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11. 发明申请

WO00059851A1 DERIVATIVES OF VENLAFAXINE AND METHODS OF PREPARING AND USING THE SAME 审中-公开
标题翻译：维生素D的衍生物及其制备和使用方法
公开(公告)号：WO00059851A1
公开(公告)日：2000-10-12
申请号：PCT/US2000/008705
申请日：2000-03-31
IPC分类号： A61K9/20 , A61K9/48 , A61K31/135 , A61K31/137 , A61K47/12 , A61K47/26 , A61K47/38 , A61P3/04 , A61P15/10 , A61P23/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07C209/50 , C07C215/46 , C07C215/64 , C07C217/14 , C07C217/74 , C07C231/02 , C07C233/18 , C07C235/34 , C07C255/36 , C07C255/37 , C07D295/192 , C07C17/74
CPC分类号： C07D295/192 , A61K9/2054 , A61K9/2059 , A61K9/4866 , A61K31/135 , C07C215/64 , C07C217/74 , C07C233/18 , C07C255/36 , C07C255/37 , C07C2601/14
摘要： Methods of preparing, and compositions comprising, derivatives of venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.
摘要翻译：公开了制备方法和包含文拉法辛衍生物的组合物。还公开了治疗和预防疾病和病症的方法，包括但不限于情感障碍如抑郁，双相和躁狂症，注意力缺陷障碍，具有多动症的注意缺陷障碍，帕金森病，癫痫，脑功能障碍，肥胖症和体重增加，失禁，痴呆和相关疾病。

12. 发明申请

WO99029655A1 NOVEL ANTIARRHYTHMIC COMPOUNDS 审中-公开
标题翻译：新型抗菌化合物
公开(公告)号：WO99029655A1
公开(公告)日：1999-06-17
申请号：PCT/HU1998/000101
申请日：1998-12-10
IPC分类号： A61P9/06 , A61K31/131 , A61K31/135 , A61K31/165 , A61K31/167 , A61K31/17 , A61K31/18 , C07C217/14 , C07C217/18 , C07C233/36 , C07C233/43 , C07C233/78 , C07C233/80 , C07C275/40 , C07C311/08 , C07C335/20
CPC分类号： C07C233/36 , C07C217/18 , C07C233/78 , C07C275/40 , C07C311/08 , C07C335/20 , Y10S514/821
摘要： The invention relates to compounds of formula (I), wherein R and R , independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R , R and R , independently from each other, stand for hydrogen or C1-4 alkyl group; R represents hydrogen, C1-4 alkyl or benzyl group; R means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R is different from hydrogen, when R is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds. The invention relates also to the pharmaceutical compositions comprising the above compounds. The compounds according to the invention possess valuable antiarrhythmic effect.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2彼此独立地表示氢，卤素或C 1-4烷基; R 3，R 4和R 5彼此独立地代表氢或C 1-4烷基; R 6表示氢，C 1-4烷基或苄基; R 7表示任选被C 1-4烷基，苯甲酰基，C 1-4烷基羰基，C 1-4烷基磺酰基，C 1-4烷基氨基甲酰基或C 1-4烷基硫代氨基甲酰基单取代的硝基或氨基; n和m均为0或1，条件是R 2不同于氢，当R 1为氢时，其立体异构体或其立体异构体的混合物，其酸加成盐和水合物，前药和代谢物的所有这些化合物。本发明还涉及包含上述化合物的药物组合物。根据本发明的化合物具有有价值的抗心律失常作用。

