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131. 发明申请

WO0053168A3 SYNERGY BETWEEN LOW MOLECULAR WEIGHT HEPARIN AND PLATELET AGGREGATION INHIBITORS, FOR PREVENTING AND TREATING THROMBOEMBOLIC DISORDERS 审中-公开
标题翻译：低分子量肝素与血小板聚集抑制剂之间的协同作用，用于预防和治疗血栓性疾病
公开(公告)号：WO0053168A3
公开(公告)日：2002-01-24
申请号：PCT/US0006452
申请日：2000-03-10
申请人： DU PONT PHARM CO
发明人： WONG PANCRAS C , MOUSA SHAKER A
IPC分类号： C07D261/10 , A61K31/222 , A61K31/4015 , A61K31/402 , A61K31/42 , A61K31/422 , A61K31/445 , A61K31/4465 , A61K31/60 , A61K31/616 , A61K31/715 , A61K31/727 , A61K38/00 , A61K38/46 , A61K39/395 , A61K45/00 , A61K45/06 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , C07K16/28 , A61K31/175
CPC分类号： A61K31/727 , A61K31/42 , A61K31/60 , A61K31/715 , A61K39/39541 , A61K45/06 , A61K2039/505 , C07K16/2848 , A61K2300/00
摘要： This invention is directed to a combination therapy comprising the administration of a low molecular weight heparin such as tinzaparin and a platelet GPIIb/IIIa antagonist such as roxifiban for treating, preventing and reducing the risk of thromboembolic disorders.
摘要翻译：本发明涉及包括施用低分子量肝素如锡扎肝素和血小板GPIIb / IIIa拮抗剂如罗西非班的组合疗法，用于治疗，预防和降低血栓栓塞障碍的风险。

132. 发明申请

WO01005404A1 USE OF BETA-NAPTHOQUINONE FOR MAKING MEDICINES HAVING AN INHIBITING EFFECT ON THE RELEASE OF GLUTAMATE BY THE BRAIN 审中-公开
标题翻译：用于制造具有抑制作用的药物用于脑部释放谷氨酸的药物
公开(公告)号：WO01005404A1
公开(公告)日：2001-01-25
申请号：PCT/FR2000/002120
申请日：2000-07-21
IPC分类号： C07H15/203 , A61K31/15 , A61K31/16 , A61K31/175 , A61K31/70 , A61K31/704 , A61P9/10 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P43/00
CPC分类号： A61K31/12 , A61K31/175 , A61K31/70
摘要： The invention concerns the use of beta-naphthoquinone for making medicines with an inhibiting effect on the release of glutamate by the brain, said compounds corresponding to formula (I) wherein: R represents a -NH-CO-NH2, -NH-CO-CH3, or -OH group, glucuronide derivatives corresponding to formula (II) and their pharmaceutically acceptable additive salts with acids. The invention is applicable to neurological diseases.
摘要翻译：本发明涉及β-萘醌用于制备对脑的谷氨酸盐释放具有抑制作用的药物的用途，所述化合物对应于式（I），其中：R表示-NH-CO-NH 2，-NH-CO- CH3或-OH基团，对应于式（II）的葡糖苷酸衍生物及其与酸的药学上可接受的添加剂盐。本发明适用于神经系统疾病。

