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公开(公告)号：US6117869A
公开(公告)日：2000-09-12
申请号：US361077
申请日：1999-07-26
IPC分类号： C07D311/82 , C07D327/08 , C07D339/08 , C07D409/04 , A61K31/385 , A61K31/39
CPC分类号： C07D409/04 , C07D311/82 , C07D327/08 , C07D339/08
摘要： The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds ##STR1## More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilatation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
摘要翻译： 本发明涉及抑制基质金属蛋白酶的式I化合物和使用该化合物抑制基质金属蛋白酶的方法。更具体地，本发明涉及治疗涉及基质金属蛋白酶的疾病的方法，例如多发性硬化，动脉粥样硬化斑块 破裂，再狭窄，主动脉瘤，心力衰竭，牙周病，角膜溃疡，烧伤，褥疮性溃疡，慢性溃疡或创伤，癌症转移，肿瘤血管发生，骨质疏松症，类风湿或骨关节炎，肾脏疾病，左心室扩张或其他自身免疫或炎症 依赖于白细胞组织侵袭的疾病。
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公开(公告)号：US5693657A
公开(公告)日：1997-12-02
申请号：US786062
申请日：1997-01-21
申请人： Helen Tsenwhei Lee , Patrick Michael O'Brien , Joseph Armand Picard , Claude Forsey Purchase, Jr. , Bruce David Roth , Drago Robert Sliskovic , Andrew David White
发明人： Helen Tsenwhei Lee , Patrick Michael O'Brien , Joseph Armand Picard , Claude Forsey Purchase, Jr. , Bruce David Roth , Drago Robert Sliskovic , Andrew David White
IPC分类号： A61K31/41 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07D207/337 , C07D215/38 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/64 , C07D233/88 , C07D239/42 , C07D249/04 , C07D249/06 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/20 , C07D277/22 , C07D277/30 , C07D285/12 , C07D307/54 , C07D333/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D471/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/04 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04
摘要： Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 .dbd.R.sub.3 .dbd.H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.
摘要翻译： 对于除了四唑之外的X，n = 2，然后R2 = R3 = H，具有式（IMAGE）的具有ACAT抑制活性的药学上有用的化合物，其中n为0,1或2。 R 1是苯基，取代的苯基，萘基，取代的萘基，杂芳基或具有1至18个碳原子的烃基; R2和R3是氢，卤素，羟基，烷基，烯基，环烷基，苯基，取代的苯基，杂芳基或形成螺烷基; X是含有一至四个杂原子的杂单环五元环，所述杂原子是氮，氧或硫，以及它们的组合; 并且描述了R4是具有1至20个碳原子的烃基以及它们的制备方法。
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公开(公告)号：US6093744A
公开(公告)日：2000-07-25
申请号：US117748
申请日：1998-08-10
申请人： Helen Tsenwhei Lee , Joseph Armand Picard , William Howard Roark , Bruce David Roth , Drago Robert Sliskovic
发明人： Helen Tsenwhei Lee , Joseph Armand Picard , William Howard Roark , Bruce David Roth , Drago Robert Sliskovic
IPC分类号： C07C307/02 , C07C311/08 , C07C311/16 , C07C311/44 , C07C331/08 , C07C335/16 , C07D209/20 , C07D333/34 , A01N41/06 , A01K31/18 , C07C303/00 , C07C307/00
CPC分类号： C07C311/08 , C07C307/02 , C07C311/16 , C07C311/44 , C07C331/08 , C07C335/16 , C07D209/20 , C07D333/34
摘要： The instant invention is new compounds of Formula I ##STR1## their use as cerebrovascular agents in diseases such as stroke, peripheral vascular disease, restenosis, and as agents for regulating plasma cholesterol concentrations, for treating hypercholesterolemia and atherosclerosis, and for lowering the serum or plasma level of Lp(a). A pharmaceutical composition is also claimed.
