JPH08501080A - ビス‐スタウロスポリンおよびK‐252a誘導体 - Google Patents
ビス‐スタウロスポリンおよびK‐252a誘導体Info
- Publication number
- JPH08501080A JPH08501080A JP6504731A JP50473194A JPH08501080A JP H08501080 A JPH08501080 A JP H08501080A JP 6504731 A JP6504731 A JP 6504731A JP 50473194 A JP50473194 A JP 50473194A JP H08501080 A JPH08501080 A JP H08501080A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- neurons
- compound
- neuronal degeneration
- neuron
- 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.)
- Granted
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic 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
- A61K31/407—Heterocyclic 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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
-
- 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
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/28—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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Molecular Biology (AREA)
- Virology (AREA)
- Psychology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Communicable Diseases (AREA)
- Physical Education & Sports Medicine (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式: [Stau]-N(CH3)-W-N(CH3)-[Stau] (I) [式中、[Stau]は式: の残基を表し、Wは式: -C(=Y)-NH-W'-NH-C(=Y)- の基を表し、ここに、W’は2−20個の炭素原子のヒドロカルビレン基であっ て、YはOまたはSを意味する] で示される組成物。 2.請求項1記載の組成物の治療量を哺乳動物に投与することを特徴とする哺 乳動物において感覚ニューロンの機能を高める方法。 3.該感覚ニューロンがコリン作動性ニューロン、線条体ニューロン、または 後根神経節ニューロンである請求項2記載の方法。 4.請求項1記載の組成物の治療量を哺乳動物に投与することを特徴とする興 奮性アミノ酸により誘導される神経細胞変性を治療する方法。 5.該神経細胞変性がアルツハイマー病と関連している請求項4記載の方法。 6.該神経細胞変性が運動ニューロン病と関連している請求項4記載の方法。 7.該運動ニューロン病が筋萎縮硬化症である請求項6記載の方法。 8.該神経細胞変性がパーキンソン病と関連している請求項4記載の方法。 9.該神経細胞変性が脳血管疾患と関連している請求項4記載の方法。 10.該脳血管疾患が虚血症である請求項9記載の方法。 11.該神経細胞変性がAIDS痴呆と関連している請求項4記載の方法。 12.該神経細胞変性が癲癇と関連している請求項4記載の方法。 13.該神経細胞変性が脳への振盪損傷と関連している請求項4記載の方法。 14.該神経細胞変性が脊髄への振盪損傷と関連している請求項4記載の方法。 15.該神経細胞変性が脳への穿通損傷と関連している請求項4記載の方法。 16.該神経細胞変性が脊髄への穿通損傷と関連している請求項4記載の方法。 17.該神経細胞変性がハンチントン舞踏病と関連している請求項4記載の方法 。 18.哺乳動物に、式: [式中、以下の置換基がある: (1)Z1およびZ2は共に水素であるか、または示す場合は一緒になって酸素 を表す; (2)NH−アミノ酸連合は、該アミノ酸のカルボキシル基を介するアミド結 合である; (3)XおよびRは、一緒になって連結基を形成する; (4)R3はCH2CH=CH2;R4はHである; (5)R3およびR4は各々Hである; (6)R3およびR4は各々CH2CH=CH2である; (7)化合物は塩酸塩の形態である; (8)R3はHであってR4はCH2CH=CH2であり; (9)IV−1およびIV−4は、2つの成分の1.5ないし1.0混合物である ]で示されるK−252aの機能性誘導体の治療量を投与することを特徴とする 、該哺乳動物において、感覚ニューロン、コリン作動性ニューロン、および線条 体ニューロンよりなる群から選択されるニューロンの機能を高める方法。 19.該ニューロンがコリン作動性ニューロンである請求項18記載の方法。 20.該感覚ニューロンが後根神経節ニューロンであって、該機能性誘導体が 式(II)または(III): [式中、以下の置換基がある: (1)R2は水素、但し化合物II-20およびII-32においてはR2=Br; (2)Z1およびZ2は共に水素であるか、または示す場合は一緒になって酸素 を表す; (3)XおよびRは一緒になって連結基を形成する] で示される請求項18記載の方法。 21.該組成物を神経栄養因子と組み合わせて投与する請求項2記載の方法。 22.該組成物を栄養因子と組み合わせて投与する請求項4記載の方法。 23.該機能性誘導体を栄養因子と組み合わせて投与する請求項18記載の方法 。 24.該機能性誘導体を栄養因子と組み合わせて投与する請求項20記載の方法 。 25.該栄養因子がニューロトロフィンファミリーのメンバーである請求項21 、22、23または24記載の方法。 26.該ニューロトロフィンファミリーのメンバーが神経成長因子(NGF)で ある請求項25記載の方法。 27.該ニューロンがコリン作動性ニューロンであって、該機能性誘導体が、式 (II): [式中、R1およびR2はH、XはCO2CH3、RはOHであって、Z1およびZ2 は各々Hを意味する] で示される請求項18記載の方法。 28.