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1. 发明申请

WO1995033723A1 PHENOXYALKYL SUBSTITUTED PIPERIDINES, PYRROLIDINES, MORPHOLINES AND THIOMORPHOLINES AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：苯氧基取代的哌啶，吡咯烷酮，吗啉和三羟基磷酰胺作为钙通道拮抗剂
公开(公告)号：WO1995033723A1
公开(公告)日：1995-12-14
申请号：PCT/EP1995002003
申请日：1995-05-24
申请人： SMITHKLINE BEECHAM PLC , BROWN, Thomas, Henry , COPPER, David, Gwyn
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D211/22
CPC分类号： C07D211/22
摘要： Compounds of formula (I), in which W is -(CH2)4, (CH2)5, -(CH2)2O(CH2)2 or -(CH2)2S(CH2)2 n is 0 to 6; m is 0 to 3; A is a bond, -CH=CH-, -CC-, oxygen, sulphur or NR ; R is hydrogen, C1-8alkyl or phenyl C1-4alkyl; and Ar is a group (a) where X is a bond, O, CH2, CO or OCH2 and Hal is fluoro or chloro; and salts thereof are calcium channel antagonists with activity in neurons and are useful in the treatment of conditions such as ischaemic stroke.
摘要翻译：其中W为 - （CH 2）4，（CH 2）5， - （CH 2）2 O（CH 2）2或 - （CH 2）2 S（CH 2）2 n的式（I）化合物为0至6; m为0〜3; A是键，-CH = CH-，-CC-，氧，硫或NR 1; R 1是氢，C 1-8烷基或苯基C 1-4烷基; 并且Ar是其中X是键的基团（a），O，CH 2，CO或OCH 2，Hal是氟或氯; 其盐是在神经元中具有活性的钙通道拮抗剂，可用于治疗缺血性中风等病症。

2. 发明申请

WO1992002501A1 3-SUBSTITUTED PIPERIDINE DERIVATIVES 审中-公开
标题翻译： 3-取代的哌啶衍生物
公开(公告)号：WO1992002501A1
公开(公告)日：1992-02-20
申请号：PCT/GB1991001339
申请日：1991-08-05
申请人： SMITHKLINE & FRENCH LABORATORIES LIMITED , BROWN, Thomas, Henry , COOPER, David, Gwynn
发明人： SMITHKLINE & FRENCH LABORATORIES LIMITED
IPC分类号： C07D211/18
CPC分类号： C07D405/12 , C07D211/20 , C07D211/22 , C07D211/26
摘要： Compounds of structure (I) in which R is C1-8alkyl(phenyl)p, C2-8alkenyl(phenyl)p, C2-8alkynyl(phenyl)p, C3-8cycloalkyl or C1-8alkylC3-8cycloalkyl; p is 0 to 2; n is 0 to 6; A is a bond, oxygen, sulphur or NR ; R is hydrogen, C1-8alkyl or phenylC1-4alkyl; m is 0 to 3; and Ar is aryl or heteroaryl, each of which may be optionally substituted, and salts thereof; processes for preparing compounds (I), pharmaceutical compositions containing them and their use in medicine, in particular as calcium blocking agents.
摘要翻译：结构（I）的化合物，其中R是C 1-8烷基（苯基）p，C 2-8烯基（苯基）p，C 2-8炔基（苯基）p，C 3-8环烷基或C 1-8烷基C 3-8环烷基; p为0〜2; n为0〜6; A是键，氧，硫或NR 1; R 1是氢，C 1-8烷基或苯基C 1-4烷基; m为0〜3; 并且Ar是芳基或杂芳基，其各自可以被任选取代，及其盐; 制备化合物（I）的方法，含有它们的药物组合物及其在医药中的用途，特别是作为钙阻断剂。

