The Polycyclo Ring System Is Bicyclo-carbocyclic Patents (Class 546/205)
  • Patent number: 11377422
    Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
    Type: Grant
    Filed: March 11, 2020
    Date of Patent: July 5, 2022
    Assignee: Nocion Therapeutics, Inc.
    Inventors: Bridget McCarthy Cole, James Lamond Ellis
  • Patent number: 9758477
    Abstract: The present invention provides sulfamoylbenzamide derivatives, and pharmaceutical compositions thereof. In certain embodiments, the compounds and pharmaceutical compositions of the invention inhibit pregenomic RNA encapsidation. In other embodiments, the compounds and pharmaceutical compositions of the invention are useful for treating Hepatitis B virus (HBV) infection.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: September 12, 2017
    Assignees: Drexel University, Baruch S. Blumberg Institute
    Inventors: Ju-Tao Guo, Xiaodong Xu, Timothy M. Block
  • Patent number: 8987458
    Abstract: The present invention provides a process for preparing donepezil or a salt thereof, the process comprising reducing a 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methylene]pyridonium halide of formula II, wherein X is bromide or chloride, in the presence of an ionic compound, a solvent, a catalyst and a source of hydrogen, to form donepezil and optionally converting the donepezil to the salt thereof.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: March 24, 2015
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Srinivas Laxminarayan Pathi
  • Publication number: 20150080400
    Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 19, 2015
    Applicant: TAKEDA GMBH
    Inventors: Angelika Hoffmeyer, Rainer Boer, Manuela Hessmann, Andreas Pahl, Torsten Dunkern, Simone Hartung, Christof Zitt, Jurgen Volz, Christiane Praechter, Mahindra Makhija, Hiteshkumar Jain, Sandip Gavade, Arati Prabhu, Manojkumar Tiwari, Ashish Keche, Sarvesh Patel
  • Publication number: 20150057443
    Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
    Type: Application
    Filed: August 21, 2014
    Publication date: February 26, 2015
    Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
  • Patent number: 8906938
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: December 9, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Patent number: 8865741
    Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.
    Type: Grant
    Filed: February 18, 2012
    Date of Patent: October 21, 2014
    Assignee: Asana Biosciences, LLC
    Inventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
  • Publication number: 20140288301
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan M. Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Kowalczyk-Przewloka
  • Publication number: 20140249183
    Abstract: Treatments are described for stress disorders and substance use disorders, for example, substance use disorders associated with use of alcohol, cocaine, amphetamines, and the like.
    Type: Application
    Filed: February 22, 2014
    Publication date: September 4, 2014
    Applicant: Baylor College of Medicine
    Inventors: Thomas F. Newton, Colin N. Haile
  • Patent number: 8822679
    Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: September 2, 2014
    Assignee: California Institute of Technology
    Inventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
  • Publication number: 20140243334
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20140243335
    Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
  • Patent number: 8703957
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: April 22, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
  • Patent number: 8691993
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: April 8, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Tai-An Lin, Eric Mertz, Achyutharao Sidduri, Sung-Sau So, Jefferson Wright Tilley
  • Patent number: 8680159
    Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
  • Patent number: 8623875
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.
    Type: Grant
    Filed: June 10, 2008
    Date of Patent: January 7, 2014
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Ty Wagerle, Ming Xu
  • Patent number: 8618133
    Abstract: The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereof. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: December 31, 2013
    Assignee: Jiangsu Hengyi Pharmaceutical Co., Ltd.