該ニューロンが線条体ニューロンであって、該機能性誘導体が式(II)、 (III)または(IV): [式中、以下の置換基がある: (1)Z1およびZ2は共に水素であるか、または示す場合は一緒になって酸素 を表す; (2)R3はCH2-CH=CH2;R4はHを意味する] で示される請求項18記載の方法。 29.該方法をハンチントン舞踏病の治療に用いる請求項19、27または28 記載の方法。 30.式(II-4): [式中、R1、R2、Z1およびZ2は各々H、XはCH2OHであって、RはOC H3を意味する]で示される組成物。 31.式(II-14): [式中、R1、R2、Z1およびZ2は各々H、XはCH2-NH-Serであって、 RはOHを意味する] で示される組成物。 32.式(II-49): [式中、R2、Z1およびZ2は各々H、RはOH、R1はCH2SO2C2H5であっ て、XはCO2CH3を意味する] で示される組成物。 33.式(II-38): [式中、R1、R2、Z1およびZ2は各々H、RはOHであって、XはCH2NH CO2C6H5を意味する] で示される組成物。 34.式(II-45): [式中、R1およびR2は各々Br、RはOH、Z1およびZ2は各々Hであって、 XはCONHC6H5を意味する] で示される組成物。 35.式(II-57): [式中、R1、R2、Z1およびZ2は各々H、RはOHであって、XはCH2NH CO2CH3を意味する] で示される組成物。 36.式(V): [式中: XはCO2R5またはCH2NHCO2R6を表し; R1は水素またはCH2SO2R7を表し; R5は低級アルキルを表し; R6は低級アルキルまたはアリールを表し;および R7は低級アルキルを表すが;但し、X=CO2R5の場合、R1は水素ではない ]で示される組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US92010292A | 1992-07-24 | 1992-07-24 | |
US07/920,102 | 1992-07-24 | ||
PCT/US1993/006974 WO1994002488A1 (en) | 1992-07-24 | 1993-07-26 | BIS-STAUROSPORINE AND K-252a DERIVATIVES |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2002244111A Division JP3723533B2 (ja) | 1992-07-24 | 2002-08-23 | ビス−スタウロスポリンおよびK−252a誘導体 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH08501080A true JPH08501080A (ja) | 1996-02-06 |
JP3762427B2 JP3762427B2 (ja) | 2006-04-05 |
Family
ID=25443161
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50473194A Expired - Lifetime JP3762427B2 (ja) | 1992-07-24 | 1993-07-26 | ビス‐スタウロスポリンおよびK‐252a誘導体 |
JP2002244111A Expired - Fee Related JP3723533B2 (ja) | 1992-07-24 | 2002-08-23 | ビス−スタウロスポリンおよびK−252a誘導体 |
JP2005019891A Pending JP2005170955A (ja) | 1992-07-24 | 2005-01-27 | ビス−スタウロスポリンおよびK−252a誘導体 |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2002244111A Expired - Fee Related JP3723533B2 (ja) | 1992-07-24 | 2002-08-23 | ビス−スタウロスポリンおよびK−252a誘導体 |
JP2005019891A Pending JP2005170955A (ja) | 1992-07-24 | 2005-01-27 | ビス−スタウロスポリンおよびK−252a誘導体 |
Country Status (18)
Country | Link |
---|---|
US (1) | US5461146A (ja) |
EP (4) | EP0768312B1 (ja) |
JP (3) | JP3762427B2 (ja) |
KR (1) | KR100276008B1 (ja) |
AT (3) | ATE152111T1 (ja) |
AU (1) | AU675236B2 (ja) |
BR (1) | BR9306789A (ja) |
CA (1) | CA2140924A1 (ja) |
DE (3) | DE69329397T2 (ja) |
DK (3) | DK0651754T3 (ja) |
ES (3) | ES2151629T3 (ja) |
GR (2) | GR3023817T3 (ja) |
HK (1) | HK1028206A1 (ja) |
HU (5) | HU225341B1 (ja) |
NO (2) | NO305481B1 (ja) |
NZ (2) | NZ254662A (ja) |
PT (1) | PT768312E (ja) |
WO (1) | WO1994002488A1 (ja) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000021531A1 (fr) * | 1998-10-13 | 2000-04-20 | Kyowa Hakko Kogyo Co., Ltd. | Medicaments pour maladies oculaires |
JP2011126893A (ja) * | 1998-09-25 | 2011-06-30 | Cephalon Inc | 感覚毛細胞及び蝸牛ニューロンへの損傷を予防する/処置するための方法 |
Families Citing this family (59)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5756494A (en) * | 1992-07-24 | 1998-05-26 | Cephalon, Inc. | Protein kinase inhibitors for treatment of neurological disorders |
US5621101A (en) * | 1992-07-24 | 1997-04-15 | Cephalon, Inc. | Protein kinase inhibitors for treatment of neurological disorders |
