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1. 发明申请

US20050004126A1 Method of determining potential allosterically-binding matrix metalloproteinase inhibitors 审中-公开
标题翻译：确定潜在的变构结合基质金属蛋白酶抑制剂的方法
公开(公告)号：US20050004126A1
公开(公告)日：2005-01-06
申请号：US10835619
申请日：2004-04-29
申请人： Charles Andrianjara , Daniel Ortwine , Alexander Pavlovsky , William Roark
发明人： Charles Andrianjara , Daniel Ortwine , Alexander Pavlovsky , William Roark
IPC分类号： C07D239/90 , A61K31/00 , A61K31/36 , A61K31/444 , A61K31/517 , A61K31/519 , A61P1/02 , A61P1/04 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/04 , A61P29/00 , A61P35/00 , A61P43/00 , C07C69/76 , C07C69/92 , C07C205/57 , C07C229/62 , C07C235/60 , C07D213/30 , C07D213/40 , C07D239/96 , C07D285/14 , C07D285/24 , C07D285/32 , C07D317/54 , C07D317/58 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04 , A61K31/535 , A61K31/47 , A61K31/50
CPC分类号： C07D471/04 , A61K31/00 , C07C235/60 , C07D213/30 , C07D213/40 , C07D239/96 , C07D285/14 , C07D285/24 , C07D285/32 , C07D317/54 , C07D317/58 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/12 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Compounds are provided that bind allosterically to the catalytic domain of MMP-13 and comprise a hydrophobic group, first and second hydrogen bond acceptors and at least one, and preferably both, of a third hydrogen bond acceptor and a second hydrophobic group. Cartesian coordinates for centroids of the above features are defined in the specification. When the ligand binds to MMP-13, the first, second and third (when present) hydrogen bond acceptors bond respectively with Thr245, Thr 247 and Met 253, the first hydrophobic group locates within the S1′ channel of MMP-13 and the second hydrophobic group (when present) is relatively open to solvent. The compounds specifically inhibit the matrix metalloproteinase-13 enzyme and thus are useful for treating diseases resulting from tissue breakdown, such as heart disease, multiple sclerosis, arthritis, atherosclerosis, and osteoporosis.
摘要翻译：提供化合物，其以构象方式与MMP-13的催化结构域结合，并且包含疏水基团，第一和第二氢键受体以及至少一个，优选两个第三氢键受体和第二疏水基团。上述特征的质心的笛卡尔坐标在本说明书中定义。当配体结合MMP-13时，第一，第二和第三（当存在）氢键受体分别与Thr245，Thr 247和Met 253键合时，第一个疏水基团位于MMP-13的S1'通道内，第二个疏水基团（当存在时）对溶剂相对开放。所述化合物特异性地抑制基质金属蛋白酶-13酶，因此可用于治疗由组织破坏引起的疾病，例如心脏病，多发性硬化，关节炎，动脉粥样硬化和骨质疏松症。

2. 发明授权

US06828315B1 1-Amino triazoloc4,3-a! quinazoline-5-ones and/or -5-thiones inhibiting phosphodiesterase IV 失效
标题翻译： 1-氨基三唑并[3,4-a] 喹唑啉-5-酮和/或5-硫代磷酸二酯酶IV
公开(公告)号：US06828315B1
公开(公告)日：2004-12-07
申请号：US09980540
申请日：2001-10-25
申请人： Bernard Gaudilliere , Remi Lavalette , Charles Andrianjara , Francine Breuzard
发明人： Bernard Gaudilliere , Remi Lavalette , Charles Andrianjara , Francine Breuzard
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives. The compounds act as inhibitors of phosphodiesterase IV (PDE-4) and, as such, have utility in treating asthma, chronic bronchitis, acutte pulmonary attack, atopic dermatitis, pulmonary hypertension, pulmonary insufficiency, cardiac insufficiency, psoriasis, inflammatory conditions of the digestive system such as haemorrhagic rectocolitis and Crohn's disease, acute respiratory distress syndrome, acute pancreatitis, benign hypertrophy of the prostate, rheumatoid arthritis, multiple sclerosis, depression, ischaemia-induced neuronal damage, partial cerebral ischaemia, and cancer such as malignant tumor and chronic lymphoid leukemia.
摘要翻译：本发明涉及式I和式II的三唑并[4,3-a]喹唑啉-5-酮和5-硫杂，其中I和II是氮3或4上基团R的位置异构体。任选地，本发明也涉及其外消旋形式，异构体和药学上可接受的盐。本发明还涉及其制备方法和含有所述衍生物的组合物。这些化合物作为磷酸二酯酶IV（PDE-4）的抑制剂，因此可用于治疗哮喘，慢性支气管炎，急性肺部发作，特应性皮炎，肺动脉高压，肺功能不全，心功能不全，牛皮癣，消化道炎症状况系统如出血性直肠结肠炎和克罗恩病，急性呼吸窘迫综合征，急性胰腺炎，前列腺良性肥大，类风湿性关节炎，多发性硬化症，抑郁症，局部缺血诱发的神经元损伤，部分脑缺血和恶性肿瘤和慢性淋巴细胞癌白血病。

