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1. 发明申请

WO2011027106A1 THERAPEUTIC ARYL-AM I DO-ARYL COMPOUNDS AND THEIR USE 审中-公开
标题翻译：治疗ARYL-AM我做ARYL化合物及其使用
公开(公告)号：WO2011027106A1
公开(公告)日：2011-03-10
申请号：PCT/GB2010/001650
申请日：2010-09-01
申请人： KING'S COLLEGE LONDON , CORCORAN, Jonathan Patrick Thomas , KALINDJIAN, Sarkis Barret , BORTHWICK, Alan David , ADAMS, David Reginald , BROWN, Jane Theresa , TADDEI, David Michel Adrien , SHIERS, Jason, John
发明人： CORCORAN, Jonathan Patrick Thomas , KALINDJIAN, Sarkis Barret , BORTHWICK, Alan David , ADAMS, David Reginald , BROWN, Jane Theresa , TADDEI, David Michel Adrien , SHIERS, Jason, John
IPC分类号： C07C233/75 , C07C235/56 , C07C237/42 , C07D213/30 , C07D213/80 , C07D213/81 , C07D237/24 , A61K31/235 , A61K31/192 , A61K31/166 , A61K31/44 , A61P25/28
CPC分类号： C07C235/84 , C07C233/75 , C07C235/56 , C07C237/42 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/30 , C07D213/80 , C07D213/81 , C07D237/24
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as "AAA compounds"), which, inter alia, are (selective) retinoic acid receptor α (RARα) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RARα, and in the treatment of diseases and conditions that are mediated by RARα, that are ameliorated by the activation of RARα, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.
摘要翻译：本发明一般涉及治疗化合物的领域，更具体地涉及以下式的某些芳基 - 酰氨基 - 芳基化合物（为了方便起见，统称为“AAA化合物”），其特别是（选择性的）视黄酸受体a（RARa）激动剂。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途（选择性地）活化RARa，以及在治疗由RARa介导的疾病和病症中的应用，该通过RARa等的激活改善，包括认知障碍，记忆障碍，记忆缺陷，老年痴呆，阿尔茨海默病，早期阿尔茨海默病，中期阿尔茨海默氏病，晚期阿尔茨海默病，认知障碍和轻度认知障碍。

2. 发明申请

WO2004110435A1 1-PHENYL-2-OXO-3-SULFONYLAMINO-PYRROLIDINE DERIVATIVES AND RELATED COMPOUNDS AS FACTOR XA INHIBITORS FOR THE TREATMENT OF ACUTE VASCULAR DISEASES 审中-公开
标题翻译： 1-苯基-2-氧代-3-磺酰氨基吡咯烷酮衍生物及相关化合物作为治疗急性血管疾病的因子XA抑制剂
公开(公告)号：WO2004110435A1
公开(公告)日：2004-12-23
申请号：PCT/EP2004/006592
申请日：2004-06-17
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , CHAN, Chuen , KELLY, Henry, Anderson , KLEANTHOUS, Savvas , MASON, Andrew, McMurtrie , WATSON, Nigel, Stephen
发明人： BORTHWICK, Alan, David , CHAN, Chuen , KELLY, Henry, Anderson , KLEANTHOUS, Savvas , MASON, Andrew, McMurtrie , WATSON, Nigel, Stephen
IPC分类号： A61K31/4025
CPC分类号： C07D413/14 , C07D409/12 , C07D409/14
摘要： The invention relates to compounds of formula (I) wherein: R 1 represents a group selected from: formula (II) each ring of which optionally contains a further heteroatom N, Z represents an optional substituent halogen, alk represents alkylene or alkenylene, T represents S, O or NH; R 2 represents -C 1-6 alkyl, -C 1-3 alkylCN, -C 0-3 alkylR c , -C 1-3 alkylR f , -C 2-3 alkylNR a R b , -C 2-3 alkylOC 1-6 alkyl, -C 2-3 alkylOC 1-3 alkylCONR a R b , with the proviso that R 2 does not represent C 2-3 alkylmorpholino; X represents phenyl or a 5- or 6- membered aromatic heterocyclic group containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by 0-2 groups selected from: halogen, -C 1-4 alkyl, -C 2-4 alkenyl, -CN, -CF 3 , -NR a R b , -C 0-4 alkylOR e , -C(O)R d and -C(O)NR a R b ; Y represents a substituent selected from hydrogen, halogen, -C 1-4 alkyl, -C 2-4 alkenyl, -NR a R b , -NO 2 , -C(O)NR a R b , -N(C 1-4 alkyl)(CHO), -NHCOC 1-4 alkyl, -NHSO 2 R d , -C 0-4 alkylOR e , -C(O)R d , -S(O) n R d , or -S(O) 2 NR a R b ; The other substituents are as defined in claim 1.
摘要翻译：本发明涉及式（I）化合物，其中：R 1表示选自以下的基团：式（II）其各环任选含有另外的杂原子N，Z表示任选的取代基卤素，alk表示亚烷基或亚烯基， T表示S，O或NH; R 2表示-C 1-6烷基，-C 1-3烷基CN，-C 0-3烷基，R c，-C 1-3烷基R f，-C 2 - 3烷基，NR a R b，-C 2 - 3烷基，C 1-6烷基， -C 2-3烷基OC 1-3烷基CONR a R a，条件是R 2不表示C 2-3烷基吗啉代; X表示苯基或含有至少一个选自O，N或S的杂原子的5-或6-元芳族杂环基团，每个选自O，R，C 1-4烷基，-C 2 - 烷基，-C（O）R d和-C（O）NR a R b， ; Y表示选自氢，卤素，-C 1-4烷基，-C 2-4链烯基，-NR a R b，-NO 2，-C（O）NR a R b，-N（ C 1-4烷基）（CHO），-NHCOC 1-4烷基，-NHSO 2 R d，-C 0-4烷基OR e，-C（O）R d，-S（O）n R d或-S （O）2 NR - [R的; 其它取代基如权利要求1中所定义。

3. 发明申请

WO2004111045A1 PYRROLIDINE - 2- ONES AS FACTOR XA INHIBITORS 审中-公开
标题翻译：吡咯烷-2-酮作为因子XA抑制剂
公开(公告)号：WO2004111045A1
公开(公告)日：2004-12-23
申请号：PCT/EP2004/006603
申请日：2004-06-17
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , KELLY, Henry, Anderson , WATSON, Nigel, Stephen , YOUNG, Robert, John
发明人： BORTHWICK, Alan, David , KELLY, Henry, Anderson , WATSON, Nigel, Stephen , YOUNG, Robert, John
IPC分类号： C07D409/14
CPC分类号： C07D409/14
摘要： The invention relates to compounds of formula (I): wherein: R 1 represents a group selected from: formula (II), each ring of which optionally contains a further heteroatom N, Z represents an optional substituent halogen, alk represents alkylene or alkenylene, T represents S, O or NH; R 2 represents hydrogen, -C 1-6 alkyl, -C 1-3 alkylCONR a R b , -C 1-3 alkylCO 2 C 1-4 alkyl, -CO 2 C 1-4 alkyl or -C 1-3 alkylCO 2 H; R a and R b independently represent hydrogen, -C 1-6 alkyl, or together with the N atom to which they are bonded form a 5-, 6- or 7- membered non-aromatic heterocyclic ring optionally containing an additional heteroatom selected from O, N or S, optionally substituted by -C 1-4 alkyl, and optionally the S heteroatom is substituted by O, i.e. represents S(O) n ; n represents 0-2; X represents phenyl or a 5- or 6- membered aromatic heterocyclic group containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by 0-2 groups selected from: halogen, -C 1-4 alkyl, -C 2-4 alkenyl, -CN, -CF 3 , -NR a R b , -C 0-4 alkylOR e , -C(O)R f and -C(O)NR a R b ; R e represents hydrogen or -C 1-6 alkyl; R f represents -C 1-6 alkyl; Y represents phenyl or a 5- or 6- membered aromatic heterocyclic group containing at least one heteroatom selected from O, N or S, each of which is substituted by a group -C 1-2 alkylNR c R d . R c and R d , together with the nitrogen atom to which they are bonded, form a 4-membered heterocyclic ring optionally substituted by halogen, OH or -OC 1-6 alkyl, or a 5- or 6- membered non-aromatic heterocyclic ring substituted by OH, -OC 1-6 alkyl or 1 to 2 halogens, with the proviso that the substituent is not attached to a ring carbon atom adjacent to a heteroatom; and/or pharmaceutically acceptable derivatives thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
摘要翻译：本发明涉及式（I）的化合物：其中：R 1表示选自：式（II）的基团，其每个环任选地含有另外的杂原子N，Z表示任选的取代基卤素，alk表示亚烷基或亚烯基，T表示S，O或NH; R 2表示氢，-C 1-6烷基，-C 1-3烷基CONR a R b，-C 1-3烷基CO 2 C 1-4烷基，-CO 2 C 1-4烷基或-C 1-3烷基CO 2 H; R a和R b独立地表示氢，-C 1-6烷基或与它们所键合的N原子一起形成任选含有另外的杂原子的5-，6-或7-元非芳族杂环选自O，N或S，任选被-C 1-4烷基取代，并且任选地，S杂原子被O取代，即表示S（O）n; n表示0-2; X表示苯基或含有至少一个选自O，N或S的杂原子的5-或6-元芳族杂环基团，每个选自O，R，C 1-4烷基，-C 2 - 烯基，-CN，-CF 3，-NR a R b，-C 0-4烷基OR e，-C（O）R f和-C（O）NR a R b， ; R e表示氢或-C 1-6烷基; R f表示-C 1-6烷基; Y表示苯基或含有至少一个选自O，N或S的杂原子的5-或6-元芳族杂环基团，其各自被-C 1-2烷基NR c R基团取代。 R c和R d与它们所键合的氮原子一起形成任选被卤素，OH或-OC 1-6烷基取代的4-元杂环，或者5-或6-元非 - 由OH，-OC 1-6烷基或1至2个卤素取代的芳族杂环，条件是取代基未连接到与杂原子相邻的环碳原子上; 和/或其药学上可接受的衍生物。本发明还涉及制备式（I）化合物的方法，包含式（I）化合物的药物组合物和式（I）化合物在医药中的用途，特别是在改善临床病症方面指示因子Xa抑制剂。

