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1. 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.

2. 发明申请

WO2007124123A3 METHOD OF TREATING INFLAMMATION 审中-公开
公开(公告)号：WO2007124123A3
公开(公告)日：2007-11-01
申请号：PCT/US2007/009773
申请日：2007-04-20
申请人： INSPIRE PHARMACEUTICALS, INC. , BRUBAKER, Kurt, E. , SHAVER, Sammy, R. , DOUGLASS, James, G., III
发明人： BRUBAKER, Kurt, E. , SHAVER, Sammy, R. , DOUGLASS, James, G., III
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00 , C07H19/16
摘要： This invention provides methods of preventing and/or treating diseases or conditions associated with inflammation in a mammal, particularly a human. The method comprises administering to a mammal in need thereof an effective amount of a compound of Formula (I), IA, or IB, wherein said amount is effective to inhibit inflammation. The invention also provides methods for inhibiting chemotaxis of leukocytes.

3. 发明申请

WO2007056217A3 DRUG-ELUTING STENTS COATED WITH NON-NUCLEOTIDE P2Y12 RECEPTOR ANTAGONIST COMPOUND 审中-公开
公开(公告)号：WO2007056217A3
公开(公告)日：2007-05-18
申请号：PCT/US2006/043089
申请日：2006-11-02
申请人： INSPIRE PHARMACEUTICALS, INC. , BOYER, José L. , DOUGLASS, James G., III , SHAVER, Sammy R.
发明人： BOYER, José L. , DOUGLASS, James G., III , SHAVER, Sammy R.
IPC分类号： C07H19/20
摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The present invention also provides a drug-eluting stent, wherein the stent is coated with one or more non-mucleotide P2Y 12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged blood vessel, a therapeutically effective amount of the P2Y 12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y 12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting thrombus formation, inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.

4. 发明申请

WO2006121856B1 PYRIMIDINE-BASED NON-NUCLEOTIDE COMPOSITION AND METHOD FOR INHIBITING PLATELET AGGREGATION 审中-公开
标题翻译：基于PYRIMININE的非核苷酸组合物和抑制血小板聚集的方法
公开(公告)号：WO2006121856B1
公开(公告)日：2007-03-22
申请号：PCT/US2006017407
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： A61K31/70 , A61K31/7068
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

WO2003072067A3 COMPOSITIONS AND METHODS FOR TREATING EPITHELIAL AND RETINAL TISSUE DISEASES 审中-公开
公开(公告)号：WO2003072067A3
公开(公告)日：2003-09-04
申请号：PCT/US2003/006691
申请日：2003-02-27
申请人： INSPIRE PHARMACEUTICALS, INC. , YERXA, Benjamin, R. , DOUGLASS, James, G. III , SHAVER, Sammy, Ray , PETERSON, Ward, M. , BROWN, Edward, G. , CREAN, Christopher, S.
发明人： YERXA, Benjamin, R. , DOUGLASS, James, G. III , SHAVER, Sammy, Ray , PETERSON, Ward, M. , BROWN, Edward, G. , CREAN, Christopher, S.
IPC分类号： A61K31/70
摘要： The present invention relates to mononucleoside phosphate compoundsthat have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified byattaching a degradation resistant substituent on the terminal phosphate of apolyphosphate mononucleotide. By attaching this degradation resistant substituent,the stability from degradation matches or exceeds those of certain dinucleotides.