3. 发明授权

US07122565B2 Thiadiazoles and oxadiazoles and their use as phosphodiesterase-7 inhibitors 失效
标题翻译：噻二唑和恶二唑及其作为磷酸二酯酶-7抑制剂的用途
公开(公告)号：US07122565B2
公开(公告)日：2006-10-17
申请号：US09968371
申请日：2001-10-01
申请人： Fabrice Vergne , Pierre Ducrot , Charles Andrianjara , Patrick Bernardelli , Edwige Lorth Ois
发明人： Fabrice Vergne , Pierre Ducrot , Charles Andrianjara , Patrick Bernardelli , Edwige Lorth Ois
IPC分类号： C07D285/135 , A61K31/433
CPC分类号： C07D285/135 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/02
摘要： The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following Formula I: in which, Y is S or O, R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted, R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted, R3 is X2—R′3, in which X2 is a binding group and R′3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted, or their pharmaceutically acceptable derivatives, a compound of Formula I, for their preparation, and processes for pharmaceutical compositions containing methods of using the compounds for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.
摘要翻译：本发明提供具有下式I的1,3,4-噻二唑和1,3,4-恶二唑：其中Y是S或O，R 1是烷基，烯基，炔基，环烷基，杂环烷基，环烯基，芳基，杂芳基或多环基团，任选取代的R 2是烷基，烯基，炔基，环烷基，杂环烷基，任选取代的环烯基或芳基，R 3 >其中X 2是结合基团，并且R'3'是X 2 - ， - 环烷基，杂环烷基，环烯基，芳基，杂芳基或多环基团; 任选取代的，或其药学上可接受的衍生物，式I化合物及其制备方法，以及含有使用该化合物治疗PDE7抑制剂治疗相关疾病的方法的药物组合物的方法。

4. 发明授权

US06849637B2 Triazolo compounds as MMP inhibitors 失效
标题翻译：三唑酚化合物作为MMP抑制剂
公开(公告)号：US06849637B2
公开(公告)日：2005-02-01
申请号：US10075654
申请日：2002-02-14
申请人： Charles Andrianjara , Francine Breuzard , Bernard Gaudilliere , Henri Jacobelli
发明人： Charles Andrianjara , Francine Breuzard , Bernard Gaudilliere , Henri Jacobelli
IPC分类号： A61K31/519 , A61P1/02 , A61P1/04 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： A compound selected from those of formula (I): in which: W represents N or C—R1; in which R1 is as defined in the description, X represents N or C—R2 in which R2 is as defined in the description, Y represents a group selected from oxygen, sulfur, —NH, and —Nalkyl, Z represents a group selected from oxygen, sulphur, —NR8 in which R8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z1 represents a group —CR9R10 wherein R9 and R10, are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R4 is (are) as defined in the description, R3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula: in which p, Z2, B, q, and R13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.
摘要翻译：选自式（I）的化合物：其中：W表示N或C-R 1; 其中R1如说明书中所定义，X表示N或C-R2，其中R2如说明书中所定义，Y表示选自氧，硫，-NH和-N烷基的基团，Z表示选自氧，硫，-NR 8，其中R8如说明书中所定义，可选地取决于Y的定义，n为0至8的整数，其中Z 1为基团-CR 9 R 10，其中R 9和R 10如描述，该组包含任选的多个键或杂原子，A表示环状基团，m是0至7的整数，包括端值，其中R 4是如在说明书中所定义的（是），R 3表示选自氢，烷基，烯基，炔基和下式的基团：其中p，Z2，B，q和R13如说明书中所定义，任选地，其外消旋形式，异构体，其N-氧化物及其其药学上可接受的盐和含有它们的药物可用作特异性抑制剂的13型基质金属蛋白酶。

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