Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
  • Publication number: 20130172367
    Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.
    Type: Application
    Filed: November 27, 2012
    Publication date: July 4, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventor: Bayer CropScience AG
  • Publication number: 20130172232
    Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cath
    Type: Application
    Filed: June 16, 2011
    Publication date: July 4, 2013
    Applicant: MEDIVIR UK LTD
    Inventors: Susana Ayesa, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Bjorn Klasson, Pia Kahnberg, Stina Lundgren, Jan Tejbrant, Daniel Wiktelius
  • Publication number: 20130172316
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8476451
    Abstract: The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The compounds of the invention are highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.
    Type: Grant
    Filed: July 21, 2008
    Date of Patent: July 2, 2013
    Assignee: The Regents of the University of California
    Inventors: Jonathan A. Ellman, Andrew W. Patterson, Hillary Peltier
  • Publication number: 20130165443
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: August 23, 2012
    Publication date: June 27, 2013
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Patent number: 8470855
    Abstract: Compounds of the general formulae (1) and (2) A-B-D-B?-A???(1) and A-B-D-E??(2) in which A and A? may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B? may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residu
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: June 25, 2013
    Assignee: IMTM GmbH
    Inventors: Siegfried Ansorge, Klaus Neubert, Ute Bank, Irene Reichstein, Jürgen Faust, Michael Täger, Petra Fuchs, Bianca Senns
  • Publication number: 20130158018
    Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 20, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
  • Publication number: 20130158004
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Application
    Filed: December 14, 2012
    Publication date: June 20, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Niklas HEINE, Gerald Juergen ROTH
  • Patent number: 8466145
    Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: June 18, 2013
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
  • Patent number: 8455658
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: June 4, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
  • Patent number: 8440837
    Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: May 14, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Mathivanan Packiarajan, Michel Grenon
  • Patent number: 8426606
    Abstract: The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2?,2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: April 23, 2013
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Wei Tang
  • Publication number: 20130096124
    Abstract: The present invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
    Type: Application
    Filed: June 11, 2011
    Publication date: April 18, 2013
    Inventors: Steve Nanchen, Noelle Gauvry, Thomas Goebel
  • Patent number: 8420145
    Abstract: The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: April 16, 2013
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Sara L. Adamski-Werner, Jeffrey M. Yamamoto, Guy Servant
  • Publication number: 20130090479
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.
    Type: Application
    Filed: July 3, 2012
    Publication date: April 11, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Ronald Knegtel, Daniel Robinson, Philip Collier
  • Patent number: 8415480
    Abstract: The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: April 9, 2013
    Assignee: Merck Serono SA
    Inventors: Patrick Naxos Page, Catherine Jorand-Lebrun, Anna Quattropani, Vincent Pomel, Matthias Schwarz, Estelle Hamelin, Russell J. Thomas
  • Publication number: 20130059895
    Abstract: The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2?,2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability.
    Type: Application
    Filed: March 16, 2011
    Publication date: March 7, 2013
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Wei Tang
  • Publication number: 20130053382
    Abstract: The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.
    Type: Application
    Filed: April 28, 2011
    Publication date: February 28, 2013
    Inventors: Sunil Paliwal, Matthew Paul Rainka, Ang Li, May Xiaowu Jiang, Hon-chung Tsui, Ronald J. Doll
  • Publication number: 20130053402
    Abstract: The present invention relates to compounds of the formulae Ia and Ib, wherein G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: July 26, 2012
    Publication date: February 28, 2013
    Applicant: SANOFI
    Inventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Klaus WIRTH
  • Patent number: 8383653
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: June 30, 2004
    Date of Patent: February 26, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20130045999
    Abstract: The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.
