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71. 发明申请

US20130289036A1 SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL)-IMIDAZO[1,2-B][1,2,4]TRIAZIN-2-YL]BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME 有权
标题翻译： 2-氟-N-甲基-4- [7-（喹啉-6-基甲基） - 咪唑并[1,2-B] [1,2,4]三嗪-2-基]苯甲酰胺和方法的相关准备相同
公开(公告)号：US20130289036A1
公开(公告)日：2013-10-31
申请号：US13793864
申请日：2013-03-11
申请人： Lingkai WENG , Lei QIAO , Jiacheng ZHOU , Pingli LIU , Yongchun PAN
发明人： Lingkai WENG , Lei QIAO , Jiacheng ZHOU , Pingli LIU , Yongchun PAN
IPC分类号： C07D487/04
CPC分类号： A61K31/53 , C07D253/07 , C07D401/10 , C07D487/04
摘要： The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.
摘要翻译：本发明涉及c-Met激酶抑制剂2-氟-N-甲基-4- [7-（喹啉-6-基甲基） - 咪唑并[1,2-b] [1]的二氯氯酸和二苯磺酸盐，2,4]三嗪-2-基]苯甲酰胺及其药物组合物，其可用于治疗与激酶途径失调相关的癌症和其它疾病。本发明还涉及制备2-氟-N-甲基-4- [7-（喹啉-6-基甲基）咪唑并[1,2-b] [1,2,4]三嗪-2-酮的方法和中间体，吡啶-2-基]苯甲酰胺及其盐。

72. 发明申请

US20130198974A1 Non-Metal Tanning Process 有权
标题翻译：非金属鞣制工艺
公开(公告)号：US20130198974A1
公开(公告)日：2013-08-08
申请号：US13879207
申请日：2011-10-05
申请人： Claus Reineking , Roberta Gamarino , Licia Trimarco , Maurizio Quaglierini , Markus Gisler , Rainer Nusser
发明人： Claus Reineking , Roberta Gamarino , Licia Trimarco , Maurizio Quaglierini , Markus Gisler , Rainer Nusser
IPC分类号： C14C3/26 , C14C3/28
CPC分类号： C14C3/00 , C07D251/44 , C07D253/00 , C07D253/07 , C07D253/075 , C14C3/02 , C14C3/04 , C14C3/08 , C14C3/26 , C14C3/28
摘要： Tanned leather, skin or pelt is produced by non-metal tanning, comprising the step of tanning a bated hide, skin or pelt with a tanning agent (A), the tanning agent (A) being at least one compound of formula (I), wherein X signifies fluorine or chlorine, and/or (+NR3)0-1, wherein R is a substituted C1 to C6 alkyl group or an unsubstituted C1 to C6 alkyl group, an unsubstituted C6 to C10 aryl group or a substituted C6 to C10 aryl group or a C5 to C6 heteroaryl group. R1 signifies hydrogen, C1-8-alkyl or an alkyleneoxy radical of formula (Ia), —(—C2-3 alkylene—O—)q—H (Ia) R2 signifies hydrogen, hydroxy, C1-4-alkyl or C1-4-alkoxy, m signifies 1 or 2, n signifies 0 to 2, q is of from 1 to 10, M signifies hydrogen or an alkali metal cation or an ammonium cation, the ammonium cation being a protonated tertiary amine or a quaternary ammonium cation, in a tanning bath, the tanning bath having a pH of from 6 to 10 at the beginning of tanning step, wherein the bated hide or skin or pelt is subjected to tanning with (A) without previous pickling.
摘要翻译：鞣制的皮革，皮肤或毛皮是通过非金属鞣制制成的，包括用鞣剂（A），鞣制剂（A）为至少一种式（I）化合物鞣制皮肤，皮肤或皮肤的步骤，，其中X表示氟或氯，和/或（+ NR3）0-1，其中R是取代的C1至C6烷基或未取代的C1至C6烷基，未取代的C6至C10芳基或取代的C6至 C10芳基或C5〜C6杂芳基。 R 1表示氢，C 1-8 - 烷基或式（Ia）的亚烷基氧基， - （ - C 2-3亚烷基-O-）q H（Ia）R 2表示氢，羟基，C 1-4 - 烷基或C 1-4 - 烷氧基，表示1或2，n表示0至2，q表示1至10，M表示氢或碱金属阳离子或铵阳离子，铵阳离子为质子化叔胺或季铵阳离子，鞣制浴，在鞣制步骤开始时pH为6至10的鞣制浴，其中所述皮革或皮肤或毛皮在不进行酸洗的情况下经受鞣制（A）。