133. 发明申请

WO0038668A3 USE OF A NITROSOUREA DERIVATIVE FOR PREVENTION OR TREATMENT OF ACUTE ALLOGRAFT REJECTION 审中-公开
标题翻译：使用NITROSOUREA衍生物预防或治疗急性乙型肝炎病毒
公开(公告)号：WO0038668A3
公开(公告)日：2000-12-07
申请号：PCT/US9930985
申请日：1999-12-28
申请人： SOUTHERN RES INST , BLATTER HERBERT M , KAHN DONALD R , PIPER JAMES R , SECRIST JOHN A III , STRUCK ROBERT F , TEMPLE CARROLL
发明人： BLATTER HERBERT M , KAHN DONALD R , PIPER JAMES R , SECRIST JOHN A III , STRUCK ROBERT F , TEMPLE CARROLL
IPC分类号： A61K31/175 , A61K31/45 , A61K31/17 , A61K31/445 , A61K31/4468 , A61P37/06
CPC分类号： A61K31/175 , A61K31/45 , Y10S514/885
摘要： A method for treating an organ donor prior to harvesting organ to reduce graft rejection in a recipient. An amount effective to reduce graft rejection of at least one compound selected from the group consisting of compounds having formulae (I), (II), (III), (IV), (V), (VI), and (VII) is administered to the organ donor, wherein Y is (a); X is F or Cl; R1 is a straight or branched alkyl group having from 1 to 7 carbon atoms; R2 is a straight or branched alkyl group having from 1 to 7 carbon atoms; R3 is H or a straight or branched alkyl group having from 1 to 7 carbon atoms; Z is H, OH, or a straight or branched alkyl group including from 1 to 7 carbon atoms; and in Formula (II), the OH groups may be substituted anywhere except where Y is present and are not on the same carbon atom; in Formula (III), the OH group may be substituted anywhere except where Y is present; in Formula (IV), the OH group may be substituted anywhere except where Y is present; in Formula (V), Z may be substituted anywhere except at C-1, C-6, and C-4 if Z is OH; in Formula (VI), Z may be substituted anywhere except at C-1, C-3, and C-5 if Z is OH; and in Formula (VII), Z may be at C-1, C-2, and C-3 except not on C-1 if Z is OH.
摘要翻译：在收获器官之前处理器官供体以减少受体中的移植物排斥的方法。降低至少一种选自具有式（I），（II），（III），（IV），（V），（VI）和（VII）的化合物的化合物的移植排斥反应的量）给予器官供体，其中Y为（a）; X是F或Cl; R1是具有1至7个碳原子的直链或支链烷基; R2是具有1至7个碳原子的直链或支链烷基; R3是H或具有1至7个碳原子的直链或支链烷基; Z是H，OH或包含1至7个碳原子的直链或支链烷基; 在式（II）中，除了存在Y并且不在相同碳原子上之外，OH基团可以被取代; 在式（III）中，除了存在Y之外，OH基团可以被取代; 在式（IV）中，除了存在Y之外，OH基团可以被取代; 在式（Ⅴ）中，如果Z是OH，则Z可以在C-1，C-6和C-4之外的任何地方被取代; 在式（VI）中，Z可以在C 1，C 3和C 5上的任何地方被取代，如果Z是OH; 并且在式（VII）中，Z可以是C-1，C-2和C-3，但如果Z是OH，则不在C-1上。

134. 发明申请

WO9853839A3 ANTI-CANCER PRODUCTS FOR TREATING CYSTIC FIBROSIS 审中-公开
标题翻译：用于治疗CYSTIC FIBROSIS的抗癌产品
公开(公告)号：WO9853839A3
公开(公告)日：1999-09-10
申请号：PCT/FR9801074
申请日：1998-05-28
申请人： CENTRE NAT RECH SCIENT , STOVEN VERONIQUE , LENOIR GERARD , LALLEMAND JEAN YVES , ANNEREAU JEAN PHILIPPE , BARTHE JOEL , BLANQUET SYLVAIN
发明人： STOVEN VERONIQUE , LENOIR GERARD , LALLEMAND JEAN-YVES , ANNEREAU JEAN-PHILIPPE , BARTHE JOEL , BLANQUET SYLVAIN
IPC分类号： A61K45/00 , A61K31/00 , A61K31/131 , A61K31/15 , A61K31/165 , A61K31/175 , A61K31/255 , A61K31/282 , A61K31/36 , A61K31/439 , A61K31/475 , A61K31/66 , A61K31/664 , A61K31/675 , A61K31/70 , A61K31/704 , A61K31/7052 , A61K38/00 , A61P11/00 , A61P35/00 , C07K14/47 , G01N21/64
CPC分类号： A61K31/00 , A61K31/165 , A61K31/198 , A61K31/475 , A61K31/675 , A61K31/704 , A61K45/06 , A61K2300/00
摘要： The invention concerns a novel approach for treating cystic fibrosis using, in particular, anti-cancer chemotherapy. For the treatment of cystic fibrosis it proposes the use of at least one product which when administered to a patient brings about the expression or overexpression of an ABC carrier compound, in particular glutathione carrier. Preferably, the products used are anti-cancer products whose administration brings about the expression of MRP and/or MDR protein. The invention is also applicable to the treatment of rheumatoid polyarthritis or asthma. More specifically, the compounds are selected among cyclophosphamide, aclarubicin, doxorubicin, daunorubicin, epirubicin, idarubicin, zorubicin, pirabucin, colchicine, videsine, vinorelbine, vincristine, binblastine, azithromycin, erythromycin, ifosmamide, N-acetyl cysteine, N-acetyl lysine and/or a CFTR protein fragment comprising the NBF1 domain.
摘要翻译：本发明涉及使用特别是抗癌化学疗法治疗囊性纤维化的新方法。对于囊性纤维化的治疗，它提出使用至少一种产品，其在给予患者时引起ABC载体化合物，特别是谷胱甘肽载体的表达或过表达。优选地，所用的产品是抗癌产品，其给药引起MRP和/或MDR蛋白的表达。本发明也适用于治疗类风湿关节炎或哮喘。更具体地说，这些化合物选自环磷酰胺，阿柔比星，多柔比星，柔红霉素，表柔比星，伊达比星，阿维菌素，比拉布丁，秋水仙碱，维他星，长春瑞滨，长春新碱，倍贝星，阿奇霉素，红霉素，异环酰胺，N-乙酰半胱氨酸，N-乙酰赖氨酸和 /或包含NBF1结构域的CFTR蛋白片段。

