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1. 发明申请

WO1997044053A1 PHARMACEUTICAL COMPOSITIONS CONTAINING CYCLOSPORINE AND A CARRIER COMPRISING AT LEAST AN ESTER OF ALPHA-GLYCEROPHOSPHORIC ACID 审中-公开
标题翻译：含有CYPOSPORINE的药物组合物和至少包含ALPHA-甘氨酸的酯的载体
公开(公告)号：WO1997044053A1
公开(公告)日：1997-11-27
申请号：PCT/EP1997002553
申请日：1997-05-20
申请人： FLARER S.A. , SALINI, Alberto
发明人： FLARER S.A.
IPC分类号： A61K38/13
CPC分类号： A61K38/13 , Y02A50/411 , Y02A50/423 , Y10S514/825 , Y10S514/863 , Y10S514/895 , A61K31/685 , A61K31/66 , A61K2300/00
摘要： A description is given of new pharmaceutical compositions containing cyclosporine, combined with a carrier comprising at least a derivative of alpha -glycerophosphoric acid, such as alpha -glycerophosphorylcholine, alpha -glycerophosphorylserine, alpha -glycerophosphorylethanolamine and alpha -glycerophosphoryl-myo-inositol, which allow cyclosporine bioavailability to significantly increase.
摘要翻译：给出了含有环孢菌素的新药物组合物，与包含至少一种α-甘油磷酸衍生物的载体组合，例如α-甘油磷酰胆碱，α-甘油磷酰丝氨酸，α-甘油磷酸乙醇胺和α-甘油磷酸肌醇 - 肌醇，其允许环孢菌素的生物利用度显着增加。

2. 发明申请

WO1995024189A1 INCREASING FETAL HEMOGLOBIN LEVELS USING CARBOXYLIC ESTERS 审中-公开
标题翻译：使用羧酸酯增加天冬氨酸蛋白酶水平
公开(公告)号：WO1995024189A1
公开(公告)日：1995-09-14
申请号：PCT/US1995002769
申请日：1995-03-06
申请人： REPHAELI, Ada
发明人： NUDELMAN, Abraham , SHAKLAI, Matityahu
IPC分类号： A61K31/265
CPC分类号： A61K31/355 , A61K31/22 , A61K31/23 , A61K31/265 , A61K31/335 , A61K31/365 , Y02A50/411 , Y10S514/815 , Y10S514/895
摘要： This invention relates to novel methods of increasing the level of fetal hemoglobin (HbF) in a subject and methods of treating, preventing or ameliorating beta -globin or other HbF-related disorders by increasing the level of HbF in a subject in need of such treatment comprising administering one or more compounds of the formulae: (I) XCH2-CHX-CHX-C(=O)-O-Z, (II) CH3-CO-CH2-C(=O)-O-Z or (III) CH3-CH2-CO-C(=O)-O-Z, wherein X is H, or one of X only may be OH; Z is -CHR-O-C(=O)R', -CHR-O-C(=O)-O-R', or (IV); R is H, alkyl, aryl, arylalkyl; and R' is alkyl, aminoalkyl, aralkyl, aryl, alkoxy, aralkoxy and aryloxy, in which aryl by itself, and aryl in aralkyl, aralkoxy and aryloxy are each selected from the group consisting of phenyl, naphthyl, furyl, or thienyl, each of which is unsubstituted or substituted by at least one substituent selected from the group consisting of alkyl, alkoxy, or halogen; and pharmaceutically acceptable salts and prodrugs thereof.
摘要翻译：本发明涉及增加受试者胎儿血红蛋白（HbF）水平的新方法以及通过增加需要这种治疗的受试者中HbF水平来治疗，预防或改善β-珠蛋白或其他HbF相关疾病的方法包括施用一种或多种下式的化合物：（I）XCH2-CHX-CHX-C（= O）-OZ，（II）CH3-CO-CH2-C（= O）-OZ或（III）CH3-CH2 -CO-C（= O）-OZ，其中X是H，或者X中的一个可以是OH; Z是-CHR-O-C（= O）R'，-CHR-O-C（= O）-O-R'或（IV）; R是H，烷基，芳基，芳基烷基; 和R'是烷基，氨基烷基，芳烷基，芳基，烷氧基，芳烷氧基和芳氧基，其中芳基本身和芳烷基，芳烷氧基和芳氧基中的芳基各自选自苯基，萘基，呋喃基或噻吩基，各自其中未取代或被至少一个选自烷基，烷氧基或卤素的取代基取代; 及其药学上可接受的盐和前药。

