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1. 发明授权

US5288748A Centrally acting 6,7,8,9-tetrahydro-3H-benz(e)indole heterocyclics 失效
标题翻译：中心作用的6,7,8,9-四氢-3H-苯并（e）吲哚杂环
公开(公告)号：US5288748A
公开(公告)日：1994-02-22
申请号：US907932
申请日：1992-07-01
申请人： Hakan V. Wikstrom , Per A. E. Carlsson , Bengt R. Andersson , Kjell A. I. Svensson , Stig T. Elebring , Nils P. Stjernlof , Arthur G. Romero , Susanne R. Haadsma-Svensson , Chiu-Hong Lin , Michael D. Ennis
发明人： Hakan V. Wikstrom , Per A. E. Carlsson , Bengt R. Andersson , Kjell A. I. Svensson , Stig T. Elebring , Nils P. Stjernlof , Arthur G. Romero , Susanne R. Haadsma-Svensson , Chiu-Hong Lin , Michael D. Ennis
IPC分类号： A61K31/40 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/4427 , A61K31/4433 , A61K31/454 , A61K31/475 , A61P11/14 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D209/56 , C07D209/60 , C07D209/66 , C07D401/06 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/04 , C07D471/04 , C07D491/04 , C07D491/052 , C07D495/04
CPC分类号： C07D401/12 , C07D209/66 , C07D409/12 , C07D491/04
摘要： A compound of Formula I ##STR1## or pharmaceutically acceptable salts of Formula I, where R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, --(CH.sub.2).sub.n CONH.sub.2 where n is 2 to 6, (CH2).sub.n -1-(4,4-dimethylpiperidine-2,6-dione-yl), or cyclopropylmethyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl or combined with R.sup.1 to form a C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 akynyl, (CH.sub.2).sub.n --R"--Ar where R" is O, S, or NH, 3,3,3-trifluoropropyl, --(CH.sub.2).sub.m --R.sup.9 where m is 2 or 3 and R.sup.9 is phenyl, 2-thienyl or 3-thienyl; R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, formyl, CN, halogen, CH.sub.2 OR.sup.2, C(O)C(O)OR.sup.1, C(O)CO NR.sup.1 R.sup.2, --(CH.sub.2).sub.q --NR.sup.1 R.sup.2 where q is 0 to 5, C.dbd.NOR.sup.2, 2(4,5-dihydro)oxazolyl, or COR.sup.10 where R.sup.10 is H, R.sup.1, NR.sup.1 R.sup.2 or CF.sub.3 ; R.sup.4 is hydrogen, C.sub.1 -C.sub.3 alkyl, cyclopropylmethyl, CF.sub.3, 2,2,2-trifluoroethyl, CN, CONR.sup.1 R.sup.2, .dbd.O, 2(4,5-dihydro)imidazolyl, 2(4,5-dihydro)oxazolyl, 2-oxazolyl, 3-oxadiazolyl, or 3,3,3-trifluoropropyl; R.sup.5 is hydrogen, R.sup.1, OCH.sub.3, C(O)CH.sub.3 or C(O)OR.sup.1 ; X is (a) a valence bond, (b) CH.sub.2, or (c) O, S or NR.sup.5 where R.sup.5 is H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, benzyl, COR.sup.6 where R.sup.6 is a C.sub.1 -C.sub.3 alkyl, phenyl, or CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are independently H or C.sub.1 -C.sub.3 alkyl; andZ is a hydrogen or halogen;provided that when X is CH.sub.2, at least one of R.sub.3 and R.sub.4 is other than hydrogen or C.sub.1 -C.sub.3 alkyl. The compounds of Formula I are suitable for treating disorders of the central nervous system, particularly as 5-HT.sub.1A receptor agonists.
摘要翻译：其中R1为H，C1-C3烷基， - （CH2）nCONH2，其中n为2-6，（CH2）n-1-（4,4-二甲氧基苯基）二甲基哌啶-2,6-二酮基）或环丙基甲基; R2是氢，C1-C8烷基，C3-C8环烷基或与R1结合以形成C 3 -C 8环烷基，C 2 -C 8烯基，C 2 -C 8炔基，（CH 2）n -R“'Ar，其中R” O，S或NH，3,3,3-三氟丙基， - （CH 2）m -R 9，其中m为2或3，R 9为苯基，2-噻吩基或3-噻吩基; R3是氢，C1-C3烷基，2,2,2-三氟乙基，3,3,3-三氟丙基，甲酰基，CN，卤素，CH2OR2，C（O）C（O）OR1，C（O） - （CH2）q-NR1R2其中q为0至5，C = NOR2,2（4,5-二氢）恶唑基或COR 10，其中R 10为H，R 1，NR 1 R 2或CF 3; R4是氢，C1-C3烷基，环丙基甲基，CF3,2,2,2-三氟乙基，CN，CONR1R2，= 2,2（4,5-二氢）咪唑基，2（4,5-二氢）恶唑基，恶唑基，3-恶二唑基或3,3,3-三氟丙基; R5是氢，R1，OCH3，C（O）CH3或C（O）OR1; X是（a）价键，（b）CH 2或（c）O，S或NR 5，其中R 5是H，C 1 -C 8烷基，C 3 -C 8环烷基，苄基，COR 6，其中R 6是C 1 -C 3烷基，苯基或CONR 7 R 8，其中R 7和R 8独立地为H或C 1 -C 3烷基; Z为氢或卤素; 条件是当X是CH 2时，R 3和R 4中的至少一个不是氢或C 1 -C 3烷基。式I化合物适用于治疗中枢神经系统疾病，特别是5-HT 1A受体激动剂。

