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    Alkynylated quinazoline compounds
    1.
    发明授权
    Alkynylated quinazoline compounds 失效
    炔烃基喹唑啉化合物

    公开(公告)号：US06962922B2

    公开(公告)日：2005-11-08

    申请号：US10269197

    申请日：2002-10-11

    申请人： Bernard Gaudilliere ,  Henri Jacobelli ,  Joseph Armand Picard ,  Michael William Wilson

    发明人： Bernard Gaudilliere ,  Henri Jacobelli ,  Joseph Armand Picard ,  Michael William Wilson

    IPC分类号： C07D239/96 ,  C07D403/06 ,  C07D471/04 ,  A61K31/517 ,  A61P19/02 ,  C07D401/10

    CPC分类号： C07D403/06 ,  C07D239/96 ,  C07D471/04

    摘要： A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N═X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.

    摘要翻译： 选自式（I）的化合物的化合物：其中W 1代表O，S或-NR 3，其中R 3表示氢 ，烷基，OH或CN; W 2表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基， 环烷基烷基，杂环，这些基团任选被取代，或者W 1和W 2 2一起形成式-NX 4 -W 3 < - >如描述中所定义，X 1，X 2和X 3表示N或C任选取代的n 是0至8，Z表示-CR 12 R 13，其中R 12和R 13定义同上 在描述中，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和药物产品 含有它们的特异性抑制剂可用作13型基质金属蛋白酶的特异性抑制剂。

    Benzo thiadiazine matrix metalloproteinase inhibitors
    2.
    发明授权
    Benzo thiadiazine matrix metalloproteinase inhibitors 失效
    苯并噻二嗪基质金属蛋白酶抑制剂

    公开(公告)号：US06656932B2

    公开(公告)日：2003-12-02

    申请号：US10074646

    申请日：2002-02-13

    申请人： Joseph Armand Picard ,  Michael William Wilson

    发明人： Joseph Armand Picard ,  Michael William Wilson

    IPC分类号： C07D28522

    CPC分类号： C07D285/22 ,  C07D285/24 ,  C07D417/12

    摘要： Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.

    摘要翻译： 选择性MMP-13抑制剂是其配制剂的药学上可接受的盐的苯并噻二嗪，其中R 2是氢或烷基; R 1和R 3包括氢，烷基和芳基，条件是R 3不是（CH 2）m联苯基或（CH 2）m取代的联苯基; X是O或NH，n是0,1或2.式I化合物或其药学上可接受的盐可用于治疗由MMP-13酶介导的疾病，包括选自骨关节炎，类风湿性关节炎， 癌症，炎症和心力衰竭。

    Pyrimidinone fused bicyclic metalloproteinase inhibitors
    3.
    发明授权
    Pyrimidinone fused bicyclic metalloproteinase inhibitors 失效
    嘧啶酮稠合双环金属蛋白酶抑制剂

    公开(公告)号：US06828326B2

    公开(公告)日：2004-12-07

    申请号：US10634225

    申请日：2003-08-05

    申请人： Joseph Armand Picard ,  Michael William Wilson

    发明人： Joseph Armand Picard ,  Michael William Wilson

    IPC分类号： C07D51304

    CPC分类号： C07D487/04 ,  C07D513/04

    摘要： The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.

    摘要翻译： 本发明涉及式I，B，X，Y和R 1的稠合双环金属蛋白酶抑制剂如说明书中所定义，以及治疗关节炎，炎症，癌症和其它病症的药物组合物和方法。

    Compounds for and methods of inhibiting matrix metalloproteinases
    4.
    发明授权
    Compounds for and methods of inhibiting matrix metalloproteinases 失效
    化合物和抑制基质金属蛋白酶的方法

    公开(公告)号：US6117869A

    公开(公告)日：2000-09-12

    申请号：US361077

    申请日：1999-07-26

    申请人： Joseph Armand Picard ,  Bruce David Roth ,  Drago Robert Sliskovic

    发明人： Joseph Armand Picard ,  Bruce David Roth ,  Drago Robert Sliskovic

    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。

    Tricyclic inhibitors of matrix metalloproteinases
    5.
    发明授权
    Tricyclic inhibitors of matrix metalloproteinases 失效
    基质金属蛋白酶三环抑制剂

    公开(公告)号：US5665764A

    公开(公告)日：1997-09-09

    申请号：US460436

    申请日：1995-06-02

    申请人： Donald Hupe ,  Linda Lea Johnson ,  Joseph Armand Picard ,  Andrew David White ,  Qi-Zhuang Ye

    发明人： Donald Hupe ,  Linda Lea Johnson ,  Joseph Armand Picard ,  Andrew David White ,  Qi-Zhuang Ye

    IPC分类号： C07D307/91 ,  A61K31/34

    CPC分类号： C07D307/91

    摘要： Tricyclic compounds 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 (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angionenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.

    摘要翻译： 描述了三环化合物以及其制备方法及其药物组合物，其可用作基质金属蛋白酶抑制剂，特别是明胶酶A（72kD明胶酶）和基质溶素-1的抑制剂，并用于治疗多发性硬化，动脉粥样硬化斑块破裂， 主动脉瘤，心力衰竭，再狭窄，牙周病，角膜溃疡，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症性疾病。

    Azaisoquinoline derivatives as matrix metalloproteinase inhibitors
    6.
    发明授权
    Azaisoquinoline derivatives as matrix metalloproteinase inhibitors 失效
    偶氮喹啉衍生物作为基质金属蛋白酶抑制剂

    公开(公告)号：US06977261B2

    公开(公告)日：2005-12-20

    申请号：US10634289

    申请日：2003-08-05

    申请人： Amy Mae Bunker ,  Joseph Armand Picard

    发明人： Amy Mae Bunker ,  Joseph Armand Picard

    IPC分类号： A61P9/00 ,  A61P29/00 ,  C07D237/32 ,  C07D403/06 ,  C07D471/04 ,  A61K31/4375

    CPC分类号： C07D471/04 ,  C07D237/32 ,  C07D403/06

    摘要： This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, Y, R2, R3, R4, R5, and n are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.

    摘要翻译： 本发明提供由式I定义的化合物或其药学上可接受的盐，其中R 1，Q，Y，R 2，R 3， R 4，R 5，和n如说明书中所定义。 本发明还提供药物组合物，其包含本说明书中定义的式I化合物或其药学上可接受的盐以及药学上可接受的载体，稀释剂或赋形剂。 本发明还提供了在动物中抑制MMP-13酶的方法，包括向动物施用式I化合物或其药学上可接受的盐。 本发明还提供了治疗患者中由MMP-13酶介导的疾病的方法，包括单独或在药物组合物中向患者施用式I化合物或其药学上可接受的盐。 本发明还提供了治疗诸如心脏病，多发性硬化，骨关节炎和类风湿性关节炎，除了骨关节炎或类风湿性关节炎之外的关节炎，心功能不全，炎性肠病，心力衰竭，年龄相关性黄斑变性，慢性阻塞性肺 疾病，哮喘，牙周疾病，牛皮癣，动脉粥样硬化和骨质疏松症，其包括单独或在药物组合物中向患者施用式I化合物或其药学上可接受的盐。 本发明还提供了包含式I化合物或其药学上可接受的盐以及说明书中描述的另一种药学活性成分的组合。

    Hydroxamic acid compounds useful as matrix metalloproteinase inhibitors
    7.
    发明授权
    Hydroxamic acid compounds useful as matrix metalloproteinase inhibitors 失效
    羟肟酸化合物可用作基质金属蛋白酶抑制剂

    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。

    Dibenzofuran sulfonamide matrix metalloproteinase inhibitors
    8.
    发明授权
    Dibenzofuran sulfonamide matrix metalloproteinase inhibitors 失效
    二苯并呋喃磺酰胺基质金属蛋白酶抑制剂

    公开(公告)号：US06294674B1

    公开(公告)日：2001-09-25

    申请号：US09254403

    申请日：1999-03-02

    申请人： Joseph Armand Picard ,  Drago Robert Sliskovic

    发明人： Joseph Armand Picard ,  Drago Robert Sliskovic

    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。

    Tricyclic inhibitors of matrix metalloproteinases
    9.
    发明授权
    Tricyclic inhibitors of matrix metalloproteinases 失效
    基质金属蛋白酶三环抑制剂

    公开(公告)号：US5958972A

    公开(公告)日：1999-09-28

    申请号：US859437

    申请日：1997-05-20

    申请人： Donald Hupe ,  Linda Lea Johnson ,  Joseph Armand Picard ,  Andrew David White ,  Qi-Zhuang Ye

    发明人： Donald Hupe ,  Linda Lea Johnson ,  Joseph Armand Picard ,  Andrew David White ,  Qi-Zhuang Ye

    IPC分类号： C07D307/91 ,  A61K31/215 ,  A61K31/44

    CPC分类号： C07D307/91

    摘要： Tricyclic compounds 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 (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.

    摘要翻译： 描述了三环化合物以及其制备方法及其药物组合物，其可用作基质金属蛋白酶抑制剂，特别是明胶酶A（72kD明胶酶）和基质溶素-1的抑制剂，并用于治疗多发性硬化，动脉粥样硬化斑块破裂， 主动脉瘤，心力衰竭，再狭窄，牙周病，角膜溃疡，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症性疾病。