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公开(公告)号：US5900414A
公开(公告)日：1999-05-04
申请号：US922836
申请日：1997-08-26
IPC分类号： A61K31/551 , A61K31/495 , A61K31/50
CPC分类号： A61K31/551
摘要： The compositions and methods of the invention provide a convenient means for systemically administering an integrin receptor antagonist or a pharmaceutically effective amount thereof to a patient by introducing the antagonist, in an ophthalmic formulation, to the patient's eye.
摘要翻译： 本发明的组合物和方法提供了一种方便的方法，通过将眼药物中的拮抗剂引入患者的眼睛，将整联蛋白受体拮抗剂或其药学有效量全身给予患者。
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2.发明授权Method of inhibiting osteoclast-mediated bone resorption by administration of N-heterocyclicalkyl-substituted phenyl derivatives 失效通过管理N-取代的羟基取代的苯基衍生物抑制骨质疏松的骨质还原的方法
公开(公告)号：US5204350A
公开(公告)日：1993-04-20
申请号：US742970
申请日：1991-08-09
IPC分类号： A61K31/27 , A61K31/215 , A61K31/395 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/495 , A61P3/02 , A61P19/10 , A61P43/00 , C07C271/22 , C07C317/50 , C07D211/22
CPC分类号： A61K31/215 , A61K31/40 , A61K31/445 , A61K31/495 , Y10S514/835
摘要： Compounds of the general formula ##STR1## Y is an integer of from 0 to 6 is chosen from: O,SO.sub.2,--CONH--,--NHCO--,--CH2-- or ##STR2## R.sup.1 is substituted or unsubstituted mono- or polycyclic saturated hetero-cyclic ring system having 1, 2 or 3 heteroatoms where said heteroatoms are independently chosen from N, O and S and said substituents are chosen from the group comprising R.sup.2 ;R.sup.2 isC.sub.1-6 alkyl,aryl C.sub.0-6 alkyl,hydroxy C.sub.0-6 alkyl,C.sub.1-6 alkoxy C.sub.0-6 alkyl,carboxy C.sub.0-6 alkyloxo,halogen,CF.sub.3,C.sub.0-4 alkylamino-C.sub.0-6 alkyl orC.sub.0-4 dialkylamino-C.sub.0-6 alkyl;R.sup.3 isC.sub.1-8 alkyl or cycloalkyl,aryl C.sub.0-4 alkyl,hydroxy C.sub.0-4 alkylC.sub.1-4 alkyloxy C.sub.0-4 alkyl,carboxy C.sub.0-4 alkyl,halogen,CF.sub.3 orhydrogen;R.sup.4 ishydrogen,C.sub.1-6 alkyl,aryl C.sub.0-4 alkyl orC.sub.1-6 alkylcarbonyloxymethyl; andR.sup.5 isC.sub.1-6 alkyl,aryl C.sub.0-4 alkyl orheterocycly C.sub.0-4 alkyland the pharmaceutically acceptable salts thereof; are used in a method of treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.
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公开(公告)号：US5646000A
公开(公告)日：1997-07-08
申请号：US315034
申请日：1994-09-29
IPC分类号： C07D401/06 , C07D405/14 , C07D491/22 , C07D495/04 , G01N33/569 , G01N33/80 , G01N33/86 , G01N33/567 , C07D401/14
CPC分类号： C07D401/06 , C07D405/14 , C07D495/04 , G01N33/56966 , G01N33/80 , G01N33/86 , G01N2500/00 , Y10S436/80 , Y10S436/811
摘要： The invention is directed to a series of novel compounds, and their pharmaceutically acceptable salts, of the formula ##STR1## wherein R is C.sub.0-6 alkyl substituted with R.sup.5 or a mono or polycyclic aromatic or heteroaromatic system comprised of 5 or 6-membered aromatic or heteroaromatic rings that are either unsubstituted or substituted with one or more of R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently C.sub.1-6 alkyl, carboxyl, hydroxyl, azido, nitro, amino, C.sub.1-6 alkylamino, C.sub.1-6 dialkylamino, arylamino, aryl C.sub.1-6 alkylamino, hydroxysulfonyl or arylazo; aryl is a phenyl or naphthyl ring which is unsubstituted or substituted with one or more of R.sup.3 and R.sup.4 ; R.sup.3 and R.sup.4 are independently C.sub.1-6 alkyl, azido, nitro, amino, C.sub.1-6 dialkylamino or hydroxysulfonyl; R.sup.5 is ##STR2## provided that when R is an unsubstituted monocyclic ring, the monocyclic ring is not phenyl or pyridyl. Such compounds are useful as fluorescent probes for identifying antiplatelet agents which selectively bind to activated platelets.