摘要翻译： PCT No.PCT / US97 / 06725 Sec。 371日期：1998年8月10日 102（e）日期1998年8月10日PCT 1997年4月21日PCT PCT。 WO97 / 44314 PCT公开号 日期1997年11月27日本发明是式I化合物的新化合物，其用作中风，外周血管疾病，再狭窄等疾病，作为调节血浆胆固醇浓度的药剂，用于治疗高胆固醇血症和动脉粥样硬化的脑血管药， 血清或血浆中的Lp（a）水平。 还要求药物组合物。
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公开(公告)号：US5646170A
公开(公告)日：1997-07-08
申请号：US433776
申请日：1995-05-03
申请人： Helen Tsenwhei Lee , Patrick Michael O'Brien , Joseph Armand Picard , Claude Forsey Purchase, Jr. , Bruce David Roth , Drago Robert Sliskovic , Andrew David White
发明人： Helen Tsenwhei Lee , Patrick Michael O'Brien , Joseph Armand Picard , Claude Forsey Purchase, Jr. , Bruce David Roth , Drago Robert Sliskovic , Andrew David White
IPC分类号： A61K31/41 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07D207/337 , C07D215/38 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/64 , C07D233/88 , C07D239/42 , C07D249/04 , C07D249/06 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/20 , C07D277/22 , C07D277/30 , C07D285/12 , C07D307/54 , C07D333/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D471/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/04 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04
摘要： Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 .dbd.R.sub.3 .dbd.H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.
摘要翻译： 对于除了四唑之外的X，n = 2，然后R2 = R3 = H，具有式IMAImage的ACAT抑制活性的药学上有用的化合物，其中n为0,1或2。 R 1是苯基，取代的苯基，萘基，取代的萘基，杂芳基或具有1至18个碳原子的烃基; R2和R3是氢，卤素，羟基，烷基，烯基，环烷基，苯基，取代的苯基，杂芳基或形成螺烷基; X是含有一至四个杂原子的杂单环五元环，所述杂原子是氮，氧或硫，以及它们的组合; 并且描述了R4是具有1至20个碳原子的烃基以及它们的制备方法。
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5.发明授权公开(公告)号：US06677355B1
公开(公告)日：2004-01-13
申请号：US10049544
申请日：2002-02-13
申请人： Christopher Alan Conrad , Patrick Michael O'Brien , Daniel Fred Ortwine , Joseph Armand Picard , Drago Robert Sliskovic
发明人： Christopher Alan Conrad , Patrick Michael O'Brien , Daniel Fred Ortwine , Joseph Armand Picard , Drago Robert Sliskovic
IPC分类号： C07D30791
CPC分类号： C07D307/91 , C07C311/19 , C07C311/20 , C07C2601/08 , C07C2601/14 , C07D307/93 , C07D407/12
摘要： Compounds of the formula; are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues. Also disclosed are methods for the preparation of such compounds, pharmaceutical compositions including the same, and methods of treating diseases in which matrix metalloproteinases are involved including multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
摘要翻译： 式的化合物可用于抑制动物中的基质金属蛋白酶，因此预防和治疗由结缔组织破裂引起的疾病。 还公开了制备这些化合物的方法，包括其的药物组合物，以及治疗其中涉及基质金属蛋白酶的疾病的方法，包括多发性硬化，动脉粥样硬化斑块破裂，再狭窄，主动脉瘤，心力衰竭，牙周病，角膜溃疡， 烧伤，褥疮性溃疡，慢性溃疡或创伤，癌症转移，肿瘤血管发生，骨质疏松症，类风湿性关节炎，骨关节炎，肾脏疾病，左心室扩张或依赖于白细胞组织侵袭的其他自身免疫性或炎性疾病。
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公开(公告)号：US06294674B1
公开(公告)日：2001-09-25
申请号：US09254403
申请日：1999-03-02
IPC分类号： C07D30791
CPC分类号： C07D307/91 , C07C311/19 , C07D333/76
摘要： The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds. wherein Q is an un-natural amino acid. More particurlarly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthiritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
摘要翻译： 本发明涉及抑制基质金属蛋白酶的式I化合物和使用该化合物抑制基质金属蛋白酶的方法。其中Q是非天然氨基酸。 更具体地，本发明涉及一种治疗其中涉及基质金属蛋白酶的疾病的方法，例如多发性硬化，动脉粥样硬化斑块破裂，再狭窄，主动脉瘤，心力衰竭，牙周病，角膜溃疡，烧伤，褥疮性溃疡，慢性溃疡或 伤口，癌症转移，肿瘤血管生成，关节炎或依赖于白细胞组织侵袭的其他自身免疫性或炎性疾病。
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公开(公告)号：US6020366A
公开(公告)日：2000-02-01
申请号：US171833
申请日：1998-10-27
IPC分类号： A61K31/343 , A61K31/381 , A61K31/4192 , A61K31/443 , A61K31/4985 , A61P1/02 , A61P9/00 , A61P19/02 , A61P25/28 , A61P43/00 , C07D307/91 , C07D405/12 , C07D407/12 , C07D409/12 , C07D491/052 , A61K31/34
CPC分类号： C07D307/91 , C07D405/12 , C07D407/12 , C07D409/12
摘要： Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 include hydrogen, alkyl, substituted alkyl, halo, and arylalkyl; R.sub.3 is hydroxy, alkoxy, or hydroxyamino; X is O, S, or NOH; and R.sub.4 and R.sub.5 include hydrogen, alkyl, and aryl are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues.