2. 发明授权

US5225596A Halo substituted aminotetralins 失效
标题翻译：卤代替氨基四氢化萘
公开(公告)号：US5225596A
公开(公告)日：1993-07-06
申请号：US721532
申请日：1991-07-08
申请人： Per A. E. Carlsson , Hakan V. Wikstrom , Kjell A. I. Svensson , Bengt R. Andersson , Barbro A. Ekman , Nils P. Stjernlof , Nils A. Svensson
发明人： Per A. E. Carlsson , Hakan V. Wikstrom , Kjell A. I. Svensson , Bengt R. Andersson , Barbro A. Ekman , Nils P. Stjernlof , Nils A. Svensson
IPC分类号： C07C211/42 , C07C217/74
CPC分类号： C07C211/42 , C07C217/74 , C07C2101/02 , C07C2102/10
摘要： This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## wherein X.sub.1 is halogen, CF.sub.3, --OR.sub.3, or --SR.sub.4 ; wherein R.sub.3 is alkyl(C.sub.1 -C.sub.8); alkenyl(C.sub.1 -C.sub.8); --CH.sub.2 -cycloalkyl(C.sub.3 -C.sub.8) or benzyl; wherein R.sub.4 is alkyl(C.sub.1 -C.sub.3); wherein X.sub.2 is hydrogen, CF.sub.3 or halogen; wherein R.sub.7 is hydrogen or methyl; wherein R.sub.1 is hydrogen, alkyl(C.sub.1 -C.sub.3), or cyclopropylmethyl; wherein R.sub.2 is --CH.sub.2 -cycloalkyl(C.sub.3 -C.sub.8), alkyl(C.sub.1 -C.sub.8), --(CH.sub.2).sub.q --R.sub.5 or --CH.sub.2 CH.sub.2 --Z--(CH.sub.2).sub.r CH.sub.3 ; wherein R.sub.5 is phenyl, 2-thiophene or 3-thiophene; wherein Z is oxygen or sulfur; and wherein p is one or 2, q is 2 or 3, and r is zero to 3; with the provisos that (1) when X.sub.1 is --OR.sub.3, X.sub.2 is halogen or CF.sub.3 ; and (2) when X.sub.1 is halogen, X.sub.2 is hydrogen, and p is 2, X.sub.1 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化合物及其药学上可接受的酸式加成盐，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）; -CH 2 - 环烷基（C 3 -C 8）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是1或2，q是2或3，并且r是0-3; 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。

