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公开(公告)号：EP1105394A1
公开(公告)日：2001-06-13
申请号：EP99945079.4
申请日：1999-08-18
IPC分类号： C07D498/04 , A61K31/505
CPC分类号： C07D498/04
摘要： The present invention describes novel isoxazolo[1,5-a]pyrimidines of formula (I), wherein R is an aromatic or heteroaromatic ring, or pharmaceutically acceptable salt form thereof, which are useful as CRF antagonists.
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22.发明公开SUCCINOYLAMINO LACTAMS AS INHIBITORS OF A BETA PROTEIN PRODUCTION 有权一个beta蛋白生产SUCCINOYLAMINOLACTAMDERIVATE作为抑制剂
公开(公告)号：EP1102752A1
公开(公告)日：2001-05-30
申请号：EP99939010.7
申请日：1999-08-07
IPC分类号： C07D223/12 , A61K31/55 , C07D401/06 , C07D405/12 , C07D401/10 , C07D243/24
CPC分类号： C07D223/12 , C07D243/24 , C07D401/06 , C07D401/10 , C07D405/12
摘要： This invention relates to novel lactams of Formula (I) or a pharmaceutically acceptable salts or prodrug thereof, having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
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公开(公告)号：EP1091941A1
公开(公告)日：2001-04-18
申请号：EP99932151.6
申请日：1999-07-01
IPC分类号： C07D235/08 , C07D235/26 , C07D401/04 , A61K31/415
CPC分类号： C07D401/04 , C07D235/08 , C07D235/26 , C07D403/04 , C07D405/04 , C07D409/04
摘要： The present invention describes novel benzimidazoles of formula (I) wherein D is an aryl or heteroaryl group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
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公开(公告)号：EP1090005A1
公开(公告)日：2001-04-11
申请号：EP99930438.9
申请日：1999-06-18
IPC分类号： C07D487/04 , A61K31/53
CPC分类号： C07D487/04
摘要： The present invention describes novel pyrazolo[1,5-a]triazines of formula (I), wherein R3 is an alkyl, alkenyl, alkynyl, or cycloalkyl group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
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25.发明公开5-AMINOINDENO(1,2-C)PYRAZOL-4-ONES AS ANTI-CANCER AND ANTI-PROLIFERATIVE AGENTS 有权5- AMINOINDENO [1,2-c]吡唑-4-酮作为抗肿瘤和生长抑制剂
公开(公告)号：EP1071668A1
公开(公告)日：2001-01-31
申请号：EP99918695.0
申请日：1999-04-20
IPC分类号： C07D231/54 , A61K31/41 , C07D409/12 , C07D403/12 , C07D401/12 , C07D417/12 , C07D413/12 , C07D413/14
CPC分类号： C07D405/12 , C07D231/54 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/14 , C07D405/04 , C07D409/04 , C07D409/12 , C07D409/14
摘要： The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I), that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits known as cyclines A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
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公开(公告)号：EP1066250A2
公开(公告)日：2001-01-10
申请号：EP99914246.6
申请日：1999-03-29
发明人： ZHOU, Jicheng , OH, Lynette, May , MA, Philip
IPC分类号： C07C253/00
CPC分类号： C07C253/00 , C07D201/08 , C07C255/17 , C07C255/40
摘要： The present invention relates to processes for the production of α-aryl-β-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
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公开(公告)号：EP1054871A2
公开(公告)日：2000-11-29
申请号：EP99914248.2
申请日：1999-03-29
IPC分类号： C07D239/48 , C07D239/42 , A61K31/505
CPC分类号： C07D239/47 , C07D239/49 , C07D239/95 , C07D251/18 , C07D403/06 , C07D487/04
摘要： This invention relates to novel heterocycles which are useful as antagonists of the αvβ3 integrin, the α2bβ3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
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28.发明公开1,3,4-THIADIAZOLES AND 1,3,4-OXADIAZOLES AS $g(a) v?$g(b) 3? ANTAGONISTS 审中-公开-1,3,4-噻二唑和1,3,4-恶二唑ALS抑制剂avß3
公开(公告)号：EP1049693A1
公开(公告)日：2000-11-08
申请号：EP98959432.0
申请日：1998-11-12
IPC分类号： C07D417/12 , A61K31/41 , A61K31/44
CPC分类号： C07D417/12
摘要： This invention relates to 1,3,4-thiadiazoles and 1,3,4-Oxadiazoles of formula (I), which are useful as antagonists of αvβ3 and related integrin receptors, to pharmaceutical compositions containing such compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion and the treatment of angioginic disorders, inflammation, bone degradation, tumors, metastases, thrombosis, and other cell aggregation-related conditions, including their enantiomeric, diastereomeric, pharmaceutically acceptable salt or prodrug forms thereof wherein R1 is selected from formulas (a), (b), (c), (d), (e), (f) or (g); U, V, G, W, X, R20 are as defined in the application.
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公开(公告)号：EP0998572A2
公开(公告)日：2000-05-10
申请号：EP98936003.7
申请日：1998-07-24
发明人： ARNER, Elizabeth, C. , BURN, Timothy, C. , COPELAND, Robert, A. , DECICCO, Carl, P. , LIU, Ruiqin , MAGOLDA, Ronald , PRATTA, Michael , SOLOMON, Kimberly, A. , TORTORELLA, Micky, D. , TRZASKOS, James, M. , YANG, Fude
IPC分类号： C12N15/57 , C12N9/64 , C07K16/40 , C12N1/19 , C12N5/10 , C12Q1/68 , C12Q1/37 , A61K38/55 , A61K39/395 , G01N33/573 , G01N33/68
CPC分类号： C12N9/6489 , A61K38/00 , C07K16/40 , C12Q1/37 , G01N33/6887 , G01N2333/96486 , G01N2500/00 , G01N2800/102
摘要： The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu?373-Ala374¿. The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.
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30.发明公开ASYMMETRIC SYNTHESIS OF BENZOXAZINONES VIA NEW INTERMEDIATES 失效不对称合成VEN BENZOXAZINOENÜBERNEUE ZWISCHENPRODUKTE
公开(公告)号：EP0973755A1
公开(公告)日：2000-01-26
申请号：EP98914408.4
申请日：1998-04-02
发明人： PIERCE, Michael, E. , CHEN, Cheng, Y. , CHOUDHURY, Anusuya , RADESCA, Lilian, A. , TAN, Lushi , ZHAO, Dalian
IPC分类号： C07D265/18 , C07C215/68 , C07C211/52
CPC分类号： C07D265/18 , C07C213/00 , C07C213/02 , C07C221/00 , C07C2601/02 , C07C215/68 , C07C217/58 , C07C225/22
摘要： The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In an embodiment, the present invention provides a process for the preparation of an amino alcohol compound of formula (V-i) comprising adding a toluene solution of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone to a toluene solution of a compound of formula (III-i), via a compound of formula (IV-i).
摘要翻译： 本发明提供了用于不对称合成式（Ⅵ-ⅰ）的（S）-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的新方法 ），其可用作人类免疫缺陷病毒（HIV）逆转录酶抑制剂。
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