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11. 发明申请

WO98030546A1 TRICYCLIC BENZO[e]ISOINDOLES AND BENZO[h]ISOQUINOLINES 审中-公开
标题翻译：三氯苯并[e] ISOINDOLES和BENZO [h]异喹啉
公开(公告)号：WO98030546A1
公开(公告)日：1998-07-16
申请号：PCT/EP1998/000043
申请日：1998-01-07
IPC分类号： C07D209/62 , C07D221/10 , C07D491/04 , C07D491/056 , A61K31/40 , A61K31/435
CPC分类号： C07D491/04 , C07D209/62 , C07D221/10
摘要： The present invention is concerned with novel benzo[e]-isoindoles and benzo[h]isoquinolines. Since the compounds in accordance with the invention can bind to serotonin receptors (5HT2), they are especially suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic attacks, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioural disorders, addiction, obesity, bulimia, etc., nervous system damage caused by trauma, stroke, neurodegenerative diseases, etc.; cardiovascular disorders such as hypertension, thrombosis, stroke, etc; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
摘要翻译：本发明涉及新的苯并[e] - 异吲哚和苯并[h]异喹啉。由于根据本发明的化合物可以结合5-羟色胺受体（5HT2），它们特别适用于治疗或预防中枢神经障碍，例如沮丧，双相情感障碍，焦虑状态，睡眠和性障碍，精神病，精神分裂症，偏头痛以及与头痛或不同类型的疼痛，人格障碍或强迫症，社交恐惧症或惊恐发作，精神有机疾病，儿童精神障碍，侵略性，与年龄有关的记忆障碍和行为障碍，成瘾，肥胖，贪食症等，由创伤，中风，神经变性疾病等引起的神经系统损伤; 心血管疾病如高血压，血栓形成，中风等; 和胃肠道疾病如胃肠道运动功能障碍。

12. 发明申请

WO9811101A3 CYCLOPROPYLINDOLE COMPOUNDS AND THEIR USE AS PRODRUGS 审中-公开
标题翻译：环丙基化合物及其作为PRODRUGS的用途
公开(公告)号：WO9811101A3
公开(公告)日：1998-04-23
申请号：PCT/NZ9700117
申请日：1997-09-12
申请人： CANCER SOC AUCKLAND DIV NZ INC , DENNY WILLIAM ALEXANDER , TERCEL MOANA , ATWELL GRAHAM JOHN
发明人： DENNY WILLIAM ALEXANDER , TERCEL MOANA , ATWELL GRAHAM JOHN
IPC分类号： A61K31/403 , A61K31/407 , A61K31/4155 , A61P35/00 , C07D209/60 , C07D209/62 , C07D403/14 , C07D405/14 , C07D487/04 , C07D403/00 , C07D209/00
CPC分类号： C07D487/04 , C07D209/60
摘要： The invention provides compounds of general formula (I), wherein: X is halogen or OSO2R, where R represents H or is unsubstituted or hydroxy- or amino-substituted lower alkyl; Y is a nitro or amine group or a substituted derivative thereof; W is selected from the structures of formulae (Ia, Ib or Ic), where E is -N= or -CH=, G is O, S, or NH, and Q is either up to three of R, OR, NRR, NO2, CONHR, NHCOR or NHCONHR, or is an additional group of formulae (Ia, Ib or Ic) and HET represents a 5- or 6-membered carbocycle or heterocycle; and A and B collectively represent a fused benzene or 2-CO2R pyrrole ring. In one embodiment, the group Y is an amine derivative substituted by a group which is a substrate for a nitroreductase or carboxypeptidase enzyme such that one of said enzymes is able to bring about removal of that group.

13. 发明申请

WO9221654A3 CARBOXAMIDO-(3,2N)-CARBOCYCLIC-2-AMINOTETRALIN DERIVATIVES 审中-公开
标题翻译：碳酰氧基 - （3,2N） - 链烷酰基-2-氨基嘌呤衍生物
公开(公告)号：WO9221654A3
公开(公告)日：1993-01-07
申请号：PCT/US9201652
申请日：1992-03-11
申请人： UPJOHN CO
发明人： LIN CHIU-HONG , PIERCEY MONTFORD E , HAADSMA-SVENSSON SUSANNE R
IPC分类号： A61K31/40 , A61K31/403 , A61K31/47 , A61K31/473 , A61P25/00 , A61P25/18 , C07D209/60 , C07D209/62 , C07D221/08 , C07D227/06 , C07D , A61K
CPC分类号： C07D209/60
摘要： This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of formula (I), wherein R is C1-C8 alkyl and n is 1 or 2.