3. 发明授权

US4612316A Tricyclic amines with central dopaminergic activity 失效
标题翻译：具有中枢多巴胺能活性的三环胺
公开(公告)号：US4612316A
公开(公告)日：1986-09-16
申请号：US601981
申请日：1984-04-19
申请人： Bengt R. Andersson , Folke L. Arvidsson , Per A. E. Carlsson , John S. M. Hjort , Anette M. Johansson , Per L. Lindberg , John L. G. Nilsson , Domingo Sanchez , Kjell A. I. Svensson , Hakan V. Wikstrom
发明人： Bengt R. Andersson , Folke L. Arvidsson , Per A. E. Carlsson , John S. M. Hjort , Anette M. Johansson , Per L. Lindberg , John L. G. Nilsson , Domingo Sanchez , Kjell A. I. Svensson , Hakan V. Wikstrom
IPC分类号： A61K31/435 , A61P25/00 , C07D20060101 , C07D221/10 , C07D401/12 , C07D413/12 , C07D417/12 , C07D419/12 , A61K31/445
CPC分类号： C07D221/10
摘要： Compounds of the formula ##STR1## wherein C.sup.1 and N.sup.4 are in trans configuration to each other, wherein R and Y are defined herein below, as bases and pharmaceutically acceptable acid addition salts thereof, processes for their preparation and pharmaceutical preparations and methods of treatment employing such compounds. The compounds are useful for treatment of disorders in the central nervous system.
摘要翻译：其中C1和N4彼此反式构型，其中R和Y定义如下的化合物作为碱及其药学上可接受的酸加成盐，其制备方法和药物制剂以及治疗方法使用这种化合物。该化合物可用于治疗中枢神经系统疾病。

4. 发明授权

US5462947A Centrally acting substituted phenylazacycloalkanes 失效
公开(公告)号：US5462947A
公开(公告)日：1995-10-31
申请号：US133606
申请日：1993-10-12
申请人： Kjell A. I. Svensson , Hakan V. Wikstrom , Per A. E. Carlsson , Anna M. P. Boije , R. Nicholas Waters , Clas A. Sonesson , Nils P. Stjernlof , Bengt R. Andersson , Lars O. Hansson
发明人： Kjell A. I. Svensson , Hakan V. Wikstrom , Per A. E. Carlsson , Anna M. P. Boije , R. Nicholas Waters , Clas A. Sonesson , Nils P. Stjernlof , Bengt R. Andersson , Lars O. Hansson
IPC分类号： A61K31/44 , A61K31/40 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/535 , A61K31/55 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P43/00 , C07D207/08 , C07D207/09 , C07D211/08 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/34 , C07D211/76 , C07D223/04 , C07D227/04 , C07D401/00 , C07D401/10 , C07D403/00 , C07D405/00 , C07D405/10 , C07D409/06 , C07D409/10 , C07D411/10 , C07D413/00 , C07D413/10 , C07D417/00 , C07D455/02 , C07D471/04 , C07D487/04
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 ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2-- or 4--CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub. 2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, --(CH.sub.2).sub.m --R.sup.5 (where m is 1-8), CH.sub.2 SCH.sub.3 or a C.sub.4 -C.sub.8 alkylene bonded to said nitrogen and one of its adjacent carbon atoms inclusive whereby a heterocyclic structure is formed; R.sup.4 and R are independently selected from hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, --(CH.sub.2).sub.m --R.sup.5 where m is 1-8; R.sup.5 is phenyl, phenyl (substituted with a CN, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl), 2-thiophenyl, 3-thiophenyl, --NR.sup.6 CONR.sup.6 R.sup.7, or --CONR.sup.6 R.sup.7 ; R.sup.6 and R.sup.7 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkylmethyl, C.sub.2 -C.sub.8 alkenyl or C.sub.2 -C.sub.8 alkynyl; and with the proviso that when R.sup.1 is CN, R.sup.2 and R.sup.4 are H, R.sup.3 is n-Pr and n is 1, then such compound is a pure enantiomer, and when R.sup.1 or R.sup.2 is OH, halogen, CONH.sub.2 or alkyl, then R.sup.4 is not hydrogen. 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.