13. 发明申请

WO1992019585A1 TRIPHENYLETHYLENE DERIVATIVE AND PHARMACEUTICAL PREPARATION CONTAINING THE SAME 审中-公开
标题翻译：三烯衍生物和含有其的药物制剂
公开(公告)号：WO1992019585A1
公开(公告)日：1992-11-12
申请号：PCT/JP1992000570
申请日：1992-04-30
申请人： ASAHI KASEI KOGYO KABUSHIKI KAISHA , KOUJI, Hiroyuki , ANDO, Satoshi
发明人： ASAHI KASEI KOGYO KABUSHIKI KAISHA
IPC分类号： C07C217/14
CPC分类号： C07D295/088 , C07C217/18 , C07C217/30 , C07C217/34 , C07C217/42 , C07C219/06 , C07C251/48 , C07C251/60 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D317/50 , C07D317/54 , C07F9/12 , C07F9/65517 , C07F9/65586
摘要： A triphenylalkene derivative represented by general formula (1), a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutical composition thereof having a tumor inhibitory action and an osteoporosis curing activity. In general formula (1) R1 represents a group selected among those represented by formulae (2), (3) and (4); R6 and R7 represent each hydrogen, alkyl or cycloalkyl, or R6 and R7 together form a heterocyclic group with the adjacent nitrogen atom, provided that R6 and R7 should not be hydrogen atoms at the same time; R8 represents hydrogen or alkylcarbonyl; R2 represents alkyl or cycloalkyl; R3 represents phenyl or 3,4-methylenedioxyphenyl, provided that when R3 represents phenyl, the case where R1 represents a group of formula (4) is excluded; R4 represents hydrogen, hydroxyl, R9C(O)O-, R10OCH2O-, -OPO(OH)2 or CH=NOR11; R9 represents alkyl; R10 represents alkyl or alkylcarbonyl; R5 represents hydrogen or CH=NOR11; and R11 represents hydrogen, alkyl or substituted alkyl.

14. 发明申请

WO2019008156A1 INHIBITORS OF THE PD-1/PD-L1 PROTEIN/PROTEIN INTERACTION 审中-公开
公开(公告)号：WO2019008156A1
公开(公告)日：2019-01-10
申请号：PCT/EP2018/068419
申请日：2018-07-06
申请人： RIJKSUNIVERSITEIT GRONINGEN
发明人： DÖMLING, Alexander
IPC分类号： C07C255/54 , C07C271/12 , C07C205/34 , C07D335/02 , C07C217/14 , C07C217/48 , C07C217/76 , C07C323/25 , C07D213/30 , C07D213/36 , C07D305/06 , C07D309/14 , A61K31/4409 , A61P35/00 , A61P31/00
CPC分类号： C07D213/30 , A61P25/00 , A61P31/00 , A61P35/00 , C07C205/34 , C07C217/14 , C07C217/48 , C07C217/76 , C07C255/54 , C07C271/12 , C07C323/25 , C07D213/36 , C07D305/06 , C07D309/14 , C07D335/02
摘要： The present invention provides novel compounds of formula (I) that are useful as inhibitors of the PD-1/PD-L1 protein/protein interaction. The compounds may be used in the treatment of cancer, infectious diseases and neurodegenerative diseases such as schizophrenia, Alzheimer, multiple sclerosis or Parkinson.

15. 发明申请

WO2014045263A3 PROCESS FOR PREPARATION OF INTERMEDIATES OF TELAPREVIR 审中-公开
标题翻译：制备TELAPREVIR中间体的方法
公开(公告)号：WO2014045263A3
公开(公告)日：2014-05-15
申请号：PCT/IB2013058808
申请日：2013-09-24
申请人： REDDYS LAB LTD DR
发明人： IQBAL JAVED , DAHANUKAR VILAS HARESHWAR , ORUGANTI SRINIVAS , KANDAGATLA BHASKAR , KUNHIMON SYAM KUMAR UNNIARAN , SAGYAM RAJESHWAR REDDY , IRENI BABU , KONDEPUDI VEERA VENKATA SATYANARAYANA MURTHY , MUTTAVARAPU MURALI MOHAN , BUCCHIKONDA RAVINDER , GANGIREDDY RAJENDAR REDDY
IPC分类号： C07D209/52 , C07C205/28 , C07C217/14 , C07D317/16 , C07D317/28
CPC分类号： C07D209/52 , C07B2200/07 , C07C35/06 , C07C43/315 , C07C215/20 , C07C217/44 , C07C223/02 , C07C255/46 , C07C271/16 , C07C271/18 , C07C309/66 , C07C2601/08 , C07D317/18 , C07D317/28 , C07F7/1856 , C07K5/0202 , C07K5/1024
摘要： Provided are novel processes for preparation of (1S, 3aR, 6aS)-octahydrocyclopenta[c]pyrrole-1-carboxylic acid and its derivatives; land their use in preparation of Telaprevir.
摘要翻译：提供（1S，3aR，6aS） - 八氢环戊二烯并[c]吡咯-1-羧酸及其衍生物的制备方法; 将其用于制备特拉匹韦尔。