14. 发明申请

WO9100856A3 (1,2N) AND (3,2N)-CARBOCYCLIC-2-AMINO TETRALIN DERIVATIVES 审中-公开
标题翻译：（1,2N）和（3,2N） - 芳基-2-氨基四氢萘衍生物
公开(公告)号：WO9100856A3
公开(公告)日：1991-03-21
申请号：PCT/US9003551
申请日：1990-06-27
申请人： UPJOHN CO
发明人： LIN CHIU-HONG
IPC分类号： A61K31/395 , A61K31/397 , A61K31/435 , A61P9/10 , A61P9/12 , A61P25/20 , A61P25/24 , A61P25/26 , C07C217/74 , C07D205/12 , C07D209/60 , C07D209/62 , C07D221/08 , C07D221/10 , A61K31/40
CPC分类号： C07C217/74 , C07D209/60 , C07D221/08 , C07D221/10
摘要： This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of formula (I) wherein R, R1 and A are as defined in claim 1. These compounds are useful to treat central nervous system disorders.

15. 发明申请

WO2020086691A1 NEAR-INFRARED HEPTAMETHINE DYES FOR GENERATION OF SINGLET OXYGEN 审中-公开
公开(公告)号：WO2020086691A1
公开(公告)日：2020-04-30
申请号：PCT/US2019/057615
申请日：2019-10-23
申请人： CALIFORNIA INSTITUTE OF TECHNOLOGY
发明人： JARMAN, John, B. , DOUGHERTY, Dennis, A.
IPC分类号： C09B23/00 , C07D209/04 , C07D209/56 , C07D209/62 , C07D309/34 , C07D335/02 , G02B5/20 , A61K41/00
摘要： This current disclosure is directed to charge-transfer heptamethine dyes for NIR singlet oxygen generation, each such dye comprising a near-infrared (NIR) absorbing dye having heptamethine linkages orthogonally coupled to an optionally substituted cationic heteroaryl ring moiety as a charge-transfer partner and uses thereof.

16. 发明申请

WO2012035061A1 PROCESS FOR THE PREPARATION OF 1,2-DIAMINES BY INTERMOLECULAR TRANSFER OF TWO NITROGEN GROUPS ONTO ALKENES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：通过两个硝基组成的分子间转移制备1,2-二氨基酸的方法及其中间体
公开(公告)号：WO2012035061A1
公开(公告)日：2012-03-22
申请号：PCT/EP2011/065929
申请日：2011-09-14
申请人： INSTITUT CATALÀ D'INVESTIGACIÓ QUÍMICA (ICIQ) , MUÑIZ, Kilian
发明人： MUÑIZ, Kilian
IPC分类号： C07D209/46 , C07D209/48 , C07D209/62 , C07D275/06 , C07C209/60 , C07C211/10
CPC分类号： C07D209/62 , C07C209/62 , C07D209/46 , C07D209/48 , C07D275/06 , C07C211/09
摘要： A new process for the diamination of alkenes is provided, as well as the new compounds prepared thereof. A process for the preparation of the primary amines obtained from the diaminated alkenes of the provided preparation process is also provided.
摘要翻译：提供了一种新的烯烃二胺化方法，以及其制备的新化合物。还提供了由所提供的制备方法的二胺烯制得的伯胺的制备方法。

17. 发明申请

WO2009157015A2 SYNTHESIS OF L-(CARBAZOL-4-YLOXY)-3-[[2-(O- METHOXYPHENOXY)ETHYL]AMINO]-2-PROPANOL 审中-公开
标题翻译：合成L-（卡巴唑-4-基）-3 - [[2-（O-甲氧基苯氧基）乙基]氨基] -2-丙醇
公开(公告)号：WO2009157015A2
公开(公告)日：2009-12-30
申请号：PCT/IN2009000314
申请日：2009-06-01
申请人： INOGENT LAB PRIVATE LTD 1 , RAY PURNA CHANDRA , LAKONDA NAGAPRASADA RAO , SATYENDER APURI , REDDY R BUCHI
发明人： RAY PURNA CHANDRA , LAKONDA NAGAPRASADA RAO , SATYENDER APURI , REDDY R BUCHI
IPC分类号： C07D209/62
CPC分类号： C07D209/88
摘要： The present invention relates to an improved process for the preparation of Carvedilol, wherein, the process involves the use of organic base in the reaction of 4-(oxirane-2ylmethoxy)-9H-carbazole with 2-(2-methoxyphenoxy) ethylamine in presence of a solvent. While preparing Carvedilol minimum amount of bis-impurity was obtained without purification.
摘要翻译：本发明涉及一种制备卡维地洛的改进方法，其中该方法涉及在4-（环氧乙烷-2-基甲氧基）-9H-咔唑与2-（2-甲氧基苯氧基）乙胺的反应中使用有机碱，的溶剂。在制备卡维地洛时，不经纯化即可获得最少量的双杂质。

