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1. 发明申请

WO1992018475A2 NEW CENTRALLY ACTING SUBSTITUTED PHENYLAZACYCLOALKANES 审中-公开
标题翻译：新的中央行动取代的苯甲酰氯
公开(公告)号：WO1992018475A2
公开(公告)日：1992-10-29
申请号：PCT/US1992002227
申请日：1992-03-26
申请人： THE UPJOHN COMPANY , SVENSSON, Kjell, Anders, Ivan , WIKSTRÖM, Håkan, Vilhem , CARLSSON, Per, Arvid, Emil , BOIJE, Anna, Maria, Persdotter , WATERS, Ross, Nicholas , SONESSON, Clas, Ake , STJERULOF, Nils, Peter , ANDERSSON, Bengt, Ronny , HANSSON, Lars, Olor
发明人： THE UPJOHN COMPANY
IPC分类号： C07D0
CPC分类号： C07D207/08 , C07D207/09 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/24 , C07D211/28 , C07D211/34 , C07D211/76 , C07D223/04 , C07D409/06 , C07D409/10 , C07D455/02 , C07D487/04
摘要： A compound of formula (I), or a pharmaceutically acceptable salt thereof wherein n is 0-3; R and R are independently H (provided only one is H at the same time), -OH (provided R is other than hydrogen), CN, CH2CN, 2- or 4-CF3, CH2CF3, CH2CHF2, CH=CF2, (CH2)2CF3, ethenyl, 2-propenyl, OSO2CH3, OSO2CF3, SSO2CF3, COR , COOR , CON(R )2, SOxCH3 (where, x is 0-2), SOxCF3, O(CH2)xCF3, SO2N(R )2, CH=NOR , COCOOR , COCOON(R )2, C1-8 alkyls, C3-8 cycloalkyls, CH2OR , CH2(R )2, NR SO2CF3, NO2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R is hydrogen, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, -(CH2)m-R (where m is 1-8), CH2SCH3 or a C4-C8 alkyl bonded to said nitrogen and one of its adjacent carbon atoms inclusive to form a cyclic structure; R is independently hydrogen, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, -(CH2)m-R where m is 1-8; R is phenyl, phenyl (substituted with a CN, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl), 2-thiophenyl, 3-thiophenyl, -NR CONR R , or -CONR R ; R and R are independently hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkylmethyl, C2-C8 alkenyl or C2-C8 alkynyl; and with the proviso that when R is 2-CN or 4-CN, R is H, R is n-Pr and n is 1 or 3 then such compound is a pure enantiomer. The formula (I) compounds possess selective pharmacological properties and are useful in treating central nervous system disorders related to dopamine receptor activity including depression symptoms, geriatric disorders in the improvement of mental and motor functions, schizophrenia, narcolepsy, MBD, obesitas, and disturbances of sexual functions and impotence.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中n为0-3; R 1和R 2独立地是H（同时只有一个是H），-OH（提供的R 4不是氢），CN，CH 2 CN，2-或4- CF 3，CH 2 CF 3 ，CH 2 CF 2，（CH 2）2 CF 3，乙烯基，2-丙烯基，OSO 2 CH 3，OSO 2 CF 3，SSO 2 CF 3，COR 4，COOR 4，CON（R 4）2，SO x CH 3（其中，x为0 -2），SO x CF 3，O（CH 2）x CF 3，SO 2 N（R 4）2，CH = NOR 4，COCOOR 4，COCOON（R 4）2，C 1-8烷基，环烷基，CH 2 OR 4，CH 2（R 4）2，NR 4 SO 2 CF 3，NO 2，卤素，2,3或4位的苯基，噻吩基，呋喃基，吡咯，恶唑，噻唑，N-吡咯啉，三唑，四唑或吡啶; R 3是氢，CF 3，CH 2 CF 3，C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 9环烷基 - 甲基，C 2 -C 8烯基，C 2 -C 8炔基，3,3,3-三氟丙基，（CH 2）m R 5（其中m为1-8），CH 2 SCH 3或与所述氮键合的C 4 -C 8烷基及其相邻碳原子之一，以形成环状结构; R 4独立地是氢，CF 3，CH 2 CF 3，C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 9环烷基 - 甲基，C 2 -C 8烯基，C 2 -C 8炔基，3,3,3-三氟丙基，，4-三氟丁基， - （CH 2）m R 5，其中m为1-8; R 5是苯基（被CN，CF 3，CH 2 CF 3，C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 9环烷基 - 甲基，C 2 -C 8烯基，C 2 -C 8炔基），2-噻吩基， 3-噻吩基，-NR 6 CONR 6 R 7或-CONR 6 R 7; R 6和R 7独立地是氢，C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 9环烷基甲基，C 2 -C 8烯基或C 2 -C 8炔基; 并且条件是当R 1为2-CN或4-CN时，R 2为H，R 3为n-Pr，n为1或3，则该化合物为纯对映异构体。式（I）化合物具有选择性药理学性质，并且可用于治疗与多巴胺受体活性相关的中枢神经系统疾病，包括抑郁症状，改善精神和运动功能的老年疾病，精神分裂症，发作性睡病，脑血管疾病，肥胖症和干扰性功能和阳。。

2. 发明申请

WO2012039660A1 PHENYLPIPERIDINE COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS 审中-公开
标题翻译：用于治疗神经病学和心理疾病的苯并吡啶化合物
公开(公告)号：WO2012039660A1
公开(公告)日：2012-03-29
申请号：PCT/SE2011/000163
申请日：2011-09-20
申请人： A. CARLSSON RESEARCH AB , CARLSSON, Lizzie Maria , KLOBERG, Angélica , BURSTEIN, Ethan, S. , CARLSSON, Per Arvid Emil
发明人： CARLSSON, Lizzie Maria , KLOBERG, Angélica , BURSTEIN, Ethan, S. , CARLSSON, Per Arvid Emil
IPC分类号： A61K31/445
CPC分类号： A61K31/451 , A61K31/445
摘要： The present invention relates to a novel use of both enantiomers of the phenylpiperidine derivativ OSU6162, i.e. (-) and (+)-OSU6162 as partial agonists on 5-hydroxytryptamine (5hHT) receptors. As a result, both (-) OSU6162 and (+)-OSU6162 may be used for the treatment and/or prevention of one or more diseases associated with a need for modulation of monoaminergic neurotransmitter receptors, wherein at least one of the monoaminergic neurotransmitter receptors is a 5-hydroxytryptamine receptor (5-HT receptor). Thus, said compounds act as stabilizers not only on dopaminergic, but also on serotonergic brain signaling and will act as partial agonists on such monoaminergic neurotransmitter receptors.
摘要翻译：本发明涉及苯基哌啶衍生物OSU6162的两种对映异构体，即（ - ）和（+） - OSU6162作为5-羟色胺（5hHT）受体的部分激动剂的新用途。因此，（ - ）OSU6162和（+） - OSU6162可用于治疗和/或预防与需要调节单胺能神经递质受体相关的一种或多种疾病，其中至少一种单胺能神经递质受体是5-羟色胺受体（5-HT受体）。因此，所述化合物不仅用作多巴胺能的稳定剂，而且用作5-羟色胺能脑信号传导，并且将作为单胺能神经递质受体的部分激动剂。

