TWI335221B - Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma - Google Patents

Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma Download PDF

Info

Publication number
TWI335221B
TWI335221B TW091120600A TW91120600A TWI335221B TW I335221 B TWI335221 B TW I335221B TW 091120600 A TW091120600 A TW 091120600A TW 91120600 A TW91120600 A TW 91120600A TW I335221 B TWI335221 B TW I335221B
Authority
TW
Taiwan
Prior art keywords
alkyl
amine
nr6r7
gsk
pharmaceutical composition
Prior art date
Application number
TW091120600A
Other languages
English (en)
Chinese (zh)
Inventor
P Hellberg Mark
F Clark Abbot
Iok Hou Pang
E Magnino Peggy
M Mcnatt Loretta
Wang Wan-Heng
Original Assignee
Alcon Inc
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 Alcon Inc filed Critical Alcon Inc
Application granted granted Critical
Publication of TWI335221B publication Critical patent/TWI335221B/zh

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW091120600A 2001-09-27 2002-09-10 Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma TWI335221B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US32539001P 2001-09-27 2001-09-27

Publications (1)

Publication Number Publication Date
TWI335221B true TWI335221B (en) 2011-01-01

Family

ID=23267686

Family Applications (2)

Application Number Title Priority Date Filing Date
TW099127943A TW201041580A (en) 2001-09-27 2002-09-10 Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma
TW091120600A TWI335221B (en) 2001-09-27 2002-09-10 Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma

Family Applications Before (1)

Application Number Title Priority Date Filing Date
TW099127943A TW201041580A (en) 2001-09-27 2002-09-10 Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma

Country Status (15)