5. 发明授权

US5214156A Therapeutically useful tetralin derivatives 失效
标题翻译：治疗上有用的四氢化萘衍生物
公开(公告)号：US5214156A
公开(公告)日：1993-05-25
申请号：US866391
申请日：1992-04-10
申请人： Bengt R. Andersson , Per Arvid E. Carlsson , Kjell A. I. Svensson , Hakan V. Wikstrom
发明人： Bengt R. Andersson , Per Arvid E. Carlsson , Kjell A. I. Svensson , Hakan V. Wikstrom
IPC分类号： C07C217/74 , C07C323/38 , C07D333/20
CPC分类号： C07C323/38 , C07C217/74 , C07D333/20 , C07C2102/10
摘要： This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## wherein YR.sub.1 is OR.sub.1 at the 8 position where R.sub.1 is --CH.sub.2 --(C.sub.3-8 cycloalkyl);R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 is --CH.sub.2 --(C.sub.3-8 cycloalkyl);R.sub.4 is hydrogen, C.sub.1-8 alkyl, --CH.sub.2 --(C.sub.3-4 cycloalkyl), --(CH.sub.2).sub.m --R.sub.5 or --CH.sub.2 --CH.sub.2 --X--(CH.sub.2).sub.n CH.sub.3 ; n is zero to 3 and m is 2 or 3; X is oxygen or sulfur;R.sub.5 is phenyl, C.sub.1-3 alkoxy, C.sub.1-3 alkyl, 2-thiophene, 3-thiophene, or phenyl substituted with one or two substituent groups selected from chlorine, bromine or fluorine; and with the proviso that when R.sub.3 contains more than four carbon atoms and R.sub.4 is alkyl, said alkyl contains from 1 to 3 carbon atoms.Alternatively, --YR.sub.1 is --S--(C.sub.1-3 alkyl) at the 5, 6, 7 or 8 position of the aromatic ring or OR.sub.1 at the 8 position where R.sub.1 is selected from the group consisting of C.sub.1-8 alkyl, C.sub.2-8 alkenyl, --CH.sub.2 --(C.sub.3-8 cycloalkyl) or benzyl;R.sub.2 is hydrogen or (C.sub.1 -C.sub.3) alkyl;R.sub.3 is --CH.sub.2 --(C.sub.3 -C.sub.8) cycloalkyl;R.sub.4 is --(CH.sub.2).sub.m --(2-thiophenyl or 3-thiophenyl); and m is 2 or 3.
摘要翻译：本发明是治疗上有用的式Ⅰ化合物及其药学上可接受的酸加成盐，其中YR1为OR1，其中R1为-CH2-（C3-8环烷基）; R2是氢或C1-3烷基; R3是-CH2-（C3-8环烷基）; R 4是氢，C 1-8烷基，-CH 2 - （C 3-4环烷基）， - （CH 2）m -R 5或-CH 2 -CH 2 -X-（CH 2）n CH 3; n为0〜3，m为2或3; X是氧或硫; R5是苯基，C1-3烷氧基，C1-3烷基，2-噻吩，3-噻吩或被一个或两个选自氯，溴或氟的取代基取代的苯基; 并且条件是当R 3含有多于4个碳原子且R 4是烷基时，所述烷基含有1至3个碳原子。或者，-YR1是芳环的5,6,7或8位的-S-（C1-3烷基）或在8位的OR1，其中R1选自C1-8烷基，C2- 8链烯基，-CH 2 - （C 3-8环烷基）或苄基; R2是氢或（C1-C3）烷基; R3是-CH2-（C3-C8）环烷基; R4是 - （CH2）m-（2-噻吩基或3-噻吩基）; m为2或3。