4. 发明申请

WO2004052851A1 PYRROLYDIN-2-ONE DERIVATIVES AS INHIBITORS OF THROMBIN AND FACTOR XA 审中-公开
标题翻译：作为硫蛋白和因子XA的抑制剂的吡咯烷-2-酮衍生物
公开(公告)号：WO2004052851A1
公开(公告)日：2004-06-24
申请号：PCT/EP2003/013799
申请日：2003-12-04
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , CHAN, Chuen , KELLY, Henry, Anderson , PEACE, Simon , SENGER, Stefan , SHAH, Gita, Punjabhai , SMITH, Stephen, Allan , SMITH, Steven , WATSON, Nigel, Stephen , WEST, Robert, Ian , YOUNG, Robert, John
发明人： BORTHWICK, Alan, David , CHAN, Chuen , KELLY, Henry, Anderson , PEACE, Simon , SENGER, Stefan , SHAH, Gita, Punjabhai , SMITH, Stephen, Allan , SMITH, Steven , WATSON, Nigel, Stephen , WEST, Robert, Ian , YOUNG, Robert, John
IPC分类号： C07D207/26
CPC分类号： C07D207/273 , C07D401/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The invention relates to compounds of formula (I), wherein : R 1 represents hydrogen, C 1-4 alkyl, -CH 2 CO 2 H, -CH 2 CO 2 C 1 - 2 alkyl, or -CH 2 CONR7R 8 ; R 2 and R 3 independently represent hydrogen, -C 1-6 alkyl, -C 1-3 alkylCN, -C 1-3 alkylCO 2 H, -C 1-4 alkylOC 1-4 alkyl, -C 1-4 alkylS(O) n C 1-4 alkyl, -C 1-4 alkylNR 10 R 11 , -C 1-3 alkylNCO 2 C 1-4 alkyl, -C 1-3 alkylCONR 7 R 8 , -C 1-3 alkylCO 2 C 0-2 alkylR 9 , -C 1-3 alkylCOC 0-2 alkylR 9 , -C 1-3 alkylCON(R 8 ) C 0-2 alkylR 9 , -C 1-3 alkylNCO 2 C 0-2 alkylR 9 , -C 1-3 alkylNCOC 0-2 alkylR 9 or -C 0-2 alkylR 9 , with the proviso that one of R 2 and R 3 is hydrogen and the other is a substituent other than hydrogen; n is an integer between 0 and 2; R 4 and R 5 together with the nitrogen atom to which they are attached form a morpholino ring; R 6 represents a group selected from formula (II) wherein T 1 and T 2 independently represent CH 2 , NH, S or O with the proviso that when one of T 1 or T 2 represents NH, S or O the other represents CH 2 ; M represents CH 3 , -OH or PO; V represents CH or N; W represents H, CH 3 , Cl or F; X represents C1, Br, F or -CH 3 ; Y represents CH 3 or CF 3 ; Z represents -CH 3 or F; R 7 and R 8 are independently hydrogen, C 1-4 alkyl or together with the N atom to which they are bonded form a 5- or 6- membered non-aromatic heterocyclic ring, optionally