公开(公告)号：US20240117306A1

公开(公告)日：2024-04-11

申请号：US18323075

申请日：2023-05-24

申请人： CASSAVA SCIENCES, INC.

发明人： Hoau-Yan WANG ,  Lindsay BURNS BARBIER

IPC分类号： C12N5/079 ,  C07D205/04 ,  C07D207/08 ,  C07D211/14 ,  C07D211/74 ,  C07D217/04 ,  C07D265/30 ,  C07D265/36 ,  C07D277/02 ,  C07D277/04 ,  C07D279/12 ,  C07D295/08 ,  C07D295/088 ,  C07D471/10 ,  C07D491/04 ,  C07D491/056 ,  C07D498/10 ,  G01N33/50 ,  G01N33/68 ,  G01N33/94

CPC分类号： C12N5/0622 ,  C07D205/04 ,  C07D207/08 ,  C07D211/14 ,  C07D211/74 ,  C07D217/04 ,  C07D265/30 ,  C07D265/36 ,  C07D277/02 ,  C07D277/04 ,  C07D279/12 ,  C07D295/08 ,  C07D295/088 ,  C07D471/10 ,  C07D491/04 ,  C07D491/056 ,  C07D498/10 ,  G01N33/50 ,  G01N33/6896 ,  G01N33/94 ,  G01N2333/70571 ,  G01N2800/2821 ,  G01N2800/52

摘要： A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

公开(公告)号：US20220372007A1

公开(公告)日：2022-11-24

申请号：US17628904

申请日：2021-04-25

申请人： NANJING MEDICAL UNIVERSITY

发明人： Yong JI ,  Liping XIE ,  Shuang ZHAO ,  Tianyu SONG ,  Yi HAN

IPC分类号： C07D277/02 ,  C07D417/14 ,  A61P11/06

摘要： Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is: Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.

公开(公告)号：US10760052B2

公开(公告)日：2020-09-01

申请号：US16030494

申请日：2018-07-09

申请人： Pain Therapeutics, Inc.

发明人： Hoau-Yan Wang ,  Lindsay Burns Barbier

IPC分类号： C12N5/079 ,  C07D265/30 ,  C07D211/14 ,  C07D277/04 ,  C07D295/088 ,  C07D205/04 ,  C07D491/056 ,  C07D498/10 ,  C07D217/04 ,  C07D471/10 ,  C07D491/04 ,  C07D207/08 ,  C07D265/36 ,  C07D277/02 ,  C07D279/12 ,  C07D295/08 ,  C07D211/74

摘要： A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

公开(公告)号：US10759765B2

公开(公告)日：2020-09-01

申请号：US16093688

申请日：2017-04-14

申请人： CE Pharm CO., LTD.

发明人： Dawei Ma ,  Wei Zhou ,  Mengyang Fan ,  Haibo Wu ,  Junli Yin ,  Xi Jiang ,  Yuntong Zhai ,  Songtao Niu

IPC分类号： C07D241/02 ,  B01J31/22 ,  C07C231/02 ,  C07C233/00 ,  C07D207/32 ,  C07D209/08 ,  C07D209/12 ,  C07D213/06 ,  C07D235/08 ,  C07D239/02 ,  C07D277/02 ,  C07D277/62 ,  C07D307/02 ,  C07D307/78 ,  C07C209/60

摘要： Provided are a heterocyclic carboxylic acid amide ligand and applications thereof in a copper catalyzed coupling reaction. Specifically, provided are uses of a compound represented by formula (I), definitions of radical groups being described in the specifications. The compound represented by formula (I) can be used as the ligand in the copper catalyzed coupling reaction of the aryl halogeno substitute, and is used or catalyzing the coupling reaction for forming the aryl halogeno substitute having C—N, C—O, C—S and other bonds.

公开(公告)号：US20130131124A1

公开(公告)日：2013-05-23

申请号：US13701403

申请日：2011-06-01

申请人： Jörg Nico Greul ,  Jürgen Benting ,  Peter Dahmen ,  Ulrike Wachendorff-Neumann

发明人： Jörg Nico Greul ,  Jürgen Benting ,  Peter Dahmen ,  Ulrike Wachendorff-Neumann

IPC分类号： A01N43/40 ,  A01N43/56 ,  C07C237/00 ,  C07D211/04 ,  C07D277/02 ,  C07D231/14 ,  A01N43/78 ,  A01N37/44

CPC分类号： C07D231/18 ,  A01N37/18 ,  A01N37/44 ,  A01N43/40 ,  A01N43/50 ,  A01N43/56 ,  A01N43/78 ,  A01N43/80 ,  C07C211/35 ,  C07C233/65 ,  C07C237/00 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/04 ,  C07D213/82 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D277/02 ,  C07D277/56

摘要： The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

摘要翻译： 本发明涉及式（I）的O-环丙基甲基环己基 - 羧酰胺衍生物; 其制备方法，它们作为杀真菌剂的用途，特别是杀真菌剂组合物的形式，以及使用这些化合物或组合物控制植物病原真菌，特别是植物的方法。

公开(公告)号：US08334316B2

公开(公告)日：2012-12-18

申请号：US12368206

申请日：2009-02-09

申请人： Xiao Xu ,  Haoyun An ,  Xiaobo Wang

发明人： Xiao Xu ,  Haoyun An ,  Xiaobo Wang

IPC分类号： A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/425 ,  A61K31/428 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/495 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  C07D279/08 ,  C07D277/02 ,  C07D277/62 ,  C07D275/02 ,  C07D285/02 ,  C07D271/02 ,  C07D263/02 ,  C07D261/02 ,  C07D251/02 ,  C07D249/02 ,  C07D241/02 ,  C07D241/46 ,  C07D239/02 ,  C07D237/02 ,  C07D237/28 ,  C07D237/30 ,  C07D235/04 ,  C07D233/54 ,  C07D231/02 ,  C07D219/00 ,  C07D217/00 ,  C07D215/00 ,  C07D213/02 ,  C07D209/04 ,  C07D207/30

CPC分类号： C07C323/07 ,  C07C321/20 ,  C07C323/16 ,  C07C323/20

摘要： The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.

摘要翻译： 本发明提供取代的二，三，四和五硫化物化合物和组合物，及其用于治疗和/或预防细胞增殖性疾病的方法。 本发明还提供了制备三硫化物和组合物的方法。

公开(公告)号：US20100076034A1

公开(公告)日：2010-03-25

申请号：US12519567

申请日：2007-12-18

申请人： Marcello Allegretti ,  Andrea Aramini ,  Maria Candida Cesta

发明人： Marcello Allegretti ,  Andrea Aramini ,  Maria Candida Cesta

IPC分类号： A61K31/192 ,  C07C317/00 ,  C07C309/02 ,  C07D277/02 ,  C07D207/00 ,  A61K31/195 ,  A61K31/426 ,  A61K31/40 ,  A61P11/00

CPC分类号： C07D277/42 ,  C07B2200/07 ,  C07C59/88 ,  C07C235/78 ,  C07C309/65 ,  C07C311/51 ,  C07D207/09 ,  C07D295/027 ,  C07D295/13

摘要： The present invention relates to (R,S) 2-aryl-2-fluoropropanoic acids, their single enantiomers (R) and (S), their derivatives amides and acylsulfonamides and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the treatment of damages caused by ischemia and reperfusion.

摘要翻译： 本发明涉及（R，S）2-芳基-2-氟丙酸，它们的单一对映异构体（R）和（S），它们的衍生物酰胺和酰基磺酰胺以及含有它们的药物组合物，其用于预防和治疗 的组织损伤由于多发性中性粒细胞（PMN白细胞）在炎症部位的加剧引起。 本发明提供了用于治疗牛皮癣，溃疡性结肠炎，黑素瘤，慢性阻塞性肺疾病（COPD），大疱性呼吸系统感染，类风湿性关节炎，特发性纤维化，肾小球性肾炎和治疗由缺血和再灌注引起的损伤的化合物。

公开(公告)号：US20090048226A1

公开(公告)日：2009-02-19

申请号：US12009829

申请日：2008-01-22

申请人： Marion W. Wannamaker ,  Guy W. Bemis ,  Paul S. Charifson ,  David J. Lauffer ,  Michael D. Mullican ,  Mark A. Murcko ,  Keith P. Wilson ,  James W. Janetka ,  Robert J. Davies ,  Anne-Laure Grillot ,  Zhan Shi ,  Cornelia J. Forster

发明人： Marion W. Wannamaker ,  Guy W. Bemis ,  Paul S. Charifson ,  David J. Lauffer ,  Michael D. Mullican ,  Mark A. Murcko ,  Keith P. Wilson ,  James W. Janetka ,  Robert J. Davies ,  Anne-Laure Grillot ,  Zhan Shi ,  Cornelia J. Forster

IPC分类号： C07C237/02 ,  A61K31/16 ,  A61K31/40 ,  C07D207/00 ,  C07D277/62 ,  A61K31/428 ,  C07D277/02 ,  C07D237/30 ,  A61K31/496 ,  C07D405/14 ,  C07D405/02 ,  A61K31/5377 ,  C07D205/02 ,  A61K31/397 ,  A61K31/497 ,  C07D413/14 ,  C07D403/02 ,  C07D401/02 ,  A61P1/00 ,  A61P35/02 ,  A61P35/00 ,  A61P17/00 ,  A61P31/00 ,  A61P19/00 ,  A61P7/00 ,  A61P25/00 ,  A61P37/00 ,  A61P29/00 ,  A61K31/502 ,  C07D471/04 ,  A61K31/44 ,  A61K31/47 ,  C07D215/16 ,  A61K31/415 ,  C07D231/02

CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07D401/12 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/475

摘要： The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), or interferon-γ-(“IFN-γ”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-γ production and methods for treating interleukin-1, apoptosis-, and interferon-γ-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.

公开(公告)号：US07455827B2

公开(公告)日：2008-11-25

申请号：US11337542

申请日：2006-01-24

申请人： Subhash Chandra Ray ,  Baldev Singh ,  Hiralal Prasad ,  Prodyot Kumar Sarkar ,  Pashupati Dutta ,  Shyam Kishore Roy ,  Anup Kumar Bandyopadhyay ,  Raja Sen

发明人： Subhash Chandra Ray ,  Baldev Singh ,  Hiralal Prasad ,  Prodyot Kumar Sarkar ,  Pashupati Dutta ,  Shyam Kishore Roy ,  Anup Kumar Bandyopadhyay ,  Raja Sen

IPC分类号： C01G45/02 ,  B01J23/34 ,  C07D213/04 ,  C07D207/44 ,  C07D277/02

CPC分类号： C07D213/82

摘要： Nicotinamides and isonicotinamides, used in the preparation of anti-TB drugs i.e. isoniazid and as an intermediate of vitamin B12 are prepared from cyanopyridines and nicotinamides. Catalysts useful for the preparation of nicotinamide and isonicotinamide.

摘要翻译： 用于制备抗TB药物即异烟肼和作为维生素B 12的中间体的烟酰胺和异烟酰胺由氰基吡啶类和烟酰胺制备。 用于制备烟酰胺和异烟酰胺的催化剂。

公开(公告)号：US20080269283A1

公开(公告)日：2008-10-30

申请号：US12163088

申请日：2008-06-27

申请人： Pingchen Fan ,  Hiroyuki Goto ,  Xiao He ,  Makoto Kukutani ,  Marc Labelle ,  Dustin L. McMinn ,  Jay P. Powers ,  Yosup Rew ,  Daqing Sun ,  Xuelei Yan

发明人： Pingchen Fan ,  Hiroyuki Goto ,  Xiao He ,  Makoto Kukutani ,  Marc Labelle ,  Dustin L. McMinn ,  Jay P. Powers ,  Yosup Rew ,  Daqing Sun ,  Xuelei Yan

IPC分类号： A61K31/47 ,  A61K31/40 ,  A61K31/277 ,  A61K31/165 ,  A61K31/10 ,  C07C317/26 ,  C07D215/12 ,  C07D207/06 ,  C07C255/00 ,  C07C381/00 ,  C07C317/14 ,  C07D233/56 ,  A61K31/4164 ,  C07D277/02 ,  C07D409/00 ,  A61K31/4439 ,  A61K31/426 ,  A61K31/427 ,  A61P3/04 ,  A61P3/10 ,  C12N5/00

CPC分类号： C07C317/44 ,  C07C317/14 ,  C07C317/22 ,  C07C2601/02 ,  C07D215/36 ,  C07D233/54 ,  C07D277/36 ,  C07D277/54 ,  C07D277/56 ,  C07D295/096 ,  C07D295/112 ,  C07D417/04

摘要： Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:

摘要翻译： 描述了式I和II的芳基砜化合物，并具有治疗效用，特别是在治疗糖尿病，肥胖症和相关病症和病症中：