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1. 发明申请

WO2009085880A3 C-21 THIOETHERS AS GLUCOCORTICOID RECEPTOR AGONISTS 审中-公开
标题翻译：作为糖皮质激素受体激动剂的C-21硫酯
公开(公告)号：WO2009085880A3
公开(公告)日：2009-09-17
申请号：PCT/US2008087301
申请日：2008-12-18
申请人： SCHERING CORP , ANTHES JOHN C , MCCORMICK KEVIN D , HEY JOHN A , ASLANIAN ROBERT G , BIJU PURAKKATTLE J , BERLIN MICHAEL Y , SOLOMON DANIEL M , WANG HONGWU , LIM YEON HEE , LEE YOON JON , BITAR REMA DANIELLE
发明人： ANTHES JOHN C , MCCORMICK KEVIN D , HEY JOHN A , ASLANIAN ROBERT G , BIJU PURAKKATTLE J , BERLIN MICHAEL Y , SOLOMON DANIEL M
IPC分类号： C07J43/00 , A61K31/573 , A61K31/58 , A61P5/44 , C07J31/00 , C07J71/00
CPC分类号： C07J43/003 , C07J31/006 , C07J71/0031
摘要： The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activiy. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.
摘要翻译：本发明提供具有通式结构式（VII）的所述化合物和所述11-酮基类似物的式（VII）化合物及其11-酮基类似物及其药学上可接受的盐，溶剂化物，酯，前药，互变异构体和异构体，：其中L，R 1，R 2，R 3，R 4和R 5彼此独立地选择和如本文所定义。还提供了药物组合物，制备方法以及使用这些化合物治疗和预防各种免疫，自身免疫和炎性疾病和病症的方法。本发明的新化合物具有有用的药理学活性，同时具有意想不到的低全身活性。因此，本发明的化合物代表了那些副作用较差的已知糖皮质激素的安全替代品。

2. 发明申请

WO2009085880A2 C-21 THIOETHERS AS GLUCOCORTICOID RECEPTOR AGONISTS 审中-公开
标题翻译： C-21三醇作为葡萄糖激素受体激动剂
公开(公告)号：WO2009085880A2
公开(公告)日：2009-07-09
申请号：PCT/US2008087301
申请日：2008-12-18
申请人： SCHERING CORP , WANG HONGWU , LIM YEON HEE , LEE YOON JON , BITAR REMA DANIELLE , ANTHES JOHN C , MCCORMICK KEVIN D , HEY JOHN A , ASLANIAN ROBERT G , BIJU PURAKKATTLE J , BERLIN MICHAEL Y , SOLOMON DANIEL M
发明人： ANTHES JOHN C , MCCORMICK KEVIN D , HEY JOHN A , ASLANIAN ROBERT G , BIJU PURAKKATTLE J , BERLIN MICHAEL Y , SOLOMON DANIEL M
IPC分类号： C07J43/00 , A61K31/573 , A61K31/58 , A61P5/44 , C07J31/00 , C07J71/00
CPC分类号： C07J43/003 , C07J31/006 , C07J71/0031
摘要： The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activiy. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.
摘要翻译：本发明提供具有通式（Ⅶ）的所述化合物和所述11-酮类似物的式（Ⅶ）化合物及其11-酮类似物及其药学上可接受的盐，溶剂合物，酯，前药，互变异构体和异构体，：其中L，R 1，R 2，R 3，R 4和R 5彼此独立地选择并如本文所定义。还提供了药物组合物，制备方法和使用这些化合物在治疗和预防广泛范围的免疫，自身免疫和炎性疾病和病症中的方法。本发明的新化合物具有有用的药理活性，同时具有出人意料的低全身活性。因此，本发明的化合物代表具有差的副作用特征的已知糖皮质激素的更安全的替代方案。