DE4243321A1 (de) * | 1992-12-21 | 1994-06-23 | Goedecke Ag | Aminosäurederivate von Heterocyclen als PKC-Inhibitoren |
EP0699204B1 (en) * | 1993-05-28 | 1998-04-15 | Cephalon, Inc. | Use of indolocarbazole derivatives to treat a pathological condition of the prostate |
US5468872A (en) * | 1993-09-16 | 1995-11-21 | Cephalon, Inc. | K-252a functional derivatives potentiate neurotrophin-3 for the treatment of neurological disorders |
US5843935A (en) * | 1993-12-07 | 1998-12-01 | Eli Lilly And Company | Protein kinase C inhibitors |
KR100340159B1 (ko) * | 1993-12-07 | 2002-11-23 | 일라이 릴리 앤드 캄파니 | 단백질키나제c억제제 |
DE69418978T2 (de) * | 1993-12-07 | 1999-10-28 | Lilly Co Eli | Synthese von Bisindolylmaleimiden |
US5723456A (en) * | 1993-12-07 | 1998-03-03 | Eli Lilly & Company | Therapeutic treatment for cardiovascular diseases |
US5624949A (en) * | 1993-12-07 | 1997-04-29 | Eli Lilly And Company | Protein kinase C inhibitors |
US5541347A (en) * | 1993-12-07 | 1996-07-30 | Eli Lilly And Company | Synthesis of bisindolylmaleimides |
ATE456367T1 (de) * | 1993-12-23 | 2010-02-15 | Lilly Co Eli | Proteinkinase c inhibitoren |
AU1911095A (en) * | 1994-02-18 | 1995-09-04 | Cephalon, Inc. | Aqueous indolocarbazole solutions |
KR100464907B1 (ko) * | 1994-10-26 | 2005-07-04 | 세파론, 인코포레이티드 | 신경계질환치료용단백질키나아제억제제 |
US5686444A (en) | 1995-04-05 | 1997-11-11 | Cephalon, Inc. | Selected soluble esters of hydroxyl-containing indolocarbazoles |
US5650407A (en) * | 1995-04-05 | 1997-07-22 | Cephalon, Inc. | Selected soluble esters of hydroxyl-containing indolocarbazoles |
US5808060A (en) * | 1995-12-11 | 1998-09-15 | Cephalon, Inc. | Fused isoindolones |
US6232299B1 (en) | 1996-05-01 | 2001-05-15 | Eli Lilly And Company | Use of protein kinase C inhibitors to enhance the clinical efficacy of oncolytic agents and radiation therapy |
AU2819397A (en) * | 1996-05-07 | 1997-11-26 | Presidents And Fellows Of Harvard College | Inhibitors of glycogen synthase kinase-3 and methods for identifying and using the same |
UA67725C2 (en) | 1996-06-03 | 2004-07-15 | Cephalon Inc | K-252a derivatives and a method for improvement of functioning and cell survival enhancement |
US6875865B1 (en) * | 1996-06-03 | 2005-04-05 | Cephalon, Inc. | Selected derivatives of K-252a |
ES2184106T3 (es) | 1996-06-25 | 2003-04-01 | Cephalon Inc | Utilizacion del derivado de k-252a en el tratamiento de trastornos del sistema nervioso periferico o central, y de la hiperproduccion de citoquinas. |
US7144997B2 (en) | 1997-07-24 | 2006-12-05 | Curis, Inc. | Vertebrate embryonic patterning-inducing proteins, compositions and uses related therto |
EP1011648B2 (en) * | 1997-08-15 | 2005-07-20 | Cephalon, Inc. | Combination of tyrosine kinase inhibitor and chemical castration to treat prostate cancer |
ES2194385T3 (es) | 1997-12-31 | 2003-11-16 | Cephalon Inc | Derivados del k-252a 3'-epimeros. |
US6811992B1 (en) | 1998-05-14 | 2004-11-02 | Ya Fang Liu | Method for identifying MLK inhibitors for the treatment of neurological conditions |