16. 发明申请

WO2004072016A1 アミノアルコール誘導体、それを含有する医薬組成物およびそれらの用途审中-公开
标题翻译：氨基醇衍生物，含有它们的药物组合物及其用途
公开(公告)号：WO2004072016A1
公开(公告)日：2004-08-26
申请号：PCT/JP2004/000893
申请日：2004-01-30
申请人：キッセイ薬品工業株式会社 , 小林淳一 , 中村哲也 , 鈴木律 , 村仲秀幸 , 小沢知永 , 甲斐裕一郎 , 石川健宏 , 近藤龍大 , 玉井哲郎 , 赤羽敏
发明人：小林淳一 , 中村哲也 , 鈴木律 , 村仲秀幸 , 小沢知永 , 甲斐裕一郎 , 石川健宏 , 近藤龍大 , 玉井哲郎 , 赤羽敏
IPC分类号： C07C217/14
CPC分类号： C07D307/79 , A61K31/195 , C07C217/18 , C07C217/20 , C07C323/62 , C07C2601/04
摘要： Compounds represented by the general formula (I) which exhibit potent stimulating activity on beta3-adrenaline receptor and high selectivity therefor, or pharmacologically acceptable salts thereof; pharmaceutical compositions containing the same; and use thereof: (I) wherein R and R are each hydrogen or lower alkyl; R , R , R , and R are each hydrogen, halogeno, lower alkyl, or lower alkoxy; R and R are each hydrogen, halogeno, lower alkyl, halo lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, hydroxyl, lower acyl, carboxyl, or the like; and R is -C(O)-R , -A -C(O)-R , -O-A -C(O)-R , or tetrazol-5-yl.
摘要翻译：由通式（I）表示的化合物，其对β3-肾上腺素受体表现出有力的刺激活性，对其具有高选择性，或其药理学上可接受的盐; 含有该组合物的药物组合物; 及其用途：（I）其中R 1和R 2各自为氢或低级烷基; R 3，R 4，R 5和R 6各自为氢，卤代，低级烷基或低级烷氧基; R 7和R 8各自为氢，卤代，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基，羧基等。并且R 9为-C（O）-R 10，-A 1 -C（O）-R 10，-OA 2 -C（O）-R 10，或四唑-5-基。

17. 发明申请

WO01044167A1 QUATERNARY AMMONIUM AND THEIR USE AS ANTI-TUSSIVE AGENT 审中-公开
标题翻译：季铵盐及其作为抗真菌剂使用
公开(公告)号：WO01044167A1
公开(公告)日：2001-06-21
申请号：PCT/CA2000/001508
申请日：2000-12-15
IPC分类号： A61K31/404 , A61K31/135 , A61K31/14 , A61P11/14 , C07C215/40 , C07C217/14 , C07C217/18 , C07C217/30 , C07D209/08 , C07D211/14
CPC分类号： C07D209/08 , C07C217/18 , C07C217/30
摘要： In one aspect, the present invention concerns the use of certain quaternary ammonium compounds as active ingredient in the manufacture of a medicament for use in the treatment and/or prevention of cough in warm-blooded animals, including humans, such as compounds of formula Y-J-E An (I), wherein J is independently selected from a group represented by one of formulae (II), (III) and (IV).
摘要翻译：一方面，本发明涉及某些季铵化合物作为活性成分在制备用于治疗和/或预防包括人在内的温血动物（例如式YJE化合物）中治疗和/或预防咳嗽的药物中的用途（I），其中J独立地选自由式（II），（III）和（IV）中的一个表示的基团。