18. 发明申请

WO2006040180A1 AMINOMETHYL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
标题翻译：适用于治疗多巴胺D3受体调节障碍的氨基甲酸替代双相芳族化合物
公开(公告)号：WO2006040180A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/011093
申请日：2005-10-14
申请人： ABBOTT GMBH & CO. KG , DRESCHER, Karla , HAUPT, Andreas , UNGER, Liliane , TURNER, Sean, C. , BRAJE, Wilfried , GRANDEL, Roland
发明人： DRESCHER, Karla , HAUPT, Andreas , UNGER, Liliane , TURNER, Sean, C. , BRAJE, Wilfried , GRANDEL, Roland
IPC分类号： C07C317/34 , C07D209/14 , C07D209/62 , C07D235/14 , A61K31/136 , A61P25/00 , A61K31/145 , A61K31/403 , A61K31/407 , A61K31/4174
CPC分类号： C07D471/04 , C07D209/14 , C07D209/62 , C07D235/14
摘要： The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula (I) wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR 8 , where R 8 is H, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkylcarbonyl or fluorinated C 1 -C 4 -alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents R a , wherein the variable R a has the meanings given in the claims and in the description; X is a covalent bond or N-R 2 , CHR 2 , CHR 2 CH 2 , N or C-R 2 ; Y is N-R 2a , CHR 2a , CHR 2a CH 2 or CHR 2a CH 2 CH 2 ; is a single bond or a double bond; E is CH 2 or NR 3 ; R 1 is H, C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, formyl or C 1 -C 3 -alkylcarbonyl; R 1a is H, C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -alkenyl, R 2 and R 2a each independently are H, CH 3 , CH 2 F, CHF 2 or CF 3 or R 1a and R 2 or R 1a and R 2a together are (CH 2 ) n with n being 1, 2 or 3; R 3 is H or C 1 -C 4 -alkyl; R 4 and R 5 independently of each other are H, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl or C 1 -C 4 -alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring; R 6 and R 7 independently of each other are H or halogen; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
摘要翻译：本发明涉及式（I）的氨基甲基取代的双环芳族化合物，其中Ar是选自苯基，5-或6-元C-结合的杂芳族基团的环状基团，其包含作为环成员1,2 或3个彼此独立地选自O，S和N的杂原子和稠合于饱和或不饱和的5-或6-元碳环或杂环的苯环，其中杂环包含作为环成员1， 2或3个选自N，O和S的杂原子和/或1,2或3个含杂原子的基团，各自独立地选自NR 8，其中R 8是H， C 1 -C 4 - 亚烷基，氟化C 1 -C 4 - 烷基，C 1 -C 1-4烷基，C 1 -C 4烷基，C 1 -C 4 - 其中环状基团Ar可以带有1个碳原子的烷基羰基或氟化C 1 -C 4 - 烷基羰基， 2或3个取代基R a a，其中变量R a a具有在声明和说明书; X是共价键或NR 2，CHR 2，CHR 2 CH 2，N或CR ^{2 ; Y是NR 2a，CHR 2，H 2，CH 2，CH 2或CHR 2 O 2， CH _{2 CH _{2 ; 是单键或双键; E是CH 2或NR 3; R 1是H，C 1 -C 4 - 烷基，C 3 -C 4 - C 3 -C 4 - 环烷基甲基，C 3 -C 4 - 亚烷基，C 3 -C 4 - 环烷基，C 3 -C 4 - 氟化C 1 -C 4 - 亚烷基，氟化C 3 -C 4 - 环烷基，氟化C _{-C _{3 - 烷基羰基; R 1a是H，C 1 -C 4 - 烷基，C 3 -C 4烷基， C 3 -C 4 - 亚烷基，氟化C 1 -C 4 - 亚烷基，C 3 -C 4 - 氟化C 3 -C 4 - 环烷基，氟化C 3 -C 4 - 亚烯基，R SUP > 2和R 2a各自独立地为H，CH 3，CH 2，F，CHF 2， >或CF 3或R 1a和R 2或R 1a和R 2a和R 2b 一起是n为1,2或3的（CH 2）2 n。 R 3是H或C 1 -C 4 - 烷基; R 4和R 5彼此独立地为H，C 1 -C 4 - 烷基，氟化C C 1 -C 4 - 烷基或C 1 -C 4 - 烷氧基，或者可以与N， 4-，5-或6-元饱和或不饱和环; R 6和R 7彼此独立地为H或卤素; 及其生理上耐受的酸加成盐。本发明还涉及式（I）化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。}}}}}

