Ring Chalcogen In The Five-membered Hetero Ring Patents (Class 544/367)
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Patent number: 8623875Abstract: 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: GrantFiled: June 10, 2008Date of Patent: January 7, 2014Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Ty Wagerle, Ming Xu
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Patent number: 8618110Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: GrantFiled: February 9, 2010Date of Patent: December 31, 2013Assignee: VM Discovery Inc.Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20130324538Abstract: The 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 warm-blooded animals.Type: ApplicationFiled: February 9, 2012Publication date: December 5, 2013Inventors: Noëlle Gauvry, Steve Nanchen
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Patent number: 8598179Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 17, 2010Date of Patent: December 3, 2013Assignee: SanofiInventors: Marc Nazaré, Gernot Zech, Jochen Goerlitzer, Melitta Just, Tilo Weiss, Gerhard Hessler, Werngard Czechtizky, Sven Ruf
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Patent number: 8598162Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: October 11, 2011Date of Patent: December 3, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Jun Matsubara, Yohji Sakurai
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Patent number: 8592498Abstract: Disclosed herein are a reaction method and a production method of an organic compound which are capable of achieving high reaction selectivity according to the purpose and a high production rate of a target substance. The methods include at least two fluids, wherein at least one kind of the fluids is a fluid containing at least one organic compound and at least one kind of the fluids other than the above fluid is a fluid containing at least one reactant in the form of a liquid or solution, and the respective fluids join together in a thin film fluid foamed between processing surfaces arranged to be opposite to each other so as to be able to approach to and separate from each other, at least one of which rotates relative to the other, whereby an organic reaction is performed in the thin film fluid.Type: GrantFiled: September 11, 2008Date of Patent: November 26, 2013Assignee: M. Technique Co., Ltd.Inventor: Masakazu Enomura
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Publication number: 20130296334Abstract: Disclosed are organic amine salts of azilsartan, a preparation method and use thereof. In particular, disclosed are organic amine salts of azilsartan, their preparation method, the pharmaceutical composition comprising the compound in a therapeutically effective quantity, and their use for the manufacture of antihypertensive medicaments.Type: ApplicationFiled: January 11, 2012Publication date: November 7, 2013Applicants: JIANGSU HANSOH PHARMACEUTICAL CO., LTD., JIANGSU HANSOH MEDICINE INSTITUTE CO., LTD., JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTDInventors: Bigao Pan, Longbin Huang, Baohai Yang
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Patent number: 8575161Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).Type: GrantFiled: March 30, 2009Date of Patent: November 5, 2013Assignee: Merck Patent GmbHInventors: Didier Roche, Gisèle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
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Patent number: 8569307Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: GrantFiled: June 11, 2012Date of Patent: October 29, 2013Assignee: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Publication number: 20130267537Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: February 5, 2013Publication date: October 10, 2013Applicant: Cytokinetics, Inc.Inventors: Bradley Paul MORGAN, Fady MALIK, Erica Anne KRAYNACK, Alexander Ramon MUCI, Xiangping QIAN, David J. MORGANS, JR.
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Patent number: 8546375Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.Type: GrantFiled: July 5, 2011Date of Patent: October 1, 2013Assignee: AstraZeneca ABInventors: Susanne Doris Margit Bökman-Winiwarter, Marlene Fredenwall, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
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Patent number: 8541595Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.Type: GrantFiled: November 3, 2009Date of Patent: September 24, 2013Assignee: Merch Sharp & Dohme Corp.Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
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Publication number: 20130237548Abstract: Polymorphs of 7-methyl-5-(3-piperazin-1-ylmethyl-[1,2,4]oxadiazol-5-yl)-2-(4-trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one mesylate salt, methods of making these polymorphs and uses thereof.Type: ApplicationFiled: April 21, 2011Publication date: September 12, 2013Applicant: ASTRAZENECA ABInventors: Helen Blade, Stephen David Cosgrove
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Patent number: 8530476Abstract: Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: GrantFiled: September 11, 2009Date of Patent: September 10, 2013Assignee: Janssen Pharmaceutica NVInventors: Richard Apodaca, J. Guy Breitenbucher, Kanaka Pattabiraman, Mark Seierstad, Wei Xiao
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Publication number: 20130231326Abstract: 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 are 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: ApplicationFiled: January 14, 2013Publication date: September 5, 2013Applicant: RECEPTOS, INC.Inventors: Esther Martinborough, Marcus F. Boehm, Adam Richard Yeager, Junko Tamiya, Liming Huang, Enugurthi Brahmachary, Manisha Moorjani, Gregg Alan Timony, Jennifer L. Brooks, Robert Peach, Fiona Lorraine Scott, Michael Allen Hanson
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Publication number: 20130225600Abstract: The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).Type: ApplicationFiled: October 31, 2011Publication date: August 29, 2013Applicant: LUPIN LIMITEDInventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Vijay Pandurang Karche, Santosh Madhukar Jachak, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20130225586Abstract: The present invention provides a compound having Formula I or II: wherein B, R, X, Ar, and Y are defined herein, pharmaceutically acceptable salts thereof and pharmaceutically acceptable prodrugs thereof. The present invention also provides methods of making and using the compound.Type: ApplicationFiled: September 25, 2012Publication date: August 29, 2013Applicant: CPSI STOCKHOLDER TRUSTInventor: CPSI Stockholder Trust
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Publication number: 20130217699Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.Type: ApplicationFiled: May 8, 2012Publication date: August 22, 2013Applicant: ELI LILLY AND COMPANYInventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
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Patent number: 8513257Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 30, 2011Date of Patent: August 20, 2013Assignee: Cytokinetics, IncorporatedInventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, Jr.
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Patent number: 8507538Abstract: 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: GrantFiled: November 15, 2010Date of Patent: August 13, 2013Assignee: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
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Patent number: 8507474Abstract: This invention is directed to compounds of the formula (I) and salts therefore that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds of this invention, pharmaceutical compositions and kits comprising the compounds of this invention, uses of the compounds of this invention to make medicaments, and treatments comprising the administration of the compounds of this invention to animals in need of the treatments.Type: GrantFiled: June 16, 2010Date of Patent: August 13, 2013Assignee: Intervet International B.V.Inventors: Christophe Pierre Alain Chassaing, Thorsten Meyer
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Publication number: 20130203995Abstract: Processes for making 7-methyl-5-(3piperazin-1-ylmethyl-[1,2,4]oxadiazol-5-yl)-2-(4-trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-oneType: ApplicationFiled: January 4, 2011Publication date: August 8, 2013Applicant: ASTRAZENECA ABInventors: Alistair Boyd, Mark Richard Fielding, James Gair Ford, Lianne Frodsham, Michael D. Golden, Kevin William Leslie, Ben Mckeever-Abbas, Paula Tomlin
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Patent number: 8501781Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).Type: GrantFiled: October 27, 2010Date of Patent: August 6, 2013Assignee: Bayer Cropscience AGInventors: Pierre Cristau, Nicola Rahn, Tomoki Tsuchiya, Joachim Kluth, Pierre Wasnaire, Sebastian Hoffmann, Jürgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
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Publication number: 20130196996Abstract: One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stage bladder cancer, T1 stage bladder cancer, T2 stage bladder cancer, T3 stage bladder cancer, T4 stage bladder cancer, lymph node metastasis therefrom, solid organ metastasis therefrom, bony metastasis therefrom, cachexia/anorexia associated with bladder cancer, generalized wasting syndrome associated with bladder cancer, or a combination thereof, by administering to a subject in need thereof one or more compounds described herein, prodrug thereof, salt thereof, or a combination thereof.Type: ApplicationFiled: January 19, 2011Publication date: August 1, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: John Arthur Taylor, III, Thais Sielecki-Dzurdz
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Patent number: 8492378Abstract: For the purpose of providing a GSK-3? inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3?-related pathology or disease, the present invention provides a GSK-3? inhibitor containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: GrantFiled: August 2, 2007Date of Patent: July 23, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Fumio Itoh, Jun Kunitomo, Hiromi Kobayashi, Eiji Kimura, Morihisa Saitoh, Tomohiro Kawamoto, Hiroki Iwashita, Katsuhito Murase
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Publication number: 20130184251Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.Type: ApplicationFiled: March 4, 2013Publication date: July 18, 2013Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20130184278Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: November 20, 2012Publication date: July 18, 2013Applicant: Abbott LaboratoriesInventor: Abbott Laboratories
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Publication number: 20130172553Abstract: Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described.Type: ApplicationFiled: November 26, 2010Publication date: July 4, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: Thais Sielecki-Dzurdz, James Pruitt
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Publication number: 20130165433Abstract: The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection.Type: ApplicationFiled: September 6, 2011Publication date: June 27, 2013Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Zoe Alicia Harrison, Katherine Louise Jones, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Charlotte Jane Mitchell, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christopher Alan Paul Smethurst, Yoshiaki Washio
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Patent number: 8461159Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: GrantFiled: November 24, 2009Date of Patent: June 11, 2013Assignee: Jannsen Pharmaceutica BVInventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Seierstad
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Patent number: 8455476Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: June 4, 2013Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Patent number: 8450310Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.Type: GrantFiled: June 18, 2012Date of Patent: May 28, 2013Assignees: Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Patent number: 8445477Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Patent number: 8431563Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: GrantFiled: August 23, 2011Date of Patent: April 30, 2013Assignee: Amgen Inc.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Patent number: 8426420Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 17, 2010Date of Patent: April 23, 2013Assignee: SanofiInventors: Marc Nazaré, Gernot Zech, Melitta Just, Tilo Weiss, Gerhard Hessler, Markus Kohlmann
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Patent number: 8420639Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: April 21, 2010Date of Patent: April 16, 2013Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Jared Andrew Forrester
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Patent number: 8415341Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: April 9, 2013Assignee: Janssen Pharmaceutica, NVInventors: Kristen Chevalier, Jose Clemente, Scott Dax, Chris Flores, Li Liu, Mark Macielag, Mark McDonnell, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang, Bin Zhu
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Publication number: 20130072490Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: September 29, 2010Publication date: March 21, 2013Applicant: Amira Pharmaceuticals INC.Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
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Publication number: 20130060025Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 12, 2012Publication date: March 7, 2013Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Publication number: 20130053372Abstract: The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.Type: ApplicationFiled: February 15, 2011Publication date: February 28, 2013Inventors: Prashant Bhimrao Kapadnis, Robert Glen, Robin Hiley, James Bell, David Spring
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Patent number: 8383616Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.Type: GrantFiled: June 30, 2009Date of Patent: February 26, 2013Assignee: Sigma-Tau Industrie Farmaceutiche Riunite SpAInventors: Giuseppe Giannini, Walter Cabri, Daniele Simoni, Riccardo Baruchello, Claudio Pisano, Gabriella Singrossi, Silvia Carminati, Giuseppe Paolo Carminati
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Patent number: 8377940Abstract: Compounds of Formula (I) wherein R1 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: GrantFiled: June 5, 2008Date of Patent: February 19, 2013Assignee: AstraZeneca ABInventors: Joshua Clayton, Ian Egle, James Empfield, James Folmer, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi
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Patent number: 8377939Abstract: Compounds of Formula I: wherein R1 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: GrantFiled: June 6, 2008Date of Patent: February 19, 2013Assignee: AstraZeneca ABInventors: Joshua Clayton, Ian Egle, James Empfield, James Folmer, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi
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Publication number: 20130040930Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Publication number: 20130040948Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: ApplicationFiled: February 10, 2012Publication date: February 14, 2013Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20130035329Abstract: Compounds and compositions comprising compounds useful in the treatment of cancer are described herein.Type: ApplicationFiled: June 8, 2012Publication date: February 7, 2013Inventors: Jeffrey O. Saunders, Francesco G. Salituro
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Patent number: 8367653Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: February 5, 2013Assignee: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark MacIelag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20130029978Abstract: There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.Type: ApplicationFiled: December 24, 2010Publication date: January 31, 2013Inventors: Tomoyuki Kamino, Yoshitaka Maeda
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Patent number: 8362004Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, or —CH?CH2; W is —NO2, —Cl, —Br, —CHO, —CH?CH2, or —CN; X is —Cl, —CH3, or —CN; Y is —CH or —N; and Z is C1-C6 alkyl, C3-C6 cycloalkyl, substituted aryl, substituted heteroaryl, OR1, or NHR1, wherein R1 is selected from the group of H, aryl, heteroaryl, C1-C6 alkyl and C3-C6 cycloalkyl. This compound is useful in compositions for the prevention and treatment of influenza virus.Type: GrantFiled: September 6, 2011Date of Patent: January 29, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Christopher W. Cianci, Samuel Gerritz, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
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Patent number: 8338599Abstract: The present invention relates to the use of compounds with a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, for the preparation of a medicament for preventing and/or treating mycobacterial infections such as tuberculosis and leprosy, to pharmaceutical compositions comprising them in combination with an antibiotic that is activatable via the EthA pathway, to compounds having a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, to pharmaceutical compositions comprising them and to their use as medicaments, especially medicaments for preventing and/or treating mycobacterial infections such as tuberculosis and leprosy.Type: GrantFiled: July 4, 2007Date of Patent: December 25, 2012Assignees: Institut Pasteur de Lille, Centre National de la Recherche Scientifique, Universite de Lille 2, Universite du Droit et de la Sante, Institut National de la Sante et de la Recherche Medicale (Inserm)Inventors: Benoît Deprez, Nicolas Willand, Bertrand Dirie, Patrick Toto, Vincent Villeret, Camille Locht, Alain Baulard