3. 发明申请

WO1994024093A1 ORNITHINE DECARBOXYLASE INHIBITING CYCLIC AMINOOXY COMPOUNDS 审中-公开
标题翻译：异丙肾上腺素抑制循环氨基化合物
公开(公告)号：WO1994024093A1
公开(公告)日：1994-10-27
申请号：PCT/EP1994001035
申请日：1994-04-02
申请人： CIBA-GEIGY AG , FREI, Jörg , STANEK, Jaroslav
发明人： CIBA-GEIGY AG
IPC分类号： C07C239/20
CPC分类号： C07C239/20 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , Y10S514/895
摘要： Compounds of the formula (I): H2N-(CH2)n-A-(CH2)m-O-NH2 and salts thereof are described in which the radical A is C3-C6cycloalkylene; n is 0 or 1 and, independently thereof, m is 0 or 1; with the provisos that a) the distance between the aminooxy radical H2N-O- and the amino group -NH2 is at least 3 and not more than 4 carbon atoms and that b) the two radicals H2N-(CH2)n- and -(CH2)m-O-NH2 are not bonded to the same ring carbon atom of A. The compounds of formula (I) and their salts are ornithine decarboxylase inhibitors.
摘要翻译：描述式（I）化合物：H 2 N-（CH 2）n -A-（CH 2）m -O-NH 2及其盐，其中基团A是C 3 -C 6亚环烷基; n为0或1，独立地，m为0或1; 条件是a）氨基氧基H2N-O-和氨基-NH2之间的距离为至少3并且不超过4个碳原子，并且b）两个基团H 2 N-（CH 2）n - 和 - （ CH2）mO-NH2不与A的相同环碳原子键合。式（I）化合物及其盐是鸟氨酸脱羧酶抑制剂。