Country Link
US (2) US7598288B2 (enExample)
EP (2) EP1430120A4 (enExample)
JP (2) JP2005504101A (enExample)
KR (1) KR20040047824A (enExample)
CN (2) CN101380319A (enExample)
AR (1) AR036684A1 (enExample)
AU (1) AU2002334635B2 (enExample)
BR (1) BR0212924A (enExample)
CA (1) CA2460000C (enExample)
MX (1) MXPA04002137A (enExample)
PL (1) PL207022B1 (enExample)
RU (1) RU2297243C2 (enExample)
TW (2) TW201041580A (enExample)
WO (1) WO2003027275A1 (enExample)
ZA (1) ZA200401846B (enExample)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2400543C (en) * 2001-08-31 2011-11-01 Centre For Addiction And Mental Health The involvement of the bdnf gene in mood disorders
RU2332213C2 (ru) * 2002-04-30 2008-08-27 Алькон, Инк. Агенты, которые регулируют, ингибируют или модулируют активность и/или экспрессию факторов роста соединительной ткани (фрст), в качестве уникальных средств для снижения внутриглазного давления и лечения глаукоматозных ретинопатий/оптических невропатий
EP1616568A3 (en) * 2002-04-30 2006-06-21 Alcon, Inc GSK-3 inhibitors and CDK inhibitors as anti-glaucoma agents
WO2004103958A2 (en) 2003-05-19 2004-12-02 Michigan State University Preparation of hymenialdisine derivatives and use thereof
CN1897972A (zh) * 2003-12-22 2007-01-17 爱尔康公司 用于治疗青光眼性视网膜病和视神经病的活性剂
TW200526224A (en) * 2003-12-22 2005-08-16 Alcon Inc Short form c-Maf transcription factor antagonists for treatment of glaucoma
US20050137147A1 (en) * 2003-12-22 2005-06-23 Alcon, Inc. Agents for treatment of diabetic retinopathy and drusen formation in macular degeneration
CA2550891A1 (en) * 2003-12-24 2005-07-14 Bayer Cropscience Gmbh Plant growth regulation
WO2005102345A1 (en) * 2004-03-30 2005-11-03 Alcon, Inc. Use of rho kinase inhibitors in the treatment of hearing loss, tinnitus and improving body balance
US20080096238A1 (en) * 2004-03-30 2008-04-24 Alcon, Inc. High throughput assay for human rho kinase activity with enhanced signal-to-noise ratio
CA2566392A1 (en) * 2004-05-12 2005-11-17 Bayer Cropscience Gmbh Plant growth regulation
WO2006089874A1 (en) * 2005-02-22 2006-08-31 Gpc Biotech Ag Benzo[2,3]azepino[4,5-b]indol-6-ones
EP1856259A1 (en) * 2005-03-11 2007-11-21 Alcon Inc. Rnai-mediated inhibition of frizzled related protein-1 for treatment of glaucoma
RU2284192C1 (ru) * 2005-04-01 2006-09-27 Государственное учреждение Межотраслевой научно-технический комплекс "Микрохирургия глаза" им. акад. С.Н. Федорова Министерства здравоохранения РФ Способ лечения глаукомной оптической нейропатии
US20080207594A1 (en) 2005-05-04 2008-08-28 Davelogen Aktiengesellschaft Use of Gsk-3 Inhibitors for Preventing and Treating Pancreatic Autoimmune Disorders
EP1757607A1 (en) 2005-08-24 2007-02-28 Molisa GmbH N5-substituted benzo¬2,3|azepino¬4,5-b|indol-6-ones for treating tropical diseases
US7884119B2 (en) 2005-09-07 2011-02-08 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as Axl inhibitors
WO2007146136A2 (en) * 2006-06-12 2007-12-21 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
CA2710230C (en) 2006-12-29 2016-02-23 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
EP2079736B1 (en) 2006-12-29 2017-10-18 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
JP5567837B2 (ja) 2006-12-29 2014-08-06 ライジェル ファーマシューティカルズ, インコーポレイテッド Axlインヒビターとして有用なN3−ヘテロアリール置換トリアゾールおよびN5−ヘテロアリール置換トリアゾール
CA2710043C (en) 2006-12-29 2016-02-09 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
WO2008083367A2 (en) 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
WO2009054864A1 (en) 2007-10-26 2009-04-30 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
JP5592884B2 (ja) 2008-07-09 2014-09-17 ライジェル ファーマシューティカルズ, インコーポレイテッド Axl阻害剤として有用な多環式ヘテロアリール置換トリアゾール
WO2010005879A1 (en) 2008-07-09 2010-01-14 Rigel Pharmaceuticals, Inc. Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
CN102281875B (zh) 2009-01-16 2017-09-22 里格尔药品股份有限公司 预防、治疗或应对转移癌的使用axl抑制剂的组合疗法
UA103918C2 (en) * 2009-03-02 2013-12-10 Айерем Элелси N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators
RU2456266C1 (ru) * 2011-04-06 2012-07-20 Максим Эдуардович Запольский Производные 4,4'-бифениламидов, обладающие фармакологической активностью, и лекарственные средства на их основе
EP3272880B1 (en) 2013-03-15 2020-11-25 Fundació Institut de Recerca Biomèdica (IRB Barcelona) Method for the diagnosis, prognosis and treatment of metastatic cancer
EP3089748A4 (en) * 2014-01-02 2017-09-27 Massachusetts Eye & Ear Infirmary Treating ocular neovascularization
WO2015155738A2 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
US12396889B2 (en) 2014-05-12 2025-08-26 Gholam A. Peyman Lamellar corneal autologous or homologous graft in refractive surgery
US11565023B2 (en) 2014-05-12 2023-01-31 Gholam A. Peyman Method of corneal transplantation or corneal inlay implantation with cross-linking
US10583221B2 (en) 2014-05-12 2020-03-10 Gholam A. Peyman Method of corneal transplantation or corneal inlay implantation with cross-linking
US11045352B2 (en) 2014-05-12 2021-06-29 Gholam A. Peyman Methods for treatment of dry eye and other acute or chronic inflammatory processes
US11338059B2 (en) 2014-05-12 2022-05-24 Gholam A. Peyman Method of corneal and scleral inlay crosslinking and preservation
US10881503B2 (en) 2014-05-12 2021-01-05 Gholam A. Peyman Method of corneal transplantation or corneal inlay implantation with cross-linking
US11648261B2 (en) 2014-05-12 2023-05-16 Gholam A. Peyman Method of treating, reducing, or alleviating a medical condition in a patient
US10925889B2 (en) 2014-05-12 2021-02-23 Gholam A. Peyman Method of treating, reducing, or alleviating a medical condition in a patient
US11666777B2 (en) 2014-05-12 2023-06-06 Gholam A. Peyman Photodynamic therapy technique for preventing damage to the fovea of the eye or another body portion of a patient
TWI677489B (zh) 2014-06-20 2019-11-21 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
WO2019221959A1 (en) * 2018-05-16 2019-11-21 Peyman Gholam A Method of treating, reducing, or alleviating a medical condition in a patient
US11707518B2 (en) 2019-04-28 2023-07-25 Gholam A. Peyman Method of treating, reducing, or alleviating a medical condition in a patient
US12226478B2 (en) 2019-04-28 2025-02-18 Gholam A. Peyman Method of treating, reducing, or alleviating a medical condition in a patient
US12110278B2 (en) * 2020-10-13 2024-10-08 Yale University Selective JAK2 pseudokinase ligands and methods of use