73. 发明申请

US20130085276A1 CARBOXYLATION CATALYSTS 有权
标题翻译：羧氧化催化剂
公开(公告)号：US20130085276A1
公开(公告)日：2013-04-04
申请号：US13702886
申请日：2011-06-09
申请人： Steven P. Nolan , Catherine Cazin
发明人： Steven P. Nolan , Catherine Cazin
IPC分类号： C07B41/08 , C07D263/34 , C07D261/18 , C07D263/58 , C07D277/56 , C07D275/03 , C07D277/68 , C07D233/90 , C07D235/24 , C07D237/24 , C07D249/10 , C07D253/07 , C07D473/00 , C07F1/08 , C07F1/10 , C07B59/00 , C07D307/68
CPC分类号： C07B41/08 , B01J31/185 , B01J31/2226 , B01J31/2265 , B01J31/2269 , B01J31/2273 , B01J31/24 , B01J2531/16 , B01J2531/17 , B01J2531/18 , C07B59/002 , C07D233/90 , C07D235/24 , C07D237/24 , C07D249/10 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D275/03 , C07D277/56 , C07D277/68 , C07D307/68 , C07D473/00 , C07F1/08 , C07F1/10
摘要： The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives.
摘要翻译：描述了在底物羧化中使用Z-M-OR形式的络合物。基团Z是双电子供体配体，M是金属，OR选自OH，烷氧基和芳氧基。底物可以在C-H或N-H键被羧化。金属M可以是铜，银或金。双电子供体配体可以是膦，卡宾或亚磷酸酯配体。还描述了制备复合物的方法和用于制备同位素标记的木糖酸和羧酸衍生物的方法。

74. 发明授权

US08053573B2 Monomer 5, 6-diphenyl-1.2.4-traizinic derivatives and the use thereof 有权
标题翻译：单体5,6,6-二苯基-1.2.4-衍生物及其用途
公开(公告)号：US08053573B2
公开(公告)日：2011-11-08
申请号：US11579341
申请日：2005-05-04
申请人： Jérôme Rey , Pascal Bordat , Roger Tarroux
发明人： Jérôme Rey , Pascal Bordat , Roger Tarroux
IPC分类号： C07D253/065 , C07D253/07 , A61K31/53 , A61K8/49 , A61Q5/12 , A61Q17/04
CPC分类号： C07D253/065 , A61K8/4966 , A61Q17/04 , C07D253/07
摘要： The invention relates to the use of 5,6-diphenyl-1,2,4-triazinic compounds of general formula (I), wherein cycle penetrating bonds display an ortho, meta or para indifferent substitution position, identical or different R1 and R2 represent a hydrogen, fluoride, chloride or bromine atom, C1 to C12 linear or branched alkyl, C1 A C18 linear or branched hydroxy, alkoxy poly(ethoxy)-alkoxy with a C1 to C4 alkyl fragment and an ethoxy number ranging from 1 to 4, amino or mono or di-alkylamino with a C1 to C4 alkyl fragment group, R3 represents a chlorine atom, a hydroxy, amino, a phenyl possibly 1 to 3 times substituted by a hydroxy radical situated at least in a para or phenyl position possibly 1 to 3 times substituted in an ortho, meta or para position by a C1 to C12 alkoxy or cyano or alkymino group with a C1 to C7 alkyl fragment in the form of active sun filters or light-protective agents and to cosmetic composition containing said compounds.
摘要翻译：本发明涉及通式（I）的5,6-二苯基-1,2,4-三嗪化合物的用途，其中循环穿透键显示相邻或不同的取代位置，相同或不同的R 1和R 2表示 C 1 -C 12直链或支链烷基，C 1 -C 18直链或支链羟基，具有C1至C4烷基片段的烷氧基聚（乙氧基） - 烷氧基和1至4的乙氧基，氨基或一或二烷基氨基与C 1至C 4烷基片基，R 3表示氯原子，羟基，氨基，可被1至3倍被至少位于对位或苯基位置的羟基取代的苯基，可能为1 以C1-C12烷氧基或氰基或烷基氨基取代邻位，间位或对位至活性阳离子或光保护剂形式的C 1至C 7烷基片段，并含有所述化合物的化妆品组合物。

75. 发明申请

US20110245251A1 MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
标题翻译：用于治疗相关疾病的前列腺素（PGI2）受体的调节剂
公开(公告)号：US20110245251A1
公开(公告)日：2011-10-06
申请号：US13133036
申请日：2009-12-07
申请人： Thuy-Anh Tran , Rena Hayashi , Jason B. Ibarra , Brett Ullman , Ning Zou
发明人： Thuy-Anh Tran , Rena Hayashi , Jason B. Ibarra , Brett Ullman , Ning Zou
IPC分类号： A61K31/53 , C07D237/14 , C07D401/04 , C07D409/04 , C07D403/04 , C07D253/07 , A61K31/50 , A61K31/501 , C12N5/071 , A61P9/12 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/06 , A61P3/10 , A61P13/12 , A61P27/02 , A61P25/02 , A61P27/06 , A61P29/00 , A61P17/06 , A61P19/02 , A61P37/06 , A61P25/28 , A61P17/10 , A61P11/00
CPC分类号： C07D237/14 , C07D253/07 , C07D401/04 , C07D403/04 , C07D409/04
摘要： Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
摘要翻译：式Ia的环己烷衍生物及其药物组合物，其调节PGI 2受体的活性。本发明的化合物及其药物组合物涉及可用于治疗肺动脉高压（PAH）和相关疾病的方法; 血小板聚集; 冠状动脉疾病; 心肌梗死; 短暂性脑缺血发作; 心绞痛行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化动脉粥样硬化血栓形成哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎类风湿关节炎; 克罗恩病; 移植排斥反应多发性硬化症系统性红斑狼疮（SLE）; 溃疡性结肠炎缺血再灌注损伤; 再狭窄; 动脉粥样硬化粉刺; 1型糖尿病; 2型糖尿病; 败血症和慢性阻塞性肺疾病（COPD）。

76. 发明授权

US07981900B2 2-phenyl pyrimidines which are tubulin inhibitors 有权
标题翻译：作为微管蛋白抑制剂的2-苯基嘧啶
公开(公告)号：US07981900B2
公开(公告)日：2011-07-19
申请号：US10581534
申请日：2004-12-03
申请人： Christopher John Burns , Andrew Frederick Wilks , Michael Francis Harte , Harrison Sikanyika , Emmanuelle Fantino
发明人： Christopher John Burns , Andrew Frederick Wilks , Michael Francis Harte , Harrison Sikanyika , Emmanuelle Fantino
IPC分类号： A01N43/54
CPC分类号： C07D253/07 , C07D213/74 , C07D239/42 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of general formula (I), (II) (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
摘要翻译：描述了通式（I），（II）（III）和（V）的化合物用于调节微管聚合和治疗相关疾病状态。还描述了化合物（I），（III）和（V）在激酶相关疾病状态的治疗中的用途。进一步描述的是式（II），（III）和（V）的新化合物。

77. 发明申请

US20110053941A1 IDO Inhibitors 审中-公开
标题翻译： IDO抑制剂
公开(公告)号：US20110053941A1
公开(公告)日：2011-03-03
申请号：US12744860
申请日：2008-12-01
申请人： Mario Mautino , Firoz Jaipuri , Agnieszka Marcinowicz-Flick , Tanay Kesharwani , Jesse Waldo , Steven James Collier
发明人： Mario Mautino , Firoz Jaipuri , Agnieszka Marcinowicz-Flick , Tanay Kesharwani , Jesse Waldo , Steven James Collier
IPC分类号： A61K31/5375 , A61P37/00 , A61K31/135 , C07D209/14 , A61K31/4045 , A61K31/404 , C07D403/12 , C07D401/12 , A61K31/4709 , C07D405/12 , C07D413/12 , A61K31/423 , C07C333/04 , A61K31/27 , C07D213/53 , A61K31/4406 , A61K31/4402 , A61K31/36 , A61K31/381 , A61K31/47 , A61K31/357 , A61K31/428 , A61K31/505
CPC分类号： C07D333/56 , A61K31/138 , A61K31/506 , C07C259/06 , C07C311/48 , C07C327/44 , C07C327/48 , C07C333/20 , C07D209/14 , C07D209/18 , C07D213/40 , C07D215/26 , C07D253/07 , C07D261/20 , C07D263/22 , C07D277/36 , C07D277/64 , C07D279/06 , C07D307/80 , C07D307/81 , C07D333/58 , C07D333/60 , C07D335/06 , C07D401/06 , C07D405/12 , C07D409/12 , C07D417/06 , C07D417/12 , Y02A50/409 , Y02A50/465
摘要： Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.
摘要翻译：目前提供的是（a）调节吲哚胺2,3-双加氧酶的活性的方法，包括使吲哚胺2,3-双加氧酶与调节有效量的化合物的接触，如本文所述的一个方面所述; （b）在有需要的受试者中治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制，包括施用有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （c）治疗受抑于吲哚胺-2,3-双加氧酶的酶活性的医学病症，包括给予有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （d）增强抗癌治疗的有效性，包括给予本文所述方面之一所述的抗癌剂和化合物; （e）治疗与癌症相关的肿瘤特异性免疫抑制，包括施用有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （f）治疗与感染性疾病例如HIV-1感染相关的免疫抑制，包括给予有效的吲哚胺2,3-双加氧酶抑制量的化合物，如本文所述方面之一所述。

78. 发明申请

US20110041471A1 ELECTRET WEBS WITH CHARGE-ENHANCING ADDITIVES 有权
标题翻译：带电荷增强添加剂的电极织物
公开(公告)号：US20110041471A1
公开(公告)日：2011-02-24
申请号：US12746112
申请日：2008-11-25
申请人： John M. Sebastian , Fuming B. Li , Marvin E. Jones , Luke T. Dressel , Daniel A. Japuntich
发明人： John M. Sebastian , Fuming B. Li , Marvin E. Jones , Luke T. Dressel , Daniel A. Japuntich
IPC分类号： D06B19/00 , D04H3/16 , D04H3/14 , B01D39/08 , B01D39/16
CPC分类号： D01F1/10 , B01D39/1623 , B01D2239/0435 , C07D253/07 , D04H1/4291 , D04H1/56 , D04H3/007 , D04H3/02 , D06M10/025 , D06M11/05 , Y10T442/2418 , Y10T442/2459
摘要： Electret webs are presented which include a blend of a thermoplastic resin and a charge additive. The charge additives include ester-substituted and amide-substituted trianilino triazine materials. The webs prepared from the blends may be in the form of films or non-woven fibrous webs. Non-woven microfiber webs are useful as filtration media.
摘要翻译：提出了驻极体纤维网，其包括热塑性树脂和电荷添加剂的共混物。电荷添加剂包括酯取代和酰胺取代的三苯胺三嗪材料。由共混物制备的网可以是薄膜或非织造纤维网的形式。非织造超细纤维网可用作过滤介质。

79. 发明申请

US20100158860A1 HETEROCYCLIC ANTIVIRAL COMPOUNDS 失效
标题翻译：杂环抗病毒化合物
公开(公告)号：US20100158860A1
公开(公告)日：2010-06-24
申请号：US12636999
申请日：2009-12-14
申请人： Sandra Steiner , Jim Li , Ryan Craig Schoenfeld , Francisco Xavier Talamas
发明人： Sandra Steiner , Jim Li , Ryan Craig Schoenfeld , Francisco Xavier Talamas
IPC分类号： A61K38/20 , C07D241/18 , C07D239/46 , A61K31/495 , A61K31/505 , A61K38/19 , A61K38/21 , A61P31/14
CPC分类号： C07D405/04 , C07D237/14 , C07D239/36 , C07D239/52 , C07D239/54 , C07D241/18 , C07D253/07
摘要： Compounds having the formula I wherein A, R1, R2, R3, R4a, R4b, R4c, R5, R6, R7a, R7b, Ar1, Rc, Rd, Re, Rf, X, n and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
摘要翻译：具有式I的化合物，其中A，R1，R2，R3，R4a，R4b，R4c，R5，R6，R7a，R7b，Ar1，Rc，Rd，Re，Rf，X，n和p如本文所定义是丙型肝炎病毒NS5b聚合酶抑制剂。还公开了用于治疗HCV感染和抑制HCV复制的组合物和方法。

80. 发明授权

US07700594B2 Fused bicyclic mTOR inhibitors 有权
标题翻译：融合双环mTOR抑制剂
公开(公告)号：US07700594B2
公开(公告)日：2010-04-20
申请号：US11599663
申请日：2006-11-15
申请人： Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A. R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
发明人： Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A. R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
IPC分类号： C07D487/04 , C07D401/14 , C07D403/04 , A61K31/53 , A61K31/4523 , A61K35/00
CPC分类号： C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐是mTOR的抑制剂，可用于治疗癌症。

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