公开(公告)号：US08017773B2

公开(公告)日：2011-09-13

申请号：US12689064

申请日：2010-01-18

Applicant: Matthias Nettekoven ,  Olivier Roche

Inventor： Matthias Nettekoven ,  Olivier Roche

IPC: C07D241/04 ,  A61K31/4965

CPC classification number: C07D295/185 ,  C07D213/71 ,  C07D233/84 ,  C07D241/18 ,  C07D261/10 ,  C07D277/36 ,  C07D295/22 ,  C07D333/34

Abstract: The present invention relates to compounds of formula I wherein R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract translation: 本发明涉及式I化合物，其中R 1至R 3如说明书和权利要求中所定义，及其药学上可接受的盐。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

公开(公告)号：US20110118505A1

公开(公告)日：2011-05-19

申请号：US12925702

申请日：2010-10-26

Applicant: Dongcheng Dai ,  Tove Bolken ,  Dennis E. Hruby ,  Thomas R. Bailey

Inventor： Dongcheng Dai ,  Tove Bolken ,  Dennis E. Hruby ,  Thomas R. Bailey

IPC: C07C281/02

CPC classification number: A61K31/175 ,  A61K31/18 ,  A61K31/277 ,  A61K31/40 ,  A61K31/415 ,  A61K31/433 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/675 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C275/42 ,  C07C281/06 ,  C07C311/49 ,  C07D213/70 ,  C07D233/84 ,  C07D261/10 ,  C07D277/36 ,  C07D285/06 ,  C07D295/20 ,  C07D295/22 ,  C07D317/66 ,  C07D319/18

Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).

Abstract translation: 公开了通过以治疗有效量施用某些新型磺酰氨基脲，羰基氨基脲，氨基脲，脲和相关化合物来治疗病毒感染的化合物，方法和药物组合物。 还公开了制备化合物的方法和使用该化合物的方法及其药物组合物。 具体地，公开了治疗和预防由出血热病毒引起的病毒感染，即，包括但不限于：金杆菌科（Junin，Machupo，Guanarito，Sabia，Lassa，Tacaribe，Pinchinde和VSV），丝状病毒科 埃博拉病毒和马尔堡病毒），黄病毒科（黄热病，o疮出血热和Kyasanur森林病毒病毒）和布亚病毒科（裂谷热）。

公开(公告)号：US20110076721A1

公开(公告)日：2011-03-31

申请号：US12993716

申请日：2009-05-18

Applicant: Ranjit Desai ,  Lihu Yang

Inventor： Ranjit Desai ,  Lihu Yang

IPC: C12P21/02 ,  C07D277/36

CPC classification number: C12P21/005 ,  C07D277/36 ,  C12P21/02

Abstract: Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidine-diones inhibitors of Pmt-mediated O-linked glycosylation.

Abstract translation: 描述了用于生产具有降低量的O-连接糖基化的蛋白质组合物的化合物和方法。 该方法包括在存在Pmt介导的O-连接糖基化的某些亚苄基噻唑烷二酮抑制剂存在下培养的细胞中产生蛋白质。

公开(公告)号：US20100285957A1

公开(公告)日：2010-11-11

申请号：US12809501

申请日：2008-12-09

Applicant: Klaus Kunz ,  Pierre Cristau ,  Joerg Nico Greul ,  Ulrich Heinemann ,  Kerstin Ilg ,  Amos Mattes ,  Oswald Ort ,  Thomas Seitz ,  Ulrike Wachendorff-Neumann ,  Peter Dahmen ,  Arnd Voerste ,  Heinz Kehne ,  Dirk Schmutzler ,  Hiroyuki Hadano

Inventor： Klaus Kunz ,  Pierre Cristau ,  Joerg Nico Greul ,  Ulrich Heinemann ,  Kerstin Ilg ,  Amos Mattes ,  Oswald Ort ,  Thomas Seitz ,  Ulrike Wachendorff-Neumann ,  Peter Dahmen ,  Arnd Voerste ,  Heinz Kehne ,  Dirk Schmutzler ,  Hiroyuki Hadano

IPC: A01C1/06 ,  C07D285/08 ,  C07D277/34 ,  A01N43/836 ,  A01N43/78 ,  C07D405/12 ,  A01N43/40 ,  A01P1/00

CPC classification number: C07D277/36 ,  C07D285/08

Abstract: The present invention relates to thiazolyloxyphenylamidines or thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.

Abstract translation: 本发明涉及通式（I）的噻唑基氧基苯基脒或噻二唑基氧基苯基脒与其制备方法相关的本发明脒用于对抗不希望的微生物以及用于此目的的组合物，其包含根据以下的噻二唑基氧基苯基脒 本发明。 本发明还涉及通过将根据本发明的化合物应用于微生物和/或其栖息地来防治不期望的微生物的方法。

公开(公告)号：US07754890B2

公开(公告)日：2010-07-13

申请号：US12163088

申请日：2008-06-27

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

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

IPC: C07D277/26 ,  A61K31/425

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

Abstract: 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:

Abstract translation: 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：

公开(公告)号：US20100120791A1

公开(公告)日：2010-05-13

申请号：US12689064

申请日：2010-01-18

Applicant: Matthias Nettekoven ,  Olivier Roche

Inventor： Matthias Nettekoven ,  Olivier Roche

IPC: A61K31/4965 ,  C07D241/04

CPC classification number: C07D295/185 ,  C07D213/71 ,  C07D233/84 ,  C07D241/18 ,  C07D261/10 ,  C07D277/36 ,  C07D295/22 ,  C07D333/34

Abstract: The present invention relates to compounds of formula I wherein R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract translation: 本发明涉及式I化合物，其中R 1至R 3如说明书和权利要求中所定义，及其药学上可接受的盐。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

公开(公告)号：US20100029609A1

公开(公告)日：2010-02-04

申请号：US12440143

申请日：2007-09-06

Applicant: Frederic Berst ,  Philipp Grosche ,  Philipp Janser ,  Frederic Zecri ,  Birgit Bollbuck

Inventor： Frederic Berst ,  Philipp Grosche ,  Philipp Janser ,  Frederic Zecri ,  Birgit Bollbuck

IPC: A61K31/397 ,  C07D207/00 ,  A61K31/40 ,  C07D265/30 ,  A61K31/535 ,  C07D205/04 ,  A61P25/00

CPC classification number: C07C311/21 ,  C07C311/29 ,  C07D205/04 ,  C07D207/16 ,  C07D213/30 ,  C07D213/76 ,  C07D231/18 ,  C07D233/84 ,  C07D241/04 ,  C07D241/24 ,  C07D257/04 ,  C07D277/36 ,  C07D307/79 ,  C07D307/82 ,  C07D333/34 ,  C07D333/62

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1-R5, R10 and X1-X7 are as defined in the specification.

Abstract translation: 式（I）化合物或其药学上可接受的盐或前药酯：其中R1-R5，R10和X1-X7基团如说明书中所定义。

公开(公告)号：US07655641B2

公开(公告)日：2010-02-02

申请号：US10542579

申请日：2004-02-10

Applicant: Scott Eugene Conner ,  Lynn Stacy Gossett ,  Jonathan Edward Green ,  Winton Dennis Jones, Jr. ,  Nathan Bryan Mantlo ,  Donald Paul Matthews ,  Daniel Ray Mayhugh ,  Daryl Lynn Smith ,  Jennifer Ann Vance ,  Xiaodong Wang ,  Alan M Warshawsky ,  Leonard Larry Winneroski, Jr. ,  Yanping Xu ,  Guoxin Zhu

Inventor： Scott Eugene Conner ,  Lynn Stacy Gossett ,  Jonathan Edward Green ,  Winton Dennis Jones, Jr. ,  Nathan Bryan Mantlo ,  Donald Paul Matthews ,  Daniel Ray Mayhugh ,  Daryl Lynn Smith ,  Jennifer Ann Vance ,  Xiaodong Wang ,  Alan M Warshawsky ,  Leonard Larry Winneroski, Jr. ,  Yanping Xu ,  Guoxin Zhu

IPC: A61K31/66 ,  A61K31/38 ,  C07D409/12 ,  C07D209/04

CPC classification number: C07D207/08 ,  A61K31/00 ,  A61K45/06 ,  C07C311/13 ,  C07C311/17 ,  C07C311/19 ,  C07C311/29 ,  C07C317/14 ,  C07C323/49 ,  C07C323/52 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/08 ,  C07D209/48 ,  C07D213/64 ,  C07D213/71 ,  C07D213/74 ,  C07D215/36 ,  C07D231/12 ,  C07D231/18 ,  C07D263/32 ,  C07D271/12 ,  C07D277/36 ,  C07D307/79 ,  C07D307/82 ,  C07D319/18 ,  C07D333/34 ,  C07D333/62 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  A61K2300/00

Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐，溶剂合物，水合物或立体异构体，其可用于治疗或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，例如综合征X型 II型糖尿病，高血糖症，高脂血症，肥胖症，凝血病，高血压，动脉硬化以及与X综合症和心血管疾病有关的其他疾病。

公开(公告)号：US20100016337A1

公开(公告)日：2010-01-21

申请号：US12486144

申请日：2009-06-17

Applicant: Hartmut STROBEL ,  Paulus WOHLFART ,  Heinz-Werner KLEEMANN ,  Gerhard ZOLLER ,  David William WILL

Inventor： Hartmut STROBEL ,  Paulus WOHLFART ,  Heinz-Werner KLEEMANN ,  Gerhard ZOLLER ,  David William WILL

IPC: A61K31/505 ,  C07D401/12 ,  A61K31/4545 ,  C07D401/06

CPC classification number: C07D409/06 ,  C07D213/56 ,  C07D213/65 ,  C07D213/74 ,  C07D213/89 ,  C07D239/26 ,  C07D271/113 ,  C07D277/36 ,  C07D277/46 ,  C07D285/135 ,  C07D333/24 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12

Abstract: The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Abstract translation: 本发明涉及式I的杂芳基取代的甲酰胺，其中Het，A，X，R 1，R 2和R 3具有权利要求所述的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的 药理活性化合物。 具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。 本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于 治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

公开(公告)号：US20100004241A1

公开(公告)日：2010-01-07

申请号：US12541447

申请日：2009-08-14

Applicant: Richard Apodaca ,  Nicholas I. Carruthers ,  Curt A. Dvorak ,  Dale A. Rudolph ,  Chandravadan R. Shah ,  Wei Xiao

Inventor： Richard Apodaca ,  Nicholas I. Carruthers ,  Curt A. Dvorak ,  Dale A. Rudolph ,  Chandravadan R. Shah ,  Wei Xiao

IPC: A61K31/5377 ,  A61K31/445 ,  A61P25/28 ,  A61P25/18 ,  A61P25/24 ,  A61K31/496 ,  A61K31/4523 ,  A61K31/4725 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/438 ,  A61K31/439

CPC classification number: C07D207/325 ,  A61K31/4402 ,  A61K31/4465 ,  A61K45/06 ,  C07C217/22 ,  C07C323/25 ,  C07C335/32 ,  C07D207/335 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D213/36 ,  C07D213/74 ,  C07D215/06 ,  C07D231/12 ,  C07D233/42 ,  C07D233/54 ,  C07D233/56 ,  C07D233/84 ,  C07D233/88 ,  C07D235/06 ,  C07D235/26 ,  C07D239/34 ,  C07D249/08 ,  C07D257/04 ,  C07D277/36 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/205 ,  C07D307/52 ,  C07D317/28 ,  C07D333/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/08 ,  A61K2300/00

Abstract: Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

Abstract translation: 式（I）的取代的芳氧基烷基胺，含有它们的组合物，以及制备和使用它们来治疗组胺介导的病症的方法。