3. 发明申请

WO2007001975A8 PIPERIDINE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS 审中-公开
标题翻译：哌嗪衍生物作为组胺H3拮抗剂有用
公开(公告)号：WO2007001975A8
公开(公告)日：2008-01-24
申请号：PCT/US2006023800
申请日：2006-06-19
申请人： SCHERING CORP , ASLANIAN ROBERT G , BERLIN MICHAEL Y , BOYCE CHRISTOPHER W , CHAO JIANHUA , DE LERA RUIZ MANUEL , MANGIARACINA PIETRO , MCCORMICK KEVIN D , MUTAHI MWANGI W , ROSENBLUM STUART B , SHIH NENG-YANG , SOLOMON DANIEL M , TOM WING C , VACCARO HENRY A , ZHENG JUNYING , ZHU XIAOHONG
发明人： ASLANIAN ROBERT G , BERLIN MICHAEL Y , BOYCE CHRISTOPHER W , CHAO JIANHUA , DE LERA RUIZ MANUEL , MANGIARACINA PIETRO , MCCORMICK KEVIN D , MUTAHI MWANGI W , ROSENBLUM STUART B , SHIH NENG-YANG , SOLOMON DANIEL M , TOM WING C , VACCARO HENRY A , ZHENG JUNYING , ZHU XIAOHONG
IPC分类号： C07D401/12 , A61P3/04 , A61P29/00 , A61P37/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04
CPC分类号： C07D295/185 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: M 1 and M 3 are CH or N; M 2 is CH, CF or N; Y is -C(=O)-, -C(=S)-, -(CH 2 ) q -, -C(=NOR 7 )- or -SO 1-2 -; Z is a bond or optionally substituted alkylene or alkenylene; R 1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula (II) where ring A is a heteroaryl ring; R 2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R 3 is H, -C(O)NH 2 , or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.
摘要翻译：公开了式（I）的新化合物或其药学上可接受的盐，其中：M 1和M 3是CH或N; M 2是CH，CF或N; Y是-C（= O） - ， - C（= S） - ， - （CH 2 CH 2）q - ， - / SO 2 - ） - 或-SO 2 1-2。 Z是键或任选取代的亚烷基或亚烯基; R 1是H或烷基，环烷基，芳基，杂芳基，杂环烷基，全部任意取代，或其中环A是杂芳基环的式（II）基团; R 2是任选取代的烷基，烯基，芳基，杂芳基，环烷基或杂环烷基; R 3是H，-C（O）NH 2或烷基，芳基，环烷基，杂环烷基或杂芳基，全部任选被取代; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应，充血，肥胖，代谢综合征，酒精性脂肪肝疾病，肝脂肪变性，非酒精性脂肪性肝炎，肝硬化，肝细胞癌和认知缺陷障碍的组合物和方法。

4. 发明申请

WO2007075688A3 SUBSTITUTED ANILINE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS 审中-公开
标题翻译：取代的苯胺衍生物有用于组胺H3拮抗剂
公开(公告)号：WO2007075688A3
公开(公告)日：2007-09-07
申请号：PCT/US2006048440
申请日：2006-12-19
申请人： SCHERING CORP , SOLOMON DANIEL M , ASLANIAN ROBERT G , BERLIN MICHAEL Y , DE LERA RUIZ MANUEL , MCCORMICK KEVIN D , MUTAHI MWANGI W , TOM WING C
发明人： SOLOMON DANIEL M , ASLANIAN ROBERT G , BERLIN MICHAEL Y , DE LERA RUIZ MANUEL , MCCORMICK KEVIN D , MUTAHI MWANGI W , TOM WING C
IPC分类号： C07D213/74 , A61K31/44 , A61P29/00 , C07D401/12 , C07D401/14
CPC分类号： C07D401/12 , C07D213/73 , C07D213/74 , C07D401/14 , C07D471/04
摘要： Disclosed are compounds of the formula Chemical formula (I) or a pharmaceutically acceptable salt thereof, wherein M 2 is N; X is a bond, optionally substituted alkylene, alkenylene, -O-, -CH 2 N(R 12 )-, -N(R 12 )CH 2 -, -N(R 12 )-, -NHC(O)-, -OCH 2 -, -CH 2 O-, or -S(O) 0-2 -; and Y is -(CH 2 ) 1-2 -, -C(=O)-, -C(=NOR 13 )- or -SO0-2-; or M 1 is N; M 2 is N or CH; X is a bond, alkylene, alkenylene, -C(O)-, -NHC(O)-, -OC(O)- or -S(O) 1-2 -; Y is -(CH 2 ) 1-2 -, -C(=O)- or -SO 0-2 -; and when M 2 is CH, Y is also Y is -O- or -C(=NOR 13 )-; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R 1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R 2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combination with other agents.
摘要翻译：公开了下式的化合物：化学式（I）或其药学上可接受的盐，其中M 2是N; X是一个键，任选取代的亚烷基，亚烯基，-O - ， - CH 2 N（R 12） - ， - N（R 12） CH 2 - ， - N（R 12） - ， - NHC（O） - ， - OCH 2 - ， - O - 或-S（O）0-2 - ; - 并且Y是 - （CH 2）2 - ， - C（= O） - ， - C（= NOR 13） - 或-SOO 2 - ; 或M 1是N; N 2是N或CH; X是一个键，亚烷基，亚烯基，-C（O） - ， - NHC（O） - ， - OC（O） - 或-S（O） Y是 - （CH 2）2 - ， - C - （= O） - 或-SO 0-2 - 。当M 2是CH时，Y也是Y是-O-或-C（= NOR 13） - ; Z是键或任选取代的亚烷基或亚烯基; U和W是CH，或一个是CH，一个是N; R 1是任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基，杂环烷基; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 以及单独或与其他药物组合治疗肥胖症，代谢综合征和认知缺陷障碍的组合物和方法。

5. 发明申请

WO2007075629A2 PHENOXYPIPERIDINES AND ANALOGS THEREOF USEFUL AS HISTAMINE H3 ANTAGONISTS 审中-公开
标题翻译：苯氧基哌啶及其类似物可用作组胺H3拮抗剂
公开(公告)号：WO2007075629A2
公开(公告)日：2007-07-05
申请号：PCT/US2006048349
申请日：2006-12-19
申请人： SCHERING CORP , MUTAHI MWANGI W , ASLANIAN ROBERT G , BERLIN MICHAEL Y , BOYCE CHRISTOPHER W , DE LERA RUIZ MANUEL , MCCORMICK KEVIN D , SOLOMON DANIEL M , VACCARO HENRY A , ZHENG JUNYING , PURAKKATTLE BIJU J , YU YOUNONG , ZHOU WEI , ZHU XIAOHONG
发明人： MUTAHI MWANGI W , ASLANIAN ROBERT G , BERLIN MICHAEL Y , BOYCE CHRISTOPHER W , DE LERA RUIZ MANUEL , MCCORMICK KEVIN D , SOLOMON DANIEL M , VACCARO HENRY A , ZHENG JUNYING , PURAKKATTLE BIJU J , YU YOUNONG , ZHOU WEI , ZHU XIAOHONG
CPC分类号： C07D471/04 , C07D213/38 , C07D213/73 , C07D277/40 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/06 , C07D417/14 , C07D473/00
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, -C(O)-, -C(N-OR 5 )-, -C(N-OR 5 )-CH(R 6 )-, -CH(R 6 )-C(N-OR 5 )-, -O-, -OCH 2 -, -CH 2 O- or -S(O) 0-2 -; Y is -O-, -(CH 2 ) 2 -, -C(=O)-, -C(=NOR 7 )- or -SO 0-2 -; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R 1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R 2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中：M是CH或N; U和W各自是CH，或者U和W中的一个是CH而另一个是N; X是键，亚烷基，-C（O） - ， - C（N-OR 5） - ， - C（N-OR 5）-CH（R -CH（R 6） - C（N-OR 5） - ， - O - ， - OCH _{2 - ， - CH - ， - 2 - 或-S（O）0-2 - ; - Y是-O - ， - （CH 2）2 - ，-C（= O） - ， - C（= NOR 7） - 或-SO _{0-2 - ; Z是键，被杂原子或杂环基团插入的任选取代的亚烷基或亚烷基; R 1是任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基，杂环烷基或苯并咪唑基或其衍生物; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 其余变量如说明书中所定义; 使用所述化合物单独或与其他药剂联合治疗变态反应诱发的气道反应，充血，糖尿病，肥胖症，肥胖相关病症，代谢综合征和认知缺陷病症的组合物和方法。}}

6. 发明申请

WO9924421A8 IMIDAZOYLALKYL SUBSTITUTED WITH A FIVE, SIX OR SEVEN MEMBERED HETEROCYCLIC RING CONTAINING ONE NITROGEN ATOM 审中-公开
标题翻译：用五分之一取代的咪唑啉酮，六种或七种含有一个氮原子的成员杂环
公开(公告)号：WO9924421A8
公开(公告)日：1999-08-26
申请号：PCT/US9823224
申请日：1998-11-05
申请人： SCHERING CORP , VACCARO WAYNE D , WOLIN RONALD L , SOLOMON DANIEL M , ASLANIAN ROBERT G , PIWINSKI JOHN J , ROSENBLUM STUART B
发明人： VACCARO WAYNE D , WOLIN RONALD L , SOLOMON DANIEL M , ASLANIAN ROBERT G , PIWINSKI JOHN J , ROSENBLUM STUART B
IPC分类号： A61K31/4178 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/495 , A61P1/00 , A61P3/04 , A61P9/00 , A61P9/02 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/28 , A61P27/06 , A61P37/08 , C07D401/06 , C07D403/06 , A61K31/415
CPC分类号： C07D401/06 , A61K31/445 , A61K31/495 , C07D403/06 , A61K31/415 , A61K2300/00
摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula (I). Further disclosed is a method of treating allergy (for example asthma), inflammation, hypotension, raised intraocular pressure (such as glaucoma) i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's, Schizophrenia, obesity and migraine) comprising administering an effective amount of a compound of Formula (I) to a patient in need of such treatment. Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of Formula (I) in combination or admixture with a histamine H1 receptor antagonist.
摘要翻译：公开了式（I）的化合物或其药学上可接受的盐或溶剂化物。还公开了包含药学上可接受的载体和有效量的式（I）的化合物的药物组合物。进一步公开的是治疗过敏（例如哮喘），炎症，低血压，升高的眼内压（例如青光眼）的方法，即降低眼内压，睡眠障碍，超低运动性状态和胃肠酸性分泌的方法中枢神经系统（例如，激动和抑郁）和其它CNS疾病（例如阿尔茨海默病，精神分裂症，肥胖症和偏头痛）的多发，低血压和多动症（包括向患者施用有效量的式（I）化合物）需要这样的治疗。还公开了治疗上呼吸道过敏反应的方法，包括与组胺H1受体拮抗剂组合或混合施用式（I）的化合物或其盐或溶剂合物。

7. 发明申请

WO0224659A2 SUBSTITUTED IMIDAZOLES AS DUAL HISTAMINE H1 AND H3 AGONISTS OR ANTGONISTS 审中-公开
标题翻译：取代的咪唑烷作为双组胺H1和H3激素或拮抗剂
公开(公告)号：WO0224659A2
公开(公告)日：2002-03-28
申请号：PCT/US0129095
申请日：2001-09-18
申请人： SCHERING CORP
发明人： SHIH NENG-YANG , SOLOMON DANIEL M , PIWINSKI JOHN J , LUPO ANDREW T JR , GREEN MICHAEL J
IPC分类号： A61K31/4545 , A61K31/496 , A61P1/04 , A61P3/04 , A61P9/10 , A61P11/00 , A61P25/00 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/12 , C07D401/14 , C07D233/00
CPC分类号： C07D401/12 , C07D401/14
摘要： The present invention discloses novel substituted imidazole compounds which have dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.
摘要翻译：本发明公开了具有双重组胺H1和H3受体拮抗剂活性的新型取代的咪唑化合物以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含这种咪唑的药物组合物以及使用它们治疗过敏，炎性和CNS相关疾病等的方法。

8. 发明申请

WO0053596A3 IMIDAZOLE COMPOUNDS AS HISTAMINE H3 LIGANDS 审中-公开
标题翻译：咪唑化合物作为组胺H3配体
公开(公告)号：WO0053596A3
公开(公告)日：2001-01-11
申请号：PCT/US0005897
申请日：2000-03-06
申请人： SCHERING CORP
发明人： VACCARO WAYNE D , PIWINSKI JOHN J , TOM WING C , SOLOMON DANIEL M , ASLANIAN ROBERT G
IPC分类号： C07D233/64 , A61K31/496 , A61K45/00 , A61P1/06 , A61P9/12 , A61P11/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/28 , A61P27/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D233/54 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , A61K31/50
CPC分类号： C07D233/64 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14
摘要： This invention discloses a compound having general formula depicted in Formula (I), wherein G is a spacer moiety selected from the group consisting of C1-C7 alkyl, C2-C7 alkenyl, C2-C7 alkynyl, C1-C7 alkyl-NHCO-, and -SO2-, T is a six-membered ring or a seven-membered ring containing two ring nitrogens and belonging to formula (a), with said T ring being c onnected to said G moiety at either a ring carbon atom of ring T or a ring nitrogen atom of ring T: wherein n is 1 or 2. These compounds have excellent histamine-H3 receptor antagonist activity.
摘要翻译：本发明公开了具有式（I）所示通式的化合物，其中G是选自C 1 -C 7烷基，C 2 -C 7烯基，C 2 -C 7炔基，C 1 -C 7烷基-NHCO-，和-SO 2 - ，T是含有两个环氮并且属于式（a）的六元环或七元环，所述T环在环T的环碳原子上连接到所述G部分或环T的环氮原子：其中n为1或2.这些化合物具有优异的组胺H3受体拮抗剂活性。

9. 发明申请

WO9748368A3 NAPHTHYRIDINES WHICH AFFECT IL-4 AND G-CSF 审中-公开
标题翻译：影响IL-4和G-CSF的萘啶类
公开(公告)号：WO9748368A3
公开(公告)日：1998-02-05
申请号：PCT/US9709202
申请日：1997-06-18
申请人： SCHERING CORP
发明人： SOLOMON DANIEL M , GRACE MICHAEL J , FINE JAY S , BOBER LORETTA A , SHERLOCK MARGARET H
IPC分类号： C07D241/12 , A61K31/4375 , A61K31/444 , A61K31/4965 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , C07D471/04 , A61K
CPC分类号： C07D471/04
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein E, Q, T, U, V, L, Z, X, W, M, Y and Y' are as set forth herein, are described. These compounds are useful as agents in the treatment of allergy, inflammation, autoimmune diseases, B-cell lymphomas, tumors, and the after effects of bone marrow transplantation.
摘要翻译：描述了式（I）化合物或其药学上可接受的盐，其中E，Q，T，U，V，L，Z，X，W，M，Y和Y'如本文所述。这些化合物可用作治疗过敏，炎症，自身免疫性疾病，B细胞淋巴瘤，肿瘤和骨髓移植的后期作用的药剂。

10. 发明专利

JP2008255119A Naphthyridine which affect il-4 and g-csf 审中-公开
标题翻译：影响IL-4和G-CSF的萘啶
公开(公告)号：JP2008255119A
公开(公告)日：2008-10-23
申请号：JP2008117917
申请日：2008-04-28
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： SOLOMON DANIEL M , GRACE MICHAEL J , FINE JAY S , BOBER LORETTA A , SHERLOCK MARGARET H
IPC分类号： C07D241/12 , C07D471/04 , A61K31/4375 , A61K31/444 , A61K31/4965 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08
CPC分类号： C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide a compound, a composition and a method, described in the specification, concerning to naphthyridines affecting on IL-4 and G-CSF. SOLUTION: The compound is an antagonist of IL-4 and is an antagonist useful as a medicine for treating allergy, inflammation, autoimmune diseases and specific B-cell lymphomas. The compound and another compound are also a stimulator for production of granulocyte colony stimulus factor (G-CSF) produced from human peripheral blood mononuclear cell (PBMNC) and monocyte/macrophage. So, since the compounds stimulate neutrophile granulopoiesis, the compounds are useful as a treatment medicine for treating a cancer patient and for treating a bone marrow transplanted patient. And pharmaceutical compositions containing a therapeutically effective amount of the compound or another compound with a pharmaceutically permissible carrier are also provided. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：提供说明书中描述的关于影响IL-4和G-CSF的萘啶的化合物，组合物和方法。解决方案：该化合物是IL-4的拮抗剂，并且是用作治疗过敏，炎症，自身免疫疾病和特异性B细胞淋巴瘤的药物的拮抗剂。该化合物和另一种化合物也是用于产生由人外周血单核细胞（PBMNC）和单核细胞/巨噬细胞产生的粒细胞集落刺激因子（G-CSF）的刺激剂。因此，由于化合物刺激嗜中性粒细胞生成，所以这些化合物可用作治疗癌症患者和治疗骨髓移植患者的治疗药物。还提供了含有治疗有效量的化合物或另一种化合物与药学上可允许的载体的药物组合物。版权所有（C）2009，JPO＆INPIT

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