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11. 发明申请

US20090018141A1 KINASE INHIBITORS, COMPOSITIONS THEREOF, AND METHODS OF USE THEREWITH 失效
标题翻译：激酶抑制剂，其组合物及其使用方法
公开(公告)号：US20090018141A1
公开(公告)日：2009-01-15
申请号：US12135575
申请日：2008-06-09
申请人： Robert Shoemaker , John Cardellina , Michael Currens , Sudhir Kondapaka , Yves Pommier , Andy Jobson , Dominic Scudiero , David Waugh , George Lountos , Charles M. Cook , Guangtao Zhang , Andrew Colasanti , Christopher R. Self , Janet Cicariello Cook
发明人： Robert Shoemaker , John Cardellina , Michael Currens , Sudhir Kondapaka , Yves Pommier , Andy Jobson , Dominic Scudiero , David Waugh , George Lountos , Charles M. Cook , Guangtao Zhang , Andrew Colasanti , Christopher R. Self , Janet Cicariello Cook
IPC分类号： A61K31/496 , A61K31/17 , C07C275/40 , A61K31/404 , C07D209/42 , C07D403/12 , C12N9/99 , A61P3/10 , A61K31/444 , C07D401/12 , A61K31/495 , C07D241/04
CPC分类号： C07D209/42 , C07D209/60 , C07D213/86 , C07D217/26 , C07D231/56 , C07D233/52 , C07D239/42 , C07D277/50 , C07D277/82 , C07D307/68 , C07D307/85 , C07D401/12 , C07D403/12 , C07D471/04
摘要： Provided herein are Compounds having the following structure: wherein A, L, X and ring B are as defined herein, compositions comprising an effective amount of a Compound and methods for treating or preventing cancer, hypoxia, diabetes, stroke, autoimmune disease or a condition treatable or preventable by inhibition of Chk2, the ATM-Chk2 pathway or RSK2 comprising administering an effective amount of a Compound to a patient in need thereof.
摘要翻译：本文提供具有以下结构的化合物：其中A，L，X和环B如本文所定义，包含有效量的化合物的组合物和用于治疗或预防癌症，缺氧，糖尿病，中风，自身免疫疾病或病症的方法可通过抑制Chk2，ATM-Chk2途径或RSK2治疗或预防，包括向有需要的患者施用有效量的化合物。

12. 发明授权

US07271266B2 Substituted 2,3-diphenyl pyridines 失效
标题翻译：取代的2,3-二苯基吡啶
公开(公告)号：US07271266B2
公开(公告)日：2007-09-18
申请号：US10508043
申请日：2003-03-24
申请人： Paul E. Finke , Laura C. Meurer , John S. Debenham , Richard B. Toupence , Thomas F. Walsh
发明人： Paul E. Finke , Laura C. Meurer , John S. Debenham , Richard B. Toupence , Thomas F. Walsh
IPC分类号： C07D211/82 , C07D211/60
CPC分类号： C07D213/79 , C04B35/632 , C07D213/65 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

13. 发明申请

US20050182103A1 Substituted 2,3-diphenyl pyridines 失效
标题翻译：取代的2,3-二苯基吡啶
公开(公告)号：US20050182103A1
公开(公告)日：2005-08-18
申请号：US10508043
申请日：2003-03-24
申请人： Paul Finke , Laura Meurer , John Debenham , Richard Toupence , Thomas Walsh
发明人： Paul Finke , Laura Meurer , John Debenham , Richard Toupence , Thomas Walsh
IPC分类号： C07D213/64 , A61K31/44 , A61K31/4418 , A61K31/4439 , A61K31/4545 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K45/00 , A61K47/02 , A61K47/10 , A61K47/26 , A61K47/34 , A61P1/04 , A61P1/10 , A61P1/16 , A61P3/04 , A61P9/00 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P29/00 , A61P43/00 , C07D213/56 , C07D213/65 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12 , C07D41/02
CPC分类号： C07D213/79 , C04B35/632 , C07D213/65 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