    Type: Application
    Filed: February 17, 2012
    Publication date: February 21, 2013
    Applicant: AiCuris GmbH & Co. KG
    Inventors: Kai Thede, Susanne Greschat, Kersten Matthias Gericke, Steffen Wildum, Daniela Paulsen
  • Patent number: 8372982
    Abstract: The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C1-C8-alkyl groups, and X, Z1, Z2 and Z3 represent various substituents; their process of preparation; the preparation of intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: February 12, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
  • Publication number: 20130018048
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: April 4, 2011
    Publication date: January 17, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
  • Publication number: 20130017196
    Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagnition, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
  • Publication number: 20130005663
    Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 3, 2013
    Applicant: NOVARTIS AG
    Inventors: Mark G. CHAREST, Christine Hiu-Tung CHEN, Zhuoliang CHEN, Miao DAI, Feng HE, Huangshu LEI, Ly Luu PHAM, Sushil Kumar SHARMA, Christopher Sean STRAUB, Run-Ming David WANG, Fan YANG, Leigh ZAWEL
  • Publication number: 20120328691
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Application
    Filed: October 29, 2007
    Publication date: December 27, 2012
    Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory Poker, Timothy J. Guzi
  • Patent number: 8314089
    Abstract: The present invention relates to novel substituted pyrazolamides, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: November 20, 2012
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Rudolf Schohe-Loop, Reinhold Welker, Arnold Paessens, Marcus Bauser, Friederike Stoll, Frank Dittmer, Kerstin Henninger, Daniela Paulsen, Dieter Lang
  • Publication number: 20120289505
    Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
    Type: Application
    Filed: December 30, 2010
    Publication date: November 15, 2012
    Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
  • Publication number: 20120270877
    Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
    Type: Application
    Filed: November 1, 2010
    Publication date: October 25, 2012
    Applicant: MannKind Corporation
    Inventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
  • Publication number: 20120264793
    Abstract: The present invention discloses the pharmaceutical use of a 2?,2-bis-thiazole non-nucleoside compound of formula I as an inhibitor of hepatitis C virus (HCV). The 2?,2-bis-thiazole non-nucleoside compound can inhibit the replication of HCV, and thus has an anti-HCV activity and is useful for treating hepatitis C.
    Type: Application
    Filed: November 24, 2010
    Publication date: October 18, 2012
    Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Feihong Ji, Haijun Chen, Xiankun Tong
  • Publication number: 20120258960
    Abstract: The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.
    Type: Application
    Filed: August 26, 2010
    Publication date: October 11, 2012
    Applicant: IMTM GMBH
    Inventors: Siegfried Ansorge, Ute Bank, Karsten Nordhoff, Peter Roehnert, Sofia Stefin, Frank Striggow, Michael Taeger
  • Publication number: 20120252770
    Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Application
    Filed: March 23, 2012
    Publication date: October 4, 2012
    Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
  • Patent number: 8273777
    Abstract: Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
    Type: Grant
    Filed: August 30, 2010
    Date of Patent: September 25, 2012
    Assignee: Bristol-Meyer Squibb Company
    Inventors: Yan Shi, Peter T. W. Cheng, Ying Wang, Denis E. Ryono
  • Publication number: 20120238559
    Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Application
    Filed: December 3, 2010
    Publication date: September 20, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Publication number: 20120225867
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: October 27, 2010
    Publication date: September 6, 2012
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Patent number: 8236832
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds, to methods of using the compounds and to the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: August 7, 2012
    Assignee: Vertex Pharmaceuticals Inc.
    Inventors: Juan-Miguel Jimenez, Ronald Knegtel, Daniel Robinson, Phil Collier
  • Patent number: 8236798
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: August 7, 2012
    Assignees: Abbott GmbH & Co. KG, Abbott Laboratories
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 8236964
    Abstract: The invention relates to novel thiazolidine derivatives of the formula (I) wherein A and R1 are as described in the description and their use as medicaments, especially as orexin receptor antagonists.
    Type: Grant
    Filed: March 25, 2008
    Date of Patent: August 7, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
  • Publication number: 20120196793
    Abstract: A method to predict which patients will respond to a IAP inhibiting compound comprising administering an IAP inhibitor compound to a patient/and measuring IL1B, Lymphotoxin alpha (LTa), TWEAK, LIGHT, Fas, TNF alpha or TRAIL levels.