3. 发明申请

WO1995011240A1 AMINE DERIVATIVES AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：胺衍生物作为钙通道拮抗剂
公开(公告)号：WO1995011240A1
公开(公告)日：1995-04-27
申请号：PCT/EP1994003358
申请日：1994-10-11
申请人： SMITHKLINE BEECHAM PLC , COOPER, David, Gwyn , KING, Ronald, Joseph , BROWN, Thomas, Henry
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D295/12
CPC分类号： C07D295/088 , C07D295/13
摘要： Compounds of formula (I), wherein R and R each independently represent: hydrogen, C1-8alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, arylC1-4alkyl, C2-6hydroxyalkyl or R R NC2-6alkyl (where R and R independently represent H or C1-4alkyl) or NR R represents a saturated heterocyclic ring containing 4 to 9 ring members, one of which may optionally be a further heteroatom selected from O, S or NR , (where R is H, C1-4alkyl or arylC1-4alkyl), which ring may optionally be substituted by one or two substituents selected from C1-6alkyl and C1-6alkoxy; X represents O, S or NR (where R is hydrogen, C1-4alkyl or arylC1-4alkyl); Y represents O, S, C=O or a bond; n is 2 to 5; m is 1 to 5 (providing that when m is 1, Y represents a bond); and Ar represents phenyl optionally substituted by 1-3 substituents selected from halo, C1-8alkyl, C1-8alkoxy, C1-2alkylenedioxy e.g. methylenedioxy, trifluoromethyl, trifluoromethyloxy, or by a group Ph(Alk )pA(Alk )q- where Ph isoptionally substituted phenyl, A is a bond, O, S, -C=O or CH=CH, Alk and Alk independently represent C1-4alkyl which may be straight or branched and p and q are independently 0 or 1, provided that the length of -(Alk )pA(Alk )q- does not exceed 5 atoms, or Ar is an optionally substitued tricyclic heteroaryl group (a) in which Y is Y (CH2)r where r is 0 or 1 and Y is O, S or NR where R is hydrogen or C1-4alkyl, Z is (CH2)s or -CH=CH-, s is 0, 1 or 2 or Ar is the corresponding tricyclic dehydro ring system; and pharmaceutically acceptable salts thereof are useful as atherapeutic agents, e.g. for the treatment of ischaemic stroke.
摘要翻译：式（I）化合物，其中R 1和R 2各自独立地表示：氢，C 1-8烷基，C 3-8环烷基，C 3-8环烷基C 1-4烷基，芳基C 1-4烷基，C 2-6羟烷基或R 3 R （4）其中R 3和R 4独立地表示H或C 1-4烷基）或NR 1 R 2表示含有4〜9个环成员的饱和杂环，其中之一可以任选地是选自O，S或NR 5的另外的杂原子（其中R 5是H，C 1-4烷基或芳基C 1-4烷基），该环可任选地被一个或两个选自C 1-6烷基和C 1-6烷氧基; X表示O，S或NR 6（其中R 6是氢，C 1-4烷基或芳基C 1-4烷基）; Y表示O，S，C = O或键; n为2〜5; m为1〜5（m为1时，Y为键）。并且Ar表示任选被1-3个选自卤素，C 1-8烷基，C 1-8烷氧基，C 1-2亚烷基二氧基的取代基取代的苯基。亚甲二氧基，三氟甲基，三氟甲氧基或基团Ph（Alk 1）pA（Alk 2）q-，其中Ph取代的苯基，A为键，O，S，-C = O或CH = CH， Alk 1和Alk 2独立地表示可以是直链或支链的C 1-4烷基，p和q独立地是0或1，条件是 - （Alk 1）pA（Alk 2）q - 不超过5个原子，或Ar是任选取代的三环杂芳基（a），其中Y 1是Y 2（CH 2）r，其中r是0或1，Y 2是O，S或 NR 7其中R 7是氢或C 1-4烷基，Z是（CH 2）s或-CH = CH-，s是0,1或2，或Ar是相应的三环脱氢环体系; 和其药学上可接受的盐可用作治疗剂，例如，用于治疗缺血性卒中。

