Plural Nitrogens In The Additional Five-membered Hetero Ring Patents (Class 514/254.05)
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Publication number: 20140371237Abstract: Provided are novel methods and compositions for the diagnosis, prognosis and treatment of leiomyomas, in particular uterine leiomyoma (UL). In addition, methods of identifying anti-tumor agents are described. Furthermore, novel methods and compositions are provided for the treatment of diseases characterized by an aberrant growth of mesenchymal stem cells and their descendants and for the treatment of obesity are disclosed.Type: ApplicationFiled: August 6, 2014Publication date: December 18, 2014Inventors: Jörn Bullerdiek, Dominique N. Markowski
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Publication number: 20140371213Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: May 19, 2014Publication date: December 18, 2014Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Patent number: 8912195Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts thereof, wherein A is selected from the group (II), are useful as HIV attachment inhibitors.Type: GrantFiled: December 1, 2011Date of Patent: December 16, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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Publication number: 20140348787Abstract: Compositions and methods for treating ear infections are disclosed. More specifically, these methods may refer to treatment of internal otitis using an otic composition, such as otic gel for animals and humans. Poloxamer otic gel may be in liquid state at room temperature and may change to gel at about temperature (64° F.) as poloxamer otic gel reaches body temperature, because of the thermo-reversible properties. Consequently, poloxamer otic gel may be an effective treatment in animals and humans, where poloxamer otic gel may reach otitis affected site and remain there for a longer period of time. Additionally, poloxamer otic gel may include APIs such as antifungals, antibiotics and corticosteroids, among others. Furthermore, poloxamer otic gel may be instilled inside the ear, employing calibrated delivery device into the vertical ear canal in order to reach the horizontal ear canal, without puncturing the tympanic membrane.Type: ApplicationFiled: May 22, 2013Publication date: November 27, 2014Applicant: PROFESSIONAL COMPOUNDING CENTERS OF AMERICAInventor: Chris V. Simmons
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Publication number: 20140350012Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-Type: ApplicationFiled: August 11, 2014Publication date: November 27, 2014Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Maria Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
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Patent number: 8889677Abstract: 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: GrantFiled: January 11, 2013Date of Patent: November 18, 2014Assignee: Boehringer Ingellheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Patent number: 8889665Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R3 and L are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: GrantFiled: July 1, 2008Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Steffen Steurer, Irene Waizenegger
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Publication number: 20140336202Abstract: Methods of treating subjects with cancer and screening for MDM2 inhibitors that may be effective cancer therapeutics are provided herein. The cancers that may be treated using MDM2 inhibitors using the methods described herein include those that are or may become resistant to treatment with tyrosine kinase inhibitors. Methods of treating subjects with cancers that have, or develop in response to treatment with tyrosine kinase inhibitors, elevated levels of MDM2, Mcl-1 or PP5 or decreased levels of Huwe1 or CAS using MDM2 inhibitors are provided herein. The MDM2 inhibitors may be effective at treating these cancers alone or in combination with a tyrosine kinase inhibitor regardless of p53 status (mutant or wild-type) of the cancer.Type: ApplicationFiled: December 7, 2012Publication date: November 13, 2014Applicant: DUKE UNIVERSITYInventors: Sally Kornbluth, Manabu Kurokawa, Neil Spector, Mark Dewhirst
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Patent number: 8883135Abstract: 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: GrantFiled: April 25, 2013Date of Patent: November 11, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Venkat R. Thalladi, Jerry Nzerem, Xiaojun Huang, Weijiang Zhang
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Patent number: 8883789Abstract: 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. R1, R2, R3, R4, Q have meanings given in the description.Type: GrantFiled: December 10, 2012Date of Patent: November 11, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Annekatrin Heimann, Georg Dahmann, Marc Grundl, Stephan Georg Mueller, Bernd Wellenzohn