18. 发明申请

WO99007377A1 1-[4-(SUBSTITUTED ALKOXY)BENZYL]NAPHTHALENE COMPOUNDS HAVING ESTROGEN INHIBITORY ACTIVITY 审中-公开
标题翻译： 1- [4-（取代的烷基）苄基]具有雌激素抑制活性的萘磺酸化合物
公开(公告)号：WO99007377A1
公开(公告)日：1999-02-18
申请号：PCT/US1998/016065
申请日：1998-08-04
IPC分类号： C07D295/08 , A61K31/135 , A61K31/138 , A61K31/17 , A61K31/40 , A61K31/4015 , A61K31/438 , A61K31/445 , A61K31/495 , A61K31/522 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P35/00 , C07C217/00 , C07C217/14 , C07C217/20 , C07C275/28 , C07C275/30 , C07C275/34 , C07D207/08 , C07D207/26 , C07D207/27 , C07D211/22 , C07D221/20 , C07D223/04 , C07D265/30 , C07D295/092 , C07D295/112 , C07D473/08 , A61K31/505 , A61K31/52 , C07C211/00 , C07C213/00 , C07C215/00 , C07C273/00 , C07D207/04 , C07D207/40 , C07D211/06 , C07D241/04 , C07D487/00
CPC分类号： C07D207/08 , C07C217/20 , C07C275/28 , C07C275/30 , C07C275/34 , C07D207/27 , C07D211/22 , C07D221/20 , C07D295/088 , C07D295/112 , C07D473/08
摘要： A class of substituted benzylnaphthylene compounds of structure (1) where R and R are independently hydrogen, alkyl of one to six carbon atoms, acyl of two to six carbon atoms, or phenacyl; X is -(CH2)1-6; Y is absent or is selected from 1,4-piperazinylene; ureido; N-(lower alkyl)ureido; N'-(lower alkyl)ureido; or N,N'-(di-lower alkyl)ureido; and Z is 1-, 2- or 3-pyrrolidinyl; 1-, 2-, or 3-[1-(lower alkyl)pyrrolidinyl]; 1-, 2-, 3- or 4-piperidinyl; 1-, 2-, 3- or 4-[1-lower alkyl)piperidinyl]; N,N-dialkyl; 1-azepinyl; 1- or 2-naphthylamino, 4-morpholinyl, dimethyl-4-morpholinyl, 3-azaspiro[5.5]undecan-3-yl; pyrrolidinon-1-yl; unsubstituted phenyl; or phenyl substituted with acyl of two to four carbon atoms, alkyl of one to four carbon atoms, halo, or alkoxy of one to four carbon atoms; with the proviso that n is not 2 or 3 when Z is 1-pyrrolidinyl, 1-piperidinyl, 1-azepinyl, 4-morpholinyl, N,N-dimethylamino or N,N-diethylamino; are selective estrogen receptor modulators useful in the prophylaxis or treatment of breast cancer.
摘要翻译：一类结构（1）的苄基萘酚化合物，其中R 1和R 2独立地是氢，1至6个碳原子的烷基，2至6个碳原子的酰基或苯甲酰甲基; X是 - （CH 2）1-6; Y不存在或选自1,4-哌嗪基; 脲; N-（低级烷基）脲基; N' - （低级烷基）脲基; 或N，N' - （二低级烷基）脲基; Z为1-，2-或3-吡咯烷基; 1-，2-或3- [1-（低级烷基）吡咯烷基]; 1-，2-，3-或4-哌啶基; 1-，2-，3-或4- [1-低级烷基）哌啶基]; N，N-二烷基; 1-吖庚因基; 1-或2-萘基氨基，4-吗啉基，二甲基-4-吗啉基，3-氮杂螺[5.5]十一烷-3-基; 吡咯烷酮-1-基; 未取代的苯基; 或被2-4个碳原子的酰基取代的苯基，1-4个碳原子的烷基，卤素或1-4个碳原子的烷氧基; 条件是当Z是1-吡咯烷基，1-哌啶基，1-氮杂基，4-吗啉基，N，N-二甲基氨基或N，N-二乙基氨基时，n不是2或3。是可用于预防或治疗乳腺癌的选择性雌激素受体调节剂。

