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1. 发明申请

WO2007109786A2 PROCESS FOR THE PREPARATION OF 3,4-DISUBSTITUTED-THIAZOLIDIN-2-ONES 审中-公开
标题翻译：制备3,4代替噻唑烷-2-酮的方法
公开(公告)号：WO2007109786A2
公开(公告)日：2007-09-27
申请号：PCT/US2007064786
申请日：2007-03-23
申请人： INSPIRE PHARMACEUTICALS INC , DECAMP JONATHAN B , WATSON PAUL S , SHE JIN
发明人： DECAMP JONATHAN B , WATSON PAUL S , SHE JIN
IPC分类号： C07D417/02 , C07D277/34
CPC分类号： C07D277/14 , C07C319/06 , C07C323/58
摘要： The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.
摘要翻译：本发明涉及用于制备3,4-二取代 - 噻唑烷-2-酮的实用的高产合成方法，其不损害化合物的绝对立体化学完整性。本发明还涉及3,4-二取代 - 噻唑烷-2-酮的新化合物。通过本发明制备的化合物可用于合成和制备用于治疗与抑制肌动蛋白聚合相关的疾病或病症的化合物（例如软核灰蛋白和/或其类似物）。

2. 发明申请

WO2006105529A1 PROCESS FOR THE PREPARATION OF 4,6-DISUBSTITUTED-TETRAHYDRO-FURO, THIENO, PYRROLO AND CYCLOPENTA-[3,4][1,3]DIOXOLES 审中-公开
标题翻译：用于制备4,6-取代的四氢呋喃，三烯，吡咯和环戊二烯并[3,4] [1,3]二氧化物的方法
公开(公告)号：WO2006105529A1
公开(公告)日：2006-10-05
申请号：PCT/US2006/012626
申请日：2006-03-30
申请人： INSPIRE PHARMACEUTICALS, INC. , WATSON, Paul S. , DOUGLASS III, James G. , SUCHOZAK, Bob , PANDIARAJU, Subramanian , DIXON, Craig E. , LEVIN, Daniel
发明人： WATSON, Paul S. , DOUGLASS III, James G. , SUCHOZAK, Bob , PANDIARAJU, Subramanian , DIXON, Craig E. , LEVIN, Daniel
IPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
CPC分类号： C07F9/6561 , C07F9/65616 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要： The present invention is directed to a processes for the synthesis of trans isomer of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][l ,3]dioxoles (Formula I). The process comprises the steps of: (a) obtaining a compound of Formula (II), which is a mixture of cis and trans-diastereomers, and (b) chemically decomposing the compound of Formula (II) in a solution comprising a solvent and an acid that is a hydrogen donor or an electron pair acceptor, whereby the cis diastereomer is decomposed and the compound of Formula (I) is obtained. The compounds prepared by the present invention are useful in treating diseases or conditions associated with platelet aggregation and/or platelet activation.
摘要翻译：本发明涉及合成4,6-二取代 - 四氢 - 呋喃，噻吩并，吡咯并环戊烷并[3,4] [1,3]二氧杂环戊烯（式I）的反式异构体的方法。该方法包括以下步骤：（a）得到顺式和反式 - 非对映异构体的混合物的式（II）化合物，和（b）将式（II）化合物在包含溶剂和作为氢供体或电子对受体的酸，由此使顺式非对映异构体分解并获得式（I）化合物。通过本发明制备的化合物可用于治疗与血小板聚集和/或血小板活化相关的疾病或病症。

3. 发明申请

WO2012012282A1 BIFUNCTIONAL RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译：双功能RHO激酶抑制剂化合物，组合物和用途
公开(公告)号：WO2012012282A1
公开(公告)日：2012-01-26
申请号：PCT/US2011/044148
申请日：2011-07-15
申请人： INSPIRE PHARMACEUTICALS, INC. , LAMPE, John W. , WATSON, Paul S. , VITTITOW, Jason L. , PETERSON, Ward M.
发明人： LAMPE, John W. , WATSON, Paul S. , VITTITOW, Jason L. , PETERSON, Ward M.
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07D401/12 , A61K31/454 , A61K31/4725 , A61K31/5575 , A61K47/55 , C07D401/14
摘要： This invention relates to synthetic bifunctional compounds comprising a first rho-associated kinase (ROCK) inhibiting compound and a second pharmaceutically active compound with complementary activity; the first and the second compounds are covalently linked by a biologically labile bond. This invention also relates to methods of making such compounds. The invention also relates to methods of using such bifunctional compounds in the prevention or treatment of diseases or conditions that are affected or can be assisted by altering the integrity or rearrangement of the cytoskeleton. Particularly, this invention relates to methods of treating ophthalmic diseases such as disorders in which intraocular pressure is elevated, for example primary open-angle glaucoma, using the bifunctional compounds.
摘要翻译：本发明涉及包含第一rho相关激酶（ROCK）抑制化合物和具有互补活性的第二药物活性化合物的合成双功能化合物; 第一和第二化合物通过生物不稳定的键共价连接。本发明还涉及制备这些化合物的方法。本发明还涉及使用这种双功能化合物来预防或治疗通过改变细胞骨架的完整性或重排而受影响或可以辅助的疾病或病症的方法。特别地，本发明涉及使用双功能化合物治疗眼科疾病如眼压升高的病症，例如原发性开角型青光眼的方法。

4. 发明申请

WO2006121856A2 PYRIMIDINE-BASED NON-NUCLEOTIDE COMPOSITION AND METHOD FOR INHIBITING PLATELET AGGREGATION 审中-公开
标题翻译：基于吡嗪基的非核苷酸组合物和抑制血小板聚集的方法
公开(公告)号：WO2006121856A2
公开(公告)日：2006-11-16
申请号：PCT/US2006/017407
申请日：2006-05-02
申请人： INSPIRE PHARMACEUTICALS INC. , DOUGLASS, James, G., III , WATSON, Paul, S. , SHAVER, Sammy, R. , BEDNARSKI, Krzysztof
发明人： DOUGLASS, James, G., III , WATSON, Paul, S. , SHAVER, Sammy, R. , BEDNARSKI, Krzysztof
IPC分类号： A61K31/7072 , A61K31/513 , C07H19/12 , C07D405/02
CPC分类号： C07D493/04 , C07D405/04 , C07H19/12
摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide pyrimidine-based compound, preferably a P2Y 12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formulae (I) and (Ia-Ic), or tautomers, salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae (I) and (Ia-Ic).
摘要翻译：本发明涉及一种预防或治疗与血小板聚集有关的疾病或病症的方法。该方法还涉及治疗血栓形成或相关病症的方法。该方法包括向受试者施用包含有效量的非核苷酸嘧啶类化合物，优选P2Y 12受体拮抗剂化合物的药物组合物，其中所述量有效抑制血小板聚集。可用于本发明的化合物包括通式（I）和（Ia-Ic）的化合物，或其互变异构体，盐，水合物和溶剂合物。本发明还提供式（I）和（Ia-Ic）的新化合物。

5. 发明申请

WO2005097814A3 COMPOSITION AND METHOD FOR INHIBITING PLATELET AGGREGATION 审中-公开
标题翻译：抑制血小板聚集的组合物和方法
公开(公告)号：WO2005097814A3
公开(公告)日：2005-12-22
申请号：PCT/US2005011324
申请日：2005-03-30
申请人： INSPIRE PHARMACEUTICALS INC , BOYER JOSE , DOUGLASS JAMES G III , SHAVER SAMMY RAY , WATSON PAUL S , KRISHNAMOORTHY RAMESH
发明人： BOYER JOSE , DOUGLASS JAMES G III , SHAVER SAMMY RAY , WATSON PAUL S , KRISHNAMOORTHY RAMESH
IPC分类号： A61K31/7072 , A61K31/708 , A61K31/7084 , A61K38/43 , A61K45/00 , A61P7/00 , A61P7/02 , A61P7/08 , A61P7/12 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/14 , A61P13/00 , A61P13/12 , A61P15/00 , A61P15/06 , A61P17/02 , A61P19/04 , A61P25/06 , A61P29/00 , A61P31/04 , A61P37/00 , A61P39/00 , A61P41/00 , A61P43/00 , C07F9/6561 , C07H19/04 , C07H19/10 , C07H19/20 , C07H19/207 , C07H21/00 , C07H21/02 , C07H21/04 , A61K31/7076
CPC分类号： C07H19/20 , A61K31/675 , A61K31/7072 , A61K31/7076 , A61K31/7084 , C07H19/04 , C07H19/10 , C07H19/207 , C07H21/00
摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside 5'-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5'-monophosphates and dinucleoside diphosphates. The present invention further provides pharmaceutical formulations comprising a pharmaceutical carrier and mononucleoside 5'-monophosphates or dinucleoside diphosphates.
摘要翻译：本发明涉及预防或治疗与血小板聚集有关的疾病或病症的方法。该方法还涉及治疗血栓形成的方法。该方法包括向受试者施用包含治疗有效量的P2Y12受体拮抗剂化合物的药物组合物，其中所述量有效地结合血小板上的P2Y12受体并抑制ADP诱导的血小板聚集。用于本发明的P2Y12受体拮抗剂化合物包括单核苷5'-单磷酸酯，单核苷多磷酸酯和通式I的二核苷多磷酸酯或其盐。本发明还提供了单核苷5'-单磷酸酯和二核苷二磷酸酯的新型化合物。本发明进一步提供了包含药物载体和单核苷5'-单磷酸酯或二核苷二磷酸酯的药物制剂。