containing an additional heteroatom selected from O, N or S; R 10 and R 11 independently represent C 1-4 alkyl or together with the N atom towhich they are bonded form a 5- or 6- membered non-aromatic heterocyclic ring, optionally containing an additionalheteroatom selected from O, N or S; R 9 represents phenyl or a 5- or 6- membered aromatic or non-aromatic heterocyclic group, containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by 0-2 groups selected from: C 1-3 alkyl or halogen; and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a thrombin inhibitor is indicated.
摘要翻译：本发明涉及式（I）化合物，其中：R 1表示氢，C 1-4烷基，-CH 2 CO 2 H，-CH 2 CO 2 C 1-2烷基或-CH 2 CONR 7 R 8; R 2和R 3独立地表示氢，-C 1-6烷基，-C 1-3烷基，C 1-3烷基CO 2 H，-C 1-4烷基，C 1-4烷基，-C 1-4烷基，（O）n C 1-4烷基，-C 1-4烷基NR R 11，-C 1-3烷基，CO 2 C 1-4烷基，-C 1-3烷基CONR 7 R 8，-C 1-3烷基CO 2 C 0-2烷基R 9，-C 1-3烷基C 0 -C 20 - 烷基R 9，-C 1- 3烷基CON（R 8）C 0-2烷基R 9，-C 1-3烷基，CO 2 C 0-2烷基R 9，-C 1-3烷基，C 1-10烷基，R 9或-C 0-2烷基R 9，条件是R 2和R 3是氢，另一个是氢以外的取代基; n是0和2之间的整数; R 4和R 5与它们所连接的氮原子一起形成吗啉代环; R 6表示选自式（II）的基团，其中T 1和T 2独立地表示CH 2，NH，S或O，条件是当T 1或T 2中的一个表示NH，S或O时，另一个表示CH 2; M代表CH3，-OH或PO; V表示CH或N; W表示H，CH 3，Cl或F; X表示C1，Br，F或-CH3; Y表示CH3或CF3; Z表示-CH 3或F; R 7和R 8独立地是氢，C 1-4烷基或与它们所键合的N原子一起形成5-或6-元非芳族杂环，任选地含有另外的选自O， N或S; R 10和R 11独立地表示C 1-4烷基或与其键合的N原子一起形成5-或6-元非芳族杂环，任选地含有选自O，N或S的另外的杂原子; R 9表示苯基或含有至少一个选自O，N或S的杂原子的5-或6-元芳族或非芳族杂环基，其中每一个可任选地被选自以下的0-2个基团取代：C1 烷基或卤素; 及其药学上可接受的衍生物，其制备方法，含有它们的药物组合物及其在医药中的用途，特别用于改善指示凝血酶抑制剂的临床病症。

5. 发明申请

WO2006000400A1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：替代哌替啶作为氧化蛋白拮抗剂
公开(公告)号：WO2006000400A1
公开(公告)日：2006-01-05
申请号：PCT/EP2005/006761
申请日：2005-06-21
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan David , SOLLIS, Steven, Leslie
发明人： BORTHWICK, Alan David , SOLLIS, Steven, Leslie
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： Compounds of formula (IA) wherein R 1 is 2-indanyl, R 2 is 1-methylpropyl, R 3 is 1-methyl-indazol-5-yl, R 4 represents methyl and R 5 represents hydrogen or methyl, and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译：其中R 1是2-二氢茚基，R 2的式（IA）化合物是1-甲基丙基，R 3是1-甲基 - 吲唑 -5-基，R 4代表甲基，R 5表示氢或甲基，并且其药学上可接受的衍生物被描述，其制备方法，含有它们的药物组合物以及它们在医药中的用途，特别是用作催产素拮抗剂。

