis-benzamidinios como agentes fluorogénicos para señalizar secuencias específicas de adn de doble cadena.
GB201506658D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
GB201506660D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
US12595251B2 (en) 2018-06-14 2026-04-07 Georgia State University Research Foundation, Inc. Amidines and amidine analogs for the treatment of bacterial infections and potentiation antibiotics
WO2021127452A1 (en) 2019-12-19 2021-06-24 Georgia State University Research Foundation, Inc. Compounds for the treatment of bacterial infections and potentiation of antibiotics
US20250382261A1 (en) * 2021-11-05 2025-12-18 The Broad Institute, Inc. Pentamidine analogs
CN115850219B (zh) * 2022-11-30 2024-05-28 三峡大学 泽兰素开链多聚体，制备方法及用途

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4397863A (en) * 1980-08-26 1983-08-09 Research Triangle Institute Inhibition of respiratory syncytial virus-induced cell fusion by amidino compounds
US4324794A (en) * 1980-08-26 1982-04-13 Research Triangle Institute Inhibition of respiratory syncytial virus-induced cell fusion by amidino compounds
US4515625A (en) * 1980-09-16 1985-05-07 Eli Lilly And Company Benzamides, compositions and agricultural method
US4619942A (en) * 1982-04-08 1986-10-28 University Of North Carolina Inhibition of Respiratory Syncytial virus-induced cell fusion by amidino compounds
US4522811A (en) * 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5374548A (en) * 1986-05-02 1994-12-20 Genentech, Inc. Methods and compositions for the attachment of proteins to liposomes using a glycophospholipid anchor
US5547841A (en) * 1987-10-08 1996-08-20 The Mclean Hospital Corporation In vitro method for screening for drugs that inhibit production or degradation of human A4-amyloid
US4940723A (en) * 1988-10-20 1990-07-10 University Of North Carolina, Chapel Hill Use of bis-(5-amidino-2-benzimidazolyl) methane (BABIM) to treat arthritis
US4933347A (en) * 1988-10-25 1990-06-12 University Of North Carolina At Chapel Hill Diamidines and bis(imidazolines) for the treatment of and prophylaxis against pneumocystis carinii pneumonia
US4963589A (en) * 1988-10-25 1990-10-16 The University Of North Carolina At Chapel Hill Methods for treating Giardia lamblia
US5202320A (en) * 1989-04-06 1993-04-13 Tidwell Richard R Method for treating leishmaniasis
US5206236A (en) * 1989-04-06 1993-04-27 Tidwell Richard R Method for the treatment of malaria
ES2217250T3 (es) * 1990-06-15 2004-11-01 Scios Inc. Mamifero transgenico, no humano que muestra la patologia de formacion amiloides de la enfermedad de alzheimer.
US5246965A (en) * 1991-06-11 1993-09-21 Ciba-Geigy Arylethers, their manufacture and methods of treatment
US5451700A (en) * 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
US5434050A (en) * 1991-08-13 1995-07-18 Regents Of The University Of Minnesota Labelled β-amyloid peptide and methods of screening for Alzheimer's disease
JP3008615B2 (ja) * 1991-11-15 2000-02-14 大同特殊鋼株式会社 ラジアル異方性リング磁石及びその製造方法
AU671093B2 (en) * 1992-01-07 1996-08-15 Elan Pharmaceuticals, Inc. Transgenic animal models for alzheimer's disease
US5538845A (en) * 1992-02-05 1996-07-23 Athena Neurosciences, Inc. Beta-amyloid peptide production inhibitors and methods for their identification
CA2427890A1 (en) * 1992-02-05 1993-08-19 Ralf Anderskewitz New amidine derivatives, the preparation and use thereof
US5441870A (en) * 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
US5428051A (en) * 1992-10-13 1995-06-27 University Of North Carolina Methods of combating pneumocystis carinii pneumonia and compounds useful therefor
US5605811A (en) * 1992-10-26 1997-02-25 Athena Neurosciences, Inc. Methods and compositions for monitoring cellular processing of beta-amyloid precursor protein
US5726197A (en) * 1992-11-02 1998-03-10 Syntex (U.S.A.) Inc. Isoindolinyl derivatives
US5840294A (en) * 1993-03-29 1998-11-24 Queen's University At Kingston Method for treating amyloidosis
US5643562A (en) * 1993-03-29 1997-07-01 Queen's University Of Kingston Method for treating amyloidosis
US5972328A (en) * 1993-03-29 1999-10-26 Queen's University At Kingston Method for treating amyloidosis
US5552426A (en) * 1994-04-29 1996-09-03 Eli Lilly And Company Methods for treating a physiological disorder associated with β-amyloid peptide
US5723288A (en) * 1994-05-06 1998-03-03 The University Of North Carolina At Chapel Hill Method of fluorescent detection of nucleic acids and cytoskeleton elements using bis-dicationic aryl furans, and kits useful therefor
US5667975A (en) * 1994-05-06 1997-09-16 The University Of North Carolina Method of fluorescent detection of nucleic acids and cytoskeleton elements using bis-dicationic aryl furans
US5602172A (en) * 1994-05-06 1997-02-11 The University Of North Carolina At Chapel Hill Methods of inhibiting Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium and compounds useful therefor
US5521189A (en) * 1994-05-06 1996-05-28 The University Of Nc At Ch Methods of treating pneumocystis carinii pneumonia
DE4424714A1 (de) * 1994-07-13 1996-01-18 Boehringer Ingelheim Kg Neue chemische Verbindung, ihre Herstellung und ihre Verwendung als Arnzneistoff
DE4424713A1 (de) * 1994-07-13 1996-01-18 Boehringer Ingelheim Kg Substituierte Benzamidine, ihre Herstellung und Verwendung als Arnzneistoffe
FR2726558B1 (fr) * 1994-11-03 1996-12-06 Adir Nouvelles 5-(aryloxymethyl) oxazolines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5612363A (en) * 1995-06-02 1997-03-18 Berlex Laboratories, Inc. N,N-di(aryl) cyclic urea derivatives as anti-coagulants
US5668166A (en) * 1995-06-07 1997-09-16 Georgia State University Research Foundation, Inc. Methods of inhibiting pneumocystis carinii pneumonia and compounds useful therefor
US5643935A (en) * 1995-06-07 1997-07-01 The University Of North Carolina At Chapel Hill Method of combatting infectious diseases using dicationic bis-benzimidazoles
US5574059A (en) * 1995-10-27 1996-11-12 Cornell Research Foundation, Inc. Treating disorders mediated by vascular smooth muscle cell proliferation
US5723495A (en) * 1995-11-16 1998-03-03 The University Of North Carolina At Chapel Hill Benzamidoxime prodrugs as antipneumocystic agents
DE19546452A1 (de) * 1995-12-13 1997-06-19 Boehringer Ingelheim Kg Neue Phenylamidinderivate, Verfahren zu ihrer Herstelung und ihre Verwendung als Arzneimittel
DE19636689A1 (de) * 1996-09-10 1998-03-12 Boehringer Ingelheim Kg Neue Benzamidinderivate
AU4432597A (en) * 1996-09-25 1998-04-17 Regents Of The University Of California, The Methods of using agmatine to reduce intracellular polyamine levels and to inhibit inducible nitric oxide synthase
US6133281A (en) * 1996-10-24 2000-10-17 Harbor-Ucla Research And Education Institute NMDA receptor blockers in the therapy of urogenital disease
US5871924A (en) * 1997-01-27 1999-02-16 Nexstar Pharmaceuticals, Inc. Method for the production of ligands capable of facilitating aminoacyl-RNA synthesis
US5935982A (en) * 1997-02-28 1999-08-10 The University Of North Carolina At Chapel Hill Methods of treating retroviral infection and compounds useful therefor
US6008247A (en) * 1998-02-27 1999-12-28 The University Of North Carolina At Chapel Hill 2,4-bis[(4-amidino)phenyl]furans as anti-Pneumocystis carinii agents
US6635668B1 (en) * 1998-07-22 2003-10-21 The University Of North Carolina At Chapel Hill Imidazoline receptor binding compounds
AU758563B2 (en) * 1998-08-20 2003-03-27 University Of North Carolina At Chapel Hill, The Dicationic dibenzofuran and dibenzothiophene compounds and methods of use thereof
ES2275362T3 (es) * 1998-09-17 2007-06-01 The University Of North Carolina At Chapel Hill Actividad antifungica de moleculas dicationicas.
US6319944B1 (en) * 1999-05-10 2001-11-20 Merck & Co., Inc. Aryl amidines, compositions containing such compounds and methods of use
US6627647B1 (en) * 2000-03-23 2003-09-30 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted 1-(4-aminophenyl)imidazoles and their use as anti-inflammatory agents
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
US6625612B1 (en) * 2000-06-14 2003-09-23 Ezchip Technologies Ltd. Deterministic search algorithm
WO2002002516A2 (en) * 2000-06-30 2002-01-10 Thomas Jefferson University Inhibitors of hiv integrase
US6737440B2 (en) * 2000-11-06 2004-05-18 The University Of North Carolina At Chapel Hill Synthesis and antimicrobial activity of novel dicationic “reversed amidines”
JP4368582B2 (ja) * 2001-01-13 2009-11-18 ユニバーシティ オブ ノース カロライナ アット チャペル ヒル 牛ウイルス性下痢ウイルス（ｂｖｄｖ）感染およびｃ型肝炎ウイルス（ｈｃｖ）感染を処置するのに有用な化合物、方法、および組成物