6. 发明授权

US4937346A Phenyl-azacykloalkanes 失效
标题翻译：苯基 - 氮杂烷烃
公开(公告)号：US4937346A
公开(公告)日：1990-06-26
申请号：US126916
申请日：1987-11-30
申请人： Folke L. Arvidsson , Per A. E. Carlsson , Uli A. Hacksell , John S. M. Hjorth , Per L. Lindberg , John L. G. Nilsson , Domingo Sanchez , Nils U. E. Svensson , Hakan V. Wikstrom
发明人： Folke L. Arvidsson , Per A. E. Carlsson , Uli A. Hacksell , John S. M. Hjorth , Per L. Lindberg , John L. G. Nilsson , Domingo Sanchez , Nils U. E. Svensson , Hakan V. Wikstrom
IPC分类号： C07D207/08 , C07D211/22 , C07D211/26 , C07D211/34 , C07D213/16 , C07D213/30
CPC分类号： C07D213/16 , C07D207/08 , C07D211/22 , C07D211/26 , C07D211/34 , C07D213/30
摘要： Compound of the formula ##STR1## wherein n is 1 or 2, Y is OH, R.sup.1 COO--, R.sup.2 R.sup.3 NCOO-- or R.sup.4 O whereby R.sup.1 is an alkyl group, or a possibly substituted phenyl group, R.sup.2 is an alkyl, phenethyl, or benzyl or phenyl group, R.sup.3 is H or an alkyl group and R.sup.4 is an allyl or benzyl group, and R is an alkyl, hydroxyalkyl, dimethylaminoalkyl or methylthioalkyl group or alkenyl group, processes for their 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n为1或2的化合物，Y为OH，R 1 COO - ，R 2 R 3 NCOO-或R 4，由此R 1为烷基或可能被取代的苯基，R 2为烷基，苯乙基或苄基或苯基，R3是H或烷基，R4是烯丙基或苄基，R是烷基，羟基烷基，二甲基氨基烷基或甲硫基烷基或烯基，它们的制备方法和使用这些化合物的处理方法。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。