3. 发明申请

WO1982004042A1 THERAPEUTICALLY USEFUL TETRALIN DERIVATIVES III,PROCESSES FOR PREPARATION AND PHARMACEUTICAL PREPARATIONS FOR SUCH COMPOUNDS 审中-公开
标题翻译：可治疗有用的四环素衍生物III，这些化合物的制备和药物制备方法
公开(公告)号：WO1982004042A1
公开(公告)日：1982-11-25
申请号：PCT/SE1982000160
申请日：1982-05-10
申请人： ARVIDSSON FOLKE LARS ERIK , CARLSSON PER ARVID EMIL , HACKSELL ULI ALF , HJORTH JOHN STEPHAN MIKAEL , JOHANSSON ANETTE MARGARETA , LINDBERG PER LENNART , NILSSON JOHN LARS GUNNAR , SANCHEZ DOMINGO , WIKSTROEM HAKAN VILHELM
IPC分类号： C07C93/14
CPC分类号： C07C215/64 , C07C213/00 , C07C213/02 , C07C213/06 , C07C213/08 , C07C213/10
摘要： Compounds of the formula wherein Y is OH, R COO, (R )2NCOO or R O, whereby R is an alkyl group having 1-5 carbon atoms or a possibly substituted phenyl group, R is an alkyl group having 1-5 carbon atoms and R is an allyl or benzyl group, R is an alkyl group having 1-3 carbon atoms, R is an alkyl group having 1-6 carbon atoms, and R is an alkyl group having 1-3 carbon atoms, processes and intermediates for their preparation, pharmaceutical preparations and methods of treatment employing such compounds. The compounds are useful for therapeutic purposes, especially for treatment of disorders in the central nervous system.
摘要翻译：其中Y是OH，R 4 COO，（R 5）2 NCOO或R 6 O的式（IMAGE）化合物，其中R 4是具有1-5个碳原子的烷基或可能的取代的苯基，R 5是具有1-5个碳原子的烷基，R 6是烯丙基或苄基，R 1是具有1-3个碳原子的烷基，R 2是具有1-6个碳原子的烷基，R 3是具有1-3个碳原子的烷基，其制备方法和中间体，药物制剂和使用这些化合物的治疗方法。该化合物可用于治疗目的，特别是用于治疗中枢神经系统疾病。

4. 发明申请

WO1990012795A1 SUBSTITUTED 3-AMINO CHROMANS 审中-公开
标题翻译：取代的3-AMINO CHROMANS
公开(公告)号：WO1990012795A1
公开(公告)日：1990-11-01
申请号：PCT/US1990001587
申请日：1990-03-28
申请人： THE UPJOHN COMPANY , ANDERSSON, Bengt, Ronny , CARLSSON, Per, Arvid, Emil , SVENSSON, Kjell, Anders, Ivan , WIKSTROM, Hakan, Vilhelm , HALLBERG, Anders, Rudolf
发明人： THE UPJOHN COMPANY
IPC分类号： C07D311/58
CPC分类号： C07D311/58
摘要： The present invention is directed to novel chromane derivatives substituted in the 3-position by a substituted amino moiety and substituted on the aromatic ring with one or two substituents. The novel chromane derivatives have useful CNS properties.
摘要翻译：本发明涉及通过取代的氨基部分在3-位上取代并在芳环上被一个或两个取代基取代的新的色原烷衍生物。新的色原衍生物具有有用的CNS性质。