US6127401A (en) | 1998-06-05 | 2000-10-03 | Cephalon, Inc. | Bridged indenopyrrolocarbazoles |
US6013646A (en) * | 1998-07-02 | 2000-01-11 | Bayer Corporation | Indolocarbazole derivatives useful for the treatment of neurodegenerative diseases and cancer |
US7795246B2 (en) * | 1998-08-06 | 2010-09-14 | Cephalon, Inc. | Particle-forming compositions containing fused pyrrolocarbazoles |
US6200968B1 (en) | 1998-08-06 | 2001-03-13 | Cephalon, Inc. | Particle-forming compositions containing fused pyrrolocarbazoles |
US6242473B1 (en) * | 1999-01-08 | 2001-06-05 | Maxim Pharmaceuticals, Inc. | Treatment and prevention of reactive oxygen metabolite-mediated cellular damage |
US6841567B1 (en) * | 1999-02-12 | 2005-01-11 | Cephalon, Inc. | Cyclic substituted fused pyrrolocarbazoles and isoindolones |
US6323215B1 (en) | 1999-07-09 | 2001-11-27 | Ortho-Mcneil Pharmaceutical, Inc. | Neurotrophic tetrahydroisoquinolines and tetrahydrothienopyridines, and related compositions and methods |
BR0012327A (pt) | 1999-07-09 | 2002-07-02 | Ortho Mcneil Pharm Inc | Pirrolidinas e piperidinas neurotróficas, e composições e métodos relacionados |
AU2576501A (en) * | 1999-12-08 | 2001-06-18 | Advanced Medicine, Inc. | Protein kinase inhibitors |
US20020002169A1 (en) | 1999-12-08 | 2002-01-03 | Griffin John H. | Protein kinase inhibitors |
US7129250B2 (en) | 2000-05-19 | 2006-10-31 | Aegera Therapeutics Inc. | Neuroprotective and anti-proliferative compounds |
AU2001278084A1 (en) * | 2000-07-31 | 2002-02-13 | The Regents Of The University Of California | Model for alzheimer's disease and other neurodegenerative diseases |
DE10113513A1 (de) * | 2001-03-20 | 2002-10-02 | Medinnova Ges Med Innovationen | Kombinationspräparat zur Prophylaxe und/oder Therapie von Nervenzell- und/oder Gliazellschäden durch ein neues Behandlungsverfahren |
GB0117645D0 (en) * | 2001-07-19 | 2001-09-12 | Isis Innovation | Therapeutic stratergies for prevention and treatment of alzheimers disease |
WO2003037347A1 (en) | 2001-10-30 | 2003-05-08 | Novartis Ag | Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity |
US6664266B2 (en) | 2002-03-14 | 2003-12-16 | Children's Medical Center Corporation | Axon regeneration with PKC inhibitiors |
US20050130877A1 (en) * | 2003-03-14 | 2005-06-16 | Children's Medical Center Corporation | Axon regeneration with PKC inhibitors |
CA2393720C (en) | 2002-07-12 | 2010-09-14 | Eli Lilly And Company | Crystalline 2,5-dione-3-(1-methyl-1h-indol-3-yl)-4-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1h-indol-3-yl]-1h-pyrrole mono-hydrochloride |
DE10255343B4 (de) * | 2002-11-27 | 2006-09-07 | Nad Ag | N,N-Verbrückte, Stickstoff-Substituierte Carbacyclische Indolocarbazole als Proteinkinase-Inhibitoren |
US20040175384A1 (en) * | 2003-12-12 | 2004-09-09 | Mohapatra Shyam S. | Protein kinase C as a target for the treatment of respiratory syncytial virus |
EP2305265A1 (en) | 2003-08-08 | 2011-04-06 | Novartis AG | Combinations comprising staurosporines |
US8592368B2 (en) | 2003-12-19 | 2013-11-26 | University Of South Florida | JAK/STAT inhibitors and MAPK/ERK inhibitors for RSV infection |
JP5442198B2 (ja) * | 2004-02-27 | 2014-03-12 | セファロン インコーポレイテッド | 医薬化合物の結晶形 |
CN103251953A (zh) * | 2004-07-19 | 2013-08-21 | 约翰·霍普金斯大学 | 供免疫抑制的flt3抑制剂 |
CN100513850C (zh) * | 2005-08-23 | 2009-07-15 | 浙江华夏阀门有限公司 | 三角截面密封套 |
DK1919979T4 (en) * | 2005-08-25 | 2017-07-17 | Creabilis Therapeutics Spa | Polymer conjugates of K-252A and derivatives thereof |
JP2009508868A (ja) | 2005-09-16 | 2009-03-05 | シェーリング コーポレイション | テモゾロミドおよびプロテインキナーゼインヒビターを用いる薬学的組成物および方法 |
WO2007042286A1 (en) | 2005-10-11 | 2007-04-19 | Merck Patent Gmbh | Egfr dependent modulation of chemokine expression and influence on therapy and diagnosis of tumors and side effects thereof |
WO2008130921A1 (en) * | 2007-04-16 | 2008-10-30 | Modgene, Llc | Methods and compositions for diagnosis and treatment of depression and anxiety |
US20090155352A1 (en) * | 2007-11-20 | 2009-06-18 | Cephalon, Inc. | Microemulsion containing indolocarbazole compound and dosage forms containing the same |
CA2891855A1 (en) | 2012-12-21 | 2014-06-26 | Sykehuset Sorlandet Hf | Egfr targeted therapy of neurological disorders and pain |
EP3706735A1 (en) * | 2017-11-06 | 2020-09-16 | Snap Bio, Inc. | Pim kinase inhibitor compositions, methods, and uses thereof |
WO2024018245A1 (en) | 2022-07-22 | 2024-01-25 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of calpain inhibitors for the treatment of the diabetic kidney disease |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4554402A (en) * | 1983-12-23 | 1985-11-19 | Aluminum Company Of America | Vibration damper for overhead conductor |
JPS62102388A (ja) * | 1985-10-29 | 1987-05-12 | Toppan Printing Co Ltd | Icカ−ド |
JPS62155284A (ja) * | 1985-12-27 | 1987-07-10 | Kyowa Hakko Kogyo Co Ltd | 生理活性物質k−252の誘導体 |
JPS62155285A (ja) * | 1985-12-27 | 1987-07-10 | Kyowa Hakko Kogyo Co Ltd | 生理活性物質k−252の誘導体 |
JPS62220196A (ja) * | 1986-03-20 | 1987-09-28 | Kyowa Hakko Kogyo Co Ltd | 新規物質ucn―01 |
US4816450A (en) * | 1986-09-15 | 1989-03-28 | Duke University | Inhibition of protein kinase C by long-chain bases |
JPH0826037B2 (ja) * | 1987-01-22 | 1996-03-13 | 協和醗酵工業株式会社 | 生理活性物質k−252の誘導体 |
JPH0826036B2 (ja) * | 1987-01-22 | 1996-03-13 | 協和醗酵工業株式会社 | 生理活性物質k−252の誘導体 |
US4735939A (en) * | 1987-02-27 | 1988-04-05 | The Dow Chemical Company | Insecticidal activity of staurosporine |
EP0303697B1 (en) * | 1987-03-09 | 1997-10-01 | Kyowa Hakko Kogyo Co., Ltd. | Derivatives of physiologically active substance k-252 |
IL86632A0 (en) * | 1987-06-15 | 1988-11-30 | Ciba Geigy Ag | Derivatives substituted at methyl-amino nitrogen |
US5093330A (en) * | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
JPH07113027B2 (ja) * | 1987-12-24 | 1995-12-06 | 協和醗酵工業株式会社 | K−252誘導体 |
JPH0725786A (ja) * | 1990-05-16 | 1995-01-27 | Univ Rockefeller | アルツハイマー病を伴うアミロイドーシスの治療 |
IE921315A1 (en) * | 1991-07-03 | 1993-01-13 | Regeneron Pharma | Method and assay system for neurothrophin activity |
DE4133605C2 (de) * | 1991-10-10 | 1994-05-11 | Siemens Ag | Flexibler Roboterarm |
AU3064992A (en) * | 1991-11-08 | 1993-06-07 | University Of Southern California | Compositions containing k-252 compounds for potentiation of neurotrophin activity |
DE4217964A1 (de) * | 1992-05-30 | 1993-12-02 | Goedecke Ag | Indolocarbazol-Imide und deren Verwendung |
-
1993
- 1993-07-22 US US08/096,561 patent/US5461146A/en not_active Expired - Lifetime
- 1993-07-26 ES ES96116661T patent/ES2151629T3/es not_active Expired - Lifetime
- 1993-07-26 DE DE69329397T patent/DE69329397T2/de not_active Expired - Lifetime
- 1993-07-26 EP EP96116661A patent/EP0768312B1/en not_active Expired - Lifetime
- 1993-07-26 KR KR1019950700251A patent/KR100276008B1/ko not_active IP Right Cessation
- 1993-07-26 CA CA002140924A patent/CA2140924A1/en not_active Abandoned
- 1993-07-26 HU HU0301601A patent/HU225341B1/hu unknown
- 1993-07-26 AT AT93917337T patent/ATE152111T1/de not_active IP Right Cessation
- 1993-07-26 DE DE69310178T patent/DE69310178T2/de not_active Expired - Lifetime
- 1993-07-26 NZ NZ254662A patent/NZ254662A/en not_active IP Right Cessation
- 1993-07-26 HU HU0301601A patent/HU0301601D0/hu unknown
- 1993-07-26 EP EP99120008A patent/EP1002534B1/en not_active Expired - Lifetime
- 1993-07-26 HU HU9500192A patent/HU225297B1/hu unknown
- 1993-07-26 PT PT96116661T patent/PT768312E/pt unknown
- 1993-07-26 HU HU0301425A patent/HU0301425D0/hu unknown
- 1993-07-26 EP EP04025114A patent/EP1512688A1/en not_active Withdrawn
- 1993-07-26 DE DE69333874T patent/DE69333874T2/de not_active Expired - Lifetime
- 1993-07-26 DK DK93917337.3T patent/DK0651754T3/da active
- 1993-07-26 ES ES99120008T patent/ES2248950T3/es not_active Expired - Lifetime
- 1993-07-26 DK DK99120008T patent/DK1002534T3/da active
- 1993-07-26 AT AT96116661T patent/ATE196142T1/de not_active IP Right Cessation
- 1993-07-26 JP JP50473194A patent/JP3762427B2/ja not_active Expired - Lifetime
- 1993-07-26 HU HU0301425A patent/HU225342B1/hu unknown
- 1993-07-26 ES ES93917337T patent/ES2101331T3/es not_active Expired - Lifetime
- 1993-07-26 NZ NZ286198A patent/NZ286198A/en not_active IP Right Cessation
- 1993-07-26 AU AU46881/93A patent/AU675236B2/en not_active Expired
- 1993-07-26 AT AT99120008T patent/ATE304848T1/de not_active IP Right Cessation
- 1993-07-26 DK DK96116661T patent/DK0768312T3/da active
- 1993-07-26 BR BR9306789A patent/BR9306789A/pt not_active Application Discontinuation
- 1993-07-26 WO PCT/US1993/006974 patent/WO1994002488A1/en active IP Right Grant
- 1993-07-26 EP EP93917337A patent/EP0651754B1/en not_active Expired - Lifetime
-
1995
- 1995-01-23 NO NO950242A patent/NO305481B1/no not_active IP Right Cessation
-
1997
- 1997-06-19 GR GR970401455T patent/GR3023817T3/el unknown
-
1999
- 1999-02-05 NO NO990542A patent/NO307446B1/no not_active IP Right Cessation
-
2000
- 2000-11-21 HK HK00107421A patent/HK1028206A1/xx not_active IP Right Cessation
- 2000-11-28 GR GR20000402623T patent/GR3034917T3/el not_active IP Right Cessation