4. 发明申请

WO1993016037A1 N,N'-SUBSTITUTED IMIDOCARBONIMIDIC DIAMIDES DERIVED FROM HYDROXYLAMINES 审中-公开
标题翻译：从羟氯胺衍生的N，N'-取代的偶氮二胺
公开(公告)号：WO1993016037A1
公开(公告)日：1993-08-19
申请号：PCT/US1993000395
申请日：1993-01-19
申请人： JACOBUS PHARMACEUTICAL CO., INC.
发明人： JACOBUS PHARMACEUTICAL CO., INC. , CANFIELD, Craig , JACOBUS, David , LEWIS, Neil
IPC分类号： C07C279/26
CPC分类号： C07C279/26 , C07C323/13 , Y10S514/895
摘要： There are provided compounds of formula (1) wherein R is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, aryl and aralkyl, R is selected from the group consisting of same group of values as R , R is selected from the group consisting of substituted and unsubstituted alkyl of 1-10 carbon atoms, aryl, cycloalkyl and heterocycloalkyl of 3-8 carbon atoms, wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, cycloalkyl of 3-8 carbon atoms, lower alkenyl, lower alkynyl, nitro, lower alkoxy, lower alkoxycarbonyl, phenyl lower alkyl, phenyl, mono and polyhalophenyl, phenoxy, mono and polyhalophenoxy, R and R may be the same or different and are hydrogen, alkanoyl or alkoxyalkanoyl, R may also have the same value as R , Y is oxygen or sulfur, m is 0 or 1, q is 0 or 1, wherein the prefix alk designates moieties which are straight chain or branched chain, and the term lower designates 1-6 carbon atoms and the unmodified term alk signifies 1-24 carbon atoms, the respective tautomers thereof, the parmaceutically acceptable salts and addition salts thereof and the hydrates of said salts and addition salts. There are further provided methods of protecting subjects liable thereto from infections caused by an organism of the group Plasmodium sp., Mycobacterium sp. and Pneumocystis carinii by administering to a subject liable to such infection, a prophylactically effective amount of a compound of the foregoing formula. These compounds will also reduce the level of infection where said subjects have already been infected.
摘要翻译：提供式（1）化合物，其中R 1是取代或未取代的1至16个碳原子的二价脂族基团; 其中所述取代基是单或多，并且选自低级烷基，芳基和芳烷基，R 3选自与R 5相同的值组，R 5选自由1-10个碳原子的取代和未取代的烷基，3-8个碳原子的芳基，环烷基和杂环烷基组成的基团，其中取代基是单取代或聚取代的，并且选自低级烷基，3-8 碳原子，低级烯基，低级炔基，硝基，低级烷氧基，低级烷氧基羰基，苯基低级烷基，苯基，单和多卤代苯基，苯氧基，单和多卤代苯氧基，R 6和R 7可以相同或不同，氢，烷酰基或烷氧基烷酰基，R 7也可以具有与R 5相同的值，Y是氧或硫，m是0或1，q是0或1，其中前缀alk表示直链的部分或支链，术语低级表示1-6个碳原子和未修饰的术语烷基其中1-24个碳原子，其各自的互变异构体，其药学上可接受的盐和加成盐以及所述盐和加成盐的水合物。进一步提供了保护受益于其的受试者的方法，所述受体是由疟原虫属，分枝杆菌属（Mycobacterium sp。）组成的生物引起的感染引起的。和卡氏肺囊虫，通过给予易感染的受试者，预防有效量的上述化合物。这些化合物也将降低所述受试者已被感染的感染水平。

5. 发明申请

WO2005030197A1 COMPOUND ARTEMISININ 审中-公开
公开(公告)号：WO2005030197A1
公开(公告)日：2005-04-07
申请号：PCT/CN2004/001064
申请日：2004-09-20
IPC分类号： A61K31/336
CPC分类号： A61K31/336 , A61K31/4706 , A61K31/496 , Y02A50/411 , Y10S514/895 , A61K2300/00
摘要： The present invention relates to compound artemisinin tablet which can treat multiple drug-resistant pernicious malaria, tertian malaria and quartan malaria and the relationship children formulation such as granules, suspension syrup and powder. The compound consists of artemisinin, piperaquine and primaquine. Clinical tests in southeast Asia countries where malaria prevails demonstrate that the compound is high-effective and quick-effective. It can shorten the period of treatment and the sideeffects are lowered. The material costs are lowered. The administration is convenience. It can kill off the gametocyte quickly and cut off reservoir in order to interdict the prevalence of malaria quickly

6. 发明申请

WO2003075904A2 ARTEMISININS WITH IMPROVED STABILITY AND BIOAVAILABILITY FOR THERAPEUTIC DRUG DEVELOPMENT AND APPLICATION 审中-公开
标题翻译：具有改进的治疗药物开发和应用的稳定性和生物利用度的ARTEMISININ
公开(公告)号：WO2003075904A2
公开(公告)日：2003-09-18
申请号：PCT/US2003/006283
申请日：2003-02-28
申请人： WRAIR , HARTELL, Mark, G. , BHATTACHARJEE, Apurba, K. , HICKS, Rickey, P. , VANHAMONT, John, E. , MILHOUS, Wilbur, K.
发明人： HARTELL, Mark, G. , BHATTACHARJEE, Apurba, K. , HICKS, Rickey, P. , VANHAMONT, John, E. , MILHOUS, Wilbur, K.
IPC分类号： A61K31/00
CPC分类号： B82Y5/00 , A61K31/55 , A61K31/724 , A61K47/6951 , Y02A50/411 , Y10S514/895
摘要： A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, β-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.
摘要翻译：青蒿素的稳定形式，其中木糖酸或青蒿琥酯与环糊精类似物（优选β-环糊精）络合。络合的环糊精青蒿素配方将青蒿素骨架的过氧化物部分屏蔽水解分解，使其在溶液中稳定。将阿魏酸和环糊精彼此接触以产生2:1的分子种类。青蒿琥酯和环糊精产生1：1的分子种类。络合的环糊精青蒿素制剂对于治疗疟疾是有效的，并且在溶液中长时间稳定。

7. 发明申请

WO0180809A3 MEDICAMENT FOR THE TREATMENT OF DISEASES CAUSED BY PARASITIC PROTOZOA 审中-公开
标题翻译：用于治疗由PARASITIC PROTOZOA引起的疾病的药物
公开(公告)号：WO0180809A3
公开(公告)日：2002-02-28
申请号：PCT/SE0100864
申请日：2001-04-20
申请人： HOFER ANDERS , THELANDER LARS
发明人： HOFER ANDERS , THELANDER LARS
IPC分类号： A61K31/198 , A61K31/42 , A61K31/655 , A61K31/7076 , A61P33/02 , A61P33/06 , A61K31/522
CPC分类号： A61K31/655 , A61K31/198 , A61K31/42 , A61K31/7076 , Y10S514/895 , A61K2300/00
摘要： The present invention relates to the use of an inhibitor of CTP synthetase, such as a glutamine analogue, and a substance capable of suppressing toxic effects thereof in vivo , in the manufacture of a medicament for the treatment of a disease caused by a parasitic protozoa. More specifically, said substance capable of suppressing toxic effects may be a nucleobase, such as a purine base or a nucleoside, while the glutamine analogue advantageously is 6-diazo-5-oxo-L-norleucine (DON). The invention also relates to a pharmaceutical composition as such for the treatment and/or prevention of a disease caused by a parasitic protozoa, wherein the disease is selected from the group consisting of malaria, leishmaniasis and trypanosomiasis, e.g. American trypanosomiasis (Chaga's disease), or African trypanosomiasis (African sleeping sickness).
摘要翻译：本发明涉及CTP合成酶抑制剂如谷氨酰胺类似物和能够抑制其体内毒性作用的物质在制备用于治疗由寄生原虫引起的疾病。更具体地说，能够抑制毒性作用的物质可以是核碱基，例如嘌呤碱或核苷，而谷氨酰胺类似物有利地是6-重氮基-5-氧代-L-正亮氨酸（DON）。本发明还涉及药物组合物，其用于治疗和/或预防由寄生原虫引起的疾病，其中所述疾病选自疟疾，利什曼病和锥虫病，例如疟疾。美国锥虫病（Chaga's disease）或非洲锥虫病（非洲昏睡病）。