6. 发明申请

WO2005097814A2 COMPOSITION AND METHOD FOR INHIBITING PLATELET AGGREGATION 审中-公开
标题翻译：用于抑制平板聚集的组合物和方法
公开(公告)号：WO2005097814A2
公开(公告)日：2005-10-20
申请号：PCT/US2005/011324
申请日：2005-03-30
申请人： INSPIRE PHARMACEUTICALS, INC. , BOYER, Jose , DOUGLASS, James, G., III , SHAVER, Sammy Ray , WATSON, Paul S. , KRISHNAMOORTHY, Ramesh
发明人： BOYER, Jose , DOUGLASS, James, G., III , SHAVER, Sammy Ray , WATSON, Paul S. , KRISHNAMOORTHY, Ramesh
IPC分类号： C07H
CPC分类号： C07H19/20 , A61K31/675 , A61K31/7072 , A61K31/7076 , A61K31/7084 , C07H19/04 , C07H19/10 , C07H19/207 , C07H21/00
摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y 12 receptor antagonist compound, wherein said amount is effective to bind the P2Y 12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y 12 receptor antagonist compounds useful for this invention include mononucleoside 5'-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5'-monophosphates and dinucleoside diphosphates. The present invention further provides pharmaceutical formulations comprising a pharmaceutical carrier and mononucleoside 5'-monophosphates or dinucleoside diphosphates.
摘要翻译：本发明涉及一种预防或治疗与血小板聚集有关的疾病或病症的方法。该方法还涉及治疗血栓形成的方法。该方法包括向受试者施用包含治疗有效量的P2Y12受体拮抗剂化合物的药物组合物，其中所述量有效结合血小板上的P2Y12受体并抑制ADP诱导的血小板聚集。可用于本发明的P2Y12受体拮抗剂化合物包括单核苷5'-单磷酸酯，单核苷多聚磷酸酯和通式I的二核苷多磷酸盐或其盐。本发明还提供了单核苷酸5'-单磷酸酯和二核苷二磷酸的新型化合物。本发明还提供了包含药物载体和单核苷5'-单磷酸酯或二核苷二磷酸的药物制剂。

7. 发明申请

WO2012015760A1 METHOD FOR TREATING OPHTHALMIC DISEASES USING KINASE INHIBITOR COMPOUNDS IN PRODRUG FORMS 审中-公开
标题翻译：使用激素抑制剂化合物治疗原发性疾病的方法
公开(公告)号：WO2012015760A1
公开(公告)日：2012-02-02
申请号：PCT/US2011/045244
申请日：2011-07-25
申请人： INSPIRE PHARMACEUTICALS, INC. , LAMPE, John W. , SHAVER, Sammy R. , WATSON, Paul S.
发明人： LAMPE, John W. , SHAVER, Sammy R. , WATSON, Paul S.
IPC分类号： A01N43/34
CPC分类号： C07D401/12 , A61K9/0048 , C07D401/14 , C07D403/12
摘要： This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula (I) to the eyes of the patient in need of.
摘要翻译：本发明涉及rho激酶（ROCK）抑制剂的前药。这些前药通常是母体化合物的酯或酰胺衍生物。这些前药通常是ROCK的弱抑制剂，但它们的母体化合物具有良好的活性。滴入眼中时，这些前体药物的酯或酰胺基被快速水解成醇，胺或酸，并将前体药物转化成活性碱化合物。 ROCK抑制剂的前药提供了几个优点，例如将较高浓度的活性物质递送到靶位点和减少眼部不适。本发明还涉及通过向患者的眼睛施用有效量的式（I）的ROCK前药化合物，治疗眼部疾病如青光眼，过敏性结膜炎，黄斑水肿，黄斑变性和睑炎，需要。

