Plural Nitrogens In The Additional Five-membered Hetero Ring Patents (Class 514/254.05)
-
Publication number: 20140072532Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.Type: ApplicationFiled: October 11, 2013Publication date: March 13, 2014Applicant: MICRODOSE THERAPEUTX, INC.Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
-
Publication number: 20140066455Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: November 13, 2013Publication date: March 6, 2014Applicant: AstraZeneca ABInventors: David BUTTAR, Kevin Michael FOOTE, Maria-Elena THEOCLITOU, Andrew Peter THOMAS
-
Publication number: 20140066369Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 18, 2012Publication date: March 6, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Dawei Yue, Xiuwen Zhu
-
Patent number: 8658642Abstract: 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: March 15, 2013Date of Patent: February 25, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Jared Andrew Forrester
-
Publication number: 20140038979Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: October 14, 2013Publication date: February 6, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristof VAN EMELEN, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van Heusden
-
Publication number: 20140038964Abstract: Methods of using compounds of the invention, such as compounds of Formulae IIa, IIb, IIc, or IId and pharmaceutically acceptable salts thereof are disclosed. The compounds are useful in treating, preventing, inhibiting or ameliorating the symptoms of a disease or disorder that is modulated or otherwise affected by nuclear receptor activity, or in which nuclear receptor activity is implicated.Type: ApplicationFiled: July 25, 2013Publication date: February 6, 2014Applicant: Exelixis Patent Company LLCInventors: Brett B. Busch, Brenton T. Flatt, Xiao-Hui Gu, Shao Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin J. Schweiger, William C. Stevens, JR., Tie-Lin Wang, Yinong Xie
-
Patent number: 8642025Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: October 12, 2012Date of Patent: February 4, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
-
Publication number: 20140024657Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: September 20, 2013Publication date: January 23, 2014Applicant: President and Fellows of Harvard CollegeInventors: Junying YUAN, Emily S. Hsu
-
Publication number: 20140018318Abstract: The present invention provides inhibitors of a wide variety of serine hydrolase enzymes. The inhibitors of the present invention are N1- and N2-carbamoyl-1,2,3-triazole compounds such as those of Formula (I): in which N1, N2, and N3 are the nitrogen atoms at positions 1, 2, and 3, respectively, of the triazole ring, and R4, R5, R6 and R7 in Formula (I) are as described herein. Methods of inhibiting serine hydrolase enzymes and methods of preparing carbamoyl-1,2,3-triazole compounds also are described.Type: ApplicationFiled: April 5, 2012Publication date: January 16, 2014Applicant: The Scipps Research InstituteInventors: Benjamin Cravatt, Alexander Adibekian, Katsunori Tsuboi, Ku-Lung Hsu
-
Publication number: 20140011816Abstract: The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) wherein R1, R2, R3, R4a, R4b, R5, X, Y1, Y2, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: March 22, 2012Publication date: January 9, 2014Inventors: Francois Paul Biscoff, Adriana Ingrid Velter, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
-
Publication number: 20140005176Abstract: Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.Type: ApplicationFiled: August 26, 2013Publication date: January 2, 2014Applicant: AXIKIN PHARMACEUTICALS, INC.Inventors: Yingfu Li, Kevin Bacon, Hiromi Sugimoto, Keiko Fukushima, Kentaro Hashimoto, Makiko Marumo, Toshiya Moriwaki, Noriko Nunami, Naoki Tsuno, Klaus Urbahns, Nagahiro Yoshida
-
Publication number: 20130345237Abstract: The compounds of the invention are antagonists of MDM2 and MDMX, with excellent specificity for MDM2 and MDMX over other proteins, and with selective binding affinity to MDMX over MDM2. The compounds can therefore regulate p53 activity and treat a variety of cancers. 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: September 30, 2011Publication date: December 26, 2013Inventors: R. Kiplin Guy, Yiqun Zhang, Brandon Young, Michael Dyer, Kristin Finch, Donald Bashford, Nagakumar Bharatham, Richard Kriwacki, Grace Royappa, Lie Min, Jaeki Min, Anthony Ferreira
-
Publication number: 20130330421Abstract: The present disclosure relates to the field of oncology, more particularly to the field of melanoma. Provided are methods of treating melanoma, particularly advanced cutaneous melanoma, with a combination of pharmaceutical agents comprising MDM4-specific antagonists (such as an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and PI3K-AKT, B-RAF and MEK inhibitors. Further provided are pharmaceutical formulations of MDM4-specific antagonists (be it an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e.Type: ApplicationFiled: November 29, 2012Publication date: December 12, 2013Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D, VIB VZWInventor: Jean-Christophe Marine
