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1. 发明申请

WO2005080560A1 MUTANT TACE CATALYTIC DOMAIN 审中-公开
标题翻译：突变TACE催化域
公开(公告)号：WO2005080560A1
公开(公告)日：2005-09-01
申请号：PCT/IB2005/000177
申请日：2005-01-24
申请人： WARNER-LAMBERT COMPANY LLC , FAUMAN, Eric, Benjamin , GURU, Siradanahalli Chandrasekharaiah , JOHNSON, Adam, Richard , WILDMAN, Scott, Andrew
发明人： FAUMAN, Eric, Benjamin , GURU, Siradanahalli Chandrasekharaiah , JOHNSON, Adam, Richard , WILDMAN, Scott, Andrew
IPC分类号： C12N9/64
CPC分类号： C12N9/6489
摘要： The invention relates to mutant TACE nucleic acids and amino acid sequences and methods for expressing TACE nucleic acids in host cells, such as prokaryotes.
摘要翻译：本发明涉及用于在宿主细胞中表达TACE核酸的突变TACE核酸和氨基酸序列和方法，例如原核生物。

2. 发明申请

WO2004014384A2 CYCLIC COMPOUNDS CONTAINING ZINC BINDING GROUPS AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：含有ZinC结合组的循环化合物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2004014384A2
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003518
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , JOHNSON, Adam, Richard
发明人： JOHNSON, Adam, Richard
IPC分类号： A61K31/517
CPC分类号： C07D413/04 , C07D239/91 , C07D495/04
摘要： This invention provides compounds defined by Formula I Z-L-R 1 -Q-D-(V 1 ) m -R 2 I or a pharmaceutically acceptable salt thereof, wherein Z, L, R 1 , Q, D, V 1 , m, and R 2 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 ZLR 1 -QD-（V 1）m R 2 I定义的化合物或其药学上可接受的盐，其中Z，L，R 1，Q，D，V 1 >，m和R 2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，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。

3. 发明申请

WO02064547A3 ISOPHTHALIC ACID DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：作为基质金属蛋白酶抑制剂的异丙酸衍生物
公开(公告)号：WO02064547A3
公开(公告)日：2002-12-05
申请号：PCT/IB0200344
申请日：2002-02-04
申请人： WARNER LAMBERT CO , BARVIAN NICOLE CHANTEL , CONNOR DAVID THOMAS , DYER RICHARD DENNIS , JOHNSON ADAM RICHARD , PATT WILLIAM CHESTER
发明人： BARVIAN NICOLE CHANTEL , CONNOR DAVID THOMAS , DYER RICHARD DENNIS , JOHNSON ADAM RICHARD , PATT WILLIAM CHESTER
IPC分类号： C12N9/99 , A61K31/166 , A61K31/192 , A61K31/235 , A61K31/36 , A61K31/433 , A61K31/4409 , A61K31/444 , A61P1/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C69/708 , C07C69/732 , C07C69/80 , C07C69/90 , C07C69/92 , C07C205/57 , C07C229/56 , C07C229/60 , C07C233/66 , C07C233/67 , C07C233/69 , C07C233/73 , C07C233/75 , C07C233/78 , C07C235/60 , C07C235/64 , C07D213/30 , C07D285/14 , C07D317/54 , C07D317/58 , A61K31/194
CPC分类号： C07D213/30 , C07C69/80 , C07C69/90 , C07C69/92 , C07C229/60 , C07C233/66 , C07C233/69 , C07C233/73 , C07C233/75 , C07C233/78 , C07C235/60 , C07D285/14 , C07D317/54 , C40B50/14
摘要： Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula (I) wherein: R , R , and R independently are hydrogen, halo, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR R , CN, or CF3; E is independently O or S; A and B independently are OR or NR R ; each R and R independently are H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R and R when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.
摘要翻译：选择性MMP-13抑制剂是式（I）的间苯二甲酸衍生物，其中：R 1，R 2和R 3独立地是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基， C 2 -C 6烯基，C 2 -C 6炔基，NO 2，NR 4 R 5，CN或CF 3; E独立地为O或S; A和B分别是OR 4或NR 4 R 5; 每个R 4和R 5独立地是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，（CH 2）n芳基，（CH 2）n环烷基，（CH 2）n杂芳基或R 当与它们所连接的氮一起连接时，R 5和R 5完全是3-至8-元环，任选地含有选自O，S或NH的杂原子，并且任选地被取代或未取代; n为0〜6; 或其药学上可接受的盐。该化合物可用于治疗由MMP酶介导的哺乳动物中的疾病。

4. 发明申请

WO2004014384A3 CYCLIC COMPOUNDS CONTAINING ZINC BINDING GROUPS AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：含有ZinC结合组的循环化合物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2004014384A3
公开(公告)日：2004-07-22
申请号：PCT/IB0303518
申请日：2003-08-04
申请人： WARNER LAMBERT CO , JOHNSON ADAM RICHARD
发明人： JOHNSON ADAM RICHARD
IPC分类号： A61P29/00 , C07D239/91 , C07D413/04 , C07D495/04 , A61K31/517 , A61K31/4365
CPC分类号： C07D413/04 , C07D239/91 , C07D495/04
摘要： This invention provides compounds defined by Formula I Z-L-R -Q-D-(V )m-R I or a pharmaceutically acceptable salt thereof, wherein Z, L, R , Q, D, V , m, and R are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I and the use of the compounds of Formula I as MMP-B inhibitors.
摘要翻译：本发明提供由式I ZLR 1 -QD-（V 1）m R 2 I定义的化合物或其药学上可接受的盐，其中Z，L，R 1，Q，D，V 1 >，m和R 2如说明书中所定义。本发明还提供包含式I化合物和式I化合物作为MMP-B抑制剂的药物组合物。

5. 发明申请

WO2002064599A1 BICYCLIC PYRIMIDINE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：双相PYRIMININE MATRIX金属蛋白酶抑制剂
公开(公告)号：WO2002064599A1
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000313
申请日：2002-01-30
申请人： WARNER-LAMBERT COMPANY , DYER, Richard, Dennis , HARTER, William, Glen , HICKS, James, Lester , JOHNSON, Adam, Richard , LI, Jie, Jack , ROARK, William, Howard , SHULER, Kevon, Ray
发明人： DYER, Richard, Dennis , HARTER, William, Glen , HICKS, James, Lester , JOHNSON, Adam, Richard , LI, Jie, Jack , ROARK, William, Howard , SHULER, Kevon, Ray
IPC分类号： C07D513/04
CPC分类号： C07D487/04 , C07D513/04
摘要： Selective MMP-13 inhibitors are bicyclic pyrmidines of the formula or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen or alkyl; R 2 , R 3 , and R 4 include hydrogen, halo, alkyl, C≡C(CH 2 ) m aryl; and X is O, S, SO, SO 2 , CH 2 , C=O, CHOH, NH, OR NR 5 . A compound of the formula, or a pharmaceutically acceptable salt thereof, is useful for treating cancer or arthritis.
摘要翻译：选择性MMP-13抑制剂是下式的双环哒嗪或其药学上可接受的盐，其中R 1是氢或烷基; R 2，R 3和R 4包括氢，卤素，烷基，C（CH 2）m芳基; 并且X是O，S，SO，SO 2，CH 2，C = O，CHOH，NH或NR 5。下式的化合物或其药学上可接受的盐可用于治疗癌症或关节炎。

6. 发明申请

WO2002064547A2 ISOPHTHALIC ACID DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：邻苯二甲酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2002064547A2
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000344
申请日：2002-02-04
申请人： WARNER-LAMBERT COMPANY , BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , DYER, Richard, Dennis , JOHNSON, Adam, Richard , PATT, William, Chester
发明人： BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , DYER, Richard, Dennis , JOHNSON, Adam, Richard , PATT, William, Chester
IPC分类号： C07C235/60
CPC分类号： C07D213/30 , C07C69/80 , C07C69/90 , C07C69/92 , C07C229/60 , C07C233/66 , C07C233/69 , C07C233/73 , C07C233/75 , C07C233/78 , C07C235/60 , C07D285/14 , C07D317/54 , C40B50/14
摘要： Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula (I) wherein: R 1 , R 2 , and R 3 independently are hydrogen, halo, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, NO 2 , NR 4 R 5 , CN, or CF 3 ; E is independently O or S; A and B independently are OR 4 or NR 4 R 5 ; each R 4 and R 5 independently are H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, (CH 2 ) n aryl, (CH 2 ) n cycloalkyl, (CH 2 ) n heteroaryl, or R 4 and R 5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.
摘要翻译：选择性MMP-13抑制剂是式（I）的间苯二甲酸衍生物，其中：R 1，R 2和R 4独立地选自： 3独立地为氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6烷氧基，C 2 -C 6链烯基，C 2 -C 6炔基，NO

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