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Publication number: 20140328893Abstract: The present invention relates to uses, methods and compositions for the treatment of pulmonary hypertension.Type: ApplicationFiled: October 11, 2011Publication date: November 6, 2014Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventor: Serge Adnot
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Publication number: 20140329812Abstract: The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity 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 composition containing such compounds.Type: ApplicationFiled: December 13, 2011Publication date: November 6, 2014Applicant: SIGMA-TAU RESEARCH SWITZERLAND S.A.Inventors: Giuseppe Giannini, Walter Cabri, Loredana Vesci, Maria Luisa Cervoni, Claudio Pisano, Maurizio Taddei, Serena Ferrini
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Publication number: 20140329815Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Patent number: 8865714Abstract: This invention relates to a piperazine compound represented by Formula (I), wherein R1 is C1-6 alkyl; R2 is hydroxy, C1-6 alkyl that may have one or more substituents, —(C?O)—N(R3)(R4), or —(C?O)—OR5; R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or C1-6 alkyl that may have one or more substituents; and n is 1 or 2; or a salt thereof.Type: GrantFiled: March 8, 2010Date of Patent: October 21, 2014Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Yoshihiro Urade, Makoto Kitade, Kazuhiko Shigeno, Keiko Yamane, Katsunao Tanaka
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Publication number: 20140309185Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
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Publication number: 20140309181Abstract: Small compounds that modulate the expression of and/or function of sodium channel, voltage-gated, alpha subunit (SCNxA) are presented. Pharmaceutical compositions containing such small molecules and their use in treating diseases and disorders associated with the expression of SCNxA are also presented.Type: ApplicationFiled: August 28, 2012Publication date: October 16, 2014Applicant: CuRNA, Inc.Inventors: Joseph Collard, Olga Khorkova Sherman, Jane H. Hsiao
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Patent number: 8846682Abstract: The present invention relates to a compound of formula (I): Wherein R1 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; R2 is an alkyl group with 1 to 18 carbon atoms or a substituted or unsubstituted cycloalkyl or aryl group; R3 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; L is a single bond, an alkyl group having 1 to 6 carbon atoms, NHCO, O, S, NHCONH or NHCOO; X, Y and Z are independently O, N, NH, S or CH; W is a single bond or an alkyl group having from 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of said compound or salt.Type: GrantFiled: December 16, 2010Date of Patent: September 30, 2014Assignee: Neuropore Therapies, Inc.Inventors: Eliezer Masliah, Edward M. Rockenstein, Wolfgang Wrasidlo, Igor Flint Tsigelny
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Patent number: 8846746Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.Type: GrantFiled: August 30, 2012Date of Patent: September 30, 2014Assignee: Japan Tobacco Inc.Inventors: Tomoya Miura, Yosuke Ogoshi, Kazuhito Ueyama, Dai Motoda, Toshihiko Iwayama, Koichi Suzawa, Hironobu Nagamori, Hiroshi Ueno, Akihiko Takahashi, Kazuyuki Sugimoto
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Publication number: 20140271662Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ? with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: February 14, 2014Publication date: September 18, 2014Applicants: Astex Therapeutics Ltd, Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer HospitalInventors: Valerio BERDINI, Gordon SAXTY, Marinus Leendert VERDONK, Steven John WOODHEAD, Paul Graham WYATT, Robert George BOYLE, Hannah Fiona SORE, David Winter WALKER, Ian COLLINS, Robert DOWNHAM, Robin Arthur Ellis CARR
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Publication number: 20140275049Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds.Type: ApplicationFiled: October 19, 2012Publication date: September 18, 2014Inventors: Thomas John Bleisch, David Andrew Coates, Norman Earle Hughes, Scott Alan Jones, Bryan Hurst Norman
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Publication number: 20140275076Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Katsunori Tsuboi, Yosuke Takanashi, Shingo Tojo, Tomohiro Kodama, Katsumi Kubota, Toshio Kanai
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Patent number: 8835436Abstract: A novel arylpiperazine-containing imidazole 4-carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a depressive disorder are provided.Type: GrantFiled: July 9, 2010Date of Patent: September 16, 2014Assignee: Green Cross CorporationInventors: Jinhwa Lee, Hee Jeong Seo, Suk Youn Kang, Eun-Jung Park, Min Ju Kim, Suk Ho Lee, Jong Yup Kim, Jeongmin Kim, Myung Eun Jung, Hyun Jung Kim, Mi-soon Kim, Ho Kyun Han, Kwang Woo Ahn, Min Woo Lee, Ki-Nam Lee, Ae Nim Pae, Woo-Kyu Park
