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1.发明公开NOVEL LACTAM INHIBITORS OF MATRIX METALLOPROTEINASES, TNF-ALPHA, AND AGGRECANASE 审中-公开内酰胺ALS金属蛋白酶TNF-α，聚集蛋白聚糖酶抑制剂
公开(公告)号：EP1165546A2
公开(公告)日：2002-01-02
申请号：EP00921501.3
申请日：2000-03-30
发明人： DUAN, Jingwu
IPC分类号： C07D401/12 , A61K31/47 , A61P29/00
CPC分类号： C07D207/26 , C07D401/12
摘要： The present application describes novel lactams and derivatives thereof of formula (I) or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered lactam containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as inhibitors of matrix metalloproteinases, TNF-α, and aggrecanase.
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2.发明公开
公开(公告)号：EP1158980A1
公开(公告)日：2001-12-05
申请号：EP99965321.5
申请日：1999-12-17
发明人： KO, Soo , CLARK, Cheryl, McArdle , DELUCCA, George, V. , DUNCIA, John, V. , SANTELLA, Joseph, B., III , WACKER, Dean, A.
IPC分类号： A61K31/445 , C07D211/32 , C07D211/52 , C07D211/58 , C07D211/62 , C07D211/66 , C07D211/76 , C07D221/20 , C07D401/04
CPC分类号： C07D207/08 , C07D207/06 , C07D211/14 , C07D211/18 , C07D401/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/10
摘要： The present application describes modulators of CCR3 of formula (I) or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
摘要翻译： 本申请描述了用于预防哮喘和其他过敏性疾病的式（I）的CCR3或其药学上可接受的盐形式的调节剂。
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3.发明公开1H-IMIDAZO 4,5-D]PYRIDAZIN-7-ONES, 3H-IMIDAZO 4,5-C]PYRIDIN-4-ONES AND CORRESPONDING THIONES AS CORTICOTROPIN RELEASING FACTOR (CRF) RECEPTOR LIGANDS 有权-1H-咪唑并[4,5-d]哒嗪-7-酮，3H-咪唑并[4,5-c]吡啶-4-酮和硫酮对应ALS肾上腺皮质激素释放END因子（CRF）-RECEPTORLIGANDEN
公开(公告)号：EP1140929A1
公开(公告)日：2001-10-10
申请号：EP99966736.3
申请日：1999-12-30
IPC分类号： C07D471/02 , C07D487/02 , A61K31/4188 , A61P25/00
CPC分类号： C07D471/04
摘要： Corticotropin releasing factor (CRF) antagonists of formula (I), and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
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公开(公告)号：EP1140203A2
公开(公告)日：2001-10-10
申请号：EP99967442.7
申请日：1999-12-17
CPC分类号： C07D401/14 , A61K49/0002 , B01J2219/00317 , B01J2219/00495 , B01J2219/00659 , B01J2219/00707 , C07D401/12 , C07K5/0205 , C07K5/0215 , C07K5/06139 , C07K5/06191 , C40B60/14 , G01N25/482 , G01N25/4866
摘要： The present invention describes novel compounds of the formula (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
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公开(公告)号：EP1131320A1
公开(公告)日：2001-09-12
申请号：EP99960471.3
申请日：1999-11-18
IPC分类号： C07D413/06 , A61K31/42 , A61P7/02
CPC分类号： C07D413/06
摘要： This invention relates to novel isoxazolines of formula (I) or a pharmaceutically acceptable salt form thereof. This invention also relates to novel isoxazolines of formula (I) which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, 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 platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
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6.发明公开IMIDAZO-PYRIDINES, -PYRIDAZINES, AND -TRIAZINES AS CORTICOTROPIN RELEASING FACTOR ANTAGONISTS 审中-公开咪唑，哒嗪和三嗪AS CRF拮抗剂
公开(公告)号：EP1091961A1
公开(公告)日：2001-04-18
申请号：EP99930849.7
申请日：1999-07-01
IPC分类号： C07D487/04 , A61K31/5025 , C07D471/04 , A61K31/5365 , A61K31/437