19. 发明申请

WO1995023127A1 2-(AMINOALKOXY)PHENYLALKYLAMINES WITH ANTIINFLAMMATORY ACTIVITY 审中-公开
标题翻译：具有抗炎活性的2-（氨基烷氧基）苯甲酰胺
公开(公告)号：WO1995023127A1
公开(公告)日：1995-08-31
申请号：PCT/EP1995000626
申请日：1995-02-20
申请人： THE BOOTS COMPANY PLC , RAFFERTY, Paul , TOMETZKI, Gerald, Bernard
发明人： THE BOOTS COMPANY PLC
IPC分类号： C07C217/14
CPC分类号： C07D295/096 , C07C217/58 , C07C229/38 , C07C255/58 , C07C255/59 , C07D295/088
摘要： Compounds of formula (I) including pharmaceutically acceptable salts thereof in which R1, R2, R3, and R4 independently represent hydrogen, hydroxy, halo, halogenated alkyl, halogenated alkoxy, alkyl, alkoxy, cyano, a carbamoyl group of formula CONRARB, alkoxy carbonyl group, or R1 and R2 together with the phenyl ring represent a naphthalene ring (optionally substituted); L1 represents C2-6 alkylene optionally substituted by one or more C1-4 alkyl groups; R5 represents hydrogen or alkyl, R6 represents hydrogen or alkyl, phenylalkyl (optionally substituted) or R5 and R6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; L2 represents a C1-6 alkylene chain optionally substituted by one or more C1-4 alkyl groups; and R7 and R8 independently represent hydrogen or alkyl or R7 and R8 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; are disclosed (with provisos) which are anti-inflammatory and/or anti-allergic agents and/or immunomodulants useful in treating rheumatic diseases and/or neurological damage. Compositions containing these compounds and processes to make them are also disclosed.
摘要翻译：式（I）化合物，包括其药学上可接受的盐，其中R 1，R 2，R 3和R 4独立地表示氢，羟基，卤素，卤代烷基，卤代烷氧基，烷基，烷氧基，氰基，式CONRARB的氨基甲酰基，或R 1和R 2与苯环一起代表萘环（任选取代）; L 1表示任选被一个或多个C 1-4烷基取代的C 2-6亚烷基; R5表示氢或烷基，R6表示氢或烷基，苯基烷基（任选取代的）或R 5和R 6与它们所连接的氮原子一起表示饱和的3-7元杂环; L2表示任选被一个或多个C 1-4烷基取代的C 1-6亚烷基链; 并且R 7和R 8独立地表示氢或烷基或者R 7和R 8与它们所连接的氮原子一起表示饱和的3-7元杂环; （有条件），其是可用于治疗风湿性疾病和/或神经损伤的抗炎和/或抗过敏剂和/或免疫组合物。还公开了含有这些化合物的组合物和制备它们的方法。

20. 发明申请

WO2011097336A3 HIGHLY SELECTIVE 5-HT(2C) RECEPTOR AGONISTS HAVING ANTAGONIST ACTIVITY AT THE 5-HT(2B) RECEPTOR 审中-公开
标题翻译：在5-HT（2B）受体上具有拮抗剂活性的高选择性5-HT（2C）受体激动剂
公开(公告)号：WO2011097336A3
公开(公告)日：2011-12-01
申请号：PCT/US2011023535
申请日：2011-02-03
申请人： UNIV ILLINOIS , UNIV NORTH CAROLINA , KOZIKOWSKI ALAN , ROTH BRYAN , SVENNEBRING ANDREAS , CHEN GANG , CHO SUNG JIN
发明人： KOZIKOWSKI ALAN , ROTH BRYAN , SVENNEBRING ANDREAS , CHEN GANG , CHO SUNG JIN
IPC分类号： C07C217/74 , A61K31/138 , A61P3/00 , A61P25/00 , C07C217/14
CPC分类号： C07C215/54 , A61K31/135 , A61K31/137 , A61K31/138 , A61K45/06 , C07C217/74 , A61K2300/00
摘要： Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.
摘要翻译：公开了高选择性的5-HT（2C）受体激动剂受体。 5-HT（2C）受体激动剂用于治疗疾病和病症，其中5-HT（2C）受体的调节提供益处，例如肥胖症和精神疾病。

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