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Publication number: 20140255517Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.Type: ApplicationFiled: March 5, 2014Publication date: September 11, 2014Applicant: EMORY UNIVERSITYInventors: Kerry J. Ressler, Paul J. Marvar
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Patent number: 8822464Abstract: 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: GrantFiled: November 26, 2012Date of Patent: September 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Publication number: 20140243338Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Inventors: Mimi L. Quan, Zilun Hu, Cailan Wang
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Publication number: 20140243309Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 28, 2014Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
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Patent number: 8816070Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: December 11, 2007Date of Patent: August 26, 2014Assignee: Merck Patent GmbHInventors: Hans Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
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Publication number: 20140235622Abstract: The present invention pertains to certain compounds of Formula (Ia) 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 treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: January 28, 2014Publication date: August 21, 2014Applicant: Arena Pharmaceuticals, Inc.Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
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Patent number: 8809338Abstract: The present invention refers to the field of chemical compounds bearing a 1,2,3-triazole ring of formula (I) and possessing guanidino and carboxylic groups or their isosteres, their preparation by Cu-catalyzed “click-chemistry”, and medical-diagnostic use in pathologies where angiogenesis is altered, for example pathologic conditions of tumor origin, tumor metastasis, osteoporosis, and rheumatoid arthritis.Type: GrantFiled: February 14, 2011Date of Patent: August 19, 2014Assignee: Universita' Degli Studi di FirenzeInventors: Antonio Guarna, Gloria Menchi, Nicoletta Cini, Andrea Trabocchi, Alberto Pupi, Anna Bottoncetti, Silvia Raspanti, Lido Calorini
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Publication number: 20140228351Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: March 14, 2014Publication date: August 14, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20140227340Abstract: The present invention relates generally to the field of electrospun fibers. In particular, the present invention relates to core-sheath fibers and related electrospinning methods. The fibers of the invention comprise poorly water soluble drugs and/or proteins.Type: ApplicationFiled: March 14, 2014Publication date: August 14, 2014Inventors: Toby Freyman, Quynh Pham, Robert F. Mulligan, Abby N. Picard, Xuri Yan
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Publication number: 20140206668Abstract: 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: March 25, 2014Publication date: July 24, 2014Applicant: Dow AgroSciences LLCInventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
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Publication number: 20140194422Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.Type: ApplicationFiled: June 12, 2012Publication date: July 10, 2014Applicant: EMORY UNIVERSITYInventors: Thota Ganesh, Aiming Sun, Susane M. Smith, John David Lambeth
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Publication number: 20140187556Abstract: Anti-amyloid compounds are provided along with methods of use thereof.Type: ApplicationFiled: March 2, 2012Publication date: July 3, 2014Applicant: Treventis CorporationInventors: Mark A. Reed, Arun Yadav, Scott C. Banfield, Christopher J. Barden
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Publication number: 20140178503Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: February 26, 2014Publication date: June 26, 2014Applicant: Auspex Pharmaceuticals, Inc.Inventors: Ronald C. Newbold, Chengzhi Zhang
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Publication number: 20140179699Abstract: The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications. The compounds of this invention have formula I-A: wherein the variables are as defined herein.Type: ApplicationFiled: November 19, 2013Publication date: June 26, 2014Inventors: Dean Boyall, Christopher Davis, James Dodd, Simon Everitt, Andrew Miller, Peter Weber, James Westcott, Stephen Young