摘要翻译： 本发明涉及一系列新颖的化合物及其药学上可接受的盐，其中R是被R 5取代的C 1-6烷基或由5或6元芳族的单或多环芳族或杂芳族体系 或未被取代或被一个或多个R 1和R 2取代的杂芳环; R 1和R 2独立地是C 1-6烷基，羧基，羟基，叠氮基，硝基，氨基，C 1-6烷基氨基，C 1-6二烷基氨基，芳基氨基，芳基C 1-6烷基氨基，羟基磺酰基或芳基偶氮; 芳基是未被取代或被一个或多个R 3和R 4取代的苯基或萘基环; R 3和R 4独立地为C 1-6烷基，叠氮基，硝基，氨基，C 1-6二烷基氨基或羟基磺酰基; R5是
或 ，条件是当R是未取代的单环时，单环不是苯基或吡啶基。 这样的化合物可用作识别选择性结合活化血小板的抗血小板剂的荧光探针。 -
4.发明授权Method of inhibiting osteoclast-mediated bone resorption by administration of aminoalkyl-substituted phenyl derivatives 失效通过管理氨基取代的苯衍生物抑制骨质疏松骨介导的骨质疏松的方法
公开(公告)号：US5217994A
公开(公告)日：1993-06-08
申请号：US743475
申请日：1991-08-09
IPC分类号： A61K31/27 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/495 , A61P3/02 , A61P19/10 , A61P43/00 , C07C271/22 , C07C317/50 , C07D211/22
CPC分类号： A61K31/445 , A61K31/27 , A61K31/40 , A61K31/495 , Y10S514/899
摘要： Compounds of the general formula ##STR1## and the pharmaceutically acceptable salts thereof whereinn is an integer of from 0 to 6;Y is CH.sub.2, O, SO.sub.2, --CONH--, --NHCO--, or ##STR2## R.sup.1 and R.sup.2 are independently hydrogen,C.sub.1-8 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,amino C.sub.1-4 alkyl,C.sub.1-4 alkylamino C.sub.1-4 alkyl, orC.sub.3-8 cycloalkylwherein R.sup.1 and R.sup.2 may be unsubstituted or substituted with one or more groups chosen from R.sup.3, whereR.sup.3 ishydrogen,C.sub.1-6 alkyl,hydroxy C.sub.0-4 alkyl,carboxy C.sub.0-4 alkyl,C.sub.1-4 alkyloxy C.sub.0-4 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,halogen, orCF.sub.3 ;R.sup.4 isC.sub.1-6 alkyl,heterocyclyl C.sub.0-4 alkyl, oraryl C.sub.0-4 alkyl;R.sup.5 ishydrogen,C.sub.1-6 alkyl,aryl C.sub.0-3 alkyl, orC.sub.1-6 alkylcarbonyloxymethylare used in a method of treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.
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公开(公告)号：US08629274B2
公开(公告)日：2014-01-14
申请号：US13723869
申请日：2012-12-21
IPC分类号： C07D213/00 , A01N43/00 , A61K31/445 , A01N41/06 , A61K31/18 , A01N37/18 , A61K31/165
CPC分类号： C07D401/06 , A61K31/167 , A61K31/18 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/407 , A61K31/445 , A61K31/4453 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/536 , A61K31/5375 , A61K31/551 , A61K31/675 , A61K31/7072 , A61K38/21 , A61K45/06 , C07C311/46 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/48 , C07D211/22 , C07D211/32 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/50 , C07D211/52 , C07D211/58 , C07D211/62 , C07D211/96 , C07D213/74 , C07D213/82 , C07D265/30 , C07D265/32 , C07D295/195 , C07D295/26 , C07D401/12 , A61K2300/00
摘要： The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
摘要翻译： 本发明包括在有需要的个体中抑制，抑制或预防HBV感染的方法，包括向个体施用治疗有效量的至少一种本发明的化合物。
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公开(公告)号：US07625912B2
公开(公告)日：2009-12-01
申请号：US10582826
申请日：2004-12-15
IPC分类号： C07D239/36 , A61K31/513
CPC分类号： C07D239/36
摘要： The present invention relates to 2-phenylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的2-苯基嘧啶酮化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US20090124641A1
公开(公告)日：2009-05-14
申请号：US11795448
申请日：2006-01-13
申请人： Paul J. Coleman , George D. Hartman
发明人： Paul J. Coleman , George D. Hartman
IPC分类号： A61K31/517 , C07D239/88 , C07D403/02
CPC分类号： C07D239/91
摘要： The present invention relates to fluorinated 2-aminomethylquinazolinone derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的疾病和用于抑制KSP驱动蛋白的氟化2-氨基甲基喹唑啉酮衍生物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US20080139586A1
公开(公告)日：2008-06-12
申请号：US11795435
申请日：2006-01-13
申请人： Paul J. Coleman , George D. Hartman
发明人： Paul J. Coleman , George D. Hartman
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D417/04
摘要： The present invention relates to fluorinated aminoalkyl-4-oxo-3,4-dihydropyrido[3,4-d]pyrimidine derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的氟化氨基烷基-4-氧代-3,4-二氢吡啶并[3,4-d]嘧啶衍生物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US07348440B2
公开(公告)日：2008-03-25
申请号：US10517559
申请日：2003-06-12
申请人： Kenneth L. Arrington , Paul J. Coleman , Christopher D. Cox , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , William F. Hoffman , Edward S. Tasber
发明人： Kenneth L. Arrington , Paul J. Coleman , Christopher D. Cox , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , William F. Hoffman , Edward S. Tasber
IPC分类号： C07D207/00 , C07D403/00 , C07D213/00 , C07D401/00 , C07D271/00 , C07D277/20 , C07D261/06 , C07D285/14 , C07D249/08 , C07D231/00 , A61K31/535 , A61K31/497 , A01N43/40 , A01N43/82 , A01N43/80 , A01N43/64 , A01N43/56 , A01N43/36
CPC分类号： C07D401/12 , C07D207/14 , C07D207/20 , C07D207/48 , C07D265/30 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12
摘要： The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的二氢吡咯化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US06410526B1
公开(公告)日：2002-06-25
申请号：US09583522
申请日：2000-05-31
IPC分类号： A61K3155
CPC分类号： C07D239/48 , C07D401/06 , C07D471/04
摘要： The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
摘要翻译： 本发明涉及新的壬酸衍生物，它们的合成及其作为alphav整联蛋白受体拮抗剂的用途。 更具体地说，本发明的化合物是整联蛋白受体alphavbeta3和alphavbeta5的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松，抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎症，炎症性关节炎 ，病毒性疾病，癌症和转移性肿瘤生长。
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