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41. 发明申请

US20050026916A1 Heterocyclic compounds as P2X7 ion channel blockers 失效
标题翻译：杂环化合物作为P2X7离子通道阻断剂
公开(公告)号：US20050026916A1
公开(公告)日：2005-02-03
申请号：US10896166
申请日：2004-07-21
申请人： Patrick Shum , Alexandre Gross , Liang Ma , Daniel McGarry , Gregory Merriman , David Rampe , Garth Ringheim , Jeffrey Sabol , Francis Volz
发明人： Patrick Shum , Alexandre Gross , Liang Ma , Daniel McGarry , Gregory Merriman , David Rampe , Garth Ringheim , Jeffrey Sabol , Francis Volz
IPC分类号： C07D233/20 , C07D233/22 , C07D233/24 , C07D233/42 , C07D233/46 , C07D233/48 , C07D235/30 , C07D401/04 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/10 , A61K31/5377 , A61K31/4178 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/497
CPC分类号： C07D401/04 , C07D233/20 , C07D233/22 , C07D233/24 , C07D233/42 , C07D233/46 , C07D233/48 , C07D235/30 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/10
摘要： The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.
摘要翻译：本发明涉及式II的新一系列4,5-二苯基-2-氨基-4,5-二氢咪唑衍生物：其中R 1，R 2，R 3，R 4，R 5，X和Y为本文定义。本发明还涉及制备这些化合物的方法。本发明的化合物是P2X7离子通道阻断剂，因此可用作药剂，特别是用于治疗和/或预防各种具有炎症成分的疾病，包括炎性肠病，类风湿性关节炎和与中枢相关的疾病状况神经系统，如中风，阿尔茨海默病等

42. 发明申请

US20030064980A1 Selective neurokinin antagonists 失效
标题翻译：选择性神经激肽拮抗剂
公开(公告)号：US20030064980A1
公开(公告)日：2003-04-03
申请号：US10163663
申请日：2002-06-06
发明人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
IPC分类号： C07D285/16 , C07D265/04 , A61K031/548 , A61K031/535 , A61K031/513
CPC分类号： C07D239/10 , C07C45/71 , C07C217/48 , C07D211/58 , C07D233/14 , C07D233/16 , C07D233/22 , C07D233/30 , C07D233/32 , C07D233/42 , C07D233/46 , C07D233/48 , C07D233/78 , C07D285/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07F9/6506 , C07C47/575
摘要： Compound represented by the structural formula 1 or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is nullOnull, nullSnull, nullSOnull, nullSO2null, nullNR12null, nullNCOR12null or nullNR12SO2R15; 2 is selected from the group consisting of 3 X2 is nullOnull, nullSnull or nullNR5null; Y is nullO, nullS or nullNR11; Y1 is H, C1-C6 alkyl, nullNR17R13, nullSCH3, R19-aryl(CH2)n6null, R19-heteroaryl-(CH2)n6null, null(CH2)n6-heterocycloalkyl, null(C1-C3)alkyl-NHnullC(O)O(C1-C6)alkyl or nullNHC(O)R15; R5 is H or null(CH2)n1-G, wherein n2 is 0-5, G is H, nullCF3, nullCHF2, nullCH2F, nullOH, nullOnull(C1-C6 alkyl), nullSO2R13, nullOnull(C3-C8 cycloalkyl), nullNR13R14, nullSO2NR13R14, nullNR13SO2R15nullNR13COR12, nullNR12(CONR13R14), nullCONR13R14, nullCOOR12, C3-C8 cycloalkyl, R19-aryl, R19-heteroaryl, and provided when n1null0, G is not H; R1, R2, R3 and R7 are H, alkyl, cycloalkyl, nullCHF2, nullCH2F or nullCF3; or R1 and R2, together with the carbon to which they are attached, form an alkylene ring; or R1 and R2 together are nullO; R6 is R7 or nullOH; and the remaining variables are as defined in the specification, methods of treating diseases susceptible to treatment with neurokinin antagonists with said compounds, and pharmaceutical compositions comprising said compounds are disclosed. Also disclosed are pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with an effective amount of a selective serotonin reuptake inhibitor.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O - ， - S - ， - SO - ， - SO 2 - ， - NR 12 - ， - NRCOR 12 - 或-NR 12 SO 2 R 15; 选自X2为-O - ， - S-或-NR5-; Y = O，= S或= NR11; Y1是H，C1-C6烷基，-NR17R13，-SCH3，R19-芳基（CH2）n6-，R19-杂芳基 - （CH2）n6-， - （CH2）n6-杂环烷基， - （C1-C3） NH-C（O）O（C 1 -C 6）烷基或-NHC（O）R 15; R5是H或 - （CH2）n1-G，其中n2是0-5，G是H，-CF3，-CHF2，-CH2F，-OH，-O-（C1-C6烷基），-SO2R13，-O - （C3-C8环烷基），-NR13R14，-SO2NR13R14，-NR13SO2R15-NR13COR12，-NR12（CONR13R14），-CONR13R14，-COOR12，C3-C8环烷基，R19-芳基，R19