8. 发明申请

WO00018769A2 INDOLO[2,1-b]QUINAZOLE-6,12-DIONE ANTIMALARIAL COMPOUNDS AND METHODS OF TREATING MALARIA THEREWITH 审中-公开
标题翻译：吲哚[2,1-b]喹唑啉-6,12-二酮抗微生物化合物及其治疗方法
公开(公告)号：WO00018769A2
公开(公告)日：2000-04-06
申请号：PCT/US1999/022569
申请日：1999-09-28
IPC分类号： C07D471/14 , C07D487/04 , C07D487/14 , C07D498/04 , C07D513/04 , C07D487/00
CPC分类号： C07D471/14 , C07D487/04 , C07D487/14 , C07D513/04 , Y10S514/895
摘要： New use for compounds, compositions and methods are provided for treating malaria parasites in vitro and in vivo by administering indolo[2,1-b]quinazoline-6,12-dione compounds of Formula (I), wherein A, B, C, D, E, F, G and H are independently selected from carbon and nitrogen, or A and B or C and D can be taken together to be nitrogen or sulfur, with the proviso that not more than three of A, B, C, D, E, F, G and H are other than carbon; wherein R1 through R8 are independently selected from the group consisting of, but not limited to, the halogens (F, Cl, Br, and I), alkyl groups, trifluoromethyl groups, methoxyl groups, the carboxy methyl or carboxy ethyl group (COOCH3 or COOCH2CH3), nitro, aryl, heteroaryl, cyano, amino, dialkylaminoalkyl, 1-(4-alkylpiperazinyl), and the pharmaceutically acceptable salts thereof; and wherein X is independently selected from the group consisting of any atom especially oxygen, or any side chain necessary to make the indolo[2,1-b]quinazoline-6,12-dione compound a "prodrug" as the term is understood by one of ordinary skill in the art of medicinal chemistry. In other words, a side chain having a structure where a carbon-nitrogen double bond bears substituents that make the prodrug more water soluble and bioavailable.
摘要翻译：提供化合物，组合物和方法的新用途，通过施用式（I）的吲哚并[2,1-b]喹唑啉-6,12-二酮化合物，其中A，B，C， D，E，F，G和H独立地选自碳和氮，或A和B或C和D可以一起作为氮或硫，条件是不超过三个A，B，C， D，E，F，G和H不是碳; 其中R 1至R 8独立地选自但不限于卤素（F，Cl，Br和I），烷基，三氟甲基，甲氧基，羧基甲基或羧基乙基（COOCH 3或 COOCH 2 CH 3），硝基，芳基，杂芳基，氰基，氨基，二烷基氨基烷基，1-（4-烷基哌嗪基）及其药学上可接受的盐; 并且其中X独立地选自任何原子尤其是氧，或者使吲哚并[2,1-b]喹唑啉-6,12-二酮化合物所需的任何侧链作为术语“ 药物化学领域的普通技术人员。换句话说，具有碳氮双键具有取代基的结构的侧链使得前药更具水溶性和生物利用度。

9. 发明申请

WO1997011087A1 L-NUCLEOSIDE DIMER COMPOUNDS AND THERAPEUTIC USES 审中-公开
标题翻译： L-核苷酸二聚体化合物和治疗用途
公开(公告)号：WO1997011087A1
公开(公告)日：1997-03-27
申请号：PCT/US1996015115
申请日：1996-09-23
申请人： LIPITEK INTERNATIONAL, INC. , WEIS, Alexander, L. , GOODHUE, Charles, T. , PULENTHIRAN, Kirupathevy
发明人： LIPITEK INTERNATIONAL, INC.
IPC分类号： C07H21/00
CPC分类号： C07H19/06 , C07H19/16 , C07H21/00 , Y02A50/58 , Y10S514/895
摘要： The invention relates to nucleoside dimers containing an L-sugar in at least one of the nucleosides and their pharmaceutical compositions.
摘要翻译：本发明涉及在至少一种核苷及其药物组合物中含有L-糖的核苷二聚体。

10. 发明申请

WO1988003802A1 ANTIMALARIAL COMPOSITIONS AND METHODS 审中-公开
标题翻译：抗微生物组合物和方法
公开(公告)号：WO1988003802A1
公开(公告)日：1988-06-02
申请号：PCT/US1987002987
申请日：1987-11-16
申请人： UNITED STATES OF AMERICA, as represented by THE ... , MARTIN, Samuel, K.
发明人： UNITED STATES OF AMERICA, as represented by THE ... , ODUOLA, Ayo, M., J. , MILHOUS, Wilbur, K.
IPC分类号： A61K31/44
CPC分类号： A61K31/47 , Y02A50/411 , Y10S514/895 , A61K31/44 , A61K31/275 , A61K2300/00
摘要： An antimalarial composition contains as the active ingredient a mixture of a chemical compound effective in reversing the resistance of cancer cells to chemotherapy drugs and at least one antimalarial agent. A method for treating malaria in mammals comprises administering a composition containing the active ingredient. A method for reducing the resistance of a malarial parasite to an antimalarial agent comprises administering a composition containing the active ingredient.

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