7. 发明授权

US5461061A Centrally acting 6,7,8,9-tetrahydro-3H-benz(E)indole heterocyclics 失效
标题翻译：中心作用的6,7,8,9-四氢-3H-苯并（E）吲哚杂环
公开(公告)号：US5461061A
公开(公告)日：1995-10-24
申请号：US144857
申请日：1993-10-28
申请人： Hakan V. Wikstrom , Per A. E. Carlsson , Bengt R. Andersson , Kjell A. I. Svensson , Stig T. Elebring , Nils P. Stjernlof , Arthur G. Romero , Susanne R. Haadsma-Svensson , Chiu-Hong Lin , Michael D. Ennis
发明人： Hakan V. Wikstrom , Per A. E. Carlsson , Bengt R. Andersson , Kjell A. I. Svensson , Stig T. Elebring , Nils P. Stjernlof , Arthur G. Romero , Susanne R. Haadsma-Svensson , Chiu-Hong Lin , Michael D. Ennis
IPC分类号： A61K31/40 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/4427 , A61K31/4433 , A61K31/454 , A61K31/475 , A61P11/14 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D209/56 , C07D209/60 , C07D209/66 , C07D401/06 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/04 , C07D471/04 , C07D491/04 , C07D491/052 , C07D495/04
CPC分类号： C07D401/12 , C07D209/66 , C07D409/12 , C07D491/04
摘要： A compound of Formula I ##STR1## or pharmaceutically acceptable salts of Formula I, where R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, --(CH.sub.2).sub.n CONH.sub.2 where n is 2 to 6, (CH2).sub.n -1-(4,4-dimethylpiperidine-2,6-dione-yl), or cyclopropylmethyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl or combined with R.sup.1 to form a C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 akynyl, (CH.sub.2).sub.n --X--Ar where X is O, S, or NH, 3,3,3-trifluoropropyl, --(CH.sub.2).sub.m --R.sup.9 where m is 2 or 3 and R.sup.9 is phenyl, 2-thiophenyl or 3-thiophenyl; R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, formyl, CN, halogen, CH.sub.2 OR.sup.2, C(O)C(O)OR.sup.1, C(O)CO NR.sup.1 R.sup.2, --(CH.sub.2).sub.q --NR.sup.1 R.sup.2 where q is 0 to 5, C.dbd.NOR.sup.2, 2(4,5-dihydro)oxazolyl, or COR.sup.10 where R.sup.10 is H, R.sup.1, NR.sup.1 R.sup.2 or CF.sub.3 ; R.sup.4 is hydrogen, C.sub.1 -C.sub.3 alkyl, cyclopropylmethyl, CF.sub.3, 2,2,2-trifluoroethyl, CN, CONR.sup.1 R.sup.2, .dbd.O, 2(4,5-dihydro)imidazolyl, 2(4,5-dihydro)oxazolyl, 2-oxazolyl, 3-oxadiazolyl, or 3,3,3-trifluoropropyl; R.sup.5 is hydrogen, R.sup. 1, OCH.sub.3, C(O)CH.sub.3 or C(O)OR.sup.1 ; X is (a) a valence bond, (b) CH.sub.2, or (c) O, S or NR.sup.5 where R.sup.5 is H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, benzyl, COR.sup.6 where R.sup.6 is a C.sub.1 -C.sub.3 alkyl, phenyl, or CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are independently H or C.sub.1 -C.sub.3 alkyl; andZ is a hydrogen or halogen;provided that when X is CH.sub.2, at least one of R.sub.3 and R.sub.4 is other than hydrogen or C.sub.1 -C.sub.3 alkyl. The compounds of Formula I are suitable for treating disorders of the central nervous system, particularly as 5-HT.sub.1A receptor agonists.
摘要翻译：其中R1为H，C1-C3烷基， - （CH2）nCONH2，其中n为2-6，（CH2）n-1-（4,4-二甲氧基苯基）二甲基哌啶-2,6-二酮基）或环丙基甲基; R2是氢，C1-C8烷基，C3-C8环烷基或与R1结合以形成C 3 -C 8环烷基，C 2 -C 8烯基，C 2 -C 8炔基，（CH 2）n X-Ar，其中X是O，S或NH ，3,3,3-三氟丙基， - （CH 2）m -R 9，其中m为2或3，R 9为苯基，2-噻吩基或3-噻吩基; R3是氢，C1-C3烷基，2,2,2-三氟乙基，3,3,3-三氟丙基，甲酰基，CN，卤素，CH2OR2，C（O）C（O）OR1，C（O） - （CH2）q-NR1R2其中q为0至5，C = NOR2,2（4,5-二氢）恶唑基或COR 10，其中R 10为H，R 1，NR 1 R 2或CF 3; R4是氢，C1-C3烷基，环丙基甲基，CF3,2,2,2-三氟乙基，CN，CONR1R2，= 2,2（4,5-二氢）咪唑基，2（4,5-二氢）恶唑基，恶唑基，3-恶二唑基或3,3,3-三氟丙基; R 5是氢，R 1，OCH 3，C（O）CH 3或C（O）OR 1; X是（a）价键，（b）CH 2或（c）O，S或NR 5，其中R 5是H，C 1 -C 8烷基，C 3 -C 8环烷基，苄基，COR 6，其中R 6是C 1 -C 3烷基，苯基或CONR 7 R 8，其中R 7和R 8独立地为H或C 1 -C 3烷基; Z为氢或卤素; 条件是当X是CH 2时，R 3和R 4中的至少一个不是氢或C 1 -C 3烷基。式I化合物适用于治疗中枢神经系统疾病，特别是5-HT 1A受体激动剂。

8. 发明授权

US5306830A Substituted 3-amino chromans 失效
标题翻译：取代的3-氨基苯并二氢吡喃
公开(公告)号：US5306830A
公开(公告)日：1994-04-26
申请号：US994073
申请日：1992-12-21
申请人： Bengt R. Andersson , Per A. E. Carlsson , Kjell A. I. Svensson , Hakan V. Wikstrom , Anders R. Hallberg
发明人： Bengt R. Andersson , Per A. E. Carlsson , Kjell A. I. Svensson , Hakan V. Wikstrom , Anders R. Hallberg
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. ##STR1##
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。（*化学结构*）

9. 发明授权

US4426386A Substituted phenyl piperidines 失效
标题翻译：取代的苯基哌啶
公开(公告)号：US4426386A
公开(公告)日：1984-01-17
申请号：US213633
申请日：1980-12-05
申请人： Folke L. Arvidsson , Per A. E. Carlsson , Uli A. Hacksell , John S. M. Hjorth , Per. L. Lindberg , John L. G. Nilsson , Domingo Sanchez , Nils U. E. Svensson , Hakan V. Wikstrom
发明人： Folke L. Arvidsson , Per A. E. Carlsson , Uli A. Hacksell , John S. M. Hjorth , Per. L. Lindberg , John L. G. Nilsson , Domingo Sanchez , Nils U. E. Svensson , Hakan V. Wikstrom
IPC分类号： A61K31/40 , A61K31/445 , A61K31/451 , A61P25/00 , A61P25/18 , C07D207/00 , C07D207/08 , C07D211/00 , C07D211/12 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/34 , C07D213/16 , C07D213/30 , C07D213/55 , C07D211/32
CPC分类号： C07D213/16 , C07D207/08 , C07D211/22 , C07D211/26 , C07D211/34 , C07D213/30
摘要： Compounds of the formula ##STR1## wherein n is 1 or 2, Y is OH, R.sup.1 COO--, R.sup.2 R.sup.3 NCOO-- or R.sup.4 O whereby R.sup.1 is an alkyl group, or a possibly substituted phenyl group, R.sup.2 is an alkyl, phenethyl, benzyl or phenyl group, R.sup.3 is H or an alkyl group and R.sup.4 is an allyl or benzyl group, and R is an alkyl, hydroxyalkyl, dimethylaminoalkyl or methylthioalkyl group or alkenyl group, processes for their preparation and 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n为1或2，Y为OH，R1COO-，R2R3NCOO-或R4O，其中R1为烷基或可能取代的苯基，R2为烷基，苯乙基，苄基或苯基的式基团，R3是H或烷基，R4是烯丙基或苄基，R是烷基，羟基烷基，二甲基氨基烷基或甲硫基烷基或烯基，其制备方法和药物制剂以及使用这些化合物的处理方法。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。

10. 发明授权

US5594024A Centrally actig substituted phenylazacycloalkanes 失效
公开(公告)号：US5594024A
公开(公告)日：1997-01-14
申请号：US455474
申请日：1995-05-31
申请人： Kjell A. I. Svensson , Hakan V. Wikstrom , Per A. E. Carlsson , Anna M. P. Boije , R. Nicholas Waters , Clas A. Sonesson , Nils P. Stjernlof , Bengt R. Andersson , Lars O. Hansson
发明人： Kjell A. I. Svensson , Hakan V. Wikstrom , Per A. E. Carlsson , Anna M. P. Boije , R. Nicholas Waters , Clas A. Sonesson , Nils P. Stjernlof , Bengt R. Andersson , Lars O. Hansson
IPC分类号： A61K31/44 , A61K31/40 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/535 , A61K31/55 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P43/00 , C07D207/08 , C07D207/09 , C07D211/08 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/34 , C07D211/76 , C07D223/04 , C07D227/04 , C07D401/00 , C07D401/10 , C07D403/00 , C07D405/00 , C07D405/10 , C07D409/06 , C07D409/10 , C07D411/10 , C07D413/00 , C07D413/10 , C07D417/00 , C07D455/02 , C07D471/04 , C07D487/04 , C07D207/04
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 or Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2- or 4-CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, --(CH.sub.2).sub.m --R.sup.5 (where m is 1-8), CH.sub.2 SCH.sub.3 or a C.sub.4 -C.sub.8 alkylene bonded to said nitrogen and one of its adjacent carbon atoms inclusive whereby a heterocyclic structure is formed; R.sup.4 and R are independently selected from hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, --(CH.sub.2).sub.m --R.sup.5 where m is 1-8; R.sup.5 is phenyl, phenyl (substituted with a CN, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl), 2-thiophenyl, 3-thiophenyl, --NR.sup.6 CONR.sup.6 R.sup.7, or --CONR.sup.6 R.sup.7 ; R.sup.6 and R.sup.7 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkylmethyl, C.sub.2 -C.sub.8 alkenyl or C.sub.2 -C.sub.8 alkynyl; and with the proviso that when R.sup.1 is CN, R.sup.2 and R.sup.4 are H, R.sup.3 is n-Pr and n is 1, then such compound is a pure enantiomer, and when R.sup.1 or R.sup.2 is OH, halogen, CONH.sub.2 or alkyl, then R.sup.4 is not hydrogen. 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.

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