135. 发明申请

WO98058658A1 THERAPEUTIC METHOD FOR MANAGEMENT OF DIABETES MELLITUS 审中-公开
标题翻译：用于治疗糖尿病的治疗方法
公开(公告)号：WO98058658A1
公开(公告)日：1998-12-30
申请号：PCT/US1998/006927
申请日：1998-04-08
IPC分类号： A61K45/00 , A61K31/155 , A61K31/175 , A61K31/426 , A61K31/65 , A61K38/28 , A61P3/10 , A61K31/425
CPC分类号： A61K38/28 , Y10S514/866 , A61K2300/00
摘要： A method for treating diabetes in a mammal by moderately controlling blood glucose concentration in the mammal together with administering to the mammal an amount of a tetracycline compound effective to reduce complications associated with diabetic hyperglycemia. The method enables long term management of diabetes by avoiding the problems associated with tight control of blood glucose concentrations, i.e., hypoglycemia tolerance and seizures, while simultaneously avoiding the problems associated with conventional moderate control of blood glucose concentrations, i.e., pathological complications associated with hyperglycemia, such as nephrophathy, retinopathy, etc. Blood glucose concentration can be controlled by moderate administration (e.g, fewer injections per day) of insulin or another glucose-modulating agent, while pathological complications characteristic of diabetic hyperglycemia are ameliorated through the activity of tetracycline compound, the latter preferably administered in an amount that is substantially non-antimicrobial.
摘要翻译：一种通过适度控制哺乳动物中的血糖浓度来治疗哺乳动物的糖尿病的方法，同时向哺乳动物施用一定量的有效减少与糖尿病性高血糖相关并发症的四环素化合物。该方法能够通过避免与血糖浓度的严格控制（即低血糖耐受和癫痫发作）相关的问题，同时避免与常规的中度控制血糖浓度相关的问题，即与高血糖相关的病理性并发症，如肾病，视网膜病变等。血糖浓度可以通过中度给药（例如，每天更少的注射）胰岛素或另一种葡萄糖调节剂来控制，而通过四环素化合物的活性来改善糖尿病性高血糖症状的病理并发症，后者优选以基本上非抗微生物的量施用。

136. 发明申请

WO98057926A1 ELEVATION OF HDL CHOLESTEROL BY N-[2-[ (AMINOTHIOXOMETHYL)HYDRAZONO] -2-ARYLETHYL]AMIDES 审中-公开
标题翻译：通过N- [2- [（氨基乙氧基）乙酰胺] -2-芳基]氨基甲酸酯升高HDL胆固醇
公开(公告)号：WO98057926A1
公开(公告)日：1998-12-23
申请号：PCT/US1998/010233
申请日：1998-05-19
IPC分类号： C07C337/08 , A61K31/175
CPC分类号： C07C337/08 , C07C2601/14
摘要： This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of formula (I), wherein: R , R and R are independently hydrogen, C1-C6 alkyl or -(CH2)0-6Ph, where Ph is phenyl optionally substituted by halogen, cyano, nitro, C1-C6 alkyl, C1-C6 alkoxy, trifluoromethyl, C1-C6 alkoxycarbonyl, -CO2H or OH; R is hydrogen or C1-C6 alkyl; R is hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, or -(CH2)0-6Ar , where Ar is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar can be optionally substituted by halogen, cyano, nitro, C1-C6 alkyl, phenyl, C1-C6 alkoxy, phenoxy, trifluoromethyl, C1-C6 alkoxycarbonyl, -CO2H or OH; and Ar is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro C1-C6 alkyl, phenyl C1-C6 alkoxy, phenoxy, trifluoromethyl, C1-C6 alkoxycarbonyl, -CO2H or OH.
摘要翻译：本发明涉及通过施用式（I）化合物来提高HDL胆固醇水平来治疗动脉粥样硬化，其中：R 1，R 2和R 3独立地是氢，C 1 -C 6烷基或 - （CH 2）0-6Ph，其中Ph是任选被卤素，氰基，硝基，C 1 -C 6烷基，C 1 -C 6烷氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH取代的苯基; R 4是氢或C 1 -C 6烷基; R 5是氢，C 1 -C 6烷基，C 3 -C 8环烷基或 - （CH 2）0-6Ar 1，其中Ar 1是苯基，萘基，呋喃基，吡啶基或噻吩基，Ar 1可以苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH;任选被卤素，氰基，硝基，氰基，硝基，C 1 -C 6烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH中任意取代的苯基，萘基，呋喃基，吡啶基或噻吩基。