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention describes novel imidazo-pyridines, -pyridazines, and -triazines of formula (I) wherein A and B can be C or N and D is aryl or heteroaryl or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
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7.发明公开1,3-BENZODIAZEPIN-2-ONES AND 1,3-BENZOXAZEPIN-2-ONES USEFUL AS HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开1,3-苯并二氮杂-2-酮，1,3-苯并氧氮杂-2-酮ALS逆转录酶抑制剂
公开(公告)号：EP1091944A1
公开(公告)日：2001-04-18
申请号：EP99930440.5
申请日：1999-06-18
IPC分类号： C07D243/04 , A61K31/55 , C07D401/12 , C07D471/04 , C07D487/04 , C07D267/06 , C07D281/02 , C07D405/06 , C07D409/06 , C07D401/06
CPC分类号： C07D401/12 , C07D243/04
摘要： The present invention relates to 1,3-benzodiazepin-2-ones and 1,3-benzoxazepin-2-ones of formula (I) or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
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8.发明公开THIAZOLO 4,5-d]PYRIMIDINES AND PYRIDINES AS CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONISTS 审中-公开THIAZOLO¬4,5-D嘧啶和吡啶因子促肾上腺皮质激素释放因子（CRF）拮抗剂
公开(公告)号：EP1068212A1
公开(公告)日：2001-01-17
申请号：EP99914247.4
申请日：1999-03-29
发明人： BECK, James, Peter
IPC分类号： C07D513/04 , A61K31/505 , A61K31/44 , A61K31/425
CPC分类号： C07D513/04
摘要： The present invention describes novel thiazolo[4,5-d]pyrimidines of formula (I), or a pharmaceutically acceptable salt thereof, wherein X is CR4 or N; Y is selected from the group: S, O and NR5; R1 is selected from the group: H, C¿1-4? alkyl, C2-4 alkenyl, C2-4 alkynyl, Cl, F, Br, I, -CN, C1-5 haloalkyl, -NR?6R7, -NR6COR7, -OR8¿, -SH, and -S(O)¿nR?9; R2 is selected from the group: -CR?10R11R12, -NR10aR11a, -NHCR10R11R12, -OCR10R11R12¿, and phenyl, wherein the phenyl is substituted with 0-4 Ra; R3 is selected from the group: phenyl, pyridyl, pyrimidyl, napthyl, triazinyl, furanyl, quinolinyl, isoquinolinyl, thienyl, thiazolyl, pyrrolyl, oxazolyl, benzofuranyl, benzothienyl, benzothiazolyl, isoxazolyl, and pyrazolyl, and is substituted with 1 to 4 Rb groups; R4 is selected from the group: H, C¿1-4? alkyl, and C1-4 haloalkyl, halogen, NH2, NH(C1-4 alkyl), NH(C1-4 alkyl)2, CN, OR?8; and R5¿ is -CO(C¿1-4? alkyl) or -CO2(C1-4 alkyl), which are useful as CRF antagonists.
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公开(公告)号：EP1067971A1
公开(公告)日：2001-01-17
申请号：EP99924099.7
申请日：1999-03-29
CPC分类号： A61K51/1241 , A61K51/1251
摘要： Radiotherapy agents which are solid or porous particles are described. The particles are of an inorganic material containing a suitable radionuclide and having an average particle diameter of about 0.05 to 5000 microns.
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10.发明公开5,5-DISUBSTITUTED-1,5-DIHYDRO-4,1-BENZOXAZEPIN-2(3H)-ONES USEFUL AS HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开5,5-二取代1,5-二氢-4,1- BENZOXAZEPI N-2（3H） - 酮和它们作为HIV逆转录酶INHIBITORS-
公开(公告)号：EP1009742A1
公开(公告)日：2000-06-21
申请号：EP98942117.7
申请日：1998-08-19
IPC分类号： C07D267/14 , C07D413/06 , C07D498/04 , A61K31/55
CPC分类号： C07D413/06 , C07D267/14
摘要： The present invention relates to benzoxazepinones of formula (I), or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same and methods of using the same for treating viral infection or as an assay standard or reagent.
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