Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/260.1)
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Patent number: 8211898Abstract: This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.Type: GrantFiled: July 16, 2009Date of Patent: July 3, 2012Assignee: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Zhi Hong, Stephanie Shaw, Yung-hyo Koh
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Patent number: 8211897Abstract: The present invention is directed to a method of using compounds of Formula (I) to inhibit Cathepsin B. Specifically the compounds of the present invention are useful as therapeutic agents for the treatment of tumor invasion, metastasis, Alzheimer's Disease, arthritis, inflammatory diseases such as chronic and acute pancreatitis, inflammatory airway disease, and bone and joint disorders, including osteoporosis, osteoarthritis, rheumatoid arthritis, psoriasis, and other autoimmune disorders, liver fibrosis, including liver fibrosis associated with HCV, all types of steatosis (including non-alcoholic steatohepatitis) and alcohol-associated steatohepatitis, non-alcoholic fatty liver disease, forms of pulmonary fibrosis including idiopathic pulmonary fibrosis, pathological diagnosis of interstitial pneumonia following lung biopsy, renal fibrosis, cardiac fibrosis, retinal angiogenesis and fibrosis/gliosis in the eye, schleroderma, and systemic sclerosis.Type: GrantFiled: February 5, 2009Date of Patent: July 3, 2012Assignee: ViroBay, Inc.Inventor: Leslie Holsinger
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Aryloxypropanolamines, methods of preparation therof and use of aryloxypropanolamines as medicaments
Patent number: 8207174Abstract: This invention relates to novel aryloxypropanolamines. The invention also relates to the pharmaceutically acceptable salts and solvates containing said compounds, methods for the preparation thereof and to respective synthetic intermediates. Said compounds have agonistic activity at ?3 adrenergic receptors and are useful for treatment of ailments influenced by activation of ?3 adrenergic receptors.Type: GrantFiled: January 22, 2008Date of Patent: June 26, 2012Assignee: 4SC AGInventors: Stefan Tasler, Daniel Vitt, Kristina Wolf, Andrea Aschenbrenner, Peter Ney -
Publication number: 20120157439Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: August 27, 2010Publication date: June 21, 2012Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Simon Mathieu, Rebecca Pulk, Joachim Rudolph, Zhaoyang Wen, Jonas Grina, Joshua D. Hansen, Ellen Laird, David Moreno, Li Ren, Steven Mark Wenglowsky
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Publication number: 20120157411Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: ApplicationFiled: December 15, 2011Publication date: June 21, 2012Applicant: Glenmark Pharmaceuticals, S.A.Inventors: Sukeerthi Kumar, Abraham Thomas, Sachin Sundarlal Chaudhari, Bipin Parsottam Kansagra, Venkata Ramana Yemireddy, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Girish Gudi
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Publication number: 20120157453Abstract: Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: August 27, 2010Publication date: June 21, 2012Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Steven Mark Wenglowsky
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Publication number: 20120149677Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: August 16, 2010Publication date: June 14, 2012Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
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Publication number: 20120142684Abstract: The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles.Type: ApplicationFiled: November 29, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Robert M. Burk, Wha Bin Im, Scott M. Whitcup
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Publication number: 20120136011Abstract: The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles.Type: ApplicationFiled: July 29, 2011Publication date: May 31, 2012Applicant: ALLERGAN, INC.Inventors: Guang L. Jiang, Wha-Bin Im, Frederick C. Beddingfield, Larry A. Wheeler, Scott M. Whitcup, Robert M. Burk
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Publication number: 20120128686Abstract: The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: ApplicationFiled: August 24, 2009Publication date: May 24, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Austen, Phillip Black, Wesley Blackaby, John Danilewicz, Ian Linney, Kay Schreiter, Martin Schneider
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Patent number: 8183246Abstract: The present application relates to novel, acyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: GrantFiled: December 8, 2006Date of Patent: May 22, 2012Assignee: Bayer Intellectual Property GmbHInventors: Thomas Lampe, Eva-Maria Becker, Raimund Kast, Hartmut Beck, Mario Jeske, Joachim Schuhmacher, Friederike Stoll, Martina Klein, Metin Akbaba, Andreas Knorr, Johannes-Peter Stasch, Lars Bärfacker, Alexander Hillisch, Gunter Karig, Mark Meininghaus, Karl-Heinz Schlemmer, Rudolf Schohe-Loop
