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1. 发明申请

WO0178706A9 TREATMENT OF HYPERPROLIFERATIVE, INFLAMMATORY AND RELATED MUCOCUTANEOUS DISORDERS USING INHIBITORS OF MEVALONATE SYNTHESIS AND METABOLISM 审中-公开
标题翻译：用茉莉酮酸合成和代谢抑制剂治疗过度增殖，炎性和相关性皮肤病
公开(公告)号：WO0178706A9
公开(公告)日：2002-12-27
申请号：PCT/US0112175
申请日：2001-04-12
申请人： CELLEGY PHARMA INC , PARKS THOMAS P , GRAYSON STEPHEN
发明人： PARKS THOMAS P , GRAYSON STEPHEN
IPC分类号： A61K9/00 , A61K31/015 , A61K31/045 , A61K31/047 , A61K31/19 , A61K31/22 , A61K31/235 , A61K31/366 , A61K31/40 , A61K31/4418 , A61K31/56 , A61K31/575 , A61K31/60 , A61K38/00 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/28 , A61K47/32 , A61K31/00 , A61K31/196 , A61K31/216 , A61K31/404 , A61P17/00 , A61P29/00
CPC分类号： A61K31/404 , A61K9/0014 , A61K9/0043 , A61K9/0073 , A61K31/015 , A61K31/045 , A61K31/047 , A61K31/19 , A61K31/22 , A61K31/235 , A61K31/366 , A61K31/40 , A61K31/4418 , A61K31/56 , A61K31/575 , A61K31/60 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/28 , A61K47/32 , A61K2300/00
摘要： The present invention provides methods for treating a variety of hyperproliferative and inflammatory mucocutaneous disorders, including, basal cell carcinoma, squamous cell carcinoma, psoriasis and atopic dermatitis, as well as skin irritation and disorders associated with skin aging and skin photodamage using inhibitors of cholesterol metabolism. The present invention further relates to the discovery that the combined use of several inhibitors of cholesterol metabolism produces synergistic effects. Furthermore, the present invention is directed to the use of inhibitors of cholesterol metabolism as excipients to enhance the effects of antiinflammatory drugs.
摘要翻译：本发明提供了使用胆固醇代谢抑制剂治疗多种过度增殖性和炎症性皮肤粘膜疾病，包括基底细胞癌，鳞状细胞癌，牛皮癣和特应性皮炎，以及与皮肤老化和皮肤光损伤有关的皮肤刺激和病症。本发明还涉及几种胆固醇代谢抑制剂的组合使用产生协同效应的发现。此外，本发明涉及使用胆固醇代谢抑制剂作为赋形剂来增强抗炎药的作用。

2. 发明申请

WO2002069906A2 COMPOUNDS AND METHODS FOR THE TREATMENT OF UROGENITAL DISORDERS 审中-公开
标题翻译：化合物和治疗溃疡性疾病的方法
公开(公告)号：WO2002069906A2
公开(公告)日：2002-09-12
申请号：PCT/US2002/007026
申请日：2002-03-06
申请人： CELLEGY PHARMACEUTICALS, INC. , MAK, Vivien, H., W. , GRAYSON, Stephen
发明人： MAK, Vivien, H., W. , GRAYSON, Stephen
IPC分类号： A61K
CPC分类号： A61K45/06 , A61K31/00 , A61K31/5513 , A61K31/554 , A61K31/56 , A61K38/446 , A61K38/4886 , A61K2300/00
摘要： The present invention provides methods for treating a variety of urogenital disorders, such as, for example, vaginismus, dyspareunia, vulvodynia (including vulvar vestibulitis), interstitial cystitis, nonspecific urethriris (i.e., nonspecific pain and/or burning of the urinary tract) and sexual dysfunctions, such as, for example, female sexual arousal disorders and female sexual orgasmic disorders, using a variety of compounds, including, but not limited to, NO donors, calcium channel blockers, cholinergic modulators, a-adrenergic receptor antagonists, b-adrenergic receptor agonists, phosphodiesterase inhibitors, cAMP-dependent protein kinase activators (e.g., cAMP mimetics), superoxide scavengers, potassium channel activators, estrogen-like compounds, testosterone-like compounds, benzodiazepines, adrenergic nerve inhibitors, antidiarrheal agents, HMG-CoA reductase inhibitors, smooth muscle relaxants, adenosine receptor modulators, adenylyl cyclase activators, endothelin receptor antagonists, bisphosphonates and cGMP-dependent protein kinase activators (e.g., cGMP mimetics).
摘要翻译：本发明提供了治疗各种泌尿生殖系统疾病的方法，例如阴道炎，性交疼痛，外阴（包括外阴前庭炎），间质性膀胱炎，非特异性尿道炎（即非特异性疼痛和/或尿道灼伤）和使用各种化合物，包括但不限于NO供体，钙通道阻断剂，胆碱能调节剂，α-肾上腺素能受体拮抗剂，β-肾上腺素能受体拮抗剂，β-肾上腺素能受体拮抗剂，肾上腺素能受体激动剂，磷酸二酯酶抑制剂，cAMP依赖性蛋白激酶激活剂（例如cAMP模拟物），超氧化物清除剂，钾通道激活剂，雌激素样化合物，睾酮样化合物，苯二氮卓类，肾上腺素能神经抑制剂，止泻药，HMG-CoA还原酶抑制剂，平滑肌松弛剂，腺苷受体调节剂，腺苷酸环化酶激活剂，内皮素受体拮抗剂一次性，双膦酸盐和cGMP依赖性蛋白激酶激活剂（例如，cGMP模拟物）。

3. 发明申请

WO1994021230A1 METHOD AND COMPOSITIONS FOR DISRUPTING THE EPITHELIAL BARRIER FUNCTION 审中-公开
标题翻译：用于破坏上行障碍物功能的方法和组合
公开(公告)号：WO1994021230A1
公开(公告)日：1994-09-29
申请号：PCT/US1994003030
申请日：1994-03-21
申请人： CELLEGY PHARMACEUTICALS, INC. , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , ELIAS, Peter, M. , THORNFELDT, Carl, R. , GRAYSON, Stephen
发明人： CELLEGY PHARMACEUTICALS, INC. , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
IPC分类号： A61K09/10
CPC分类号： A61K47/46 , A61K9/0014 , A61K47/183 , A61K47/22 , A61K47/26
摘要： A method for disrupting epithelial barrier function in a host in need of the topical administration of a physiologically active substance which comprises applying to the epithelium of the host, barrier-disrupting amount of at least one agent selected from the group consisting of an inhibitor of ceramide synthesis, inhibitor of acylceramide synthesis, inhibitor of glucosylceramide synthesis, and inhibitor of sphingomyelin synthesis, an inhibitor of fatty acid synthesis, an inhibitor of cholesterol synthesis, a degradation enzyme of ceramides, acylceramide, glucosylceramides, sphingomyelin, an inhibitor of phospholipid, glycosphingolipid, including glucosylceramide, acylceramide or sphingomyelin degradation, and both inhibitors and stimulators of metabolic enzymes of free fatty acids, ceramide, and cholesterol, as well as a topical composition useful therefor are disclosed.
摘要翻译：一种用于破坏需要局部施用生理活性物质的宿主中的上皮屏障功能的方法，其包括向所述宿主的上皮施用屏障破坏量的至少一种选自神经酰胺抑制剂的药剂合成抑制剂，糖基神经酰胺合成抑制剂，鞘磷脂合成抑制剂，脂肪酸合成抑制剂，胆固醇合成抑制剂，神经酰胺降解酶，酰基神经酰胺，葡糖基神经酰胺，鞘磷脂，磷脂抑制剂，鞘糖脂，包括葡萄糖神经酰胺，酰基神经酰胺或鞘磷脂降解，以及游离脂肪酸，神经酰胺和胆固醇的代谢酶的抑制剂和刺激剂以及其有用的局部组合物。

4. 发明申请

WO2002069906A3 COMPOUNDS AND METHODS FOR THE TREATMENT OF UROGENITAL DISORDERS 审中-公开
公开(公告)号：WO2002069906A3
公开(公告)日：2002-09-12
申请号：PCT/US2002/007026
申请日：2002-03-06
申请人： CELLEGY PHARMACEUTICALS, INC. , MAK, Vivien, H., W. , GRAYSON, Stephen
发明人： MAK, Vivien, H., W. , GRAYSON, Stephen
IPC分类号： A61K31/50
摘要： The present invention provides methods for treating a variety of urogenital disorders, such as, for example, vaginismus, dyspareunia, vulvodynia (including vulvar vestibulitis), interstitial cystitis, nonspecific urethriris (i.e., nonspecific pain and/or burning of the urinary tract) and sexual dysfunctions, such as, for example, female sexual arousal disorders and female sexual orgasmic disorders, using a variety of compounds, including, but not limited to, NO donors, calcium channel blockers, cholinergic modulators, a-adrenergic receptor antagonists, b-adrenergic receptor agonists, phosphodiesterase inhibitors, cAMP-dependent protein kinase activators (e.g., cAMP mimetics), superoxide scavengers, potassium channel activators, estrogen-like compounds, testosterone-like compounds, benzodiazepines, adrenergic nerve inhibitors, antidiarrheal agents, HMG-CoA reductase inhibitors, smooth muscle relaxants, adenosine receptor modulators, adenylyl cyclase activators, endothelin receptor antagonists, bisphosphonates and cGMP-dependent protein kinase activators (e.g., cGMP mimetics).

5. 发明申请

WO0178706A3 TREATMENT OF HYPERPROLIFERATIVE, INFLAMMATORY AND RELATED MUCOCUTANEOUS DISORDERS USING INHIBITORS OF MEVALONATE SYNTHESIS AND METABOLISM 审中-公开
标题翻译：使用抑制剂合成和代谢的治疗高血压，炎症和相关的神经系统疾病
公开(公告)号：WO0178706A3
公开(公告)日：2002-03-28
申请号：PCT/US0112175
申请日：2001-04-12
申请人： CELLEGY PHARMA INC , PARKS THOMAS P , GRAYSON STEPHEN
发明人： PARKS THOMAS P , GRAYSON STEPHEN
IPC分类号： A61K9/00 , A61K31/015 , A61K31/045 , A61K31/047 , A61K31/19 , A61K31/22 , A61K31/235 , A61K31/366 , A61K31/40 , A61K31/4418 , A61K31/56 , A61K31/575 , A61K31/60 , A61K38/00 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/28 , A61K47/32 , A61K31/00 , A61K31/196 , A61K31/216 , A61K31/404 , A61P17/00 , A61P29/00
CPC分类号： A61K31/404 , A61K9/0014 , A61K9/0043 , A61K9/0073 , A61K31/015 , A61K31/045 , A61K31/047 , A61K31/19 , A61K31/22 , A61K31/235 , A61K31/366 , A61K31/40 , A61K31/4418 , A61K31/56 , A61K31/575 , A61K31/60 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/28 , A61K47/32 , A61K2300/00
摘要： The present invention provides methods for treating a variety of hyperproliferative and inflammatory mucocutaneous disorders, including, basal cell carcinoma, squamous cell carcinoma, psoriasis and atopic dermatitis, as well as skin irritation and disorders associated with skin aging and skin photodamage using inhibitors of cholesterol metabolism. The present invention further relates to the discovery that the combined use of several inhibitors of cholesterol metabolism produces synergistic effects. Furthermore, the present invention is directed to the use of inhibitors of cholesterol metabolism as excipients to enhance the effects of antiinflammatory drugs.
摘要翻译：本发明提供了使用胆固醇代谢抑制剂治疗各种过度增生和炎症性皮肤病的方法，包括基底细胞癌，鳞状细胞癌，牛皮癣和特应性皮炎，以及与皮肤老化和皮肤光损伤相关的皮肤刺激和疾病。本发明进一步涉及到几种胆固醇代谢抑制剂的组合使用产生协同效应的发现。此外，本发明涉及使用胆固醇代谢抑制剂作为赋形剂来增强抗炎药物的作用。

6. 发明申请

WO2003075851A3 COMPOSITIONS AND METHODS FOR THE TREATMENT OF ANORECTAL DISORDERS 审中-公开
公开(公告)号：WO2003075851A3
公开(公告)日：2003-09-18
申请号：PCT/US2003/007106
申请日：2003-03-05
申请人： CELLEGY PHARMACEUTICALS, INC. , PARKS, Thomas, P. , MAK, Vivien, H., W. , LEE, Jung-Chung , LEE, Charles , GRAYSON, Stephen
发明人： PARKS, Thomas, P. , MAK, Vivien, H., W. , LEE, Jung-Chung , LEE, Charles , GRAYSON, Stephen
IPC分类号： A61K31/35 , A61K31/56 , A61K31/165
摘要： Compositions and methods for the treatment of patients with anorectal disorders including colostomy are provided in which certain compounds including, but not limited to, NO donors, calcium channel blockers, cholinergic modulators (including acetylcholine storage blocking agents and acetylcholine vesicle storage blocking agents), α-adrenergic receptor antagonists (including α 1 -adrenergic antagonists and α 2 -adrenergic antagonists), β-adrenergic receptor agonists (including β 2 -adrenergic antagonists and β 3 -adrenergic antagonists), phosphodiesterase inhibitors, cAMP-dependent protein kinase activators (e.g., cAMP mimetics), superoxide scavengers, potassium channel activators (including ATP-sensitive potassium channel activators and activators of the Maxi-K channels), estrogen-like compounds, testosterone-like compounds, benzodiazepines, adrenergic nerve inhibitors, antidiarrheal agents, HMG-CoA reductase inhibitors, smooth muscle relaxants, adenosine receptor modulators, adenylyl cyclase activators, endothelin receptor antagonists, bisphosphonates, cGMP-dependent protein kinase activators (e.g., cGMP mimetics), and combinations thereof are used.

7. 发明申请

WO2003075851A2 COMPOSITIONS AND METHODS FOR THE TREATMENT OF ANORECTAL DISORDERS 审中-公开
标题翻译：用于治疗异位性疾病的组合物和方法
公开(公告)号：WO2003075851A2
公开(公告)日：2003-09-18
申请号：PCT/US2003/007106
申请日：2003-03-05
申请人： CELLEGY PHARMACEUTICALS, INC. , PARKS, Thomas, P. , MAK, Vivien, H., W. , LEE, Jung-Chung , LEE, Charles , GRAYSON, Stephen
发明人： PARKS, Thomas, P. , MAK, Vivien, H., W. , LEE, Jung-Chung , LEE, Charles , GRAYSON, Stephen
IPC分类号： A61K
CPC分类号： A61K31/00
摘要： Compositions and methods for the treatment of patients with anorectal disorders including colostomy are provided in which certain compounds including, but not limited to, NO donors, calcium channel blockers, cholinergic modulators (including acetylcholine storage blocking agents and acetylcholine vesicle storage blocking agents), $g(a)-adrenergic receptor antagonists (including $g(a)¿1?-adrenergic antagonists and $g(a)¿2?-adrenergic antagonists), $g(b)-adrenergic receptor agonists (including $g(b)¿2?-adrenergic antagonists and $g(b)¿3?-adrenergic antagonists), phosphodiesterase inhibitors, cAMP-dependent protein kinase activators (e.g., cAMP mimetics), superoxide scavengers, potassium channel activators (including ATP-sensitive potassium channel activators and activators of the Maxi-K channels), estrogen-like compounds, testosterone-like compounds, benzodiazepines, adrenergic nerve inhibitors, antidiarrheal agents, HMG-CoA reductase inhibitors, smooth muscle relaxants, adenosine receptor modulators, adenylyl cyclase activators, endothelin receptor antagonists, bisphosphonates, cGMP-dependent protein kinase activators (e.g., cGMP mimetics), and combinations thereof are used.
摘要翻译：提供了用于治疗包括结肠造口术在内的肛门直肠疾病患者的组合物和方法，其中某些化合物包括但不限于NO供体，钙通道阻断剂，胆碱能调节剂（包括乙酰胆碱储存阻断剂和乙酰胆碱泡囊阻滞剂），$ g（a） - 肾上腺素受体拮抗剂（包括$ g（a）1 - 肾上腺素能拮抗剂和$ g（a）2'-肾上腺素能拮抗剂），$ g（b） - 肾上腺素能受体激动剂（包括$ g ）2'-肾上腺素能拮抗剂和$ g（b）3'-肾上腺素能拮抗剂），磷酸二酯酶抑制剂，cAMP依赖性蛋白激酶激活剂（例如cAMP模拟物），超氧化物清除剂，钾通道激活剂（包括ATP敏感钾通道 Maxi-K通道的激活剂和激活剂），雌激素样化合物，睾酮样化合物，苯并二氮杂，肾上腺素能神经抑制剂，止泻药，HMG-CoA还原酶抑制剂，平滑肌松弛剂，腺苷受体调节剂，腺苷酸环化酶激活剂，内皮素受体拮抗剂，双膦酸盐，cGMP依赖性蛋白激酶激活剂（例如，cGMP模拟物）及其组合。

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