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Publication number: 20140179712Abstract: There are provided pharmaceutical compositions comprising a compound of Formula (I) as defined herein and an amount of an alkaline effervescent agent that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.Type: ApplicationFiled: December 17, 2013Publication date: June 26, 2014Applicant: AstraZeneca ABInventors: Noel Alan Weldon BAKER, Alpesh MISTRY
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Patent number: 8759352Abstract: The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterType: GrantFiled: August 26, 2009Date of Patent: June 24, 2014Assignees: Merck Sharp & Dohme B.V., Pharmacopeia LLC.Inventors: Andrew John Cooke, David Jonathan Bennett, Andrew Stanley Edwards, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Koc-Kan Ho, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer
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Publication number: 20140171404Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
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Patent number: 8748432Abstract: 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: GrantFiled: February 8, 2012Date of Patent: June 10, 2014Assignee: Syngenta Participations AGInventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cederbaum, Guillaume Berthon
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Publication number: 20140148443Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.Type: ApplicationFiled: November 20, 2013Publication date: May 29, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Publication number: 20140142107Abstract: Antimicrobial agents, compositions that include the agent(s) and use(s) thereof are provided. Also disclosed are screening assays for identifying antimicrobial agents.Type: ApplicationFiled: September 4, 2013Publication date: May 22, 2014Applicant: University of MassachusettsInventors: Paul Kaufman, Jessica Lopes Da Rosa-Spiegler, Reeta Prusty Rao, Ahmed Fazly
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Publication number: 20140128394Abstract: This invention relates to a piperazine compound represented by Formula (I), wherein R1 is c1-6 alkyl; R2 is hydroxy, c1-6 alkyl that may have one or more substituents, —(C=0)-N(R2)(R4), or —(C=0)-0R5; R3 and R4 are the same or different, and each represents hydrogen or c1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or c1-6 alkyl that may have one or more 15 substituents; and n is 1 or 2; or a salt thereof.Type: ApplicationFiled: January 8, 2014Publication date: May 8, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Yoshihiro URADE, Makoto KITADE, Kazuhiko SHIGENO, Keiko YAMANE, Katsunao TANAKA
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Publication number: 20140128406Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: June 27, 2012Publication date: May 8, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
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Patent number: 8716277Abstract: 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: GrantFiled: December 10, 2012Date of Patent: May 6, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
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Publication number: 20140121218Abstract: It has now been found that the p53 pathway is inactivated in ocular cancers such as retinoblastoma. As such, the present invention is a method for inducing ocular cancer cell death using a p53 activator. In particular embodiments, the p53 activator blocks the interaction between DM2 or DMX and p53. As the p53 activator induces ocular cancer cell death, a method for preventing or treating ocular cancer is also provided.Type: ApplicationFiled: December 5, 2013Publication date: May 1, 2014Applicants: St. Jude Children's Research Hospital, Leiden University Medical Center, Universiteit Gent, Flanders Interuniversity Institute for Biotechnology VIBInventors: Michael A. Dyer, Jean-Christopher Marine, Aart Gerrit Jochemsen
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Publication number: 20140088029Abstract: Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.Type: ApplicationFiled: April 11, 2012Publication date: March 27, 2014Applicant: PHARMA EIGHT CO., LTD.Inventors: Hachiro Sugimoto, Michiaki Okuda, Takashi Takahashi, Ichiro Hijikuro, Hidetaka Suzuki, Shinichi Nakayama
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Publication number: 20140079667Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.Type: ApplicationFiled: August 23, 2013Publication date: March 20, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Adilah BAHADOOR, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20140073609Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.Type: ApplicationFiled: May 14, 2013Publication date: March 13, 2014Applicant: The Board of Trustees of the University of IllinoisInventors: Paul J. HERGENROTHER, Karson S. PUTT, Quinn P. PETERSON, Valerie FAKO
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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