-
Publication number: 20130331398Abstract: The instant invention is based, at least in part, on a newly-identified proteasome-independent signaling function of ubiquitinated PSD-95. Mdm2 inhibitors, Mdm4 inhibitors, PSD-95 inhibitors, and/or enantiomers and/or derivatives thereof de-crease endocytosis via preventing PSD-95 ubiquitination, and thereby increase AMPAR, NMDAR, D1 dopamine receptor surface expression in response to a given stimulus (e.g., NMDA, A?). Accordingly, the invention provides methods for modulating AM-PARS, NMDARs, or D1 dopamine receptors in a neuronal cell by contacting the neuronal cell with an Mdm2 and/or Mdm4 inhibitor or PSD-95 inhibitor and/or enantiomers and/or derivatives thereof. Mdm2 and/or Mdm4 inhibitors decrease the enzymatic activity of the respective proteins, and/or interactions with their respective substrates. Mdm2 and Mdm4 inhibitors and/or PSD-95 inhibitors of the invention are contemplated for use in the treatment of neurological disorders, neurodevelopmental disorders, and psychiatric disorders.Type: ApplicationFiled: November 14, 2011Publication date: December 12, 2013Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Maria Morabito, Michael Bianchetta
-
Patent number: 8604022Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: GrantFiled: January 26, 2012Date of Patent: December 10, 2013Assignee: AstraZeneca ABInventors: Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas, David Buttar
-
Publication number: 20130324553Abstract: The present invention provides compounds of formula (I): wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.Type: ApplicationFiled: February 8, 2012Publication date: December 5, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cederbaum, Guillaume Berthon
-
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
-
Publication number: 20130317042Abstract: An agent for treating ischemia/reperfusion injury, including a therapeutically effective amount of a p53 agonist compound including a cis-imidazoline structure.Type: ApplicationFiled: January 27, 2012Publication date: November 28, 2013Applicant: TOKYO UNIVERSITY OF SCIENCE FOUNDATIONInventors: Yoshikazu Higami, Naoyuki Okita, Shingo Matsushima
-
Publication number: 20130303493Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: July 12, 2013Publication date: November 14, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
-
Publication number: 20130303492Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: November 14, 2013Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
-
Publication number: 20130303505Abstract: TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.Type: ApplicationFiled: August 11, 2010Publication date: November 14, 2013Inventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt
-
Publication number: 20130295048Abstract: The invention provides crystalline solid forms of (((S)-1-{(S)-2-[4-(4?-{[6-((2R,5S)-2,5-dimethyl-4-methylcarbamoyl-piperazin-1-yl)-pyridine-3-carbonyl]-amino}-2?-trifluoromethoxy-biphenyl-4-yl)-1H-imidazol-2-yl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat hepatitis C virus infection, and processes useful for preparing such crystalline solid forms.Type: ApplicationFiled: April 25, 2013Publication date: November 7, 2013Inventors: Venkat R. Thalladi, Jerry Nzerem, Xiaojun Huang, Weijiang Zhang
-
Publication number: 20130296326Abstract: This disclosure provides tyrosine kinase protein and nucleic acid variants, particularly FGFR2 variants, which are linked to drug resistance. The disclosure further provides methods of diagnosis and theranosis, using these molecules and fragments thereof, and kits for employing these methods and compositions.Type: ApplicationFiled: May 7, 2013Publication date: November 7, 2013Applicant: TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventor: Pamela Michelle Pollock
-
Publication number: 20130289047Abstract: Heteroarylthio compounds covalently linked to an arylpiperazine moiety for the treatment of neurological conditions.Type: ApplicationFiled: October 14, 2011Publication date: October 31, 2013Applicant: EPIOMED THERAPEUTICS, INC.Inventors: David Helton, David Fick
-
Publication number: 20130281388Abstract: The invention relates a composition comprising an opioid agonist and Compound-1:Type: ApplicationFiled: December 17, 2012Publication date: October 24, 2013Inventor: Alkermes Pharma Ireland Limited
-
Publication number: 20130274227Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: October 17, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
-
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.