    Inventors: Jianqi Li, Kai Gao, Wangping Cai, Yongyong Zheng
  • Patent number: 8614328
    Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: December 24, 2013
    Assignee: Celgene Corporation
    Inventors: Alexander L. Ruchelman, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
  • Patent number: 8586611
    Abstract: This invention is directed to compounds of Formula (1) including all geometric and stereoisomers, N oxides, and agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides, (1) provided that the compound of Formula 1 is other than 2-[1-[(2-chlorophenyl)acetyl]-4-piperidinyl]-N-methyl-N-[(1R)-1-phenylethyl]-4-thiazolecarboxamide and R1 is other than 4-fluorophenyl; wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, Also disclosed are compositions containing the a compound having a formula corresponding to Formula (1) where the provisos are both omitted; and methods for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound having a formula corresponding to Formula (1) where the provisos are both omitted.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: November 19, 2013
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: John Joseph Bisaha, Patrick Ryan Kovacs, Renee Marie Lett, Jeffrey Keith Long, Robert James Pasteris, Boris Abramovich Klyashchitsky, Bruce Lawrence Finkelstein, Brenton Todd Smith
  • Patent number: 8580822
    Abstract: The present invention provides novel indanone derivatives which can be advantageously used for treating and/or preventing of a medical condition for which inhibition of a cholinesterase is desired.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: November 12, 2013
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra
  • Patent number: 8552195
    Abstract: The method in accordance with the present invention has: mixing E2M, an organic solvent, a weak base, sodium dithionite, and a phase transfer catalyst to obtain an E2M mixture solution; heating the E2M mixture solution and adding water to obtain a heated E2M aqueous solution having an organic layer; and extracting the organic layer from the heated E2M aqueous solution, and condensing and drying the organic layer to obtain donepezil. Employing sodium dithionite as a reducing agent improves safety over hydrogen gas used in conventional methods and lowers the cost in contrast to the conventional noble metal catalysts that are extremely expensive. Furthermore, the method of the present invention requires only 60 minutes of reaction time to synthesize donepezil with a promising yield more than 85%, which greatly raises the efficiency and economic value of the manufacture of donepezil.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: October 8, 2013
    Assignee: Taiwan Biotech Co., Ltd.
    Inventors: Kuen-Wang Sheu, Shu-Fen Huang
  • Patent number: 8541592
    Abstract: The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: September 24, 2013
    Assignees: Amgen Inc., Biovitrum AB
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle, Teresa L. Marshall
  • Publication number: 20130231319
    Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 5, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeup, Sylvaine Gren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein, Davide Pozzi
  • Publication number: 20130225588
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 29, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130225605
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: April 22, 2013
    Publication date: August 29, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Patent number: 8513285
    Abstract: There are disclosed racemic or enantiomerically enriched 3- or 4-substituted piperidine compounds represented by the following structural formula (I): or any of their isomers, or pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions containing the subject compounds. The subject compounds are useful for the treatment of diseases of the central nervous system, particularly depression, anxiety and pain disorder.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: August 20, 2013
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Ki-Ho Lee, Chun-Eung Park, Kyung-Hyan Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu
  • Patent number: 8507538
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: August 13, 2013
    Assignee: Receptos, Inc.
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Publication number: 20130203727
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).
    Type: Application
    Filed: July 1, 2011
    Publication date: August 8, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
  • Patent number: 8501779
    Abstract: Preparation methods of mesylate, para-toluenesulfonate, succinate, tartrate, sulphate, nitrate, phosphate, salicylate, fumarate, maleate, gallate, acetylsalicylate, benzenesulphonate, citrate, aspartate, glutaminate, lactate, gluconate, ascorbate, malonate, malate, sorbate, acetate or formate of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine (i.e., Donepezil). Novel polymorphs formed from these salts and their preparation methods. Co-crystals formed from Donepezil hydrochloride and maleic acid, fumaric acid, citric acid, salicylic acid, tartaric acid or succinic acid.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Tianjin Hemay Bio-Tech Co., Ltd.