19. 发明申请

WO0129000A3 BICYCLIC AND TRICYCLIC AMINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：作为化合物受体活性调节剂的双相和三元胺
公开(公告)号：WO0129000A3
公开(公告)日：2002-01-24
申请号：PCT/US0028350
申请日：2000-10-13
申请人： DU PONT PHARM CO
发明人： WACKER DEAN A , DUNCIA JOHN V , SANTELLA III JOSEPH B , GARDNER DANIEL S
IPC分类号： A61K31/403 , A61K31/439 , A61K31/46 , A61P9/10 , A61P11/06 , A61P19/02 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D209/52 , C07D209/62 , C07D451/02 , C07D453/06 , C07D471/08 , A61K31/395
CPC分类号： C07D451/02 , C07D209/52 , C07D209/62 , C07D453/06
摘要： The present application describes modulators of CCR3 of formula (I): A-E-NR -G, or pharmaceutically acceptable salt forms thereof, wherein: A is selected from (a), (b), (c) and (d). G is selected from -C(O)R , -C(O)NR R , -C(O)OR , -SO2NR R , -SO2R , -C(=S)NR R , C(=NR )NR R , C(=CHCN)NR R , C(=CHNO2)NR R , C(=C(CN)2)NR R , (e), (f) and (g); useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.
摘要翻译：本申请描述了式（I）的CCR3的调节剂：AE-NR 1 -G或其药学上可接受的盐形式，其中：A选自（a），（b），（c）和（d）。 G选自-C（O）R 3，-C（O）NR 2 R 3，-C（O）OR 3，-SO 2 NR 2 R 3，-SO 2 R C（= S）NR 2 R 3，C（= NR 1a）NR 2 R 3，C（= CHCN）NR 2 R 3， C（= CHNO 2）NR 2 R 3，C（= C（CN）2）NR 2 R 3，（e），（f）和（g）可用于预防炎性疾病如哮喘和其他过敏性疾病。

20. 发明申请

WO1996002502A1 PREPARATION OF BENZINDOLE COMPOUNDS FROM NAPHTHALENE COMPOUNDS 审中-公开
标题翻译：萘二甲酸酯化合物的制备
公开(公告)号：WO1996002502A1
公开(公告)日：1996-02-01
申请号：PCT/US1995008958
申请日：1995-07-18
申请人： AGOURON PHARMACEUTICALS, INC.
发明人： AGOURON PHARMACEUTICALS, INC. , VARNEY, Michael, D. , PALMER, Cindy, L. , DEAL, Judy, G.
IPC分类号： C07D209/62
CPC分类号： C07C255/58 , C07D209/90
摘要： The invention relates to a process for preparing a substituted 2-amino-benz[cd]indole of formula (I). The nitro group of a substituted 1-nitro-8-cyano-naphthalene compound is reduced to an amine group to form a substituted 1-amino-8-cyano-naphthalene compound, which is cyclized to form the substituted 2-amino-benz[cd]indole. The reduction and cyclization may be effected in a one-pot procedure using a reducing agent such as stannous chloride, which generates an acid that cyclizes the reduction product. The syntheses of the 1-nitro-8-cyano-naphthalene compound and its precursors are also described.
摘要翻译：本发明涉及制备式（I）的取代的2-氨基 - 苯并[cd]吲哚的方法。将取代的1-硝基-8-氰基 - 萘化合物的硝基还原为胺基，形成取代的1-氨基-8-氰基 - 萘化合物，其被环化以形成取代的2-氨基 - 苯并[ cd]吲哚。还原和环化可以使用还原剂如氯化亚锡在一锅法中进行，其产生使还原产物环化的酸。还描述了1-硝基-8-氰基 - 萘化合物及其前体的合成。

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