摘要翻译： PCT No.PCT / US97 / 12389 Sec。 371日期：1998年10月27日第 102（e）1998年10月27日PCT PCT 1997年7月16日PCT公布。 公开号WO98 / 06711 日期：1998年2月19日化学式其中R 1和R 2包括氢，烷基，取代的烷基，卤素和芳基烷基; R3是羟基，烷氧基或羟基氨基; X是O，S或NOH; 并且R4和R5包括氢，烷基和芳基可用于抑制动物中的基质金属蛋白酶，因此，预防和治疗由结缔组织破裂引起的疾病。
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公开(公告)号：US06906092B2
公开(公告)日：2005-06-14
申请号：US10603677
申请日：2003-06-25
IPC分类号： A61K31/343 , A61K31/381 , A61P9/10 , A61P17/02 , A61P27/02 , C07C311/19 , C07D307/91 , C07D333/76 , A61K31/40
CPC分类号： C07D307/91 , A61K31/343 , A61K31/381 , C07C311/19 , C07C2603/18 , C07D333/76
摘要： The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
摘要翻译： 本发明涉及使用具有式I的二苯并呋喃磺酰胺衍生物的化合物抑制基质金属蛋白酶的方法。更具体地，本发明涉及治疗涉及基质金属蛋白酶的疾病的方法，例如多发性硬化，动脉粥样硬化斑块破裂， 再狭窄，主动脉瘤，心力衰竭，牙周病，角膜溃疡，烧伤，褥疮性溃疡，慢性溃疡或创伤，癌转移，肿瘤血管生成，关节炎或依赖于白细胞组织侵袭的其他自身免疫性或炎性疾病。
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公开(公告)号：US06620835B2
公开(公告)日：2003-09-16
申请号：US10162518
申请日：2002-06-04
IPC分类号： A61K31381
CPC分类号： C07D307/91 , A61K31/343 , A61K31/381 , C07C311/19 , C07C2603/18 , C07D333/76
摘要： The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
摘要翻译： 本发明涉及使用具有式IIIO的二苯并呋喃磺酰胺衍生物的化合物抑制基质金属蛋白酶的方法，本发明涉及治疗涉及基质金属蛋白酶的疾病的方法，例如多发性硬化，动脉粥样硬化斑块破裂，再狭窄 ，主动脉瘤，心力衰竭，牙周病，角膜溃疡，烧伤，褥疮性溃疡，慢性溃疡或创伤，癌症转移，肿瘤血管生成，关节炎或依赖于白细胞组织侵袭的其他自身免疫性或炎性疾病。
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公开(公告)号：US06492422B2
公开(公告)日：2002-12-10
申请号：US10108817
申请日：2002-03-27
IPC分类号： C07C31121
CPC分类号： C07D307/91 , C07C311/21 , C07D209/88 , C07D307/93 , C07D333/76 , C07D405/04 , H04M15/00 , H04M15/28 , H04M15/30 , H04M15/31 , H04M15/49 , H04M15/8044 , H04M15/83 , H04M2215/0168 , H04M2215/42 , H04M2215/46 , H04M2215/745 , H04M2215/82 , H04M2215/92 , H04M2215/96
摘要： Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
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