    Inventor: Hesheng Zhang
  • Patent number: 8492372
    Abstract: The present invention relates to novel 1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: July 23, 2013
    Assignee: Integrated Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Peder Svensson, Mikael Andersson
  • Publication number: 20130150407
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 13, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8455520
    Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
  • Patent number: 8455521
    Abstract: Diaminoalkanes of below Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity: They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: June 4, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Publication number: 20130137720
    Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 30, 2013
    Applicant: The Regents of the University of Colorado, a body corporated
    Inventors: Xiang Wang, Wenqing Xu
  • Patent number: 8445515
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: May 21, 2013
    Assignee: Chemocentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Patent number: 8436186
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W have the meanings indicated in Claim 1, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: May 7, 2013
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Frank Stieber, Timo Heinrich, Dirk Wienke
  • Patent number: 8399676
    Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R4 have the significance given in claim 1.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: March 19, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
  • Patent number: 8394831
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: March 12, 2013
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Leo Jacobus Jozef Backx
  • Publication number: 20130030008
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 1, 2012
    Publication date: January 31, 2013
    Applicant: SANOFI
    Inventor: Sanofi
  • Publication number: 20130012701
    Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.
    Type: Application
    Filed: June 22, 2012
    Publication date: January 10, 2013
    Applicant: California Institute of Technology
    Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • Publication number: 20120302603
    Abstract: There are provided compounds and methods for the detection and treatment of amyloid deposits and diseases and disorders characterized by amyloid deposits including Alzheimer's disease and related amyloid-based neurodegenerative disorders.
    Type: Application
    Filed: December 10, 2010
    Publication date: November 29, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Jerry Yang, Emmanuel A. Theodorakis
  • Publication number: 20120302539
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 29, 2012
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
  • Patent number: 8318942
    Abstract: A process for producing a Donepezil derivative represented by the formula (I), wherein R1, R2, R3, and R4 each independently represents H, F, an alkyl having from 1 to 4 carbon atoms, or an alkoxy having from 1 to 4 carbon atoms; R5 represents a phenyl or a substituted phenyl; and n is an integer from 0 to 2, characterized in that the process comprises: (a) a reaction of 4-pyridinecarboxaldehyde with a compound of formula (II) in the presence of a strong acid HX to form a compound of formula (III); (b) a catalytic hydrogenation of a compound of formula (III) or a compound of formula (V) to yield a compound of formula (IV); and (c) an alkylation reaction of a compound of formula (IV) to yield a compound of formula (I).
    Type: Grant
    Filed: October 28, 2004
    Date of Patent: November 27, 2012
    Assignee: Tianjin Hemay Bio-Tech Co., Ltd.
    Inventor: Heshang Zhang
  • Publication number: 20120277423
    Abstract: The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.
    Type: Application
    Filed: May 19, 2010
    Publication date: November 1, 2012
    Inventors: Katsuhiko Mikoshiba, Kozo Hamada, Akiko Terauchi, Shouichirou Ozaki, Jun-ichi Goto, Etsuko Ebisui, Akinobu Suzuki
  • Publication number: 20120270901
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: December 8, 2011
    Publication date: October 25, 2012
    Applicant: Aquinox Pharmaceuticals Inc.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Publication number: 20120214809
    Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV 1 receptor activator. In one embodiment, the TRPV 1 receptor activator is lidocaine.
    Type: Application
    Filed: February 18, 2012
    Publication date: August 23, 2012
    Inventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
  • Publication number: 20120209005
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: October 22, 2010
    Publication date: August 16, 2012
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Publication number: 20120190710
    Abstract: The present invention provides bicyclo-heptan-2-amines that selectively bind to the sigma-2 receptor and are useful in the treatment of diseases related to the sigma-2 receptor, for example, cancer and neurological disorders.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 26, 2012
    Applicant: Adeboye Adejare
    Inventors: Adeboye Adejare, Zeynep Ates-Alagoz, Boyenoh Gaye
  • Publication number: 20120149693
    Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.
    Type: Application
    Filed: May 5, 2010
    Publication date: June 14, 2012
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: Raymond G. Booth
  • Publication number: 20120095000
    Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.
    Type: Application
    Filed: December 12, 2011
    Publication date: April 19, 2012
    Applicants: SRI International, The Board of Trustees of the Leland Stanford Junior University
    Inventors: Anton Wyss-Coray, Mary J. Tanga