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ227850A (en) 1988-02-10 1991-11-26 Hoffmann La Roche Indole substituted pyrrole derivatives; preparatory process and medicaments for use against inflammatory immunological, bronchopulmonary or vascular disorders
MC2096A1 (fr) 1989-02-23 1991-02-15 Hoffmann La Roche Pyrroles substitues
DE3914764A1 (de) 1989-05-05 1990-11-08 Goedecke Ag Maleinimid-derivate und deren verwendung als arzneimittel
IL94274A0 (en) 1989-05-05 1991-03-10 Goedecke Ag Maleinimide derivatives,process for the preparation thereof and pharmaceutical compositions containing the same
DE4005969A1 (de) 1990-02-26 1991-08-29 Boehringer Mannheim Gmbh Neue trisubstituierte pyrrole, verfahren zu ihrer herstellung sowie arzneimittel, die diese verbindungen enthalten
DE4005970A1 (de) 1990-02-26 1991-08-29 Boehringer Mannheim Gmbh Neue trisubstituierte maleinimide, verfahren zu ihrer herstellung sowie arzneimittel, die diese verbindungen enthalten
CA2046801C (en) 1990-08-07 2002-02-26 Peter D. Davis Substituted pyrroles
CZ213693A3 (en) 1991-04-11 1994-05-18 Schering Corp Diindolepyrrolbenzodiazocines, process of their preparation and use, and a pharmaceutical mixture based thereon
GB9123396D0 (en) 1991-11-04 1991-12-18 Hoffmann La Roche A process for the manufacture of substituted maleimides
ATE175873T1 (de) 1992-03-20 1999-02-15 Wellcome Found Weitere indolderivate mit antiviraler wirkung
AU3761393A (en) 1992-03-20 1993-10-21 Wellcome Foundation Limited, The Indole derivatives with antiviral activity
DE4217964A1 (de) 1992-05-30 1993-12-02 Goedecke Ag Indolocarbazol-Imide und deren Verwendung
DE4243321A1 (de) 1992-12-21 1994-06-23 Goedecke Ag Aminosäurederivate von Heterocyclen als PKC-Inhibitoren
GB9319297D0 (en) 1993-09-17 1993-11-03 Wellcome Found Indole derivatives
GB9416467D0 (en) 1994-08-13 1994-10-05 Wellcome Found Compounds for use in medicine
US5681854A (en) * 1995-11-22 1997-10-28 Alcon Laboratories, Inc. Use of aliphatic carboxylic acid derivatives in ophthalmic disorders
US6057117A (en) 1996-04-04 2000-05-02 Chiron Corporation Identification and use of selective inhibitors of glycogen synthase kinase 3
WO1997041854A1 (en) * 1996-05-07 1997-11-13 The Trustees Of The University Of Pennsylvania Inhibitors of glycogen synthase kinase-3 and methods for identifying and using the same
PE91698A1 (es) * 1996-07-29 1998-12-24 Hoffmann La Roche Pirroles sustituidos
PE91498A1 (es) 1996-07-29 1998-12-22 Hoffmann La Roche Pirroles sustituidos
PE91598A1 (es) 1996-07-29 1998-12-24 Hoffmann La Roche Pirroles sustituidos
SE9603285D0 (sv) 1996-09-10 1996-09-10 Astra Ab New compounds
SE9603283D0 (sv) 1996-09-10 1996-09-10 Astra Ab New compounds
CA2297967A1 (en) * 1997-08-07 1999-02-18 The Regents Of The University Of California Purine inhibitor of protein kinases, g proteins and polymerases
EP1057484A4 (en) 1998-02-23 2002-11-20 Sagami Chem Res INHIBITORS OF CELL DEATH
EP1079826B1 (en) * 1998-05-29 2003-03-05 CNRS, Centre National de la Recherche Scientifique Use of indigoid bisindole derivatives for the manufacture of a medicament to inhibit cyclin dependent kinases
DE69922526T2 (de) 1998-10-08 2005-06-02 Smithkline Beecham Plc, Brentford 3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1h-pyrrol-2,5-dion als glykogen synthase kinase-3 inhibitor (gsk-3)
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
GB9918180D0 (en) 1999-08-02 1999-10-06 Smithkline Beecham Plc Novel compositions
EP1224932A4 (en) * 1999-08-20 2002-10-16 Sagami Chem Res ACTIVE SUBSTANCES TO INHIBIT CELL DEATH
FR2801216A1 (fr) 1999-11-23 2001-05-25 Centre Nat Rech Scient Utilisation de derives d'indirubine pour la fabrication de medicaments
ES2213996T3 (es) 1999-12-08 2004-09-01 Centre National De La Recherche Scientifique (Cnrs) Uso de himenialdisina o sus derivados en la fabricacion de medicamentos.
EP1244461A2 (en) 1999-12-23 2002-10-02 The Ontario Cancer Institute INHIBITION OF GSK-3$g(b)
AU2625201A (en) 2000-01-03 2001-07-16 Ramot University Authority For Applied Research And Industrial Development Ltd. Glycogen synthase kinase-3 inhibitors
AU2001230026A1 (en) 2000-02-04 2001-08-14 Novo-Nordisk A/S 2,4-diaminothiazole derivatives
EP1259648A2 (en) 2000-02-29 2002-11-27 Alcon Laboratories, Inc. Diagnostics and therapeutics for glaucoma
AU2001248365A1 (en) * 2000-03-23 2001-10-03 Mitsubishi Pharma Corporation 2-(arylalkylamino)pyrimidone derivatives and 2-(heteroarylalkylamino)pyrimidone derivatives
EP1136099A1 (en) * 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-(Indolylalkylamino)pyrimidone derivatives as GSK3beta inhibitors
EP1136482A1 (en) * 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors
DE60227718D1 (de) 2001-09-21 2008-08-28 Sanofi Aventis Verwendung von 2-Fuoro-3-Ketoestern zur Herstellung von 3-Fuoro-6,7,8,9-tetrahydro-4H-pyrimidoÄ1,2-aÜpyrimidin-4-onen