    Type: Application
    Filed: September 17, 2010
    Publication date: August 2, 2012
    Inventors: Brant G. Firestone, Kymberly Levine, Dale A. Porter, John Sullivan, Leigh Zawel
  • Publication number: 20120190686
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Application
    Filed: December 22, 2011
    Publication date: July 26, 2012
    Applicant: H. LUNDBECK A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Publication number: 20120184521
    Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
    Type: Application
    Filed: September 24, 2010
    Publication date: July 19, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Eiji Kawaminami, Tatsuhisa Takahashi, Takatoshi Kanayama, Yuta Fukuda, Hiroyuki Kaizawa, Yutaka Kondoh, Ryushi Seo, Kazuyuki Kuramoto, Kazuhiko Take, Kazuyuki Sakamoto
  • Patent number: 8211924
    Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and to their salts which are useful for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a radical of formulae A.1 or A.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: July 3, 2012
    Assignee: BASF SE
    Inventors: Markus Kordes, Christopher Koradin, Ronan Le Vezouet, Ernst Baumann, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Cecille Ebuenga
  • Publication number: 20120165345
    Abstract: The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests, which include arthropods and especially insects, and to processes for preparing the novel compounds.
    Type: Application
    Filed: June 28, 2011
    Publication date: June 28, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Thomas BRETSCHNEIDER, Reiner FISCHER, Martin FÜßLEIN, Peter JESCHKE, Adeline KÖHLER, Joachim KLUTH, Friedrich August MÜHLTHAU, Yoshitaka SATO, Arnd VOERSTE, Eiichi SHIMOJO
  • Patent number: 8207207
    Abstract: The invention relates to a fungicidally active compound of formula (I): as defined in claim 1; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: June 26, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi
  • Patent number: 8207183
    Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: June 26, 2012
    Assignee: Novartis AG
    Inventors: Mark G. Palermo, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming Wang, Leigh Zawel, Yanling Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
  • Publication number: 20120149710
    Abstract: Bacterial infections, including Methicillin resistant Staphylococcus aureus (MRSA) infections are a major health problem that has created a pressing need for new antibiotics. Pyridazinone, rhodanine, and pyrazolethione compounds effective inhibit the enzymatic activity of sortase A (srtA) found in gram positive bacteria are disclosed. A structure activity relationship (SAR) analysis led to the identification of several pyridazinone and pyrazolethione analogs that inhibit SrtA with IC50 values in the sub-micromolar range. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Many of these molecules also inhibit the sortase enzyme from B. anthracis suggesting that they may be generalized sortase inhibitors. The novel compounds, compositions, uses, formulations, medicaments, articles of manufacture provide improved materials, uses, and treatments useful in combating infectious disorders.
    Type: Application
    Filed: August 23, 2010
    Publication date: June 14, 2012
    Inventors: Michael E. Jung, Robert T. Clubb, Sung Wook Yi, Nutee Suree, Jeremy Justin Clemens
  • Publication number: 20120128742
    Abstract: The present disclosure relates to crystalline form of (S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, salts and hydrates thereof. This disclosure also relates to solid oral formulation of (S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, pharmaceutically acceptable salts, solvates (including hydrates) thereof, as well as methods of treatment using the same.
    Type: Application
    Filed: August 11, 2010
    Publication date: May 24, 2012
    Inventors: Jeewan Thakur, Dong Yang, Lili Feng
  • Publication number: 20120129779
    Abstract: The present invention relates to novel cytotoxic molecules and their use for the treatment of cancer and other diseases.
    Type: Application
    Filed: May 9, 2008
    Publication date: May 24, 2012
    Applicant: R&D-BIOPHARMACEUTICALS GMBH
    Inventor: Wolfgang Richter
  • Patent number: 8178522
    Abstract: The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: May 15, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • Publication number: 20120115868
    Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Application
    Filed: November 2, 2011
    Publication date: May 10, 2012
    Inventors: Stephen Deems Gabriel, Andrew Thomas