4. 发明申请

WO1995011238A1 HETEROCYCLIC AMINES FOR TREATING ISCHAEMIC STROKES 审中-公开
标题翻译：用于处理异构体的杂环酰胺
公开(公告)号：WO1995011238A1
公开(公告)日：1995-04-27
申请号：PCT/EP1994003425
申请日：1994-10-18
申请人： SMITHKLINE BEECHAM PLC , COOPER, David, Gwyn , KING, Ronald, Joseph , BROWN, Thomas, Henry
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D295/088
CPC分类号： C07D295/088 , A61K31/135 , A61K31/445 , A61K31/495 , A61K31/535 , C07C217/20 , C07C2601/08 , C07D295/108
摘要： Use of compounds of formula (I), wherein R and R each independently represent: hydrogen, C1-8alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, arylC1-4alkyl, C2-6hydroxyalkyl or R R NC2-6alkyl (where R and R independently represent H or C1-4alkyl) or NR R represents a saturated heterocyclic ring containing 4 to 9 ring members, one of which may optionally be a further heteroatom selected from O, S or NR (where R is H, C1-4alkyl or arylC1-4alkyl), which ring may optionally be substituted by one or two substituents selected from C1-6alkyl and C1-6alkoxy; X represents O, S, or C=O; n is 5 to 11; and Ar represents phenyl optionally substituted by 1-3 substituents selected from halo, C1-8alkyl, C1-8alkoxy, C1-2alkylenedioxy, e.g. methylenedioxy, trifluoromethyl, trifluoromethyloxy, or by a group Ph(Alk )pA(Alk )q- where Ph is optionally substituted phenyl, A is a bond, O, S, -C=O or CH=CH, Alk and Alk independently represent C1-4alkyl which may be straight or branched and p and q are independently 0 or 1 provided that the length of -(Alk )pA(Alk )q- does not exceed 5 atoms, or Ar is an optionally substituted tricyclic heteroaryl group (a), in which Y is Y (CH2)r where r is 0 or 1 and Y is O, S or NR where R is hydrogen or C1-4alkyl, Z is (CH2)s or -CH=CH-, s is 0, 1 or 2 or Ar is the corresponding tricyclic dehydro ring system; with the provisos that (i) when X is O or S, and NR R represents a heterocyclic ring which does not contain an optional further heteroatom then Ar is phenyl substituted by a group Ph(Alk )pC(O)(Alk )q-; (ii) when n is 5 and one of R and R is hydrogen, C1-4alkyl or arylC1-4alkyl, then the other of R and R is not R R NC2-6alkyl; and pharmaceutically acceptable salts thereof; in the manufacture of a medicament for the treatment of a condition where a calcium antagonist is required. Certain novel compounds of formula (I) and processes for preparing them are also described.
摘要翻译：式（I）化合物的用途，其中R 1和R 2各自独立地表示：氢，C 1-8烷基，C 3-8环烷基，C 3-8环烷基C 1-4烷基，芳基C 1-4烷基，C 2-6羟烷基或R 3 > R 4 NC2-6烷基（其中R 3和R 4独立地表示H或C 1-4烷基）或NR 1 R 2表示含有4〜9个环成员的饱和杂环，其可以任选地是选自O，S或NR 5的另外的杂原子（其中R 5是H，C 1-4烷基或芳基C 1-4烷基），该环可任选地被一个或两个选自C 1 -C 6烷基的取代基取代， 6烷基和C 1-6烷氧基; X表示O，S或C = O; n为5〜11; 并且Ar表示任选被1-3个选自以下的取代基取代的取代基：卤素，C 1-8烷基，C 1-8烷氧基，C 1-2亚烷基二氧基，亚甲二氧基，三氟甲基，三氟甲氧基或Ph（Alk 1）pA（Alk 2）q-，其中Ph是任选取代的苯基，A是键，O，S，-C = O或CH = CH ，Alk 1和Alk 2独立地表示可以是直链或支链的C 1-4烷基，p和q独立地为0或1，条件是 - （Alk 1）pA（Alk 2）q - 不超过5个原子，或Ar是任选取代的三环杂芳基（a），其中Y 1是Y 2（CH 2）r，其中r是0或1，Y 2是O，S 或NR 6，其中R 6是氢或C 1-4烷基，Z是（CH 2）s或-CH = CH-，s是0,1或2，或Ar是相应的三环脱氢环体系; 条件是（ⅰ）当X为O或S且NR 1 R 2表示不含任选的另外的杂原子的杂环时，Ar为被Ph（Alk 1）基取代的苯基， PC（O）（ALK <2>）Q-; （ii）当n为5且R 1和R 2之一为氢，C 1-4烷基或芳基C 1-4烷基时，R 1和R 2中的另一个为R 3 R <4> NC2-6alkyl; 及其药学上可接受的盐; 在制备用于治疗需要钙拮抗剂的病症的药物中。还描述了某些新的式（I）化合物及其制备方法。