-
Patent number: 8551985Abstract: [Object] It is to provide a novel LXR? agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C?O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.Type: GrantFiled: April 28, 2010Date of Patent: October 8, 2013Assignee: Kowa Company, Ltd.Inventors: Minoru Koura, Hisashi Sumida, Takayuki Matsuda, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya, Sumiko Kurobuchi
-
Patent number: 8546374Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: GrantFiled: July 9, 2012Date of Patent: October 1, 2013Assignee: Abbvie Inc.Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
-
Publication number: 20130245039Abstract: Treatment of proliferative diseases with a combination of a b-Raf inhibitor and MDM2 inhibitor.Type: ApplicationFiled: February 5, 2013Publication date: September 19, 2013Applicant: Hoffmann-La Roche Inc.Inventors: Brian Higgins, Kenneth Kolinsky, Gwen Nichols, Kathryn Packman, Fei Su
-
Publication number: 20130237541Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.Type: ApplicationFiled: September 14, 2012Publication date: September 12, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter Ian Dosa
-
Publication number: 20130225603Abstract: Provided herein are pharmaceutical compositions for the treatment of various ocular diseases characterized by unwanted cellular proliferation. The pharmaceutical compositions may comprise one or more MDM2 inhibitors, and may further comprise one or more additional therapeutic agents. Also provided are methods of use of MDM2 inhibitors and/or formulations thereof for the treatment of ocular diseases characterized by unwanted cellular proliferation.Type: ApplicationFiled: September 26, 2011Publication date: August 29, 2013Applicant: SERRATA LLCInventors: Sai Chavala, Thomas Cramer Lee
-
Publication number: 20130224289Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.Type: ApplicationFiled: April 1, 2013Publication date: August 29, 2013Applicant: Depomed, Inc.Inventor: Depomed, Inc.
-
Publication number: 20130217687Abstract: 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: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei LY, Jared Andrew FORRESTER
-
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: 20130217700Abstract: Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: September 13, 2012Publication date: August 22, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Yifeng Xiong, Martin C. Cherrier, Jin Sun Karoline Choi, Peter I. Dosa, Brian M. Smith, Sonja Strah-Pleynet, Brett Ullman, Bradley Teegarden
-
Publication number: 20130203592Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: January 22, 2013Publication date: August 8, 2013Applicant: Dow AgroSciences LLCInventor: Dow AgroSciences LLC
-
Publication number: 20130203593Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: January 23, 2013Publication date: August 8, 2013Applicant: Dow AgroSciences LLCInventor: Dow AgroSciences LLC
-
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
-
Patent number: 8492384Abstract: Disclosed are novel imidazolylalkylcarbonyl derivatives useful as calcium channel modulators and a preparation method of the same. Also disclosed is a method for the treatment of diseases by administering the above compounds based on their inhibitory activity against calcium channel.Type: GrantFiled: June 26, 2009Date of Patent: July 23, 2013Assignee: Korea Institute of Science and TechnologyInventors: Kyung Il Choi, Ghilsoo Nam, Hye Ran Kim, Hyewhon Rhim, Seon Hee Seo, Yoon Jee Kim, Hee Sup Shin, Dong Jin Kim, Ae Nim Pae, Hye Jin Chung, Yong Seo Cho, Hyunah Choo, Eun Joo Roh, Soon Bang Kang, Kye Jung Shin, Hoh Gyu Hahn, Dong Yun Shin, Chan Seong Cheong, Kee Dal Nam, Yong Koo Kang, Jae Kyun Lee, Woong Seo Park, Youngsoo Kim, Eunice Eun-Kyeong Kim, Key-Sun Kim, Hesson Chung, Gyo Chang Keum, Cheolju Lee, Kee Hyun Choi
-
Publication number: 20130184248Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: January 11, 2013Publication date: July 18, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF
-
Publication number: 20130177529Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: ApplicationFiled: November 15, 2012Publication date: July 11, 2013Inventors: Youhong Hu, Bin Xu, Yun Liao, Kenneth Nawoschik, Yixin Liu, Anthony Sandrasagra, Reza Fathi, Zhen Yang
-
Patent number: 8481535Abstract: The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.Type: GrantFiled: May 17, 2007Date of Patent: July 9, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Tawfik Gharbaoui, Dipanjan Sengupta, Ashwin M. Krishnan, Nainesh Shah, Ryan M. Hart, Mark Macias, Edward A. Lally, Jonathan Duffield
-
Publication number: 20130172352Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38?, and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.Type: ApplicationFiled: February 25, 2013Publication date: July 4, 2013Applicant: NOVARTIS AGInventor: Novartis AG
-
Publication number: 20130171268Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.Type: ApplicationFiled: June 5, 2012Publication date: July 4, 2013Inventors: Francisco Villarreal, Alan Maisel, George Schreiner, Guillermo M. Ceballos Reyes, Pam Taub
-
Patent number: 8470829Abstract: An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted C1-4 alkyl group; E is independently selected from a C1-6 alkyl group; R2 and R3 are independently selected from C1-6 alkyls; X1 and X2 are independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is —CON(—Ra)—, —CO—, —OOO—, —NRa—C(?NH)NRb—, —NRa—C(?N—CN)NRb—, —N(—Ra)COO—, —C(?NH)—, —SO2—, —SO2N(—Ra)—, —SO2NR1—, —N(—Ra)CO—, —N(—Ra)CON(—Rb)—, —N(COR1)CO—, —N(—Ra)SO2—, —N(SO2R1)SO2—, —N(—Ra)— or —N(—Ra)SO2N(—Rb)—; R1 is independently a hydrogen atom, a hydroxyl group, or substituted or unsubstituted group selected from C1-6 alkyl group, heterocyclic group, aryl group, C3-8 cycloalkyl group and C3-8 cycloalkenyl group; or salt or prodrug thereof.Type: GrantFiled: September 9, 2005Date of Patent: June 25, 2013Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Hitoshi Yoshino, Takashi Emura, Akie Honma, Etsuro Onuma, Hiromitsu Kawata, Kenji Taniguchi
-
Publication number: 20130158029Abstract: The invention refers to compounds of general formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: May 26, 2011Publication date: June 20, 2013Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia López, Antoni Torrens Jover, José Luis Diaz Fernández, Ana Maria Caamaño Moure
-
Publication number: 20130158018Abstract: 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: ApplicationFiled: March 2, 2011Publication date: June 20, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: 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: 20130158011Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 10, 2012Publication date: June 20, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
-
Publication number: 20130150325Abstract: The present application relates to novel 3-(fluorovinyl)pyrazole derivatives, to processes for their preparation, to their use for treatment and/or prevention of diseases and to 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: July 17, 2012Publication date: June 13, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael HÄRTER, Hartmut BECK, Karl-Heinz THIERAUCH, Peter ELLINGHAUS, Susanne GRESCHAT, Joachim SCHUHMACHER