The Nitrogens Are In The 1,4-positions Of The Hetero Ring Patents (Class 540/575)
-
Publication number: 20130217680Abstract: This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 24, 2011Publication date: August 22, 2013Inventors: Alexander Pasternak, Reynalda K. deJesus, Yuping Zhu, Lihu Yang, Shawn Walsh, Haifeng Tang, Dooseop Kim, Barbara Pio, Aurash Shahripour, Kevin Belyk
-
Publication number: 20130216498Abstract: New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: December 23, 2010Publication date: August 22, 2013Inventors: Paul Robert Eastwood, Jacob Gonzales Rodriguez, Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Victor Giulio Matassa
-
Publication number: 20130210796Abstract: The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.Type: ApplicationFiled: July 8, 2011Publication date: August 15, 2013Inventors: Paul Beswick, Robert James Gleave, Shuji Hachisu, Sadie Vile, Nicholas Bertheleme, Simon E. Ward
-
Publication number: 20130210769Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
-
Publication number: 20130210811Abstract: Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11?-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11?-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11?-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerance (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.Type: ApplicationFiled: May 4, 2011Publication date: August 15, 2013Applicant: SK CHEMICALS CO., LTD.Inventors: Je Ho Ryu, Shin Ae Kim, Keun Ho Ryu, Jae Sun Kim, Nam Ho Kim, Hye Young Han, Yong Hyuk Kim, Won-No Youn, Yoon-Jung Lee, Hyun Joo Son, Bong-Yong Lee, Sung Hoon Park, Ju Young Lee, Hyun Jung Lee, Hoe Chul Jung, Young Ah Shin, Jung A Lee, Bo Ram Lee, Joon Ho Sa
-
Publication number: 20130210768Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 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 metabotropic glutamate receptors are involved, such as schizophrenia.Type: ApplicationFiled: June 6, 2011Publication date: August 15, 2013Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif
-
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
-
Publication number: 20130203730Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
-
Publication number: 20130203714Abstract: The invention concerns bicyclic compounds of Formula I wherein R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.Type: ApplicationFiled: August 1, 2012Publication date: August 8, 2013Applicant: ASTRAZENECA R&DInventors: Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
-
Patent number: 8501732Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: GrantFiled: July 11, 2012Date of Patent: August 6, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Joseph A. Bilotta, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Stuart Hayden, Nancy-Ellen Haynes, Christine M. Lukacs-Lesburg, Nicholas Marcopulos, Eric Mertz, Lida Qi, Yimin Qian, Sung-Sau So, Jenny Tan, Kshitij C. Thakkar
-
Publication number: 20130196964Abstract: The present application relates to novel aryl compounds with heterocyclic substituents, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 31, 2009Publication date: August 1, 2013Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Berhörster, Susanne Greschat, Karl-Heinz Thierauch, Frank Süssmeier
-
Publication number: 20130196973Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 13, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
-
Publication number: 20130196972Abstract: This invention relates to novel compounds of reverse-turn mimetics, having pyrazino-triazinone as a basic framework, and a method of preparing the same, and the use thereof to treat diseases such as cancer, in particular, acute myeloid leukemia.Type: ApplicationFiled: October 14, 2011Publication date: August 1, 2013Applicant: JW PHARMACEUTICAL CORPORATIONInventors: Jae-Uk Chung, Mi-Jung Kim, Yong-Sil Lee, Sang-Ho Ma, Young-Seok Cho, Sang-Hak Lee, Young-Jun Na, Myoung-Joo Kang, Woul-Seong Park
-
Publication number: 20130196975Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, m and n are defined as in the specification, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: March 12, 2013Publication date: August 1, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Tobias WUNBERG, Siegfried SCHNEIDER, Lars VAN DER VEEN
-
Publication number: 20130196979Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD Pharmaceuticals, Inc.
-
Publication number: 20130190298Abstract: The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against ALK and are useful in treating disorders related to abnormal protein kinase activities such as cancer, neurological and psychiatric diseases.Type: ApplicationFiled: October 7, 2011Publication date: July 25, 2013Applicant: Xcovery Holding Company, LLC.Inventor: Congxin Liang
-
Publication number: 20130190286Abstract: The present invention encompasses compounds of general formula (1) where in the groups R0to R3 and L are defined as in claim 1, which are suitable for the 5 treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: March 25, 2011Publication date: July 25, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
-
Publication number: 20130190489Abstract: The present invention provides compounds of general formulae A, useful as potential anti-tubercular agents against Mycobacterium tuberculosis H37Rv, and drug-resistant Mycobacterium tuberculosis and a process for the preparation thereof. Formula (A).Type: ApplicationFiled: May 6, 2011Publication date: July 25, 2013Inventors: Ahmed Kamal, Azeeza Shaik, Ahmad Ali Shaik, Mohammed Shaheer Malik, Inshad Ali Khan, Sheikh Tasdug Abdullah, Sandeep Sharma, Anshu Beulah Ram
-
Patent number: 8492375Abstract: The present invention relates to novel diazepanyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: October 26, 2010Date of Patent: July 23, 2013Assignee: Glaxo Group LimitedInventors: Gordon Bruton, Anthony Huxley, Barry Sidney Orlek, Kishore Kalidas Rana
-
Patent number: 8492374Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).Type: GrantFiled: April 28, 2010Date of Patent: July 23, 2013Assignee: Industrial Technology Research InstituteInventors: On Lee, Chih-Hung Chen, Chi-Y Hung, Yow-Lone Chang, Ting-Shou Chen
-
Publication number: 20130184259Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: November 16, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATED
-
Publication number: 20130184263Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.Type: ApplicationFiled: December 14, 2012Publication date: July 18, 2013Applicant: GlaxoSmithKline LLCInventor: GlaxoSmithKline LLC
-
Patent number: 8486931Abstract: The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/oType: GrantFiled: February 29, 2008Date of Patent: July 16, 2013Assignee: Abbott GmbH & Co. KGInventors: Herve Genesle, Thorsten Oost, Charles W. Hutchins, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Astrid Netz, Alfred Hahn
-
Publication number: 20130178420Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.Type: ApplicationFiled: December 12, 2012Publication date: July 11, 2013Applicant: RECEPTOS, INC.Inventor: RECEPTOS, INC.
-
Publication number: 20130178458Abstract: In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: December 3, 2012Publication date: July 11, 2013Applicant: Vanderbilt UniversityInventor: Vanderbilt University
-
Patent number: 8481527Abstract: The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I) wherein R1-R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: GrantFiled: October 27, 2007Date of Patent: July 9, 2013Assignee: Richter Gedeon Nyrt.Inventors: Istvan Vago, Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Monika Vastag
-
Publication number: 20130172326Abstract: The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(?O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.Type: ApplicationFiled: November 23, 2011Publication date: July 4, 2013Applicant: PIERRE FABRE MEDICAMENTInventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Christophe Pignier
-
Publication number: 20130172549Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: January 29, 2013Publication date: July 4, 2013Applicant: H. Lundbeck A/SInventor: H. Lundbeck A/S
-
Publication number: 20130172310Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: September 12, 2012Publication date: July 4, 2013Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
-
Patent number: 8476278Abstract: The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: GrantFiled: October 27, 2008Date of Patent: July 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Panduranga Adulla P. Reddy, Tzu T. Wong, Lianyun Zhao, Shuyi Tang, Marc A. Labroli, Timothy J. Guzi, M. Arshad Siddiqui
-
Patent number: 8476257Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: December 3, 2008Date of Patent: July 2, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
-
Patent number: 8470851Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: January 25, 2012Date of Patent: June 25, 2013Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
-
Publication number: 20130158259Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: February 13, 2013Publication date: June 20, 2013Applicant: JANSSEN PHARMACEUTICA NVInventor: JANSSEN PHARMACEUTICA NV
-
Publication number: 20130158258Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: February 12, 2013Publication date: June 20, 2013Applicant: Janssen Pharmaceutica NVInventor: Janssen Pharmaceutica NV
-
Publication number: 20130158015Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: AERIE PHARMACEUTICALS, INC.Inventor: Aerie Pharmaceuticals, Inc.
-
Publication number: 20130157997Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: November 16, 2012Publication date: June 20, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
-
Publication number: 20130150340Abstract: The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: October 25, 2012Publication date: June 13, 2013Applicant: SANOFIInventor: SANOFI
-
Publication number: 20130150573Abstract: Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.Type: ApplicationFiled: February 6, 2013Publication date: June 13, 2013Applicant: UCB Pharma S.A.Inventor: UCB Pharma S.A.
-
Publication number: 20130150349Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventor: Rigel Pharmaceuticals, Inc.
-
Publication number: 20130150343Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
-
Publication number: 20130143871Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: August 12, 2011Publication date: June 6, 2013Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
-
Publication number: 20130144054Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.Type: ApplicationFiled: August 25, 2011Publication date: June 6, 2013Inventors: Noriaki Gomi, Tadaaki Ohgiya, Kimiyuki Shibuya
-
Publication number: 20130137679Abstract: The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.Type: ApplicationFiled: July 1, 2011Publication date: May 30, 2013Inventors: Jian Jin, Bryan Roth, Stephen Frye
-
Patent number: 8450306Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumor pain and headache diseases.Type: GrantFiled: August 12, 2008Date of Patent: May 28, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
-
Publication number: 20130131338Abstract: A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 14, 2012Publication date: May 23, 2013Applicant: Glaxo Group LimitedInventor: Glaxo Group Limited
-
Publication number: 20130131037Abstract: Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: January 11, 2013Publication date: May 23, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRAENKTER HAFTUNGInventor: MERCK PATENT GESELLSCHAFT MIT BESCHRAENKTER HAFTUNG
-
Publication number: 20130131047Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.Type: ApplicationFiled: December 14, 2012Publication date: May 23, 2013Applicant: SURFACE LOGIX, INC.Inventor: SURFACE LOGIX, INC.
-
Publication number: 20130131034Abstract: The instant invention relates to derivatives of formula (I) and their application in therapeutics.Type: ApplicationFiled: March 1, 2011Publication date: May 23, 2013Applicant: SANOFIInventors: Markus Follmann, Pascale Goberville, Stéphanie Hachtel, Gerhard Hessler, Heinz-Werner Kleemann, Thomas Maier, Gary MC Cort, Carsten Struebing, Bérangère Thiers, Li-Hsing Wang
-
Patent number: 8445482Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: April 25, 2012Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
-
Publication number: 20130123241Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: ApplicationFiled: May 10, 2011Publication date: May 16, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer