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1. 发明授权

US5610154A Bicyclic carboxamides 失效
标题翻译：双环甲酰胺
公开(公告)号：US5610154A
公开(公告)日：1997-03-11
申请号：US448962
申请日：1995-05-24
申请人： Ian A. Cliffe , Howard L. Mansell , Terence J. Ward , James A. Nelson , Uresh S. Shah , Mira A. Kanzelberger
发明人： Ian A. Cliffe , Howard L. Mansell , Terence J. Ward , James A. Nelson , Uresh S. Shah , Mira A. Kanzelberger
IPC分类号： A61K31/495 , A61K31/55 , A61P9/12 , A61P25/18 , A61P25/20 , A61P43/00 , C07D209/44 , C07D209/52 , C07D223/14 , C07D295/185 , C07D403/12 , C07D451/02 , C07D295/16
CPC分类号： C07D295/185 , C07D209/52 , C07D223/14 , C07D451/02
摘要： Bicyclic carboxamides of formula I ##STR1## and the pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formulaX represents --CR.sup.2 .dbd.CR.sup.2 -- or --(CR.sup.2)q--;m represents 0,1 or 2; n represents 0,1 or 2; p represents 0,1,2 or 3 and q represents 0,1,2 or 3;A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is a mono or bicyclic aryl or heteroaryl radical,R.sup.1 is an aryl or aryl(lower)alkyl radicaland each R.sup.2 is independently hydrogen or lower alkyl.
摘要翻译：式I的双环甲酰胺（I）和药学上可接受的酸加成盐是5-HT1A结合剂，特别是5-HT 1A拮抗剂，并且可以用于例如抗焦虑剂。式X表示-CR2 = CR2-或 - （CR2）q-; m表示0,1或2; n表示0,1或2; p表示0,1,2或3，q表示0,1,2或3; A是任选被一个或多个低级烷基取代的1或2个碳原子的亚烷基链，R是单或双环芳基或杂芳基，R 1是芳基或芳基（低级）烷基，每个R 2独立地是氢或低级烷基。

2. 发明授权

US5430033A Piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：US5430033A
公开(公告)日：1995-07-04
申请号：US234036
申请日：1994-04-22
申请人： Ian A. Cliffe , Anderson D. Ifill , Howard L. Mansell , Terence J. Ward , Alan C. White
发明人： Ian A. Cliffe , Anderson D. Ifill , Howard L. Mansell , Terence J. Ward , Alan C. White
IPC分类号： C07D295/096 , A61K31/495 , C07D401/00 , C07D403/00 , C07D405/00
CPC分类号： C07D295/096
摘要： Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formula R is hydrogen or one or two lower alkyl groups, R.sup.1 is a mono of bicyclic aryl or heteroaryl radical, R.sup.2 is aryl and A is a C.sub.2-5 alkylene chain optionally substituted by lower alkyl.
摘要翻译：式I的哌嗪衍生物（I）及其药学上可接受的酸加成盐是5-HT1A结合剂，特别是5-HT 1A拮抗剂，并且可以用于例如抗焦虑剂。式中R是氢或一个或两个低级烷基，R 1是双环芳基或杂芳基的一个，R 2是芳基，A是任选被低级烷基取代的C 2-5亚烷基链。

3. 发明授权

US5096901A Pharmacologically active amides and esters containing an azabicycloalkane moiety 失效
标题翻译：含有氨基胆碱酯酶的药理学活性氨基酸
公开(公告)号：US5096901A
公开(公告)日：1992-03-17
申请号：US595333
申请日：1990-10-10
申请人： Terence J. Ward , Janet C. White
发明人： Terence J. Ward , Janet C. White
IPC分类号： A61K31/40 , A61K31/435 , A61K31/47 , A61P1/08 , A61P25/18 , A61P43/00 , C07D451/04 , C07D451/14 , C07D453/02 , C07D471/06 , C07D487/08
CPC分类号： C07D451/04 , C07D451/14
摘要： Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O-- or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl or R.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl, andB is a saturated azabicyclic ring (eg tropanyl or quinuclidinyl) or a N-oxide thereof and their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.
摘要翻译：其中R 1为氢或一个或多个特定取代基的化合物，X为-O-或-NR 2 - ，其中R 2为低级烷基，低级烯基，低级炔基，芳基或指定的取代的低级烷基或R 2为基团 - Z-连接到芳环的8位，以形成5至7个环成员的杂环，Y是O或NR 3，其中R 3是氢或低级烷基，B是饱和的氮杂双环（例如奎宁丙基或奎宁环基）或其N-氧化物及其酸加成盐是可用于例如治疗神经精神障碍的5-HT 3拮抗剂。

4. 发明授权

US4959375A Piperidine derivatives useful as 5-HT.sub.3 antagonists 失效
标题翻译：哌啶衍生物可用作5-HT3拮抗剂
公开(公告)号：US4959375A
公开(公告)日：1990-09-25
申请号：US313104
申请日：1989-02-21
申请人： Terence J. Ward
发明人： Terence J. Ward
IPC分类号： C07D211/56 , C07D401/06
CPC分类号： C07D401/06 , C07D211/56
摘要： Piperidine derivatives of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein A represents an aromatic radical selected from ##STR2## wherein R.sup.3 is hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy or halogen; X.sup.1 -X.sup.2 represents CH.sub.2 --CH, NR.sup.4 --CH, O--CH, S--CH, CH.sub.2 --N, O--N, S--N, NR.sup.4 --N, CH--NR.sup.4 or N--NR.sup.4 [where R.sup.4 is hydrogen, (C.sub.1-4)alkyl, phenyl or phenyl(C.sub.1-4)alkyl] or ##STR3## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, trifluoromethyl, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, hydroxy, nitro, amino, (C.sub.1-4)alkylamino, di(C.sub.1-4)alkyl-amino, (C.sub.2-4)alkanoylamino, mercapto or (C.sub.1-4)alkylthio and R.sup.1 and R.sup.2 are independently hydrogen, (C.sub.1-4)alkyl or (C.sub.1-4)alkylphenyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent pyrrolidino or piperidino possess 5-HT.sub.3 -antagonistic activity.
摘要翻译：式（I）的哌啶衍生物及其药学上可接受的酸加成盐，其中A表示选自（a）的芳族基团，其中R 3是氢，（C 1-4）烷基，（C 1-4）烷氧基或卤素; X 1 -X 2表示CH 2 -CH，NR 4 -CH，O-CH，S-CH，CH 2 -N，ON，SN，NR 4 -N，CH-NR 4或N-NR 4 [其中R 4是氢，（C 1-4）烷基，苯基或苯基（C 1-4）烷基]或（b）其中R5，R6，R7和R8独立地是氢，卤素，三氟甲基，（C1-4）烷基，（C1-4）烷氧基，羟基，硝基，氨基，（C 1-4）烷基氨基，二（C 1-4）烷基 - 氨基，（C 2-4）烷酰基氨基，巯基或（C 1-4）烷硫基，R 1和R 2独立地为氢，（C 1-4）烷基或（C 1-4）烷基苯基或R 1和R 2与它们所连接的氮原子一起代表吡咯烷子基或哌啶子基具有5-HT 3拮抗活性。

5. 发明授权

US4722930A 3-benzoyl-1-[(oxo or thioheteroaryl-ylalkyl)-piperid-4-yl]ureas and derivatives 失效
标题翻译： 3-苯甲酰基-1 - [（氧代或硫代杂芳基 - 烷基） - 哌啶-4-基]脲和衍生物
公开(公告)号：US4722930A
公开(公告)日：1988-02-02
申请号：US781832
申请日：1985-09-30
申请人： John L. Archibald , Terence J. Ward
发明人： John L. Archibald , Terence J. Ward
IPC分类号： C07D211/58 , C07D211/72 , C07D213/75 , C07D405/06 , A61K31/445
CPC分类号： C07D213/75 , C07D211/58 , C07D211/72
摘要： The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocylic or heterocyclic ring optionally carrying one or more substituents as defined above; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1, X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is -- CO-- or --CH.sub.2 --, with the proviso that when Ar is unsubstituted phenyl and R.sup.9 is hydrogen then Y is --O--. The compounds of formula I exhibit psychotropic activity and are useful as antidepressants.

6. 发明授权

US4358456A Antipsychotic piperidinomethyl-indole derivatives 失效
标题翻译：抗精神病药哌啶甲基吲哚衍生物
公开(公告)号：US4358456A
公开(公告)日：1982-11-09
申请号：US257829
申请日：1981-04-27
申请人： Terence J. Ward
发明人： Terence J. Ward
IPC分类号： C07D401/06 , A61K31/445
CPC分类号： C07D401/06
摘要： The invention relates to compounds of formula II ##STR1## and their pharmaceutically acceptable salts wherein R.sup.5 represents hydrogen, acyl, lower alkyl or cycloalkyl; R.sup.6 represents hydrogen, halogen, trifluormethyl, or lower alkyl; R.sup.7 represents hydrogen, lower alkyl, hydroxy, lower alkoxy, arylloweralkoxy; R.sup.8 represents hydrogen or lower alkyl; and R.sup.9 represents hydrogen or lower alkyl.The compounds have dopamine blockade activity and may be used in the treatment of psychoses including schizophrenia.
摘要翻译：本发明涉及式II化合物及其药学上可接受的盐，其中R5代表氢，酰基，低级烷基或环烷基; R6表示氢，卤素，三氟甲基或低级烷基; R7表示氢，低级烷基，羟基，低级烷氧基，芳基低级烷氧基; R8代表氢或低级烷基; 并且R 9表示氢或低级烷基。该化合物具有多巴胺阻断活性，可用于治疗包括精神分裂症在内的精神病。

7. 发明授权

US4235915A .beta.Adrenergic blocking piperidino ureas and thioureas 失效
标题翻译： β-肾上腺素能阻断哌啶子基脲和硫脲
公开(公告)号：US4235915A
公开(公告)日：1980-11-25
申请号：US857334
申请日：1977-12-05
申请人： John L. Archibald , Terence J. Ward
发明人： John L. Archibald , Terence J. Ward
IPC分类号： C07D319/20 , A61K31/445
CPC分类号： C07D319/20
摘要： Compounds of formula ##STR1## in which X represents oxygen or sulphur;Y represents --CHOH-- or ##STR2## Z represents ##STR3## or a direct bond; R represents cycloalkyl group having 5 to 7 carbon atoms or an optionally substituted aryl or heteroaryl radical, or when --Z-- is a direct bond R also represents hydrogen;R.sup.1 represents hydrogen or lower alkyl.andR.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy;ora pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which reduce heart rate or have hyperglycaemic activity.
摘要翻译：式（I）的化合物，其中X表示氧或硫; Y表示-CHOH-或Z表示或直接键; R表示具有5至7个碳原子的环烷基或任选取代的芳基或杂芳基，或当-Z-是直接键时，R也表示氢; R1表示氢或低级烷基。并且R 2表示氢，卤素，低级烷基或低级烷氧基; 或其药学上可接受的酸加成盐或季铵盐，其可降低心率或具有高血糖活性。

8. 发明授权

US5622951A Piperazine derivatives as 5-HT antagonists 失效
标题翻译：哌嗪衍生物作为5-HT拮抗剂
公开(公告)号：US5622951A
公开(公告)日：1997-04-22
申请号：US436413
申请日：1995-05-24
申请人： Terence J. Ward , Mark A. Ashwell
发明人： Terence J. Ward , Mark A. Ashwell
IPC分类号： C07D295/08 , A61K31/495 , A61P43/00 , C07D213/30 , C07D213/36 , C07D217/22 , C07D239/42 , C07D295/096 , A61K31/405 , C07D403/04
CPC分类号： C07D295/096 , C07D213/36 , C07D217/22 , C07D239/42 , C07C2101/14
摘要： Piperazine derivatives of formula (I) and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, R and R.sup.3 are hydrogen or lower alkyl or R.sup.3 is spirocycloalkyl, R.sup.1 and R.sup.2 are aryl or heteroaryl radicals and n is 1 or 2 and m is 1 to 3 and the total of n+m is 2-4. ##STR1##
摘要翻译： PCT No.PCT / GB93 / 02661 Sec。 371日期：1995年5月24日 102（e）日期1995年5月24日PCT 1993年12月24日PCT公布。公开号WO94 / 15928 日期1994年7月21日式（I）的哌嗪衍生物及其药学上可接受的盐是5-HT1A结合剂，可以用作例如抗焦虑剂。在该式中，R 3和R 3为氢或低级烷基或R 3为螺环烷基，R 1和R 2为芳基或杂芳基，n为1或2，m为1至3，n + m的总数为2-4。（一）

9. 发明授权

US5436251A Treatment of anxiety and gastrointestinal disorders with azabicyclo carbonyl-2-(cyclopropylmethyloxy)benzamide 失效
标题翻译：用氮杂双环羰基-2-（环丙基甲氧基）苯甲酰胺治疗焦虑和胃肠道疾病
公开(公告)号：US5436251A
公开(公告)日：1995-07-25
申请号：US106461
申请日：1993-08-13
申请人： Terence J. Ward , Gerald Bradley
发明人： Terence J. Ward , Gerald Bradley
IPC分类号： A61K31/435 , A61K31/44
CPC分类号： A61K31/435
摘要： (Endo)-N-[[[8-azabicyclo[3.2.1]octan-3-yl]amino]carbonyl]-2-(cyclopropylmethyloxy)benzamide and pharmaceutically acceptable salts thereof possess 5-HT.sub.3 antagonistic activity and are useful in the treatment of neuro-psychiatric disorders (e.g. anxiety), gastro-intestinal disorders and migraine.
摘要翻译：（内部）-N - [[[8-氮杂双环[3.2.1]辛-3-基]氨基]羰基] -2-（环丙基甲氧基）苯甲酰胺及其药学上可接受的盐具有5-HT 3拮抗活性，治疗神经精神障碍（如焦虑症），胃肠道疾病和偏头痛。

10. 发明授权

US5212179A Piperidine derivatives 失效
公开(公告)号：US5212179A
公开(公告)日：1993-05-18
申请号：US603109
申请日：1990-10-25
申请人： John L. Archibald , Terence J. Ward
发明人： John L. Archibald , Terence J. Ward
IPC分类号： C07D211/58 , C07D211/72 , C07D213/75 , C07D401/12
CPC分类号： C07D213/75 , C07D211/58 , C07D211/72 , C07D401/12
摘要： The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocylic or heterocyclic ring optionally carrying one or more substituents as defined above; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.2 --, with the proviso that when Ar is unsubstituted phenyl and R.sup.9 is hydrogen then Y is --O--. The compounds of formula I exhibit psychotropic activity and are useful as antidepressants.

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