6. 发明申请

WO2007056213A3 DRUG-ELUTING STENTS COATED WITH P2Y12 RECEPTOR ANTAGONIST COMPOUND 审中-公开
标题翻译：用P2Y12受体拮抗剂化合物包衣的药物给药
公开(公告)号：WO2007056213A3
公开(公告)日：2009-04-30
申请号：PCT/US2006043085
申请日：2006-11-02
申请人： INSPIRE PHARMACEUTICALS INC , UNIV NORTH CAROLINA , BOYER JOSE L , DOUGLASS JAMES G III , SHAVER SAMMY R
发明人： BOYER JOSE L , DOUGLASS JAMES G III , SHAVER SAMMY R
IPC分类号： A61K31/70 , A61K31/7072 , A61K31/7084 , C07H19/04 , C07H19/10 , C07H19/20 , C07H19/207 , C07H21/00
CPC分类号： C07H19/04 , A61K31/675 , A61K31/7072 , A61K31/7076 , A61K31/7084 , C07H19/10 , C07H19/20 , C07H19/207 , C07H21/00
摘要： The present invention provides a P2Y12 receptor antagonist compound-eluting stent, wherein the stent is coated with one or more P2Y12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Y12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting thrombus formation, inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.
摘要翻译：本发明提供P2Y12受体拮抗剂化合物洗脱支架，其中支架涂覆有一种或多种P2Y12受体拮抗剂化合物或其药学上可接受的盐，溶剂合物或水合物。当支架置于狭窄或损伤的动脉血管中时，将治疗有效量的P2Y12受体拮抗剂化合物从支架连续洗脱至支架的局部环境。 P2Y12受体拮抗剂化合物洗脱支架可用于预防血栓形成和再狭窄，并且有效抑制血栓形成，抑制血管平滑肌细胞的收缩，抑制细胞增殖和减少炎症。

7. 发明申请

WO2007002945A3 P2Y6 RECEPTOR AGONISTS FOR TREATING LUNG DISEASES 审中-公开
标题翻译： P2Y6受体激素治疗肺疾病
公开(公告)号：WO2007002945A3
公开(公告)日：2007-03-29
申请号：PCT/US2006026010
申请日：2006-06-29
申请人： INSPIRE PHARMACEUTICALS INC , BOYER JOSE L , SHAVER SAMMY R , DOUGLASS JAMES G III , REDICK CATHERINE C
发明人： BOYER JOSE L , SHAVER SAMMY R , DOUGLASS JAMES G III , REDICK CATHERINE C
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： A61K31/7072 , A61K31/708 , A61K31/7084
摘要： This invention is directed to a method of enhancing or facilitating the clearance of the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y 6 receptor agonist compound, wherein said amount is effective to activate the P2Y 6 receptors on the luminal surface of lung epithelia. The P2Y 6 receptor agonist compounds useful for this invention include mononucleoside 5'-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula (I), or salts, solvates, hydrates thereof.
摘要翻译：本发明涉及一种增强或促进受试者中肺粘液分泌物清除的方法。本发明还涉及促进受试者中肺粘液分泌物水合的方法。本发明还涉及一种预防或治疗与人或其他哺乳动物的肺或气道功能受损有关的疾病或病症的方法。该方法包括向受试者施用包含治疗有效量的P2Y 6受体激动剂化合物的药物组合物，其中所述量有效激活管腔上的P2Y 6受体肺上皮表面。可用于本发明的P2Y 6受体激动剂化合物包括单核苷5'-二磷酸酯，二核苷单磷酸酯，二核苷二磷酸酯或通式（I）的二核苷三磷酸盐，或其盐，溶剂合物，水合物。