43. 发明申请

US20030042471A1 Conjugated copolymers of dithienothiophene with vinylene or acetylene 失效
标题翻译：二噻吩并噻吩与亚乙烯基或乙炔的共轭共聚物
公开(公告)号：US20030042471A1
公开(公告)日：2003-03-06
申请号：US10222891
申请日：2002-08-19
申请人： Merck Patent GmbH
发明人： Mark Giles , Louise Diane Farrand , Martin Heeney , Maxim Shkunov , David Sparrowe , Steven Tierney , Marcus Thompson , Iain McCulloch
IPC分类号： H01B001/00
CPC分类号： C08G61/126 , C07D233/46
摘要： Conjugated copolymers of dithienothiophene with vinylene or acetylene are suitable for use as semiconductors or charge transport materials in optical, electrooptical or electronic devices including field effect transistors, electroluminescent, photovoltaic and sensor devices.
摘要翻译：二噻吩并噻吩与亚乙烯基或乙炔的共轭共聚物适用于包括场效应晶体管，电致发光，光伏和传感器装置的光学，电光或电子器件中的半导体或电荷传输材料。

44. 发明授权

US5840911A Imidazole derivatives, their preparation and their use as S-adenosylmethionine decarboxylase (=SAMDC) inhibitors 失效
标题翻译：咪唑衍生物，其制备及其作为S-腺苷甲硫氨酸脱羧酶（= SAMDC）抑制剂的用途
公开(公告)号：US5840911A
公开(公告)日：1998-11-24
申请号：US875299
申请日：1997-07-23
申请人： Jorg Frei , Jaroslav Stanek
发明人： Jorg Frei , Jaroslav Stanek
IPC分类号： A61K31/415 , A61P33/02 , A61P35/00 , A61P43/00 , C07D233/46 , C07D233/88
CPC分类号： C07D233/88 , C07D233/46
摘要： Described are compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or hydroxy; R.sub.2, R.sub.2 ' and R.sub.2 " are each independently of the others hydrogen or a substituent other than hydrogen; either R.sub.3 is hydrogen or a substituent other than hydrogen and R.sub.4 is hydrogen or lower alkyl, or R.sub.3 and R.sub.4 together form a divalent radical of the formula --(CH.sub.2).sub.n -- wherein n is 2 or 3; R.sub.5 and R.sub.6 are each independently of the other hydrogen, alkyl or aryl; and either R.sub.7 and R.sub.8 are each hydrogen, or R.sub.7 and R.sub.8 together form a bond; tautomers thereof, provided that at least one tautomerisable group is present; and salts thereof. The compounds inhibit the enzyme S-adenosylmethionine decarboxylase and are suitable, for example, for the treatment of tumours and protozoal infections.
摘要翻译： PCT No.PCT / EP96 / 00143 Sec。 371日期1997年7月23日 102（e）日期1997年7月23日PCT 1996年1月15日PCT PCT。出版物WO96 / 22979 日期1996年8月1日描述的是式I化合物（Ⅰ），其中R1是氢或羟基; R2，R2'和R2“各自独立于氢或氢以外的取代基; R3是氢或除氢以外的取代基，R4是氢或低级烷基，或者R3和R4一起形成式 - （CH 2）n - 的二价基团，其中n是2或3; R 5和R 6各自独立地为氢，烷基或芳基; 并且R 7和R 8各自为氢，或者R 7和R 8一起形成键; 其互变异构体，只要存在至少一种互变异构体组; 及其盐。该化合物抑制酶S-腺苷甲硫氨酸脱羧酶，并且适用于例如治疗肿瘤和原生动物感染。

45. 发明授权

US5676978A Methods of inhibiting undesirable cell growth using a combination of a cyclocreatine compound and a hyperplastic inhibitory agent 失效
标题翻译：使用环磷酸化合物和增生性抑制剂的组合来抑制不期望的细胞生长的方法
公开(公告)号：US5676978A
公开(公告)日：1997-10-14
申请号：US185438
申请日：1994-01-21
申请人： Beverly A. Teicher , Donald W. Kufe , Rima Kaddurah-Daouk
发明人： Beverly A. Teicher , Donald W. Kufe , Rima Kaddurah-Daouk
IPC分类号： A61K31/195 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/505 , A61K31/66 , A61K31/675 , A61K38/00 , A61K48/00 , C07C257/14 , C07C311/51 , C07D207/22 , C07D233/06 , C07D233/46 , C07D233/48 , C07D233/88 , C07D487/04 , C07F9/22 , C07F9/6506 , C07K14/82 , C12N9/12 , C12N15/113 , C12Q1/50 , G01N33/574 , A61K33/24 , A61K31/35 , A61K31/65
CPC分类号： A61K31/685 , A61K31/195 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/505 , A61K31/66 , A61K31/675 , A61K31/70 , C07C257/14 , C07C311/51 , C07D207/22 , C07D233/06 , C07D233/46 , C07D233/48 , C07D233/88 , C07D487/04 , C07F9/222 , C07F9/65061 , C07K14/82 , C12N15/1137 , C12N9/12 , C12Q1/50 , C12Y207/0102 , C12Y207/03002 , C12Y207/04003 , C12Y406/01001 , G01N33/57484 , A61K38/00 , A61K48/00 , G01N2333/01
摘要： The present invention provides for the use of creatine compounds and hyperplastic inhibitory agents for prophylactic and/or therapeutic treatments of undesirable cell growth, e.g. tumors. The present invention provides methods of using creatine compounds, in combination with a hyperplastic inhibitory agent, to inhibit the growth of undesirable cells in a subject. The present invention is based, at least in part, on the discovery that creatine compounds and hyperplastic inhibitory agents, such as inhibitory agents, additively and synergistically combine to inhibit cell growth. The present invention further pertains to compositions for inhibiting undesirable cell growth in a subject. The compositions of the present invention include an effective amount of the creatine compound and a hyperplastic inhibitory agent in a pharmaceutically acceptable carrier. Other aspects of the invention include packaged creatine compounds and inhibitory agents. The packaged compounds and agents also include instructions for using the creatine compound/inhibitory agent combination for inhibiting undesirable cell growth in a patient or instructions for using the compounds and agents, in selected quantities, in a pharmaceutically acceptable carrier.
摘要翻译：本发明提供了肌酸化合物和增生性抑制剂用于预防和/或治疗不期望的细胞生长的用途，例如，肿瘤。本发明提供了使用与增生性抑制剂组合的肌酸化合物抑制受试者中不想要的细胞生长的方法。本发明至少部分地基于发现肌酸化合物和增生性抑制剂，例如抑制剂，相加地并协同地组合以抑制细胞生长。本发明还涉及用于抑制受试者中不需要的细胞生长的组合物。本发明的组合物在药学上可接受的载体中包含有效量的肌酸化合物和增生性抑制剂。本发明的其它方面包括包装的肌酸化合物和抑制剂。包装的化合物和试剂还包括使用肌酸化合物/抑制剂组合来抑制患者中不期望的细胞生长的说明书或使用选定量的化合物和试剂在药学上可接受的载体中的说明书。

46. 发明授权

US4513140A 2-Amino-4,5-dihydro-1H-imizole-1-carboxanilides 失效
标题翻译： 2-氨基-4,5-二氢-1H-咪唑-1-甲酰苯胺
公开(公告)号：US4513140A
公开(公告)日：1985-04-23
申请号：US514541
申请日：1983-07-18
申请人： Leonard R. Hecker
发明人： Leonard R. Hecker
IPC分类号： C07D233/46
CPC分类号： C07D233/46
摘要： Novel 2-amino-4,5-dihydro-1H-imidazole-1-carboxanilides, which are made by reacting 2-amino-4,5-dihydroimidazole with an aryl isocyanate, are made stable to rearrangement when converted to acid addition salt form, and are useful either as antihypertensive agents and/or antisecretary agents, as well as being intermediates to prepare known pharmacologically active N-aryl-N'-(4,5-dihydro-1H-imidazol-2-yl)ureas.
摘要翻译：通过2-氨基-4,5-二氢咪唑与异氰酸芳基酯反应制备的新型2-氨基-4,5-二氢-1H-咪唑-1-甲酰苯胺在转化为酸加成盐形式时使其重排稳定并且可用作抗高血压药和/或抗原分泌剂，以及制备已知的药理学活性N-芳基-N' - （4,5-二氢-1H-咪唑-2-基）脲的中间体。

47. 发明授权

US3772291A 2-acylimino-1,3-diazacycloalkenes and-alkadienes 失效
标题翻译： 2-亚氨基-1,3-二氮杂双环十二烷酮和碱
公开(公告)号：US3772291A
公开(公告)日：1973-11-13
申请号：US3772291D
申请日：1971-03-29
申请人： CIBA GEIGY CORP
发明人： ARMISTEAD LUCAS R , MORTON BLATTER H
IPC分类号： C07D233/44 , C07D233/46 , C07D233/48 , C07D49/34 , C07D51/28 , C07D53/02
CPC分类号： C07D233/46 , C07D233/44 , C07D233/48
摘要： CERTAIN 2-TRIMETHOXYBENZOYLIMINO-1,3-DIAZACYCLOALKENES AND -ALKADIENES, USEFUL AS INTERMEDIATES, ALSO EXHIBIT CENTRAL NERVOUS SYSTEM DEPRESSING EFFECTS.

48. 发明授权

US3758473A 2-acylimino-1,3-diazacycloalkanes 失效
标题翻译： 2-乙酰氨基-1,3-二氮杂环戊烷
公开(公告)号：US3758473A
公开(公告)日：1973-09-11
申请号：US3758473D
申请日：1971-06-29
申请人： CIBA GEIGY CORP
发明人： LUCAS R , BLATTER H
IPC分类号： C07D233/44 , C07D233/46 , C07D233/48 , C07D49/30 , C07D51/18
CPC分类号： C07D233/48 , C07D233/44 , C07D233/46
摘要： 1-R1-2-TRIMETHOXYBENZOYLIMINO-1,3-DIAZACYCLOALKANES, E.G. THOSE OF THE FORMULA

(3,4,5-TRI(CH3-O-)PHENYL)-CO-N=C
R1=ALIPHATIC OR CYCLOALIPHATIC RADICAL R3=H, ALKYL OR ALKANOYL N=2-4 OR SALTS THEREOF EXHIBIT HYPNOTIC EFFECTS.

49. 发明授权

US3740412A Imidazoline-3-oxide-1-oxyl derivatives 失效
标题翻译：咪唑啉-3-氧化物-1-氧化物衍生物
公开(公告)号：US3740412A
公开(公告)日：1973-06-19
申请号：US3740412D
申请日：1970-04-08
申请人： SYNVAR ASS
发明人： ULLMAN E , OSIECKI J , CALL L , LEUTE R
IPC分类号： C07D233/06 , C07D233/28 , C07D233/38 , C07D233/42 , C07D233/44 , C07D233/46 , C07D233/48 , C07D233/70 , C07D233/88 , C07D49/30 , C07D49/34
CPC分类号： C07D233/46 , C07D233/06 , C07D233/28 , C07D233/38 , C07D233/42 , C07D233/44 , C07D233/48 , C07D233/70 , C07D233/88 , Y10T436/24
摘要： DIHYDROIMIDAAZOLES, TETRAHYDROMINIDAZOLES AND TAUTOMERIC MIXTURES OF DIHYDROIMIDAZOLES AND TETRAHYDROIMIDAZOLES HAVING TERITARY CARBON ATOMS IN THE NUMBER 4 AND NUMBER 5 POSITIONS OF THE HYDROMIDAZOLE RING, AND HAVING ATTACHED AT THE C2 POSITION OF THE IMIDAZOLE RING A RADICAL SELECTED FROM THE GROUP CONSISTING OF -NR1R2, =NR2 --NR2-,--S-, --SR1, AND --OR1, WHEREIN R1 IS HYDROGEN, ALKYL, ARYL, ALKENYL, ALKYNYL, ALKYMYL CYCLOAALKYL AND SUBSTITUTED DERATIVES THEREOF, AND R2 IS HYDROGEN, ALKYL, ARYL ALKENYL, ALKYNYL, CYCLOAKYL,

-CO-R1, -CO-N(-R1)-R2, -COO-R1, -CO-S-R1, -SO2-R1,

-C(-R1)=N-R1, -C(=N-R1)-N(-R1)2, -C(-O-R1)=N-R1,

-C(-S-R1)=N-R1, -COO-CO-N(-C2H5)2

AND SUBSTITUTED DERIVATIVES THEREOF. THERE ARE ONE OR TWO OXIDIZED NITROGEN ATOMS IN THE RING IN THE FORM OF OXIDES OR HYDROXIDES.

50. 发明授权

US3729463A P-aminoalkylbenzenesulfonamide derivatives 失效
公开(公告)号：US3729463A
公开(公告)日：1973-04-24
申请号：US3729463D
申请日：1970-09-01
申请人： CIBA GEIGY CORP
发明人： DIETRICH H , LEHMANN C
IPC分类号： C07D233/02 , A61K31/415 , C07D233/46 , C07D233/88 , C07D49/30
CPC分类号： C07D233/46 , C07C327/00
摘要： COMPOUNDS OF THE CLASS OF 1-(P-THIOCARBOXAMIDOALKYL)PHENYLSULFONYL)-2-IMINO-IMIDAZOLIDINES AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF HAVE HYPOGYLCEMIC ACTIVITY, THEY ARE ACTIVE INGREDIENTS OF PHARMACEUTICAL COMPOSITIONS AND ARE USEFUL FOR THE TREATMENT OF DIABETES MELLITUS, A TYPICAL EMBODIMENT IS 1-(P-(2-THIOACETAMIDOETHYL)-PHENYLSULFONYL) - 2 - IMINO-3-ISOBUTYLIMIDAZOLIDINE.

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