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153 条记录 (耗时 0.018 秒)

    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids
    72.
    发明授权
    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
    通过取代的联芳基氧代丁酸抑制基质金属蛋白酶

    公开(公告)号：US06225314B1

    公开(公告)日：2001-05-01

    申请号：US09343142

    申请日：1999-06-29

    申请人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    发明人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    IPC分类号： A61K31495

    CPC分类号： C07D253/08 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4706 ,  A61K31/502 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5513 ,  C07C62/38 ,  C07D237/32

    摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from arteriosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

    摘要翻译： 提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。 本发明的化合物具有以下通式：其中r为0-2，选自T，R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抑制MMP的贡献 ，如骨关节炎，类风湿关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症反应的病症，MMP活性介导的骨质减少，下颌关节病，神经系统脱髓鞘疾病 系统，肿瘤转移或创伤性关节损伤后的退行性软骨损失，以及动脉硬化斑块破裂引起的冠状动脉血栓形成。 本发明还提供了用于治疗这些病症的药物组合物和方法。

    3-imidazolylalkyl-, triazolylalkyl-, pyridinylalkyl-1,2,3-benzotriazin-4(3H)-ones and derivatives thereof
    75.
    发明授权
    3-imidazolylalkyl-, triazolylalkyl-, pyridinylalkyl-1,2,3-benzotriazin-4(3H)-ones and derivatives thereof 失效
    3-咪唑基烷基 - ，三唑基烷基 - ，吡啶基烷基-1,2,3-苯并三嗪-4（3H） - 酮及其衍生物

    公开(公告)号：US4680293A

    公开(公告)日：1987-07-14

    申请号：US835501

    申请日：1986-03-03

    申请人： William B. Wright, Jr. ,  Andrew S. Tomcufcik ,  Joseph W. Marsico, Jr.

    发明人： William B. Wright, Jr. ,  Andrew S. Tomcufcik ,  Joseph W. Marsico, Jr.

    IPC分类号： C07D253/08 ,  C07D401/06 ,  C07D403/06 ,  A61K31/53

    CPC分类号： C07D253/08 ,  C07D401/06 ,  C07D403/06

    摘要： Novel 3-heteroarylalkyl-1,2,3-benzotriazin-4(3H)-ones, having the structural formula: ##STR1## wherein A is a divalent moiety of the formula: ##STR2## wherein n is an integer from 3 to 10, inclusive; R.sub.1 and R.sub.2 may be the same or different and may be selected from the group consisting of hydrogen, halogen, trifluoromethyl, alkoxy having from one to four carbon atoms, alkyl having from one to four carbon atoms, nitro and amino; wherein Heteroaryl is ##STR3## wherein R.sub.3 and R.sub.4 may be hydrogen, alkyl having from one to four carbon atoms or phenyl and X is CH or N; together with the pharmaceutically acceptable salts thereof; processes for their preparation and their use in treating prostaglandin-related vascular disorders including ischemic heart disease, transient ischemic attack, thrombosis, migraine and hypertension.

    摘要翻译： 具有以下结构式的新颖的3-杂芳基烷基-1,2,3-苯并三嗪-4（3H） - 酮：其中A是下式的二价部分：其中n是3至10的整数 ， 包括的; R 1和R 2可以相同或不同，并且可以选自氢，卤素，三氟甲基，具有1-4个碳原子的烷氧基，具有1至4个碳原子的烷基，硝基和氨基; 其中杂芳基是其中R 3和R 4可以是氢，具有1-4个碳原子的烷基或苯基，X是CH或N; 连同其药学上可接受的盐; 其制备方法及其用于治疗前列腺素相关血管疾病，包括缺血性心脏病，短暂性脑缺血发作，血栓形成，偏头痛和高血压。

    Process for the production of 2-equivalent yellow couplers
    76.
    发明授权
    Process for the production of 2-equivalent yellow couplers 失效
    生产2-当量黄色成色剂的方法

    公开(公告)号：US4133955A

    公开(公告)日：1979-01-09

    申请号：US730204

    申请日：1976-10-06

    申请人： Gunter Renner

    发明人： Gunter Renner

    IPC分类号： G03C7/36 ,  C07D239/88 ,  C07D253/08 ,  C09B55/00 ,  G03C7/305 ,  G03C1/40

    CPC分类号： G03C7/30535 ,  C07D239/88 ,  C07D253/08

    摘要： A one-stage process for the production of a 2-equivalent acylacetamide yellow coupler, in which one hydrogen atom of the .alpha.-methylene group of the acyl acetamide coupler molecule is substituted by a group which is attached through an oxygen or nitrogen atom and which can be split off during chromogenic development with an oxidized color developer containing a primary aromatic amino group, which process is carried out by reactingA 4-equivalent acylacetamide yellow coupler withA compound containing an aromatic hydroxyl group or an --NH-- group in a heterocyclic ringIn the presence of a halogen, or an agent which releases halogen, andA basic condensation agentIn a substantially aprotic solvent.