5. 发明申请

WO1994014786A1 PIPERIDINE DERIVATIVES AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：哌啶衍生物作为钙通道拮抗剂
公开(公告)号：WO1994014786A1
公开(公告)日：1994-07-07
申请号：PCT/EP1993003629
申请日：1993-12-16
申请人： SMITHKLINE BEECHAM PLC , KING, Ronald, Joseph , BROWN, Thomas, Henry , COOPER, David, Gwyn
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D295/10
CPC分类号： C07D295/096 , C07D295/088 , C07D295/108
摘要： Compounds of formula (I): wherein R represents C1-6alkyl, halogen or phenyl; R , represents hydrogen, C1-6alkyl, halogen or phenyl; R represents hydroxyl or a group convertible thereto in vivo; R represents C1-6alkyl; p is zero, 1 or 2; X represents -CH2-, -C = O, O or S; n is an integer from 4 to 10; m is an integer from 3 to 8; and salts thereof are useful as calcium antagonists, e.g. in the treatment of conditions relating to an accumulation of calcium in brain cells.
摘要翻译：式（I）化合物：其中R 1表示C 1-6烷基，卤素或苯基; R 2表示氢，C 1-6烷基，卤素或苯基; R 3代表羟基或其在体内可转化的基团; R 4表示C 1-6烷基; p为零，1或2; X表示-CH 2 - ， - C = O，O或S; n是4至10的整数; m为3〜8的整数; 和其盐可用作钙拮抗剂，例如在治疗与脑细胞中钙积累有关的病症。

6. 发明申请

WO1993022302A1 N-ARYLOXY(THIO)ALKYL-AZACYCLOALKANES USEFUL AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译： N-ARYLOXY（THIO）ALKYL-AZACYCLOALKANES有用的钙通道拮抗剂
公开(公告)号：WO1993022302A1
公开(公告)日：1993-11-11
申请号：PCT/GB1993000801
申请日：1993-04-15
申请人： SMITHKLINE BEECHAM PLC , BROWN, Thomas, Henry , COOPER, David, Gwyn , KING, Ronald, Joseph
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D295/08
CPC分类号： C07D295/088 , C07D211/46 , C07D307/91 , C07D317/64
摘要： Use of compounds of formula (I), in which n is 3 to 8; q is 5 to 11; R represents C1-6alkyl or C1-6alkoxy; s is zero, 1 or 2; X represents oxygen or sulphur; and Ar represents phenyl optionally substituted by 1-3 substituents selected from halo, C1-8alkyl, C1-8alkoxy, C1-2alkylenedioxy, trifluoromethyl, trifluoromethyloxy, or a group Ph-(CH2)m-Y-(CH2)p-where Ph is optionally substituted phenyl, m and p are independently 0 to 4 and Y is a bond, O, S, or CH=CH, provided that m + p is not greater than 4, or Ar is an optionally substituted tricyclic heteroaryl group (a) in which Y is Y(CH2)x where x is 0 or 1 and Y is O, S or NR where R is hydrogen or C1-4alkyl, Z is (CH2)r or -CH=CH-, r is 0, 1 or 2 or Ar is the corresponding tricyclic dehydro ring system, and their pharmaceutically acceptable salts for the manufacture of medicaments for the treatment of conditions where a calcium channel antagonist is indicated. Novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them are also described.
摘要翻译：使用式（I）化合物，其中n为3至8; q是5到11; R 1表示C 1-6烷基或C 1-6烷氧基; s为零，1或2; X表示氧或硫; 和Ar表示任选被1-3个选自卤素，C 1-8烷基，C 1-8烷氧基，C 1-2亚烷基二氧基，三氟甲基，三氟甲氧基或Ph-（CH 2）m Y-（CH 2）p - 取代的苯基，其中Ph是任选的取代的苯基，m和p独立地为0〜4，Y为键，O，S或CH = CH，条件是m + p不大于4，或Ar为任选取代的三环杂芳基（a）其中Y 1是Y（CH 2）x，其中x是0或1，Y是O，S或NR，其中R是氢或C 1-4烷基，Z是（CH 2）r或-CH = CH-，r是0 ，1或2或Ar是相应的三环脱氢环系统及其药学上可接受的盐，用于制备用于治疗其中指示钙通道拮抗剂的病症的药物。还描述了新的式（I）化合物，其制备方法和含有它们的药物组合物。

7. 发明申请

WO1993015080A1 AZABICYCLO COMPOUNDS AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：作为钙通道拮抗剂的AZABICYCLO化合物
公开(公告)号：WO1993015080A1
公开(公告)日：1993-08-05
申请号：PCT/GB1993000174
申请日：1993-01-27
申请人： SMITHKLINE BEECHAM PLC , ORLEK, Barry, Sidney , BROWN, Thomas, Henry , COOPER, David, Gwyn
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D487/08
CPC分类号： C07D471/08 , C07D487/08
摘要： Compounds of formula (I) in which p, q and r each independently represent an integer from 1 to 4; n is 0 to 6; m is 0 to 6; A is a bond, -CH=CH-, -C=C-, oxygen, sulphur or NR ; R is hydrogen, C1-8alkyl or phenylC1-4alkyl; and Ar is aryl or heteroaryl, each of which may be optionally substituted; and salts thereof are useful in medicine, in particular as calcium channel antagonists. Processes for preparing compounds (I) and pharmaceutical compositions containing them are also described.
摘要翻译：其中p，q和r各自独立地表示1至4的整数的式（I）化合物; n为0〜6; m为0〜6; A是键，-CH = CH-，-C = C-，氧，硫或NR 1; R 1是氢，C 1-8烷基或苯基C 1-4烷基; 并且Ar是芳基或杂芳基，其各自可以是任选被取代的; 其盐可用于医药，特别是钙通道拮抗剂。还描述了制备化合物（I）和含有它们的药物组合物的方法。

8. 发明申请

WO1995033722A1 PHENOXYALKYL SUBSTITUTED PIPERIDINES, PYRROLIDINES, MORPHOLINES AND TIOMORPHOLINES AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：苯氧基取代的哌啶，吡咯烷酮，吗啉和酪氨酸盐作为钙通道拮抗剂
公开(公告)号：WO1995033722A1
公开(公告)日：1995-12-14
申请号：PCT/EP1995002002
申请日：1995-05-24
申请人： SMITHKLINE BEECHAM PLC , BROWN, Thomas, Henry , COOPER, David, Gwyn
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D211/22
CPC分类号： C07D211/24 , C07D211/22
摘要： Compounds of formula (I) in which W is -(CH2)4, (CH2)5, -(CH2)2O(CH2)2 or -(CH2)2S(CH2)2, n is 0 to 6; m is 0 to 3; A is a bond, -CH=CH-, -CC-, oxygen, sulphur or NR ; R is hydrogen, C1-8alkyl or phenylC1-4alkyl; and Ar is a group (a) where X is -SO2- or -C(CH3)2-, Y and Z may each be hydrogen, fluorine, chlorine, bromine, C1-4alkyl, C1-4alkoxy or trifluoromethyl; and salts thereof are calcium channel antagonists with activity in neurons and are useful in the treatment of conditions such as ischaemic stroke.
摘要翻译：其中W是 - （CH2）4，（CH2）5， - （CH2）2O（CH2）2或 - （CH2）2S（CH2）2的式（Ⅰ）化合物，n是0-6; m为0〜3; A是键，-CH = CH-，-CC-，氧，硫或NR 1; R 1是氢，C 1-8烷基或苯基C 1-4烷基; 和Ar是基团（a），其中X是-SO 2 - 或-C（CH 3）2 - ，Y和Z可各自为氢，氟，氯，溴，C 1-4烷基，C 1-4烷氧基或三氟甲基; 其盐是在神经元中具有活性的钙通道拮抗剂，可用于治疗缺血性中风等病症。

9. 发明申请

WO1995024390A1 NOVEL PHENYL(-ALKYL/ALKOXY)-1-AMINOALKYL-SUBSTITUTED PIPERIDINES AND PYRROLIDINES AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：新戊基（-ALKYL / ALKOXY）-1-氨基取代的哌啶和吡咯烷作为钙通道拮抗剂
公开(公告)号：WO1995024390A1
公开(公告)日：1995-09-14
申请号：PCT/EP1995000850
申请日：1995-03-07
申请人： SMITHKLINE BEECHAM PLC , BROWN, Thomas, Henry , COOPER, David, Gwyn
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D211/14
CPC分类号： C07D211/14 , C07D211/22
摘要： Compounds of formula (I) in which W is -CH2- or a bond; p is an integer from 3-12; NR R represents: (i) an acyclic amino group wherein R and R each independently represents: hydrogen, C1-8alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-8alkyl, arylC1-4alkyl, hydroxyC2-6alkyl or R R NC2-6alkyl (where R and R independently represent H or C1-4alkyl) provided that when one of R and R represents hydrogen, the other does not represent hydrogen, C1-8alkyl, C3-8cycloalkylC1-8alkyl, arylC1-4alkyl or hydroxy C2-6alkyl; (ii) a saturated heterocyclic ring containing 4 to 9 ring members, one of which may optionally be a further heteroatom selected from 0, S or NR , (where R is H, C1-4alkyl or arylC1-4alkyl), which ring may optionally be substituted by one or two substituents selected from C1-6alkyl and C1-6alkoxy; or (iii) when W represents a bond, NR R may also represent a pyrrolidine ring substituted by -(CH2)nA(CH2)mAr and when W represents -CH2-, NR R may also represent a piperidine ring substituted by -(CH2)nA(CH2)mAr to form a symmetrical compound of formula (I); n is 0 to 6; m is 0 to 6; A is a bond, -CH=CH-, -CC-, oxygen, sulphur or NR where R is hydrogen, C1-8alkyl or phenylC1-4alkyl; and Ar is optionally substituted phenyl; and salts thereof are calcium antagonists with activity in neurons and are useful in the treatment of conditions such as ischaemic stroke.
摘要翻译：其中W是-CH 2 - 或键的式（I）化合物; p是3-12的整数; NR 1 R 2表示：（i）无环氨基，其中R 1和R 2各自独立地表示：氢，C 1-8烷基，C 3-8环烷基，C 3-8环烷基C 1-8烷基，芳基C 1-4烷基，羟基C 2-6烷基或R 3 R 4 NC2-6烷基（其中R 3和R 4独立地表示H或C 1-4烷基），条件是当R 1和R 2之一表示氢，另一个不表示氢，C 1-8烷基，C 3-8环烷基C 1-8烷基，芳基C 1-4烷基或羟基C 2-6烷基; （ii）含有4至9个环成员的饱和杂环，其中一个可以任选地是另外的选自O，S或NR 5的杂原子（其中R 5是H，C 1-4烷基或芳基C 1-4烷基），该环可任选地被一个或两个选自C 1-6烷基和C 1-6烷氧基的取代基取代; 或（iii）当W表示键时，NR 1 R 2也可以表示被 - （CH 2）n A（CH 2）mAr取代的吡咯烷环，当W表示-CH 2 - 时，NR 1 R 2 也可以表示被 - （CH 2）n A（CH 2）mAr取代的哌啶环，以形成式（I）的对称化合物; n为0〜6; m为0〜6; A是键，-CH = CH-，-CC-，氧，硫或NR 6，其中R 6是氢，C 1-8烷基或苯基C 1-4烷基; 和Ar是任选取代的苯基; 其盐是在神经元中具有活性的钙拮抗剂，可用于治疗缺血性中风等病症。

10. 发明申请

WO1993015073A1 AZABRICYCLIC COMPOUNDS AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：作为钙通道拮抗剂的AZABRICYCLIC化合物
公开(公告)号：WO1993015073A1
公开(公告)日：1993-08-05
申请号：PCT/GB1993000175
申请日：1993-01-27
申请人： SMITHKLINE BEECHAM PLC , ORLEK, Barry, Sidney , BROWN, Thomas, Henry , COOPER, David, Gwyn
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D453/02
CPC分类号： C07D471/08 , A61K31/435 , A61K31/47 , A61K31/55 , C07D453/02 , C07D487/08
摘要： Use of compounds of formula (I), in which p, q and r each independently represent an integer from 1 to 4; A is a bond, -CH=CH-, -C=C-, oxygen, sulphur or NR , where R is hydrogen, C1-8alkyl or phenylC1-4alkyl; n is 0 to 6, and m is 0 to 6, such that the length of the chain -(CH2)nA(CH2)m is at least two atoms; and Ar is aryl or heteroaryl, each of which may be optionally substituted; and pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the treatment of disorders where a calcium channel antagonist is indicated. Novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them are also described.
摘要翻译：使用式（I）化合物，其中p，q和r各自独立地表示1至4的整数; A是键，-CH = CH-，-C = C-，氧，硫或NR 1，其中R 1是氢，C 1-8烷基或苯基C 1-4烷基; n为0〜6，m为0〜6，使得链 - （CH 2）n A（CH 2）m的长度为至少2个原子; 并且Ar是芳基或杂芳基，其各自可以是任选被取代的; 用于制备用于治疗其中指示钙通道拮抗剂的病症的药物。还描述了新的式（I）化合物，其制备方法和含有它们的药物组合物。

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