Also Published As

Publication number Publication date
JP2005320350A (ja) 2005-11-17
US20040186159A1 (en) 2004-09-23
EP1430120A1 (en) 2004-06-23
US7598288B2 (en) 2009-10-06
AR036684A1 (es) 2004-09-29
MXPA04002137A (es) 2004-06-29
RU2297243C2 (ru) 2007-04-20
CN101380319A (zh) 2009-03-11
ZA200401846B (en) 2005-03-07
PL369130A1 (en) 2005-04-18
AU2002334635B2 (en) 2007-06-21
CA2460000A1 (en) 2003-04-03
BR0212924A (pt) 2005-01-04
PL207022B1 (pl) 2010-10-29
RU2004112766A (ru) 2005-03-27
WO2003027275A1 (en) 2003-04-03
TW201041580A (en) 2010-12-01
JP2005504101A (ja) 2005-02-10
US20090312390A1 (en) 2009-12-17
EP1430120A4 (en) 2007-06-20
CA2460000C (en) 2013-01-29
KR20040047824A (ko) 2004-06-05
EP2281560A1 (en) 2011-02-09
CN1561393A (zh) 2005-01-05

Similar Documents

Publication Publication Date Title
TWI335221B (en) Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma
AU2002334635A1 (en) Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma
CN101679328B (zh) 老年黄斑变性的预防或治疗剂
JP2008247898A (ja) トリテルペノイドを有効成分として含有する酸化ストレスが関連する眼疾患の予防又は治療剤
CA2414780A1 (en) Ophthalmic formulation of a selective cyclooxygenase-2 inhibitory drug
TW309426B (enExample)
EP2319539A1 (en) Prophylactic or therapeutic agent for axial myopia
CN101048156B (zh) 用于治疗青光眼性视网膜病变及眼病的JunN端激酶抑制剂
EA027524B1 (ru) Способ ингибирования гиперпроницаемости сосудов при отеке маклы
JP2004182723A (ja) Rhoキナーゼ阻害剤とβ遮断薬からなる緑内障治療剤
CN101594884A (zh) 视网膜神经或视神经的保护剂
JP2004503601A (ja) 眼のcox−2媒介疾患の処置及び予防におけるcox−2阻害剤の使用法
JP2000198734A (ja) 胃運動性減弱および関連疾患の治療のための運動性増強薬
JP2009001591A (ja) 緑内障治療用のデプレニル化合物
AU2005292259A1 (en) Compositions and methods for treating ophthalmic diseases
WO2019131901A1 (ja) ピリジルアミノ酢酸化合物を含有する医薬製剤
CN115768433A (zh) 含有司培前列素的医药制剂
WO2005079792A1 (ja) 重症糖尿病網膜症の予防又は治療剤
US5486506A (en) Method for treating cardiac inotropic irregularities
US6090829A (en) Method for treating excessive aggression
Hoyng et al. Behaviour of IOP and pupil size after topical tranylcypromine in the rabbit eye
HK1153935A (en) Inhibitors of glycogen synthase kinase-3 (gsk-3) for treating glaucomatous optic neuropathy
WO1998005207A1 (en) Method for treating excessive aggression
WO2006062069A1 (ja) p38MAPキナーゼ阻害剤を有効成分とする掻痒治療剤
HK1008931A (en) Use of 3-(4-hexyloxy-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyridine (xanomeline ) for treating excessive aggression

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees