公开(公告)号：WO2009062087A1

公开(公告)日：2009-05-14

申请号：PCT/US2008/082873

申请日：2008-11-07

Applicant: NEUROCRINE BIOSCIENCES, INC. ,  GALLAGHER, Donald ,  TREIBER, Laszlo ,  HUGHES, Robert ,  CAMPOPIANO, Onorato ,  WANG, Peng ,  ZHAO, Yuxin ,  CHOU, Shine ,  OUELLETTE, Michael ,  HETTINGER, Donald

Inventor： GALLAGHER, Donald ,  TREIBER, Laszlo ,  HUGHES, Robert ,  CAMPOPIANO, Onorato ,  WANG, Peng ,  ZHAO, Yuxin ,  CHOU, Shine ,  OUELLETTE, Michael ,  HETTINGER, Donald

IPC: C07D239/54 ,  C07D239/553

CPC classification number: C07D239/54 ,  C07D239/553

Abstract: The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及用于制备结构（VI）的促性腺激素释放激素（GnRH）受体拮抗剂的方法和中间体; 及其立体异构体及其药学上可接受的盐。

公开(公告)号：WO2004046162A3

公开(公告)日：2004-06-03

申请号：PCT/US2003/036195

申请日：2003-11-14

Applicant: THE SCRIPPS RESEARCH INSTITUTE ,  NICOLAOU, Kyriacos, C. ,  ROECKER, Anthony, J. ,  HUGHES, Robert ,  PFEFFERKORN, Jeffrey, A.

Inventor： NICOLAOU, Kyriacos, C. ,  ROECKER, Anthony, J. ,  HUGHES, Robert ,  PFEFFERKORN, Jeffrey, A.

IPC: C07C233/61

Abstract: ABSTRACT Potent non-steroidal farnesoid X receptor (FXR) agonists are N-aryl-N-arylmethyl amido and ureido compounds having the chemical structure represented by the following formula (I): INSERT FORMULA wherein E1 is (C1-C8)alkyl, cyclohexyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, phenyl, or NH(C1-C8)alkyl; L1 and L2 are both H, or together form a pi-bond; X1 is C(O), or CH2; Y1 is H, NHZ1, NH(Z2)Z3, or OZ4; aryl moiety A1 is selected from the group of radicals consisting of: INSERT FORMULA A2 and G1 - G11 are as defined in the specification; and T1 and T2 are each independently O, S, NH, or N(C1-C8)alkyl. The FXR agonists are useful as therapeutic agents for the treatment of diseases linked to cholesterol, bile acids, and their metabolism and homeostasis.

公开(公告)号：WO2010045085A1

公开(公告)日：2010-04-22

申请号：PCT/US2009/059937

申请日：2009-10-08

Applicant: THE COCA-COLA COMPANY ,  ZIESEL, Lawrence, B. ,  CARPENTER, Gregg ,  HUGHES, Robert ,  QUARTARONE, Daniel, S.

Inventor： ZIESEL, Lawrence, B. ,  CARPENTER, Gregg ,  HUGHES, Robert ,  QUARTARONE, Daniel, S.

IPC: B67D7/74

CPC classification number: B67D1/07 ,  B67D1/0021 ,  B67D1/0043 ,  B67D1/0044 ,  B67D1/0857

Abstract: A beverage dispensing system using a sweetener. The beverage dispensing system may include a dispensing nozzle, a sweetener source with the sweetener at more than about 65° brix, a first diluent source with a first diluent, a mixing chamber in communication with the sweetener source and the first diluent source so as to dilute the sweetener to less than about 65° brix, and a second diluent source with a second diluent so as to dilute further the sweetener upstream of the dispensing nozzle.

Abstract translation: 一种使用甜味剂的饮料分配系统。 饮料分配系统可以包括分配喷嘴，甜味剂源，其甜味剂具有大于约65°的白利糖度，具有第一稀释剂的第一稀释剂源，与甜味剂源和第一稀释剂源连通的混合室， 将甜味剂稀释至小于约65°白利糖度，并用第二稀释剂稀释第二稀释剂源，以便在分配喷嘴上游进一步稀释甜味剂。

公开(公告)号：WO2004024081A2

公开(公告)日：2004-03-25

申请号：PCT/US2003/028503

申请日：2003-09-10

Applicant: ELAN PHARMACEUTICALS, INC. ,  PFIZER, INC. ,  MAILLARD, Michel ,  BALDWIN, Eric, T. ,  BECK, James, T. ,  HUGHES, Robert ,  JOHN, Varghese ,  PULLEY, Shon, R. ,  TENBRINK, Ruth

Inventor： MAILLARD, Michel ,  BALDWIN, Eric, T. ,  BECK, James, T. ,  HUGHES, Robert ,  JOHN, Varghese ,  PULLEY, Shon, R. ,  TENBRINK, Ruth

IPC: A61K

CPC classification number: C07C233/36 ,  C07C235/10 ,  C07C235/74 ,  C07C271/24 ,  C07C311/05 ,  C07C327/30 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D209/14 ,  C07D213/38 ,  C07D213/64 ,  C07D215/233 ,  C07D215/38 ,  C07D215/42 ,  C07D215/46 ,  C07D217/22 ,  C07D233/61 ,  C07D233/64 ,  C07D237/08 ,  C07D237/14 ,  C07D239/26 ,  C07D239/38 ,  C07D241/12 ,  C07D249/08 ,  C07D261/08 ,  C07D265/02 ,  C07D277/28 ,  C07D295/135 ,  C07D307/52 ,  C07D309/14 ,  C07D311/68 ,  C07D311/74 ,  C07D333/20 ,  C07D333/22 ,  C07D335/06 ,  C07D405/04 ,  C07D407/06 ,  C07D409/12 ,  C07D495/04

Abstract: Disclosed are compounds of the formula: (I) where variables Z, X, R 15 , R 2 , R 3 , and R c are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.

Abstract translation: 公开了式（I）的化合物，其中变量Z，X，R 15，R 2，R 3和R c在本文中定义。 本文公开的化合物是β-分泌酶的抑制剂，因此可用于治疗阿尔茨海默氏病和以哺乳动物中Aβ肽沉积为特征的其它疾病。

公开(公告)号：WO2011050215A1

公开(公告)日：2011-04-28

申请号：PCT/US2010/053628

申请日：2010-10-21

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  AMBHAIKAR, Narendra, Bhalchandra ,  HUGHES, Robert ,  HURLEY, Dennis, James ,  LEE, Elaine, Chungmin ,  LITTLER, Benjamin ,  NUMA, Mehdi ,  ROEPER, Stefanie ,  SHETH, Urvi

Inventor： AMBHAIKAR, Narendra, Bhalchandra ,  HUGHES, Robert ,  HURLEY, Dennis, James ,  LEE, Elaine, Chungmin ,  LITTLER, Benjamin ,  NUMA, Mehdi ,  ROEPER, Stefanie ,  SHETH, Urvi

IPC: C07D215/56 ,  C07D487/08

CPC classification number: C07D487/08 ,  C07D215/56

Abstract: The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2. 1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A- HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.

Abstract translation: 本发明涉及制备固体形式的N-（4-（7-氮杂双环[2.2.1]庚-7-基）-2-（三氟甲基）苯基）-4-氧代-5-（三氟甲基） -1,4-二氢喹啉-3-甲酰胺，包括化合物1形式A，化合物1形式A- HCl，化合物1形式B和化合物1形式B-HCl，这些形式的任何组合，其药物组合物，以及 治疗。

公开(公告)号：WO2011035139A1

公开(公告)日：2011-03-24

申请号：PCT/US2010/049306

申请日：2010-09-17

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  AMBHAIKAR, Narendra, Bhalchandra ,  BEAR, Brian, Richard ,  FANNING, Lev, T., D. ,  HUGHES, Robert ,  LITTLER, Benjamin

Inventor： AMBHAIKAR, Narendra, Bhalchandra ,  BEAR, Brian, Richard ,  FANNING, Lev, T., D. ,  HUGHES, Robert ,  LITTLER, Benjamin

IPC: C07D487/08

CPC classification number: C07D487/08

Abstract: The present invention relates to a process for preparing azabicyclic compounds that are useful intermediates for synthesizing pharmaceutical compounds or salts thereof.

Abstract translation: 本发明涉及制备作为合成药物化合物或其盐的有用中间体的氮杂双环化合物的方法。

公开(公告)号：WO2007143001A3

公开(公告)日：2007-12-13

申请号：PCT/US2007/012792

申请日：2007-05-31

Applicant: TOPCODER, INC. ,  MESSINGER, David ,  FERNANDEZ-IVERN, Javier ,  HUGHES, John, M. ,  HUGHES, Robert ,  NORMAN, Lorie, Ilene ,  JEFTS, Anthony

Inventor： MESSINGER, David ,  FERNANDEZ-IVERN, Javier ,  HUGHES, John, M. ,  HUGHES, Robert ,  NORMAN, Lorie, Ilene ,  JEFTS, Anthony

IPC: G06F9/46

Abstract: A production contest management system enables management of workflow and scoring of projects, for example in a production contest environment. A project is divided into "phases." Project managers can specify project phases, and for each phase, required timing and deliverables. For phases that involve a review (e.g., screening, review board, peer review), scorecards used to perform the review may be specified. The scorecards are made accessible electronically to one or more reviewers. The scorecards may be available on-line, or may be downloaded, completed, and then uploaded. Once received, scorecards are tallied. In this way, the management system helps coordinate production of a product that is produced using production competitions. The system allows for simultaneous management of multiple projects and production teams.

公开(公告)号：WO2005050573A1

公开(公告)日：2005-06-02

申请号：PCT/US2004/038424

申请日：2004-11-15

Applicant: CUBIC CORPORATION ,  ANDREWS, David, W. ,  CALLAWAY, Leigh, L. ,  HUGHES, Robert ,  YOUNG, Douglas

Inventor： ANDREWS, David, W. ,  CALLAWAY, Leigh, L. ,  HUGHES, Robert ,  YOUNG, Douglas

IPC: G07B15/00

CPC classification number: G06Q20/363 ,  G07B15/00 ,  G07B15/04 ,  G07F7/0866 ,  G07F17/0014

Abstract: A system and method for automatically loading a pre-selected value onto a fare card allows a patron to enter or leave a transit system gate without having to add a fare value at a vending machine. The automatic loading provides added convenience and security for the patron. The vehicle for the automatically-loaded value is either a credit card that is pre-authorized for use by the patron, or the patron’s available benefits. The automatic loading process may be utilized to autoload values of benefits only, or to load values from a combination of benefits and credit card transactions. The pre-selected autoload value is loaded onto the fare card at the gate before confirmation that the credit card transaction is authorized. The gate sends a message to a transit central computer that an autoload has occurred. The central computer determines whether benefits are available to fill the request, and forward a request for the difference to a credit processing company.

Abstract translation: 用于将预选值自动加载到票价卡上的系统和方法允许顾客进入或离开运输系统门，而不必在自动售货机添加票价。 自动加载为顾客提供了更多的便利和安全性。 自动加载价值的车辆是预先授权给顾客使用的信用卡或顾客可用的利益。 自动加载过程可以用于仅自动加载有益的价值，或者从利益和信用卡交易的组合中加载值。 在确认信用卡交易被授权之前，预先选择的自动加载值被加载到门口的票价卡上。 门向发送自动加载的中转计算机发送消息。 中央计算机确定是否可以获得利益来填补请求，并向信用处理公司转发差额请求。

公开(公告)号：WO2004045511A2

公开(公告)日：2004-06-03

申请号：PCT/US2003/036123

申请日：2003-11-14

Applicant: THE SALK INSTITUTE FOR BIOLOGICAL STUDIES ,  THE SCRIPPS RESEARCH INSTITUTE ,  DOWNES, Michael, R. ,  EVANS, Ronald, Mark ,  HUGHES, Robert ,  NICOLAOU, Kyriacos, C. ,  ROECKER, Anthony, J.

Inventor： DOWNES, Michael, R. ,  EVANS, Ronald, Mark ,  HUGHES, Robert ,  NICOLAOU, Kyriacos, C. ,  ROECKER, Anthony, J.

IPC: A61K

CPC classification number: C07D311/94 ,  A61K31/16 ,  A61K31/353 ,  A61K31/44 ,  A61K31/4433 ,  C07C233/54 ,  C07C233/63 ,  C07C233/81 ,  C07C237/22 ,  C07C275/42 ,  C07C309/66 ,  C07C323/40 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/40 ,  C07D277/28 ,  C07D307/46 ,  C07D311/04 ,  C07D311/22 ,  C07D311/64 ,  C07D311/68 ,  C07D317/58 ,  C07D333/20 ,  C07D333/22 ,  C07D407/12 ,  C07D409/12

Abstract: The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.

Abstract translation: 胆固醇合成，代谢，获取和运输的有效调节是脂质体内平衡的重要组成部分。 法尼基X受体（FXR）是胆汁酸转录传感器，胆汁酸是胆固醇代谢的主要产物。 因此，FXR的有效的，选择性的，小分子激动剂，部分激动剂和拮抗剂的开发将成为进一步去卷积FXR生理学的重要步骤。 根据本发明，描述了新型有效的FXR活化剂的鉴定。 携带二苯乙烯或联芳基部分的本发明化合物的两种衍生物含有迄今为止在基于细胞的测定中报道的最有效的FXR激动剂的成员。 这些化合物可用作进一步定义FXR的生理作用以及用于治疗与胆固醇，胆汁酸及其代谢和体内平衡相关的疾病的治疗潜能的化学工具。

公开(公告)号：WO2004004659A2

公开(公告)日：2004-01-15

申请号：PCT/US2003/021456

申请日：2003-07-09

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  BEWLEY, Carole ,  NICHOLAS, Gillian ,  NICOLAOU, K., C. ,  BARLUENGA, Sofia ,  PFEFFERKORN, Jeffrey ,  HUGHES, Robert

Inventor： BEWLEY, Carole ,  NICHOLAS, Gillian ,  NICOLAOU, K., C. ,  BARLUENGA, Sofia ,  PFEFFERKORN, Jeffrey ,  HUGHES, Robert

IPC: A61K

CPC classification number: C07C323/41

Abstract: Synthetic alkaloid derivatives useful as inhibitors of acyl gluc osaminyl inositol amidase activity, including mycothiol-S-conjugate amidase, are disclosed. In addition, methods of using the inhibitors of acyl glucosaminyl inositol amidase in the treatment of bacterial infections, including those caused by Mycobacterium tuberculosis , are also disclosed.

Abstract translation: 公开了可用作酰基葡糖胺基甲酰肌醇酰胺酶活性抑制剂的合成生物碱衍生物，包括咪唑硫醇-S-共轭酰胺酶。 此外，还公开了使用酰基葡糖胺基肌醇酰胺酶抑制剂治疗细菌感染的方法，包括由结核分枝杆菌引起的那些。