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91. 发明申请

WO2003011301A1 AS-NEEDED ADMINISTRATION OF AN ANDROGENIC AGENT TO ENHANCE FEMALE SEXUAL DESIRE AND RESPONSIVENESS 审中-公开
标题翻译：自发性促进安哥拉代理增强女性性欲和反应性
公开(公告)号：WO2003011301A1
公开(公告)日：2003-02-13
申请号：PCT/US2002/023847
申请日：2002-07-26
申请人： VIVUS, INC.
发明人： WILSON, Leland, F. , TAM, Peter, Y.
IPC分类号： A61K31/56
CPC分类号： A61K9/0034 , A61K9/02 , A61K31/00 , A61K31/15 , A61K31/21 , A61K31/295 , A61K31/48 , A61K31/5377 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61K31/56 , A61K45/06 , B82Y5/00 , A61K2300/00
摘要： A method is provided for enhancing a female individual's sexual desire and responsiveness. The method involves administration of a pharmaceutical formulation containing an effective amount of an androgenic agent, wherein administration is on an as needed basis rather than involving chronic pharmacotherapy. Local delivery may be accomplished via administration to the vagina, vulvar area or urethra of the individual, although oral administration is preferred for those androgenic agents that are orally active. Formulations and kits for carrying out the method are provided as well.
摘要翻译：提供了一种提高女性性欲和反应能力的方法。该方法包括给药含有有效量的雄激素药物的药物制剂，其中根据需要施用，而不是涉及慢性药物治疗。尽管对于那些口服有活性的那些雄激素剂，口服给药是优选的，但是可以通过给予个体的阴道，外阴区域或尿道来实现局部递送。还提供了用于实施该方法的制剂和试剂盒。

92. 发明申请

WO03011299A2 METHOD AND COMPOSITION FOR TREATMENT OF OCULAR HYPERTENSION AND GLAUCOMA 审中-公开
标题翻译：治疗高血压和糖尿病的方法和组合
公开(公告)号：WO03011299A2
公开(公告)日：2003-02-13
申请号：PCT/JP0207699
申请日：2002-07-30
申请人： SUCAMPO AG , UENO RYUJI
发明人： UENO RYUJI
IPC分类号： A61K31/557 , A61K31/5575 , A61P27/06
CPC分类号： A61K31/557 , A61K31/5575
摘要： The instant invention discloses a method for treatment of ocular hypertension and glaucoma, which comprises administrating topically to the eyes of a mammalian subject in need of such treatment more than 5 micrograms and less than 50 micrograms per eye per administration of 15-keto-prostaglandin compound having a ring structure at the end of the omega chain. The treatment of the present invention causes substantially no or reduced ophthalmic irritating side effect even in such a high dose.
摘要翻译：本发明公开了一种治疗高眼压症和青光眼的方法，该方法包括对需要这种治疗的哺乳动物受试者的局部施用超过5微克并且每次施用15-酮前列腺素化合物小于50微克在ω链的末端具有环结构。本发明的治疗即使在高剂量下也引起基本上没有或减少的眼睛刺激性副作用。

93. 发明申请

WO2002089812A1 COMPOSITION FOR TREATING DRUG-INDUCED CONSTIPATION WITH 15-KETO-PROSTAGLANDINS 审中-公开
标题翻译：用15-KETO-PROSTAGLANDIN治疗药物诱导的组合物的组合物
公开(公告)号：WO2002089812A1
公开(公告)日：2002-11-14
申请号：PCT/JP2002/004223
申请日：2002-04-26
申请人： SUCAMPO AG , UENO, Ryuji
发明人： UENO, Ryuji
IPC分类号： A61K31/557
CPC分类号： A61K31/557 , A61K31/485 , A61K31/5575 , A61K2300/00
摘要： Provided is a composition for treatment of drug-induced constipation comprising a 15-keto-prostaglandin compound as an active ingredient. The composition of the present invention has a strong antagonistic action against drug-induced constipation without substantially losing the main effect of the drug.
摘要翻译：本发明提供用于治疗药物性便秘的组合物，其包含作为活性成分的15-酮 - 前列腺素化合物。本发明的组合物对药物引起的便秘具有强烈的拮抗作用，而基本上不会丧失药物的主要作用。

94. 发明申请

WO2002066030A1 ジクロフェナクとオルノプロスチルからなる医薬組成物审中-公开
标题翻译：包含DICLOFENAC和ORNOPROSTIL的药物组合物
公开(公告)号：WO2002066030A1
公开(公告)日：2002-08-29
申请号：PCT/JP2002/001474
申请日：2002-02-20
申请人：小野薬品工業株式会社 , 酒井芳紀 , 勝部伸夫 , 西浦昭雄
发明人：酒井芳紀 , 勝部伸夫 , 西浦昭雄
IPC分类号： A61K31/196
CPC分类号： A61K45/06 , A61K31/196 , A61K31/5575 , A61K2300/00
摘要： Medicinal compositions containing diclofenac or its nontoxic salt and ornoprostil. Compared with commercially available diclofenac tablets and Arthlotec tablets, the above compositions comprising a combination of diclofenac with ornoprostil are expected as exerting a quick effect with little side effects (in particular, digestive ulcer, diarrhea/vomiting and renal failure) and having excellent antipyretic, analgesic and antiinflammatory effects.
摘要翻译：药用组合物含有双氯芬酸或其无毒盐和奥古斯丁。与市售的双氯芬酸片剂和阿曲坦片相比，上述包含双氯芬酸与奥罗前列素组合的组合物预期具有副作用（特别是消化性溃疡，腹泻/呕吐和肾衰竭）的快速作用，并且具有优异的解热，镇痛和抗炎作用。

95. 发明申请

WO0105388A3 USE OF A FATTY DERIVATIVE FOR THE TREATMENT OF EXTERNAL SECRETIONDISORDERS 审中-公开
标题翻译：使用脂肪衍生物治疗外部分泌物
公开(公告)号：WO0105388A3
公开(公告)日：2002-05-10
申请号：PCT/JP0004696
申请日：2000-07-13
申请人： SUCAMPO AG
发明人： UENO RYUJI
IPC分类号： A61K45/00 , A61K9/00 , A61K31/20 , A61K31/201 , A61K31/202 , A61K31/557 , A61K31/5575 , A61K31/558 , A61K31/5585 , A61K49/00 , A61P1/00 , A61P1/02 , A61P9/08 , A61P27/02 , A61P43/00
CPC分类号： A61K31/5575 , A61K9/0048 , A61K9/0056 , A61K31/20 , A61K31/201 , A61K31/202 , A61K31/557 , A61K31/558 , A61K31/5585 , A61K49/0008
摘要： Disclosed is a composition for treatment of external secretion disorders comprising, as an active ingredient a fatty acid derivative. The composition of the present invention is useful for treatment of at least one condition selected from hypolacrimation including disorder of basal tear secretion, dry-eye syndrome, hyposalivation and dry-mouth syndrome.
摘要翻译：公开了用于治疗外分泌障碍的组合物，其包含作为活性成分的脂肪酸衍生物。本发明的组合物可用于治疗选自以下的至少一种病症：包括基底泪液分泌紊乱，干眼综合征，低渗激素和口干mouth症的失调。

96. 发明申请

WO02024639A1 CYCLOPENTANE DERIVATIVES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：作为治疗剂的环戊烯衍生物
公开(公告)号：WO02024639A1
公开(公告)日：2002-03-28
申请号：PCT/US2001/016770
申请日：2001-05-23
IPC分类号： C07D333/16 , A61K31/5575 , A61K31/558 , A61K31/559 , A61P1/00 , A61P9/12 , A61P13/10 , A61P13/12 , A61P15/00 , A61P19/08 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/02 , C07C35/06 , C07C69/78 , C07C405/00 , C07D333/28 , A61K31/557
CPC分类号： C07D333/28 , A61K31/5575 , C07C405/0016
摘要： The present invention provides a novel compound represented by the general formula (I); wherein R is H or COR ; R is H, R , phenyl, or COR , wherein R is C1-C5 lower alkyl and R is R or phenyl; Z is CH2 or O; Y is OH, OCOR or =O; x is 0 or 1; and X is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl or substituted derivatives thereof, wherein the substituents maybe selected from the goup consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR 2, CO2R and OR wherein R is hydrogen or C1-C5 alkyl and dotted lines represent the presence or absence of a double bond and wavy lines represent a cis or trans bond. These novel compounds are especially useful for treating elevated intraocular pressure (ocular hypertension) and glaucoma.
摘要翻译：本发明提供由通式（I）表示的新化合物。其中R是H或COR 3; R 1是H，R 2，苯基或COR 3，其中R 2是C 1 -C 5低级烷基，R 3是R 2或苯基; Z是CH 2或O; Y是OH，OCOR 3或= O; x为0或1; X是C 1 -C 5正烷基，C 3 -C 7环烷基，苯基，呋喃基，噻吩基或取代的衍生物，其中取代基可以选自C1-C5烷基，卤素，CF3，CN，NO2， 4> 2，CO 2 R 4和OR 4，其中R 4是氢或C 1 -C 5烷基，虚线代表双键的存在或不存在，波浪线代表顺式或反式键。这些新型化合物特别适用于治疗高眼压（眼高压）和青光眼。

97. 发明申请

WO02020007A1 CATHARTIC COMPOSITION 审中-公开
标题翻译： CATHARTIC组合物
公开(公告)号：WO02020007A1
公开(公告)日：2002-03-14
申请号：PCT/JP2001/007628
申请日：2001-09-04
IPC分类号： C07D311/94 , A61K31/23 , A61K31/335 , A61K31/35 , A61K31/352 , A61K31/4741 , A61K31/557 , A61K31/5575 , A61K31/558 , A61P1/10
CPC分类号： C07C405/00 , A61K31/335 , A61K31/35 , A61K31/352 , A61K31/4741 , A61K31/557 , A61K31/5575 , A61K31/559 , C07D221/04 , C07D335/04 , Y10S514/892 , A61K2300/00
摘要： An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1 : 1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
摘要翻译：本发明的目的是提供一种含有卤代双环化合物作为活性成分的抗 - 便秘组合物，其双环/单环结构比至少为1:1。环状化合物由式（I）表示：其中X1和X2优选为氟原子。该组合物可用于治疗便秘，无明显副作用，如胃痛。

98. 发明申请

WO0174313A3 COMPOSITIONS AND METHODS FOR TREATING HAIR LOSS USING C16 - C20 AROMATIC TETRAHYDRO PROSTAGLANDINS 审中-公开
标题翻译：使用C16 - C20芳族四氢叶酸治疗头发损失的组合物和方法
公开(公告)号：WO0174313A3
公开(公告)日：2002-02-21
申请号：PCT/US0110368
申请日：2001-03-30
申请人： PROCTER & GAMBLE
发明人： DELONG MITCHELL ANTHONY , MCIVER JOHN MCMILLAN , YOUNGQUIST ROBERT SCOTT
IPC分类号： A61K47/02 , A61K8/00 , A61K8/11 , A61K8/31 , A61K8/34 , A61K8/365 , A61K8/37 , A61K8/40 , A61K8/46 , A61K8/49 , A61K8/97 , A61K31/5575 , A61K45/00 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/16 , A61K47/22 , A61K47/46 , A61P17/14 , A61P43/00 , A61Q1/00 , A61Q1/10 , A61Q5/00 , A61Q5/02 , A61Q7/00 , C07C405/00 , A61K7/06 , A61K31/557
CPC分类号： A61Q7/00 , A61K8/365 , A61K8/46 , A61K31/5575
摘要： A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
摘要翻译：用于治疗哺乳动物脱发的方法使用含有前列腺素F类似物的组合物。组合物可以局部施用于皮肤。组合物可以阻止脱发，逆转脱发，并促进毛发生长。

99. 发明申请

WO02007731A2 COMPOSITION FOR TREATMENT OF OCULAR HYPERTENSION AND GLAUCOMA 审中-公开
标题翻译：用于治疗高血压和糖尿病的组合物
公开(公告)号：WO02007731A2
公开(公告)日：2002-01-31
申请号：PCT/JP2001/006211
申请日：2001-07-18
IPC分类号： A61K31/5575 , A61P27/02 , A61P27/06 , A61K31/557
CPC分类号： A61K31/5575
摘要： 15-keto prostaglandin compounds containing a ring structure at the end of the omega chain are used as ocular applied intraocular pressure reducing agents. They are applied in a dose below the known dose for the corresponding 15-OH compound.
摘要翻译：使用在ω链末端含有环结构的15-酮前列腺素化合物作为眼睛施用的眼压降低剂。它们以低于相应的15-OH化合物的已知剂量的剂量施用。

100. 发明申请

WO0134138B1 COMPOSITIONS AND METHODS FOR TREATMENT OF NEUROLOGICAL DISORDERS AND NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于治疗神经疾病和神经退行性疾病的组合物和方法
公开(公告)号：WO0134138B1
公开(公告)日：2001-12-06
申请号：PCT/US0030663
申请日：2000-11-08
申请人： MASSACHUSETTS INST TECHNOLOGY
发明人： LEE ROBERT K K , WURTMAN RICHARD J
IPC分类号： A61K45/00 , A61K31/00 , A61K31/05 , A61K31/137 , A61K31/18 , A61K31/198 , A61K31/34 , A61K31/365 , A61K31/436 , A61K31/465 , A61K31/5383 , A61K31/5575 , A61K38/13 , A61K38/19 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/28 , A61P29/00 , A61P37/02 , A61P43/00 , A61K31/66
CPC分类号： A61K31/00 , A61K31/05 , A61K31/137 , A61K31/18 , A61K31/198 , A61K31/34 , A61K31/365 , A61K31/436 , A61K31/465 , A61K31/5383 , A61K31/5575 , A61K31/7076 , A61K38/13 , A61K38/193
摘要： It has been discovered that the stimulation of beta -adrenergic receptors, which activate cAMP formation, gives rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising beta -adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by beta -adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E2 (PG E2), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of beta -adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E2, or forskolin is inhibited by immunosuppressants, immunophilin ligands, or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.
摘要翻译：已经发现刺激cAMP形成的β-肾上腺素能受体的刺激引起星形胶质细胞中APP和GFAP合成的增加。因此，将神经元细胞体外或体内暴露于包含β-肾上腺素受体配体或激动剂（包括例如去甲肾上腺素，异丙肾上腺素等）的某些组合物 APP mRNA转录和随后的APP过量产生。这些增加被β-肾上腺素能受体拮抗剂如普萘洛尔所阻断。这些细胞用8Br-cAMP，前列腺素E2（PG E2），毛喉素和酒石酸二酒石酸盐进行的体外或体内治疗也增加了APP合成，包括增加 mRNA和全蛋白水平，以及胶质纤维酸性蛋白（GFAP）表达的增加。公开了调节APP过表达和通过cAMP信号传导或β-肾上腺素能受体的激活介导反应性星形胶质化的组合物和方法。进一步发现，由8Br-cAMP，PG E2或毛喉素引起的APP合成的增加被免疫抑制剂，亲免素配体或抗炎剂如环孢菌素A和FK-506（他克莫司）所抑制，如以及离子通道调节剂，包括离子螯合剂如EGTA，或钙/钙调蛋白激酶抑制剂如KN93。本发明在减轻，治疗或预防包括阿尔茨海默氏病的神经病症和神经退行性疾病方面具有广泛的意义。

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