137. 发明申请

WO98056368A1 SUPERIORITY OF FORMULATIONS CONTAINING COENZYME Q10 IN COCONUT OIL 审中-公开
标题翻译：包含COENZYME Q10在配方油中的配方优先
公开(公告)号：WO98056368A1
公开(公告)日：1998-12-17
申请号：PCT/US1998/011827
申请日：1998-06-09
IPC分类号： A61K9/48 , A61K31/122 , A61K47/44 , A61K31/175
CPC分类号： A61K31/122 , A61K9/4858 , A61K47/44
摘要： The present invention comprises a stable and non-toxic coenzyme Q10 formulation with superior bioavailability suitable for oral administration to an animal or a human to rapidly produce clinically effective blood levels of coenzyme Q10. Clinically effective blood levels of coenzyme Q10 are generally agreed to be between about 2 mu g/mL and about 4 mu g/mL. The formulation consists of saturated vegetable oil, hydrogenated vegetable oil or animal fat as a vehicle in which coenzyme Q10 is dissolved. The formulation preferably contains coenzyme Q10 at a level of about 100 mg to about 150 mg dissolved in about 350 mu L to about 500 mu L of saturated vegetable oil, hydrogenated vegetable oil or animal fat enclosed in a gelatin capsule. The clinically accepted vegetable oil is saturated, preferably coconut oil.
摘要翻译：本发明包括稳定且无毒的辅酶Q10制剂，其具有优异的生物利用度，适用于口服给予动物或人以迅速产生临床有效的辅酶Q10血液水平。辅酶Q10的临床有效血液水平通常约为约2μg/ mL至约4μg/ mL。该制剂由饱和植物油，氢化植物油或动物脂肪作为其中溶解有辅酶Q10的载体。制剂优选含有溶解在约350μL至约500μL饱和植物油中的约100mg至约150mg的水平的辅酶Q10，封闭在明胶胶囊中的氢化植物油或动物脂肪。临床上接受的植物油是饱和的，最好是椰子油。

138. 发明申请

WO98053839A2 ANTI-CANCER PRODUCTS FOR TREATING CYSTIC FIBROSIS 审中-公开
标题翻译：用于治疗CYSTIC FIBROSIS的抗癌产品
公开(公告)号：WO98053839A2
公开(公告)日：1998-12-03
申请号：PCT/FR1998/001074
申请日：1998-05-28
IPC分类号： A61K45/00 , A61K31/00 , A61K31/131 , A61K31/15 , A61K31/165 , A61K31/175 , A61K31/255 , A61K31/282 , A61K31/36 , A61K31/439 , A61K31/475 , A61K31/66 , A61K31/664 , A61K31/675 , A61K31/70 , A61K31/704 , A61K31/7052 , A61K38/00 , A61P11/00 , A61P35/00 , C07K14/47 , G01N21/64
CPC分类号： A61K31/00 , A61K31/165 , A61K31/198 , A61K31/475 , A61K31/675 , A61K31/704 , A61K45/06 , A61K2300/00
摘要： The invention concerns a novel approach for treating cystic fibrosis using, in particular, anti-cancer chemotherapy. For the treatment of cystic fibrosis it proposes the use of at least one product which when administered to a patient brings about the expression or overexpression of an ABC carrier compound, in particular glutathione carrier. Preferably, the products used are anti-cancer products whose administration brings about the expression of MRP and/or MDR protein. The invention is also applicable to the treatment of rheumatoid polyarthritis or asthma.
摘要翻译：本发明涉及使用特别是抗癌化学疗法治疗囊性纤维化的新方法。对于囊性纤维化的治疗，它提出使用至少一种产品，其在给予患者时引起ABC载体化合物，特别是谷胱甘肽载体的表达或过表达。优选地，所用的产品是抗癌产品，其给药引起MRP和/或MDR蛋白的表达。本发明也适用于治疗类风湿关节炎或哮喘。