5. 发明申请

WO1994021608A1 INDOLETETRALINS HAVING DOPAMINERGIC ACTIVITY 审中-公开
标题翻译：具有多巴胺活性的吲哚美辛
公开(公告)号：WO1994021608A1
公开(公告)日：1994-09-29
申请号：PCT/US1994002800
申请日：1994-03-21
申请人： THE UPJOHN COMPANY , ANDERSSON, Bengt, Ronny , CARLSSON, Per, Arvid, Emil , HANSSON, Lars, Olov , SONESSON, Clas, Ake , STJERNLOF, Nils, Peter , SVENSSON, Kjell, Anders, Ivan , WATERS, Ross, Nicholas , HAADSMA-SVENSSON, Susanne, R.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D209/60
CPC分类号： C07D209/58 , C07D209/60 , C07D307/92 , C07D307/93 , C07D409/12 , C07D491/04
摘要： A compound of formula (I) and pharmaceutically acceptable salts thereof, where Z is R3 and X and Y form (a), or X is R3 and Y and Z form (a), (b) or (c); R1 and R2 are independently hydrogen, C1-6 alkyl, C3-7 cycloalkyl, -CH2-C3-7 cycloalkyl, phenyl (optionally substituted with halogen or C1-6 alkyl), -thiophenyl (optionally substituted with halogen or C1-6 alkyl), or C1-6 alkyl phenyl; R3 are independently hydrogen, halogen, -O-C1-6 alkyl or C1-6 alkyl; R4 is a valence bond, CH2 or oxygen; R5 and R6 are independently hydrogen, sulfur, -S-C1-6 alkyl, halogen, CON(R3)2, -COCF3, -CO-C1-6 alkyl, -CO phenyl, oxygen, -CHO, CN except that when Y and Z form (b), R1 and R2 are hydrogen or a C1-6 alkyl and R3 is hydrogen, then at least one of R5 and R6 must be other than hydrogen. These compounds and derivatives thereof exhibit dopamine-receptor stimulating activity in mammals which are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders which respond to dopamine-receptor stimulation.
摘要翻译：其中Z是R3，X和Y形成（a），或X是R3和Y和Z形式（a），（b）或（c）的式（I）化合物及其药学上可接受的盐。 R 1和R 2独立地是氢，C 1-6烷基，C 3-7环烷基，-CH 2 -C 3-7环烷基，苯基（任选被卤素或C 1-6烷基取代） - 噻吩基（任选地被卤素或C 1-6烷基）或C 1-6烷基苯基; R 3独立地是氢，卤素，-O-C 1-6烷基或C 1-6烷基; R4是价键，CH2或氧; R 5和R 6独立地是氢，硫，-S-C 1-6烷基，卤素，CON（R 3）2，-COCF 3，-CO-C 1-6烷基，-CO苯基，氧，-CHO，和Z形式（b）中，R 1和R 2是氢或C 1-6烷基，R 3是氢，则R 5和R 6中的至少一个必须不是氢。这些化合物及其衍生物在哺乳动物中表现出多巴胺受体刺激活性，其可用于治疗响应于多巴胺受体刺激的高催乳素血症，溢乳，闭经，阳ence，帕金森综合征，糖尿病，肢端肥大症，高血压和其他中枢神经系统疾病。

6. 发明申请

WO1991011435A1 NEW CENTRALLY ACTING 6,7,8,9-TETRAHYDRO-3H-BENZ(e)INDOLE HETEROCYCLICS 审中-公开
标题翻译：新分离的6,7,8,9-四氢-3H-BENZ（e）吲哚环化合物
公开(公告)号：WO1991011435A1
公开(公告)日：1991-08-08
申请号：PCT/US1991000018
申请日：1991-01-08
申请人： THE UPJOHN COMPANY , WIKSTROM, Hakan, Vilhelm , CARLSSON, Per, Arvid, Emil , ANDERSSON, Bengt, Ronny , SVENSSON, Kjell, Anders, Ivan , ELEBRING, Stig, Thomas , STJERNLOF, Nils, Peter , ROMERO, Arthur, Glenn , HAADSMA, Susanne, Renee , LIN, Chiu-Hong , ENNIS, Michael, Dalton
发明人： THE UPJOHN COMPANY
IPC分类号： C07D209/60

7. 发明申请

WO1990007490A1 HALO SUBSTITUTED AMINOTETRALINS 审中-公开
标题翻译： HALO替代氨基酸
公开(公告)号：WO1990007490A1
公开(公告)日：1990-07-12
申请号：PCT/US1990000015
申请日：1990-01-03
申请人： THE UPJOHN COMPANY , CARLSSON, Per, Arvid, Emil , WIKSTROM, Hakan, Vilhelm , SVENSSON, Kjell, Anders, Ivan , ANDERSSON, Bengt, Ronny , EKMAN, Agneta, Barbro , STJERNLOF, Nils, Peter , SVENSSON, Nils, Arne
发明人： THE UPJOHN COMPANY
IPC分类号： C07C217/74
CPC分类号： C07C217/74 , C07C211/42 , C07C2601/02 , C07C2602/10
摘要： This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of formula (I), wherein X1 is halogen, CF3, -OR3, or -SR4; wherein R3 is alkyl(C1-C8); alkenyl(C1-C8), -CH2-cycloalkyl(C3-C8) or benzyl; wherein R4 is alkyl(C1-C3); wherein X2 is hydrogen, CF3 or halogen; wherein R7 is hydrogen or methyl; wherein R1 is hydrogen, alkyl(C1-C3), or cyclopropylmethyl; wherein R2 is -CH2-cycloalkyl(C3-C8), alkyl(C1-C8), -(CH2)q-R5 or -CH2CH2-Z-(CH2)rCH3; wherein R5 is phenyl, 2-thiophene or 3-thiophene; wherein Z is oxygen or sulfur; and wherein p is 1 or 2, q is 2 or 3, and r is 0 to 3; with the provisos that (1) when X1 is -OR3, X2 is halogen or CF3; and (2) when X1 is halogen, X2 is hydrogen, and p is 2, X1 is in a position other than the 8-position. These compounds are useful to treat central nervous system disorders.
摘要翻译：本发明是治疗上有用的式（I）的四氢化萘及其药学上可接受的酸加成盐，其中X 1是卤素，CF 3，-OR 3或-SR 4; 其中R3是烷基（C1-C8）; 烯基（C1-C8），-CH2-环烷基（C3-C8）或苄基; 其中R4是烷基（C1-C3）; 其中X 2是氢，CF 3或卤素; 其中R7是氢或甲基; 其中R1是氢，烷基（C1-C3）或环丙基甲基; 其中R2是-CH2-环烷基（C3-C8），（C1-C8）烷基， - （CH2）q-R5或-CH2CH2-Z-（CH2）rCH3; 其中R5是苯基，2-噻吩或3-噻吩; 其中Z是氧或硫; 并且其中p为1或2，q为2或3，r为0至3; 条件是（1）当X1为-OR3时，X2为卤素或CF3; 和（2）当X1为卤素时，X2为氢，p为2，X1为8位以外的位置。这些化合物可用于治疗中枢神经系统疾病。

8. 发明申请

WO1989009050A1 THERAPEUTICALLY USEFUL TETRALIN DERIVATIVES 审中-公开
标题翻译：可治疗有用的四环素衍生物
公开(公告)号：WO1989009050A1
公开(公告)日：1989-10-05
申请号：PCT/US1989000974
申请日：1989-03-15
申请人： THE UPJOHN COMPANY , ANDERSSON, Bengt, Ronny , CARLSSON, Per, Arvid, Emil , SVENSSON, Kjell, Anders, Ivan , WIKSTROM, Hakan, Vilhelm
发明人： THE UPJOHN COMPANY
IPC分类号： A61K31/13
CPC分类号： C07D333/20 , C07C217/74 , C07C323/38 , C07C2602/10
摘要： This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of formula (I), wherein -YR1 is one substituent on the 5, 6, 7 or 8 position of the aromatic ring, and is -S(C1-C3) alkyl or OR1 wherein R1 is selected from the group consisting of (C1-C8) alkyl, (C1-C8) alkenyl, -CH2-(C3-C8) cycloalkyl or benzyl; wherein R2 is hydrogen or (C1-C3) alkyl; wherein R3 is -CH2-(C3-C8) cycloalkyl; wherein R4 is hydrogen, (C3-C8) alkyl, -CH2-(C3-C4) cycloalkyl-(CH2)m-R5 or -CH2-CH2-X-(CH2)nCH3; wherein n is zero to 3 and m is 2 or 3; wherein X is oxygen or sulfur; and wherein R5 is phenyl; phenyl substituted with one or two substituent groups selected from chlorine, bromine, fluorine, (C1-C3) alkoxy or (C1-C3) alkyl; 2-thiophene; or 3-thiophene; with the proviso that when R3 contains more than four carbon atoms and R4 is alkyl said alkyl contains from one to 3 carbons atoms.

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