8. 发明申请

WO2009154940A1 PROCESS FOR THE PREPARATION OF RHO-KINASE INHIBITOR COMPOUNDS 审中-公开
标题翻译：制备RHO-激酶抑制剂化合物的方法
公开(公告)号：WO2009154940A1
公开(公告)日：2009-12-23
申请号：PCT/US2009/044889
申请日：2009-05-21
申请人： INSPIRE PHARMACEUTICALS, INC. , SHE, Jin , DECAMP, Jonathan, Bryan , WATSON, Paul, S. , SLADE, David, J.
发明人： SHE, Jin , DECAMP, Jonathan, Bryan , WATSON, Paul, S. , SLADE, David, J.
IPC分类号： A01N43/42
CPC分类号： C07D401/12 , C07C67/08 , C07C69/78
摘要： The present invention is directed to practical high-yielding synthetic processes to prepare compounds of general Formula III, IV, V, VII, VIII, IX, X, XII, XIV, and XV. Such compounds are useful as final products or can be used as intermediates and be further modified to prepare other desired products such as rho-kinase inhibitors. The present invention is also directed to certain novel compounds and/or novel solid forms of certain compounds.
摘要翻译：本发明涉及制备通式III，IV，V，VII，VIII，IX，X，XII，XIV和XV的化合物的实际高产合成方法。这些化合物可用作最终产物，或可用作中间体，并进一步修饰以制备其它所需产物如rho激酶抑制剂。本发明还涉及某些新化合物和/或某些化合物的新型固体形式。

9. 发明申请

WO2008077057A3 CYTOSKELETAL ACTIVE RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译： CYTOSKELETAL活性RHO激酶抑制剂化合物，组合物和用途
公开(公告)号：WO2008077057A3
公开(公告)日：2008-08-21
申请号：PCT/US2007087973
申请日：2007-12-18
申请人： INSPIRE PHARMACEUTICALS INC , LAMPE JOHN W , WATSON PAUL S , SLADE DAVID J , PETERSON WARD M , CREAN CHRISTOPHER S , VITTITOW JASON L , DECAMP JONATHAN BRYAN , PELZ NICHOLAS F
发明人： LAMPE JOHN W , WATSON PAUL S , SLADE DAVID J , PETERSON WARD M , CREAN CHRISTOPHER S , VITTITOW JASON L , DECAMP JONATHAN BRYAN , PELZ NICHOLAS F
IPC分类号： A61K31/505 , A61K31/47
CPC分类号： C07D401/12 , A61F9/00781 , A61K9/0048 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
摘要翻译：本发明涉及作为ρ相关蛋白激酶抑制剂的合成细胞骨架活性化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。本发明还涉及预防或治疗与细胞骨架重组有关的疾病或病症的方法。在本发明的一个实施例中，该方法治疗增加的眼内压，例如原发性开角型青光眼。该方法包括向受试者施用治疗有效量的式I或式II的细胞骨架活性化合物，其中所述量有效影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞 - 基质粘连的改变。

10. 发明申请

WO2007140333A3 MONONUCLEOSIDE PHOSPHONATE COMPOUNDS 审中-公开
公开(公告)号：WO2007140333A3
公开(公告)日：2007-12-06
申请号：PCT/US2007/069795
申请日：2007-05-25
申请人： INSPIRE PHARMACEUTICALS, INC. , SHAVER, Sammy, R. , DOUGLASS, James, G., III , WATSON, Paul, S.
发明人： SHAVER, Sammy, R. , DOUGLASS, James, G., III , WATSON, Paul, S.
IPC分类号： C12P19/30
摘要： The present invention relates to a mononucleoside phosphonate compound in which the nature of the linkage between the ribosyl or carbocyclic residue and the phosphorous atom of a mononucleotide is modified to include alkylene groups, which improve the stability of the compound. These mononucleoside phosphonate compounds optionally have a degradation-resistant substituent attached on the terminal phosphate. By modification of the linkage and the attachment of the degradation-resistant substituent, the stability of the mononucleoside phosphonate compound significantly improves. The mononucleoside phosphonate compounds of the present invention are useful in preventing and treating diseases or disorders associated with platelet aggregation.

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