139. 发明申请

WO98050540A1 MODIFIED ANTISENSE NUCLEOTIDES COMPLEMENTARY TO A SECTION OF THE HUMAN Ha-Ras GENE 审中-公开
标题翻译：人类Ha-Ras基因部分的修饰抗体核苷酸
公开(公告)号：WO98050540A1
公开(公告)日：1998-11-12
申请号：PCT/EP1998/002546
申请日：1998-04-30
IPC分类号： C12N15/113 , A61K31/133 , A61K31/175 , A61K31/407 , A61K31/513 , A61K31/519 , A61K31/664 , A61K31/675 , A61K31/70 , A61K31/704 , A61K31/711 , A61K33/24 , A61K38/00 , A61K45/06 , A61K48/00 , A61P35/00 , C07H21/00 , C07H21/02 , C12N15/09 , C12N15/11
CPC分类号： C07H21/02 , A61K38/00 , C12N15/1135 , C12N2310/11 , C12N2310/315 , C12N2310/322 , C12N2310/345 , C12N2310/351 , C12N2310/3531
摘要： The invention relates to a specific modified oligonucleotide complementary to a section of the human Ha-ras gene and mRNA, and its use to specifically regulate, modulate or inhibit expression of the Ha-ras gene, and its use as a pharmaceutical for the treatment of conditions arising from abnormal expression of the Ha-ras gene, in particular in combination with chemotherapy and radiotherapy. The modified oligodeoxynucleotide according to the invention has the sequence: 5'-TxAxTxTxCxCxGxTxCxAxT-3'-O-PO2-O-R, wherein X is o or s, with the proviso that x is 4 to 9 times equal to s and o means a phosphodiester internucleoside linkage, s means a phosphorothioate internucleoside linkage, R means a C8-C21 alkyl group, -(CH2-CH2O)n-(CH2)m-CH3 or -CH2-CH(OH)CH2O-(CH2)q-CH3 wherein n is an integer from 1 to 6, m is an integer from 0 to 20 and q is an integer from 7 to 20 and A is 2'-deoxyadenosine, G is 2'-deoxyguanosine, C is 2'-deoxycytidine and T is thymidine.
摘要翻译：本发明涉及与人Ha-ras基因和mRNA的一部分互补的特异性修饰寡核苷酸及其用于特异性调节，调节或抑制Ha-ras基因表达的用途及其作为治疗用途的药物的用途 Ha-ras基因异常表达引起的病情，特别是与化学疗法和放疗相结合。根据本发明的修饰的寡脱氧核苷酸具有序列：5'-TxAxTxTxCxCxGxTxCxAxT-3'-O-PO2-OR，其中X为o或s，条件是x为s的4至9倍，o表示磷酸二酯核苷间键合是指硫代磷酸核苷间键合，R表示C8-C21烷基， - （CH2-CH2O）n-（CH2）m-CH3或-CH2-CH（OH）CH2O-（CH2）q-CH3，其中 n为1〜6的整数，m为0〜20的整数，q为7〜20的整数，A为2'-脱氧腺苷，G为2'-脱氧鸟苷，C为2'-脱氧胞苷，T为胸苷。

140. 发明申请

WO1996011678A1 METHOD FOR ATTENUATION OF SYMPATHETIC NERVOUS SYSTEM ACTIVITY OR ONSET OF MIGRAINE BY SELECTIVELY METABOLIZED BETA-BLOCKING AGENTS 审中-公开
标题翻译：通过选择性代谢的阻断剂减轻异常神经系统活性或降低MIGRAINE的方法
公开(公告)号：WO1996011678A1
公开(公告)日：1996-04-25
申请号：PCT/US1995012545
申请日：1995-10-06
申请人： MATIER, William, Lesley , PATIL, Ghanshyam
IPC分类号： A61K31/175
CPC分类号： A61K31/216 , A61K31/222
摘要： Disclosed is method for attenuating sympathetic nervous system hyperactivity or onset of migraine in a patient in need of such treatment, by the sublingual, buccal or intranasal administration to such patient of a therapeutically effective amount of the compound of formula (I).
摘要翻译：公开了在需要这种治疗的患者中通过舌下，口腔或鼻内施用治疗有效量的式（I）化合物来减轻交感神经系统多动症或偏头痛发作的方法。

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