    摘要翻译： 用于生产2-当量酰基乙酰胺黄色成色剂的一步法，其中酰基乙酰胺偶联剂分子的α-亚甲基的一个氢原子被通过氧或氮原子连接的基团取代， 可以在显色发展期间用含有伯芳族氨基的氧化显色剂分离，该方法通过使A 4等同的乙酰胺酰黄铜偶联物与含有芳族羟基或氨基的化合物在杂环中进行 在一个卤化物存在的环中，或释放卤化物的一种物质，以及一种基本的冷凝剂在大量的溶剂中。

    4-oxo-1,2,3-benzotriazine-3-propionic acids and esters
    78.
    发明授权
    4-oxo-1,2,3-benzotriazine-3-propionic acids and esters 失效
    4-OXO-1,2,3-苯并噻吖庚因-3-丙酸和酯

    公开(公告)号：US3772279A

    公开(公告)日：1973-11-13

    申请号：US3772279D

    申请日：1972-07-24

    申请人： SANDOZ AG

    发明人： KATHAWALA F

    IPC分类号： C07C243/38 ,  C07D253/08 ,  C07D55/08

    CPC分类号： C07D253/08 ,  C07C243/38

    摘要： DISCLOSED ARE COMPOUNDS OF THE CLASS OF 4-OXO-1,2,3BENZOTRIAZINE-3-PROPIONIC ACIDS AND ESTERS THEREOF, E.G. 6CHLORO-4-OXO-1,2,3-BENZOTRIAZINE-3-B-PROPIONIC ACID ETHYL ESTER. THE COMPOUNDS HAVE PHARMACOLOGICAL ACTIVITY IN ANIMALS, E.G. ANTI-INFLAMMATORY ACTIVITY. THE COMPOUNDS MAY BE PREPARED, FOR EXAMPLE, BY ADDITION TO THE CORRESPONDING 3-UNSUBSTITUTED COMPOUNDS AND BY REACTION OF AN ANTHRANIL AMIDE WITH SODIUM NITRITE AND A STRONG INORGANIC ACID, E.G. SULFURIC ACID. THE ACID FORMS ARE PREFERABLY PREPARED FROM THE ESTERS IN A KNOWN MANNER.

    Alkoxy-1,2,3-benzotriazine-4(3h)-ones 3 - (alpha-substituted amino-beta-alkoxybenzoxypropyl)-6,7- or 6,7,8-
    80.
    发明授权
    Alkoxy-1,2,3-benzotriazine-4(3h)-ones 3 - (alpha-substituted amino-beta-alkoxybenzoxypropyl)-6,7- or 6,7,8- 失效
    烷氧基-1,2,3-苯并噻嗪-4（3H） - 酮3 - （取代的氨基 - 苯氧基苯甲酰基）-6,7-或6,7,8-

    公开(公告)号：US3757019A

    公开(公告)日：1973-09-04

    申请号：US3757019D

    申请日：1972-06-22

    申请人： CASSELLA FARBWERKE MAINKUR AG

    发明人： STACHEL A ,  NITZ R ,  RESAG K ,  STACHEL I ,  BEYERLE R ,  SCHRAVEN E

    IPC分类号： C07D253/08 ,  C07D55/08

    CPC分类号： C07D253/08 ,  Y10S514/929

    摘要： THE PRESENT INVENTION PERTAINS TO NEW, PHARMACOLOGICALLY VALUABLE BASICALLY SUBSTITUTED 1,2,3-BENZOTRIAZINE4(3H)-ONE DERIVATIVES HAVING EXCELLENT CORONARY DILATORY PROPERTIES AND WHICH HAVE THE STRUCTURAL FORMULA

    4-(O=),3-((R2)M-C6H4-COO-CH(-CH2-R'')-CH2-),(R1)N-3,4-

    DIHYDRO-1,2,3-BENZOTRIAZINE

    WHEREIN R'' IS A RADICAL SELECTED FROM THE GROUP CONSISTING OF N-METHYLPIPERAZINO, N-PHENYPIPERAZINO AND N-TRIMETHOXYBENZOXYETHYLPIPERAZINO, SAID RADICAL BEING BOUND VIA A NITROGEN ATOM; R1 IS A LOWER ALKOXY GROUP HAVING 1-4 CARBON ATOMS WHICH MAY BE IN THE 6,7 OR 6,7,8-POSITION; R2 IS AN ALKOXY HAVING 1-4 CARBON ATOMS; M IS AN INTEGER SELECTED FORM 1,2 AND 3; AND N IS AN INTEGER SELECTED FROM THE GROUP CONSISTING OF 2 AND 3 AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF.