Carbocyclic Ring Containing Patents (Class 544/321)
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Publication number: 20130079518Abstract: The present invention relates to a method of making pyrimidines of formula (III) wherein X1, X2, R1 and R2 have the meanings as defined herein.Type: ApplicationFiled: November 16, 2012Publication date: March 28, 2013Inventors: Guenter LINZ, Gerd KRAEMER, Adil DURAN
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Patent number: 8394809Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.Type: GrantFiled: October 28, 2010Date of Patent: March 12, 2013Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A. Miskowski, Scott L. Dax, Henry Breslin, Bart L. De Corte, Wei He
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Publication number: 20130053343Abstract: Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.Type: ApplicationFiled: November 2, 2010Publication date: February 28, 2013Applicant: The Trustees of Columbia University in th City ofInventors: Donald Landry, Shi-Xian Deng
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Publication number: 20130035485Abstract: In one embodiment the present invention encompasses 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile (“ETHER”), 4-(4,6-dichloropyrimidin-2-yloxy)-3,5-dimethyl-benzonitrile (“ETHER C-2 isomer”), mixtures and salts thereof of. The present invention encompasses the use of ETHER and salts thereof to prepare Etravirine and Etravirine intermediates, and salts thereof. In another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare debrometravirine (“DEBETV”) and salts thereof. In yet another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare 4-(6-chloro-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethyl-benzonitrile (“ARCPBN”) and salts thereof.Type: ApplicationFiled: March 2, 2012Publication date: February 7, 2013Inventors: Irena KRIZMANIC, Jasna Dogan, Marina Marinkovic, Maja Sepelj
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Publication number: 20130029990Abstract: There are provided inter alia compounds of formula (I): wherein R1, R2a, R2b, R3, R4, L, X, R5 and R6 are as defined in the description for use in the treatment of inflammatory diseases.Type: ApplicationFiled: April 1, 2011Publication date: January 31, 2013Inventors: John King-Underwood, George Hardy, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
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Patent number: 8362236Abstract: The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.Type: GrantFiled: February 29, 2008Date of Patent: January 29, 2013Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Nobuo Shimma, Takuo Tsukuda, Hiroshi Koyano, Atsushi Suda, Tadakatsu Hayase, Kihito Hada, Ken-Ichi Kawasaki, Susumu Komiyama, Naomi Ono, Toshikazu Yamazaki, Ryoichi Saitoh, Masami Kohchi, Kiyoshi Hasegawa
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Publication number: 20130018053Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: April 18, 2011Publication date: January 17, 2013Inventors: Changyou Zhou, Wuxin Zou, Yuxia Hua, Qun Dang
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Publication number: 20130017162Abstract: The invention relates to a cosmetic composition, especially a hair composition, and to a method for the cosmetic treatment of keratin materials, especially of the hair, employing compounds of formula: in which Z represents (i) a hydrogen atom, (ii) a linear or branched C1 to C32 (saturated) alkyl radical; (iii) a linear or branched C2 to C32 (unsaturated) alkene radical, comprising one or two C?C double bonds; (iv) an aryl-substituted alkyl radical; said radicals being optionally substituted and/or interrupted.Type: ApplicationFiled: January 4, 2011Publication date: January 17, 2013Applicant: L'OREALInventors: Anne-Claude Dublanchet, Christian Blaise, Abel Messavussu
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Publication number: 20120315230Abstract: The invention relates to a cosmetic composition comprising, in a cosmetically acceptable medium, a compound that can be obtained by reaction between an OH-functionalized or COOH-functionalized wax and a junction group capable of establishing hydrogen bonds with one or more partner junction groups, said junction group comprising at least one unit of formula (I) or (II): The invention also relates to a cosmetic treatment process using said compounds.Type: ApplicationFiled: December 13, 2010Publication date: December 13, 2012Applicant: L'OREALInventors: Sandrine Chodorowski-Kimmes, Nathalie Jager Lezer
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Patent number: 8324230Abstract: Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms.Type: GrantFiled: October 3, 2005Date of Patent: December 4, 2012Assignee: Pfizer Inc.Inventor: Jon G. Selbo