-
2002
- 2002-08-23 JP JP2002244111A patent/JP3723533B2/ja not_active Expired - Fee Related
-
2005
- 2005-01-27 JP JP2005019891A patent/JP2005170955A/ja active Pending
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2011126893A (ja) * | 1998-09-25 | 2011-06-30 | Cephalon Inc | 感覚毛細胞及び蝸牛ニューロンへの損傷を予防する/処置するための方法 |
WO2000021531A1 (fr) * | 1998-10-13 | 2000-04-20 | Kyowa Hakko Kogyo Co., Ltd. | Medicaments pour maladies oculaires |
US6451787B1 (en) * | 1998-10-13 | 2002-09-17 | Cephalon, Inc. | Remedies for ocular diseases |
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP3762427B2 (ja) | ビス‐スタウロスポリンおよびK‐252a誘導体 | |
US5621100A (en) | K-252a derivatives for treatment of neurological disorders | |
AU704314B2 (en) | Protein kinase inhibitors for treatment of neurological disorders | |
FI113537B (fi) | Menetelmä terapeuttisesti käyttökelpoisten indolokarbatsolijohdannaisten valmistamiseksi | |
US5621101A (en) | Protein kinase inhibitors for treatment of neurological disorders | |
CN102548986A (zh) | 氨基吡咯烷酮衍生物及其用途 | |
US6451761B1 (en) | N′N′-dichlorinated omega-amino acids and uses thereof | |
KR100809410B1 (ko) | 줄기세포 분화 유도용 조성물 및 그의 용도 | |
KR100464907B1 (ko) | 신경계질환치료용단백질키나아제억제제 | |
MXPA97003039A (en) | Protein kinase inhibitors for the treatment of neurologi disorders | |
JP2000136137A (ja) | 虚血再潅流性脳障害軽減剤 | |
ZA200301439B (en) | Fused pyrrolocarbazoles against inflammation. | |
HU209306B (en) | Process for producing acetic acid derivatives |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20040727 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20041124 |
|
A911 | Transfer to examiner for re-examination before appeal (zenchi) |
Free format text: JAPANESE INTERMEDIATE CODE: A911 Effective date: 20050127 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20050823 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20051124 |
|
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: 20051220 |
|
A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20060113 |
|
R150 | Certificate of patent or registration of utility model |
Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20090120 Year of fee payment: 3 |
|
S533 | Written request for registration of change of name |
Free format text: JAPANESE INTERMEDIATE CODE: R313533 |
|
FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20090120 Year of fee payment: 3 |
|
R350 | Written notification of registration of transfer |
Free format text: JAPANESE INTERMEDIATE CODE: R350 |
|
FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20100120 Year of fee payment: 4 |
|
FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20100120 Year of fee payment: 4 |
|
FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20110120 Year of fee payment: 5 |
|
FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20120120 Year of fee payment: 6 |
|
FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20130120 Year of fee payment: 7 |
|
EXPY | Cancellation because of completion of term |