8. 发明申请

WO1996038138A1 NOVEL TAXOIDS 审中-公开
标题翻译：新的TAXOIDS
公开(公告)号：WO1996038138A1
公开(公告)日：1996-12-05
申请号：PCT/US1996008245
申请日：1996-05-31
申请人： BIOPHYSICA FOUNDATION , SOVAK, Milos , DOUGLASS, James, G. , BRESSI, Jerome, C. , SELIGSON, Allen
发明人： BIOPHYSICA FOUNDATION
IPC分类号： A61K31/335
CPC分类号： C07D305/14 , A61K47/54 , A61K47/545 , A61K47/548 , A61K47/554 , A61K47/58
摘要： Novel taxoids are provided having enhanced water solubility and/or improved pharmacological properties as compared to paclitaxel. The subject taxoids comprise a functional group attached to a paclitaxel at the C-2' and/or C-7 position by a linking group. Functional groups present in the subject taxoids may be hydrophilic chains, groups capable of in vivoconversion to hydrophilic chains, targeting moieties capable of specifically binding with cellular receptors and water soluble polymers of at least 5 kD. The subject taxoids find use in the treatment of hosts suffering from a cellular proliferative disease.
摘要翻译：提供与紫杉醇相比具有增强的水溶性和/或改善的药理学性质的新型紫杉烷。受试紫杉醇包含通过连接基团连接在C-2'和/或C-7位上的紫杉醇的官能团。存在于受试者紫杉烷中的官能团可以是亲水链，能够亲水性链转移的基团，能够与细胞受体特异性结合的靶向部分和至少5kD的水溶性聚合物。主要的紫杉醇可用于治疗患有细胞增殖性疾病的宿主。

9. 发明申请

WO2007124123A2 METHOD OF TREATING INFLAMMATION 审中-公开
标题翻译：治疗炎症的方法
公开(公告)号：WO2007124123A2
公开(公告)日：2007-11-01
申请号：PCT/US2007009773
申请日：2007-04-20
申请人： INSPIRE PHARMACEUTICALS INC , BRUBAKER KURT E , SHAVER SAMMY R , DOUGLASS JAMES G III
发明人： BRUBAKER KURT E , SHAVER SAMMY R , DOUGLASS JAMES G III
IPC分类号： A61K31/7076
CPC分类号： A61K31/7076
摘要： This invention provides methods of preventing and/or treating diseases or conditions associated with inflammation in a mammal, particularly a human. The method comprises administering to a mammal in need thereof an effective amount of a compound of Formula (I), IA, or IB, wherein said amount is effective to inhibit inflammation. The invention also provides methods for inhibiting chemotaxis of leukocytes.
摘要翻译：本发明提供了预防和/或治疗哺乳动物，特别是人的与炎症相关的疾病或病症的方法。该方法包括给予有需要的哺乳动物有效量的式（I），IA或IB化合物，其中所述量有效抑制炎症。本发明还提供了抑制白细胞趋化性的方法。

10. 发明申请

WO2007056217A2 DRUG-ELUTING STENTS COATED WITH NON-NUCLEOTIDE P2Y12 RECEPTOR ANTAGONIST COMPOUND 审中-公开
标题翻译：非核苷酸P2Y12受体拮抗剂化合物的药物治疗
公开(公告)号：WO2007056217A2
公开(公告)日：2007-05-18
申请号：PCT/US2006043089
申请日：2006-11-02
申请人： INSPIRE PHARMACEUTICALS INC , BOYER JOSE L , DOUGLASS JAMES G III , SHAVER SAMMY R
发明人： BOYER JOSE L , DOUGLASS JAMES G III , SHAVER SAMMY R
IPC分类号： A61K31/519 , A61F2/00 , A61K31/52
CPC分类号： A61K31/52 , A61F2/82 , A61F2250/0067 , A61K31/519
摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The present invention also provides a drug-eluting stent, wherein the stent is coated with one or more non-mucleotide P2Y 12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged blood vessel, a therapeutically effective amount of the P2Y 12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y 12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting thrombus formation, inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.
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。本发明还提供药物洗脱支架，其中支架涂覆有一种或多种非核苷酸P2Y 12受体拮抗剂化合物或其药学上可接受的盐，溶剂化物或水合物。当支架置于狭窄或损伤的血管中时，将治疗有效量的P2Y 12受体拮抗剂化合物从支架连续洗脱至支架的局部环境。 P2Y 12受体拮抗剂化合物洗脱支架可用于预防血栓形成和再狭窄，并且有效抑制血栓形成，抑制血管平滑肌细胞的收缩，抑制细胞增殖和减少炎症。

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