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Publication number: 20120277192Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: December 15, 2010Publication date: November 1, 2012Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Publication number: 20120270889Abstract: Compound of Formula A and pharmaceutically acceptable salts thereof and crystalline Forms I and II of Compound of Formula A! Also, methods for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for their uses.Type: ApplicationFiled: November 23, 2010Publication date: October 25, 2012Inventors: Wei-Guo Su, Weihan Zhang, Hong Jia, Yumin Cui, Yongxin Ren, Yang Sai, Zhenping Wu, Wenji Li, Jiangyong Shao, Zhenping Tian
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Patent number: 8293769Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.Type: GrantFiled: May 20, 2008Date of Patent: October 23, 2012Assignee: Novartis AGInventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
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Publication number: 20120231017Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Applicants: Pharmacopeia Inc., Schering CorporationInventors: ZHAONING ZHU, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mozzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Sainoz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Patent number: 8242128Abstract: The invention relates to compounds of formula 1, the production and use thereof as a medicament for the treatment of diseases, particularly tumours and/or diseases caused, mediated or propagated by angiogenesis. The compounds of formula 1 are effective inhibitors of tyrosin kinases, particularly TIE-2 and VEGFR, and Raf-kinases.Type: GrantFiled: September 1, 2004Date of Patent: August 14, 2012Assignee: Merck Patent GmbHInventors: Wolfgang Stähle, Alfred Jonczyk, Wilfried Rautenberg
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Publication number: 20120195881Abstract: In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula (a) have the general structure: (a) wherein each variable is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.Type: ApplicationFiled: October 6, 2010Publication date: August 2, 2012Applicant: Schering CorporationInventors: Ulrich Iserloh, Andrew W. Stamford, Jared N. Cumming
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Publication number: 20120190683Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: ApplicationFiled: July 22, 2011Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Publication number: 20120190684Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: ApplicationFiled: July 22, 2011Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Publication number: 20120178666Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.Type: ApplicationFiled: September 15, 2010Publication date: July 12, 2012Applicant: SHIRE LLCInventors: Richard Franklin, Robert G. Tyson, Bernard T. Golding, Rhys Whomsley
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Publication number: 20120157484Abstract: Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:Type: ApplicationFiled: November 7, 2011Publication date: June 21, 2012Inventors: Arokiasamy DEVASAGAYARAJ, Haihong Jin, Qingyun Liu, Brett Marinelli, Lakshama Samala, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Wenxue Wu, Chengmin Zhang, Haiming Zhang
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Publication number: 20120148603Abstract: In its many embodiments, the present invention provides provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-, L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.Type: ApplicationFiled: October 6, 2010Publication date: June 14, 2012Applicant: Schering CorporationInventors: Andrew W. Stamford, Jared N Cumming
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Publication number: 20120149722Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: October 31, 2011Publication date: June 14, 2012Applicant: AVILA THERAPEUTICS, INC.Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Juswinder Singh
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Patent number: 8193204Abstract: Solid forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed.Type: GrantFiled: September 25, 2008Date of Patent: June 5, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Mark S. Bednarz, Susan De Paul, Ramanaiah C. Kanamarlapudi, Anett Perlberg, Haiming Zhang
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Patent number: 8193351Abstract: Compounds represented by formula (1) shown below, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such compounds are provided.Type: GrantFiled: May 25, 2007Date of Patent: June 5, 2012Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Takuo Tsukuda, Ken-Ichi Kawasaki, Susumu Komiyama, Yoshiaki Isshiki, Yasuhiko Shiratori, Kiyoshi Hasegawa, Takaaki Fukami, Takaaki Miura, Naomi Ono, Toshikazu Yamazaki, Young-Jun Na, Dong-Oh Yoon, Sung-Jin Kim
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Publication number: 20120129856Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.Type: ApplicationFiled: October 18, 2011Publication date: May 24, 2012Applicant: Cerenis Therapeutics SAInventors: Daniela Carmen Oniciu, Jean-Louis Henri Dasseux, Ronald Barbaras, Valery Kochubey, Dmitry Kovalsky, Oleg Gennadievich Rodin, Otto Geoffroy, Anna Rzepiela
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Patent number: 8183252Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: January 26, 2010Date of Patent: May 22, 2012Assignees: Schering Corporation, Pharmacopeia Inc.Inventors: Zhaoning Zhu, Zhong-Yue Sun, Andrew Stamford, William J. Greenlee, Jared N. Cumming, Lingyan Wang, Ulrich Iserloh, Xiaoxiang Liu, Ying Huang, Guoqing Li, Jianping Pan
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Publication number: 20120122902Abstract: A pyrimidine derivative and the preparation method and usethereof. The said pyrimidine derivative is a diaryl pyrimidine derivative or a diaryl benzo pyrimidine derivative which has the structure shown as the Formula I and IV. Present pyrimidine derivative can be used for the prevention or the treatment of HIV.Type: ApplicationFiled: December 24, 2009Publication date: May 17, 2012Applicant: FUDAN UNIVERSITYInventors: Fener Chen, Yonghong Liang, Zhaosen Zeng
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Publication number: 20120122819Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.Type: ApplicationFiled: June 14, 2010Publication date: May 17, 2012Applicant: SOCPRA - SCIENCES ET GENIE S.E.C.Inventors: Jérôme Mulhbacher, Daniel Lafontaine, François Malouin, Marianne Allard, Eric Marsault
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Publication number: 20120122904Abstract: Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed. Pharmaceutical dosage forms and methods of their use are also disclosed.Type: ApplicationFiled: November 3, 2011Publication date: May 17, 2012Inventors: Qun LI, Weifeng HU, Xiaogen YANG, Jiangqiong ZHAO, Matthew Mangzhu ZHAO
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Publication number: 20120122857Abstract: The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Applicant: NOVARTIS AGInventors: Guido BOLD, Andrea VAUPEL, Carole Pissot SOLDERMANN, Paul W. MANLEY
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Publication number: 20120108609Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.Type: ApplicationFiled: October 24, 2011Publication date: May 3, 2012Inventors: Matthias Nettekoven, Roger Norcross, Alessandra Polara
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Patent number: 8153790Abstract: In one embodiment the present invention encompasses 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile (“ETHER”), 4-(4,6-dichloropyrimidin-2-yloxy)-3,5-dimethyl-benzonitrile (“ETHER C-2 isomer”), mixtures and salts thereof of. The present invention encompasses the use of ETHER and salts thereof to prepare Etravirine and Etravirine intermediates, and salts thereof. In another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare debrometravirine (“DEBETV”) and salts thereof. In yet another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare 4-(6-chloro-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethyl-benzonitrile (“ARCPBN”) and salts thereof. The compound, 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile “ETHER” of formula (A) wherein n is either 0 or 1 and HA is an acid.Type: GrantFiled: July 27, 2010Date of Patent: April 10, 2012Inventors: Irena Krizmanić, Jasna Dogan, Marina Marinković, Maja {hacek over (S)}epelj
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Publication number: 20120083606Abstract: This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.Type: ApplicationFiled: December 14, 2011Publication date: April 5, 2012Inventors: DIDIER PHILIPPE ROBERT SCHILS, ALFRED ELISABETH STAPPERS
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Publication number: 20120076835Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 30, 2011Publication date: March 29, 2012Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts
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Publication number: 20120058985Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.Type: ApplicationFiled: April 29, 2011Publication date: March 8, 2012Applicant: DECIPHERA PHARMACEUTICALS, LLCInventors: DANIEL L. FLYNN, MICHAEL D. KAUFMAN
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Publication number: 20120059014Abstract: The present invention is directed to therapeutic compounds of the following formula (I) which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.Type: ApplicationFiled: March 12, 2010Publication date: March 8, 2012Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Tom Banksia Dupree, Peter Timothy Fry, Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Karen Lesley Schofield, Donald Smyth, Thomas Staroske, Alan John William Stewart, David French Stonehouse, Simon Andrew Swain, David Matthew Withall
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Patent number: 8119801Abstract: HIV replication inhibitors of formula pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: January 20, 2010Date of Patent: February 21, 2012Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Herman Augustinus De Kock, Piet Tom Bert Paul Wigerinck
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Publication number: 20120040968Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.Type: ApplicationFiled: May 6, 2010Publication date: February 16, 2012Applicant: Waters Technologies CorporationInventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
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Publication number: 20120035190Abstract: Disclosed is a kind of E-type phenyl acrylic ester compound containing substituted anilino pyrimidine group, which is shown by general structure formula I, wherein each substituent is defined as that in the description. The compounds of general formula I show high insecticidal and acaricidal activities to adults and nymphs of harmful insects and mites in agricultural, civil and zoic technical fields, especially to Tetranychus cinnabarinus, Tetranychidae, and the like. The said compounds show more excellent performance on inhibiting the incubation of eggs of harmful mites. The uses of the said compounds as insecticides and/or acaricides in agricultural and other fields also are disclosed.Type: ApplicationFiled: June 3, 2010Publication date: February 9, 2012Inventors: Changling Liu, Huichao Li, Hong Zhang, Baoshan Chai, Yanmei Luo, Xiaomin He, Guang Huang, Shaowu Liu, Baoxiang Sun
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Publication number: 20120035195Abstract: This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.Type: ApplicationFiled: August 3, 2011Publication date: February 9, 2012Inventors: David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Benoit Hornsperger, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
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Publication number: 20120029192Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: ApplicationFiled: October 7, 2011Publication date: February 2, 2012Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Publication number: 20120028998Abstract: Etravirine (TMC125) nicotinamide co-crystal, its preparation, and use in the treatment of HIV infection.Type: ApplicationFiled: March 26, 2010Publication date: February 2, 2012Inventors: Matthew F. Sansone, Lieven Elvire Colette Baert, Mark Tawa, Julius F. Remenar
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Patent number: 8101752Abstract: This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.Type: GrantFiled: May 24, 2006Date of Patent: January 24, 2012Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Didier Philippe Robert Schils, Alfred Elisabeth Stappers
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Publication number: 20110319615Abstract: Pyrimidinyl aryl hydrazones are effective at controlling insects.Type: ApplicationFiled: September 8, 2011Publication date: December 29, 2011Applicant: DOW AGROSCIENCES LLCInventors: Katherine A. Guenthenspberger, Timothy C. Johnson, Noormohamed M. Niyaz, Ricky Hunter, Annette V. Brown, Tony K. Trullinger
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Publication number: 20110312963Abstract: The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPDType: ApplicationFiled: December 11, 2009Publication date: December 22, 2011Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Kevin Joly, Catherine Elisabeth Charron
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Publication number: 20110312880Abstract: The present invention relates to compounds, in particular, dual antagonists comprising a nucleoside reverse transcriptase inhibitor (NRTI) or a nucleoside competititive reverse transcriptase inhibitor and a non-nucleoside reverse transcriptase inhibitor (NNRTI), linked together using a chemical linker, which may be used to inhibit HIV (HIV-1) reverse transcriptase and in the treatment of HIV infections, more severe cases of HIV infections, including ARC and AIDS, including reducing the likelihood of these infections and disease states.Type: ApplicationFiled: April 9, 2009Publication date: December 22, 2011Inventors: Karen S. Anderson, Roger Hunter
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Patent number: 8080551Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.Type: GrantFiled: June 26, 2006Date of Patent: December 20, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
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Patent number: 8080659Abstract: The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors or for the treatment of viral infections. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis, or for reducing entry of HIV in to a cell while not reducing the capacity of the stem cells to proliferate. The compounds may be useful for long term treatment regimes.Type: GrantFiled: July 11, 2007Date of Patent: December 20, 2011Assignee: Emory UniversityInventors: Dennis C. Liotta, James P. Snyder, Weiqiang Zhan
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Publication number: 20110294837Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-6, L1, R1, R4-6 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: August 7, 2009Publication date: December 1, 2011Inventors: Holly L. Deak, Brian L. Hodous, Jason B. Human, Hanh Nho Nguyen, Karina Romero