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103012200A (zh) * 2011-09-20 2013-04-03 北京大学 具有β-分泌酶抑制功能的化合物及其制备方法与应用
CN103012200B (zh) * 2011-09-20 2014-12-17 北京大学 具有β-分泌酶抑制功能的化合物及其制备方法与应用
CN109553608A (zh) * 2017-09-26 2019-04-02 北京大学 一类五元六元杂环化合物及其制备方法和治疗肿瘤的用途
CN113264925A (zh) * 2020-02-14 2021-08-17 上海美悦生物科技发展有限公司 一种杂环化合物及其制备方法和用途
WO2021160132A1 (zh) * 2020-02-14 2021-08-19 上海美悦生物科技发展有限公司 一种杂环化合物及其制备方法和用途

Also Published As

Publication number Publication date
WO2003017994A1 (en) 2003-03-06
EA200400135A1 (ru) 2004-08-26
JP2005504053A (ja) 2005-02-10
US20040006092A1 (en) 2004-01-08
KR20040036908A (ko) 2004-05-03
IL160208A0 (en) 2004-07-25
CA2455497A1 (en) 2003-03-06
US20070021483A1 (en) 2007-01-25
BR0212078A (pt) 2004-09-28
MXPA04001153A (es) 2005-02-17
EP1420773A1 (en) 2004-05-26
US20040147531A1 (en) 2004-07-29

Similar Documents

Publication Publication Date Title
CN1658852A (zh) 用于治疗淀粉样变性的脒衍生物
CN1282640C (zh) N－芳基苯乙酰胺衍生物及包含所述化合物的药物组合物
CN1253150C (zh) 单独的或与抗血小板聚集药物联合的Xa因子抑制剂
CN1100535C (zh) 用于治疗呕吐的药剂
CN100343255C (zh) 吡唑并[1,5－a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
CN1149210C (zh) 凝血酶抑制剂
CN1156445C (zh) 采用二氢异吲哚衍生物抑制淀粉样蛋白聚集和使淀粉样蛋白沉积成像的方法
CN1642904A (zh) 那格列奈的盐
CN1805743A (zh) 用作逆转淀粉样变性及其他与之相关疾病的rage拮抗剂
CN1091006A (zh) 用作降血糖药和治疗早老性痴呆症的化合物
CN1659148A (zh) 芳基肟化合物
CN101056845A (zh) 取代的苯胺衍生物
CN1070646A (zh) 咪唑并稠合碳环和杂环，它们的制备方法，含有它们的组合物以及它们的应用
CN101043887A (zh) 用作s1p受体激动剂的2－(芳基)氮杂环甲基羧酸酯、磺酸酯、膦酸酯、次膦酸酯和杂环化合物
CN1261795A (zh) 化合物和方法
CN1468211A (zh) 亚硝基二苯胺衍生物
CN1087904A (zh) 羧酸衍生物，含有这些化合物的药物组合物以及其制备方法
CN1897928A (zh) 用于功能上影响不同类型的细胞和用于治疗免疫、炎症、神经和其他疾病的新的丙氨酰氨肽酶抑制剂
CN1518541A (zh) 苯基衍生物
CN1364156A (zh) 萘脲类作为葡萄糖摄取的增强剂
CN1714076A (zh) 芳基脲基衍生物及其医药用途
CN1993120A (zh) 用于治疗阿尔茨海默氏病的芳基乙酸和相关化合物
CN101048180A (zh) 具有改善的溶解度和稳定性的固体制剂和用于制备所述制剂的方法
CN1863763A (zh) 用于治疗疾病的氨基脲敏感性胺氧化酶(ssao)和vap－1介导的粘着的抑制剂
HK1047277A1 (zh) 吡嗪酮凝血酶抑制剂

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
AD01 Patent right deemed abandoned
C20 Patent right or utility model deemed to be abandoned or is abandoned