14. 发明申请

US20040167126A1 Hydrazide and alkoxyamide angiogenesis inhibitors 失效
标题翻译：酰肼和烷氧酰胺血管生成抑制剂
公开(公告)号：US20040167126A1
公开(公告)日：2004-08-26
申请号：US10782502
申请日：2004-02-19
发明人： Richard A. Craig , Megumi Kawai , Linda M. Lynch , Jyoti R. Patel , George S. Sheppard , Jieyi Wang , Fan Yang , Nwe Ba-Maung , Xenia Beebe Searle
IPC分类号： C07D279/12 , C07D265/30 , A61K031/535 , A61K031/445
CPC分类号： C07D207/416 , C07B2200/07 , C07C243/34 , C07C243/38 , C07C251/86 , C07C255/44 , C07C255/57 , C07C259/06 , C07C281/02 , C07C323/48 , C07C323/60 , C07C323/63 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D207/50 , C07D209/14 , C07D211/98 , C07D213/42 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/42 , C07D231/38 , C07D237/20 , C07D239/28 , C07D239/42 , C07D241/44 , C07D261/18 , C07D277/54 , C07D277/56 , C07D277/82 , C07D295/15 , C07D295/32 , C07D307/68 , C07D307/84 , C07D317/68 , C07D333/38 , C07D333/68 , C07D333/72
摘要： Compounds having the formula 1 are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.
摘要翻译：具有下式的化合物是甲硫氨酸氨基肽酶2（MetAP2）抑制剂，可用于抑制血管发生。还公开了抑制哺乳动物血管生成的MetAP2抑制组合物和方法。

15. 发明申请

US20020002152A1 Hydrazide and alkoxyamide angiogenesis inhibitors 审中-公开
标题翻译：酰肼和烷氧酰胺血管生成抑制剂
公开(公告)号：US20020002152A1
公开(公告)日：2002-01-03
申请号：US09833917
申请日：2001-04-12
发明人： Richard A. Craig , Megumi Kawai , Linda M. Lynch , Jyoti R. Patel , George S. Sheppard , Jieyi Wang , Fan Yang , Nwe Ba-Maung
IPC分类号： A61K031/47 , A61K031/166 , C07C243/10 , C07D215/38
CPC分类号： C07D207/416 , C07B2200/07 , C07C243/34 , C07C243/38 , C07C251/86 , C07C255/44 , C07C255/57 , C07C259/06 , C07C281/02 , C07C323/48 , C07C323/60 , C07C323/63 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D207/50 , C07D209/14 , C07D211/98 , C07D213/42 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/42 , C07D231/38 , C07D237/20 , C07D239/28 , C07D239/42 , C07D241/44 , C07D261/18 , C07D277/54 , C07D277/56 , C07D277/82 , C07D295/15 , C07D295/32 , C07D307/68 , C07D307/84 , C07D317/68 , C07D333/38 , C07D333/68 , C07D333/72
摘要： Compounds having the formula 1 are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.
摘要翻译：具有下式的化合物是甲硫氨酸氨基肽酶2（MetAP2）抑制剂，可用于抑制血管发生。还公开了抑制哺乳动物血管生成的MetAP2抑制组合物和方法。

16. 发明授权

US4378239A N-Methylcarbamoyloxy benzaldehyde imine herbicide extenders 失效
标题翻译： N-甲基氨基甲酰氧基苯甲醛亚胺除草剂
公开(公告)号：US4378239A
公开(公告)日：1983-03-29
申请号：US257850
申请日：1981-04-27
申请人： Daniel L. Hyzak , Llewellyn W. Fancher , Edmund J. Gaughan , Joanna K. Hsu
发明人： Daniel L. Hyzak , Llewellyn W. Fancher , Edmund J. Gaughan , Joanna K. Hsu
IPC分类号： A01N25/22 , A01N47/12 , A01N47/22 , C07D213/86 , A01N37/00
CPC分类号： C07D213/86 , A01N25/22 , A01N47/12 , A01N47/22
摘要： Herbicidally active thiolcarbamates are employed in combination with certain N-methylcarbamoyloxy benzaldehyde imines having the formula ##STR1## in which R.sup.4 is selected from the group consisting of chlorophenyl, chlorophenylthiomethylphenyl, acetoxy, and ##STR2## where R.sup.5 is selected from the group consisting of phenyl, pyridyl, and cyanomethyl, and n is zero or one.In a typical application, the imine is included in sufficient quantity to lessen the rate of soil degradation of the thiolcarbamate. As a result, the herbicidal effectiveness of the thiolcarbamate is enhanced and prolonged, rendering a single application of the herbicide effective over a longer period of time.
摘要翻译：除草活性的硫代氨基甲酸酯与具有式“IMAGE”的某些N-甲基氨基甲酰氧基苯甲醛亚胺组合使用，其中R 4选自氯苯基，氯苯硫基甲基苯基，乙酰氧基和其中R 5选自苯基，吡啶基和氰基甲基，n为0或1。在典型的应用中，亚胺含量足以降低硫代氨基甲酸酯的土壤降解速率。因此，硫代氨基甲酸酯的除草效果得到增强和延长，使得除草剂的单次施用在更长的时间内有效。

17. 发明授权

US4292069A Arylthioureido pyridinecarbamino compounds and use as plant growth regulants 失效
标题翻译：芳硫基脲基吡啶甲氨基化合物，用作植物生长调节剂
公开(公告)号：US4292069A
公开(公告)日：1981-09-29
申请号：US227825
申请日：1981-01-23
申请人： Jerry L. Rutter , Charles G. Gibbs , Loren W. Hedrich
发明人： Jerry L. Rutter , Charles G. Gibbs , Loren W. Hedrich
IPC分类号： A01N47/34 , A01N47/36 , C07D213/86 , C07D213/87 , C07D471/04 , A01N43/40
CPC分类号： C07D213/86 , A01N47/34 , A01N47/36 , C07D213/87 , C07D471/04
摘要： A method of regulating the growth of plants, including combating unwanted vegetation, comprises applying to the plants, either on seed, the soil or directly on the plants an effective amount of a novel compound of the class having the general structural formula ##STR1## in which one of Q.sub.1, Q.sub.2, Q.sub.3 or Q.sub.4 is N, X is --OH or --O--(C.sub.1 -C.sub.4 alkyl) and Y is H or X and Y together represent a bond between carbon and nitrogen atoms and R is H or one or two of the following substituents: --Br, --Cl, --F, --I, --CF.sub.3, --CH.sub.3, --NO.sub.2 or --C.tbd.N, or an agriculturally acceptable salt thereof.
摘要翻译：一种调节植物生长的方法，包括防治不想要的植物，包括在种子，土壤或植物上直接施用有效量的具有一般结构式“IMAGE”的新颖化合物 Q1，Q2，Q3或Q4中的任一个为N，X为-OH或-O-（C1-C4烷基），Y为H或X，Y一起表示碳原子和氮原子之间的键，R为H或一个或两个以下取代基：-Br，-Cl，-F，-I，-CF3，-CH3，-NO2或-C3NONN，或其农业上可接受的盐。

18. 发明授权

US4252819A Antisecretory heterocyclic amidine compounds 失效
标题翻译：防雾杂环脒化合物
公开(公告)号：US4252819A
公开(公告)日：1981-02-24
申请号：US934276
申请日：1978-08-16
申请人： Yasufumi Hirata , Isao Yanagisawa , Toshinari Tamura , Masaaki Takeda
发明人： Yasufumi Hirata , Isao Yanagisawa , Toshinari Tamura , Masaaki Takeda
IPC分类号： C07D233/64 , A61K31/40 , A61K31/4402 , A61K31/4418 , A61K31/4427 , A61K31/455 , A61P43/00 , C07D213/30 , C07D213/32 , C07D213/68 , C07D213/86 , C07D233/54 , C07D277/26 , C07D307/52 , C07D401/12 , C07D401/14 , C07D413/12 , A61K31/34 , A61K31/38 , C07D307/54 , C07D333/24
CPC分类号： C07D213/30 , C07D213/32 , C07D213/68 , C07D213/86 , C07D233/64 , C07D277/26 , C07D307/52
摘要： Novel heterocyclic compounds shown by the formula ##STR1## wherein Het represents a 5-membered or 6-membered heterocyclic group which may have substituent(s); Z represents a sulfur atom or oxygen atom; X represents an oxygen atom or the unsubstituted or substituted imino group shown by N--R.sub.1 (wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a cyano group, an unsubstituted or alkyl substituted carbamoyl group, an unsubstituted or lower alkyl substituted thiocarbamoyl group, or a lower alkanoylamino group); Y represents a hydrogen atom, a lower alkyl group which may have substituent(s), a cycloalkyl group of 3-6 carbon atoms, a lower alkenyl group, a lower alkynyl group, an aryl group which may have substituent(s), an aralkyl group which may have substituent(s), a hydroxyl group, a cyano group, a carbamoyl group, an amidino group, an alkanoyl group which may have been substituted by halogen atom(s),an alkanoylamino group, an arylcarbonylamino group, an alkylamino group, an arylamino group, an arylsulfamoyl group, a lower alkoxycarbamoyl group, or an oxamoylamino group; and m and n represent an integer of 1-3; when X is N-R.sub.1, said X and Y may combine with each other to form a 5-membered or 6-membered heterocyclic ring containing 2-3 nitrogen atoms which may have substituent(s), and the pharmaceutically acceptable acid addition salts thereof.The compounds of this invention are useful as gastric acid secretion inhibitors.
摘要翻译：式中，Het表示可具有取代基的5元或6元杂环基的新型杂环化合物。 Z表示硫原子或氧原子; X表示氧原子或由N-R 1表示的未取代或取代的亚氨基（其中R 1为氢原子，低级烷基，氰基，未取代或烷基取代的氨基甲酰基，未取代或低级烷基取代的硫代氨基甲酰基，或低级烷酰氨基）; Y表示氢原子，可具有取代基的低级烷基，3-6个碳原子的环烷基，低级烯基，低级炔基，可具有取代基的芳基，可以具有取代基的芳烷基，羟基，氰基，氨基甲酰基，脒基，可被卤素原子取代的烷酰基，烷酰基氨基，芳基羰基氨基，烷基氨基，芳基氨基，芳基氨磺酰基，低级烷氧基氨基甲酰基或氨甲酰基氨基; m和n表示1-3的整数; 当X为N-R 1时，所述X和Y可以彼此结合形成含有2-3个可具有取代基的氮原子的5元或6元杂环，及其药学上可接受的酸加成盐。本发明的化合物可用作胃酸分泌抑制剂。

19. 发明授权

US4096264A Certain substituted imidazo [1,2-a] pyridines 失效
标题翻译：某些取代的咪唑并[8,1-a {9 {0]吡啶
公开(公告)号：US4096264A
公开(公告)日：1978-06-20
申请号：US718652
申请日：1976-08-26
申请人： Richard J. Bochis , Peter Kulsa
发明人： Richard J. Bochis , Peter Kulsa
IPC分类号： C07D213/79 , A61K31/435 , A61P33/10 , C07D213/38 , C07D213/42 , C07D213/53 , C07D213/86 , C07D471/04 , A61K31/44 , C07D401/02
CPC分类号： C07D213/42 , C07D213/38 , C07D213/53 , C07D213/86 , C07D471/04
摘要： Certain novel substituted imidazo [1,2-a] pyridines with a substituted amino group at the 2- or 3-position are active anthelmintic agents. The novel compounds are prepared from the appropriate substituted 2-aminopyridine precursor. Compositions which utilize said novel imidazo [1,2-a] pyridines as the active ingredient thereof for the treatment of helminthiasis are also disclosed.
摘要翻译：某些具有取代氨基的2-或3-位的取代咪唑并[1,2-a]吡啶是活性的驱肠剂。该新化合物由合适的取代的2-氨基吡啶前体制备。还公开了利用所述新型咪唑并[1,2-a]吡啶作为其活性成分用于治疗蠕虫病的组合物。

20. 发明授权

US3917626A 3,6-Dioxa-1,8-octandiamido bis (pyridinium) compounds 失效
标题翻译： 3,6-二氧杂-1,8-辛二胺二双（吡啶鎓）化合物
公开(公告)号：US3917626A
公开(公告)日：1975-11-04
申请号：US42869473
申请日：1973-12-27
申请人： ICI LTD
发明人： EDWARDS PHILIP NEIL
IPC分类号： A61K8/49 , A61Q11/00 , C07D213/16 , C07D213/40 , C07D213/63 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/86 , C07D213/87 , C07D31/28
CPC分类号： C07D213/87 , A61K8/4926 , A61Q11/00 , C07D213/06 , C07D213/16 , C07D213/40 , C07D213/63 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/86
摘要： A pyridine derivative of the formula:

wherein R1 and R2 which may be the same or different are each alkyl having 8 to 14 carbon atoms, n-undec-10-yl, 2-nhexyloxyethyl, 2-(2-butoxyethoxy)-ethyl,3,4-dichlorophenyl, 4chlorobenzyl, 2,4-dichlorobenzyl or 2-naphthylmethyl; A1 and A2 are each a direct linkage or a linking group of the formula CH2CO.NH-wherein the methylene is joined to the pyridine nitrogen; (X1.X2)2 represents two monoanions or a dianion selected from the group consisting of two halide, methanesulphonate, toluene-p-sulphonate or acetate ions or the sulphate dianion; and A3 is a linking group of the formula: NH.CO(CH2OCH2)2 CO.NH- . A process for making these salts, compositions containing them and methods of precenting the growth of, or killing, bacteria by applying one of these salts to a bacterially infected environment are also disclosed.
摘要翻译：具有下式的吡啶衍生物：A3。（X1.X2）2 - - - - - - ，其中R1和R2可以相同或不同，分别为碳原子数为8〜14的烷基，正丁氧基乙基，2-（2-丁氧基乙氧基） - 乙基，3,4-二氯苯基，4-氯苄基，2,4-二氯苄基或2-萘基甲基; A1和A2各自是式-CH 2 CO.NH的直接键合或连接基团，其中亚甲基与吡啶氮键合; （X1.X2）2 - 代表两个单阴离子或选自两个卤化物，甲磺酸盐，甲苯对磺酸盐或乙酸根离子或硫酸盐二价阴离子的二阴离子; 并且A3是下式的连接基团：-NH.CO（CH 2 OCH 2）2 CO.NH-。

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