6. 发明申请

WO2006000399A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2006000399A1
公开(公告)日：2006-01-05
申请号：PCT/EP2005/006760
申请日：2005-06-21
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew, McMurtrie
发明人： BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew, McMurtrie
IPC分类号： C07D401/06
CPC分类号： A61K31/5377 , C07D401/06 , C07D413/14
摘要： Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2, 6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译：式（I）的化合物，其中R 1是2-茚满基，R 2是1-甲基丙基，R 3是选自2,6-二甲基-3-吡啶基或4,6-二甲基-3-吡啶基的基团，R 4表示甲基和R 5 表示氢或甲基，或者R4和R5与它们所连接的氮原子一起代表吗啉代及其药学上可接受的衍生物，其制备方法，含有它们的药物组合物及其在药物中的用途，特别是其用作催产素拮抗剂。

7. 发明申请

WO2004110997A1 3- SULFONYLAMINO- PYRROLIDINE- 2- ONE DERIVATIVES AS INHIBITORS OF FACTOR XA 审中-公开
标题翻译： 3-磺酰氨基 - 吡咯烷-2-酮衍生物作为因子XA的抑制剂
公开(公告)号：WO2004110997A1
公开(公告)日：2004-12-23
申请号：PCT/EP2004/006604
申请日：2004-06-17
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HARLING, John, David , IRVING, Wendy, Rebecca , KLEANTHOUS, Savvas , WATSON, Nigel, Stephen , YOUNG, Robert, John
发明人： BORTHWICK, Alan, David , HARLING, John, David , IRVING, Wendy, Rebecca , KLEANTHOUS, Savvas , WATSON, Nigel, Stephen , YOUNG, Robert, John
IPC分类号： C07D207/26
CPC分类号： C07D207/273 , C07D401/10 , C07D403/10 , C07D409/12
摘要： The invention relates to compounds of formula (I): wherein: R 1 represents a group selected from: formula (II), each ring of which optionally contains a further heteroatom N, Z represents an optional substituent halogen, alk represents alkylene or alkenylene, T represents S, O or NH; R 2 represents hydrogen, -C 1-6 alkyl, -C 1-3 alkylCONR a R b , -C 1-3 alkylCO 2 C 1-4 alkyl, -CO 2 C 1-4 alkyl or -C 1-3 alkylCO 2 H; R a and R b independently represent hydrogen, -C 1-6 alkyl, or together with the N atom to which they are bonded form a 5-, 6- or 7- membered non-aromatic heterocyclic ring optionally containing an additional heteroatom selected from O, N or S, optionally substituted by C 1-4 alkyl, and optionally the S heteroatom is substituted by O, i.e. represents S(O) n ; n represents 0-2; X represents phenyl or a 5- or 6- membered aromatic heterocyclic group containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by 0-2 groups selected from: halogen, -C 1-4 alkyl, -C 2-4 alkenyl, -CN, -CF 3 , -NR a R b , -C 0-4 alkylOR e , -C(O)R f and -C(O)NR a R b ; Re represents hydrogen or -C 1-6 alkyl; R f represents -C 1-6 alkyl; Y represents a group -C(R x )(R z )C 0-2 alkylNR c R d ; Rx represents C 1-4 alkyl optionally substituted by halogen (e.g. CF 3 , -CH 2 CF 3 ); R z represents hydrogen or C 1-4 alkyl optionally substituted by halogen (e.g. CF 3 , -CH 2 CF 3 ); R c and R d independently represent hydrogen, -C 1-6 alkyl, -C 1-4 alkylOH, or together with the N atom to which they are bonded form a 4-, 5-, 6- or 7- membered non-aromatic heterocyclic ring, the 5-, 6- or 7- membered non-aromatic heterocyclic ring optionally containing an additional heteroatom selected from O, N or S, optionally substituted by C 1-4 alkyl; and/or pharmaceutically acceptable derivative thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
摘要翻译：本发明涉及式（I）的化合物：其中：R 1表示选自：式（II）的基团，其每个环任选地含有另外的杂原子N，Z表示任选的取代基卤素，alk表示亚烷基或亚烯基，T表示S，O或NH; R 2表示氢，-C 1-6烷基，-C 1-3烷基CONR a R b，-C 1-3烷基CO 2 C 1-4烷基，-CO 2 C 1-4烷基或-C 1-3烷基CO 2 H; R a和R b独立地表示氢，-C 1-6烷基或与它们所键合的N原子一起形成任选含有另外的杂原子的5-，6-或7-元非芳族杂环选自O，N或S，任选被C 1-4烷基取代，并且任选地，S杂原子被O取代，即表示S（O）n; n表示0-2; X表示苯基或含有至少一个选自O，N或S的杂原子的5-或6-元芳族杂环基团，每个选自O，R，C 1-4烷基，-C 2 - 烯基，-CN，-CF 3，-NR a R b，-C 0-4烷基OR e，-C（O）R f和-C（O）NR a R b， ; Re表示氢或-C 1-6烷基; R f表示-C 1-6烷基; Y表示基团-C（R x）（R））C 0-2烷基NR c R d; Rx表示任选被卤素（例如CF 3，-CH 2 CF 3）取代的C 1-4烷基; R z表示氢或任选被卤素（例如CF 3，-CH 2 CF 3）取代的C 1-4烷基; R c和R d独立地表示氢，-C 1-6烷基，-C 1-4烷基，或与它们所键合的N原子一起形成4-，5-，6-或7-元非 - 芳族杂环，任选地含有另外选自O，N或S的杂原子的5-，6-或7-元非芳族杂环，任选被C 1-4烷基取代; 和/或其药学上可接受的衍生物。本发明还涉及制备式（I）化合物的方法，包含式（I）化合物的药物组合物和式（I）化合物在医药中的用途，特别是在改善临床病症方面指示因子Xa抑制剂。

8. 发明申请

WO2004110434A1 2-PYRROLIDONE DERIVATIVES AND USE THEREOF AS FACTOR XA INHIBITORS 审中-公开
标题翻译： 2-吡咯烷酮衍生物及其作为因子XA抑制剂的用途
公开(公告)号：WO2004110434A1
公开(公告)日：2004-12-23
申请号：PCT/EP2004/006591
申请日：2004-06-17
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , KLEANTHOUS, Savvas , SENGER, Stefan , SMITH, Ian, Edward, David
发明人： BORTHWICK, Alan, David , KLEANTHOUS, Savvas , SENGER, Stefan , SMITH, Ian, Edward, David
IPC分类号： A61K31/4025
CPC分类号： C07D409/12 , C07D409/14
摘要： The invention relates to compounds of formula (I), and/or pharmaceutically acceptable derivative thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
摘要翻译：本发明涉及式（I）化合物和/或其药学上可接受的衍生物。本发明还涉及制备式（I）化合物的方法，包含式（I）化合物的药物组合物和式（I）化合物在医药中的用途，特别是在改善临床病症方面指示因子Xa抑制剂。

9. 发明申请

WO2003053443A1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：替代哌替啶作为氧化蛋白拮抗剂
公开(公告)号：WO2003053443A1
公开(公告)日：2003-07-03
申请号：PCT/EP2002/014823
申请日：2002-12-20
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
发明人： BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
IPC分类号： A61K31/495
CPC分类号： C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I)and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.
摘要翻译：一种治疗或预防通过催产素作用介导的疾病或病症的方法，其包括向有需要的哺乳动物施用有效量的式I化合物和/或其生理上可接受的衍生物，其中所述取代基具有给定的含义在说明中。公开了式I的新化合物及其制备方法。

10. 发明申请

WO2006000759A1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：替代哌替啶作为氧化蛋白拮抗剂
公开(公告)号：WO2006000759A1
公开(公告)日：2006-01-05
申请号：PCT/GB2005/002448
申请日：2005-06-21
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew McMurtrie , POLLARD, Derek, Roland , SOLLIS, Steven
发明人： BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew McMurtrie , POLLARD, Derek, Roland , SOLLIS, Steven
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D403/06 , C07D413/06
摘要： Compounds of formula (I); wherein R 1 is 2-indanyl, R 2 is 1-ethylpropyl, R 3 is a heterocyclic group optionally substituted by one or more C 1-6 alkyl groups, R 4 represents methyl and R 5 represents hydrogen or methyl and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译：式（I）化合物; 其中R 1是2-二氢化茚基，R 2是1-乙基丙基，R 3是任选地被一个或多个C 1 - SUB> 1-6个烷基，R 4代表甲基，R 5表示氢或甲基，其药学上可接受的衍生物被描述为它们的制剂，含有它们的药物组合物及其在医药中的用途，特别是其作为催产素拮抗剂的用途。

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