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Publication number: 20120122889Abstract: 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 (I)-(I), (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: December 23, 2009Publication date: May 17, 2012Applicant: President and Fellows of Harvard CollegeInventors: Junying Yuan, Emily S. Hsu
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Publication number: 20120122890Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein G1, R2, R1a, R1b, X, X1, X2, X3, Rx, J, k, n, q, and t are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: November 2, 2011Publication date: May 17, 2012Applicant: ABBOTT LABORATORIESInventors: Arturo Perez-Medrano, Sridhar Peddi, David DeGoey
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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: 20120122891Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Applicant: NEUROCRINE BIOSCIENCES, INC.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Richard Lowe, Willy Moree, Nicole Smith, Warren Wade, Liren Zhao, Yun-Fei Zhu, Martin Rowbottom, Neil Ashweek
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Patent number: 8178555Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: June 23, 2009Date of Patent: May 15, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Stephen L. Gwaltney, Angie Vassar
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Publication number: 20120101095Abstract: Novel alkoxy-thienopyrimidine derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: May 27, 2010Publication date: April 26, 2012Inventors: Guenter Hoelzemann, Dieter Dorsch, Hartmut Greiner, Christiane Amendt, Frank Zenke
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Patent number: 8158634Abstract: The invention provides compounds having Formula Ia, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and Y are as defined in the specification; as well as pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: GrantFiled: October 26, 2005Date of Patent: April 17, 2012Assignee: IRM LLCInventors: Hong Liu, Xiaohui He, Ha-Soon Choi, Kunyong Yang, David Woodmansee, Zhicheng Wang, David Archer Ellis, Baogen Wu, Yun He, Truc Ngoc Nguyen
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Patent number: 8158785Abstract: There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.Type: GrantFiled: September 27, 2007Date of Patent: April 17, 2012Assignee: AstraZeneca ABInventors: Rolf Johansson, Sofia Karlstrom, Annika Kers, Gunnar Nordvall, Tobias Rein, Can Slivo
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Patent number: 8153639Abstract: Fused pyrimidines of formula (I): wherein A, n, R1, R2, and R3 have any of the values defined herein and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.Type: GrantFiled: May 4, 2007Date of Patent: April 10, 2012Assignee: F. Hoffman-La Roche AGInventors: Irina S. Chuckowree, Adrian J. Folkes, Paul Goldsmith, Timothy C. Hancox, Stephen J. Shuttleworth
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Patent number: 8148384Abstract: Compounds of formula I wherein A1, A2, and A3 are as defined herein are inhibitors of PIM kinase. The compounds of formula I are useful for the treatment of diseases such as cancer.Type: GrantFiled: December 6, 2007Date of Patent: April 3, 2012Assignee: Abbott LaboratoriesInventors: Thomas D. Penning, Lisa A. Hasvold, Laura A. Hexamer, Vincent L. Giranda, Nan-horng Lin, Zhi-Fu Tao, Le Wang
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Publication number: 20120077814Abstract: The disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions containing these compounds, and methods of using these compounds in a variety applications, such as treatment of diseases or disorders associated with E1 type activating enzymes, and with Nedd8 activating enzyme (NAE) in particular.Type: ApplicationFiled: September 12, 2011Publication date: March 29, 2012Inventors: Zhong Wang, Emilie D. Smith, James M. Veal, Kenneth H. Huang, Robert N. Atkinson, Rong Jiang
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Publication number: 20120077815Abstract: A series of amino-substituted fused pyridine and pyrazine derivatives, in particular amino-substituted quinoline and quinoxaline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: February 11, 2010Publication date: March 29, 2012Applicant: UCB PHARMA S.A.Inventors: Daniel Rees Allen, Julien Alistair Brown, Roland Burli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
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Patent number: 8143261Abstract: The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: April 29, 2009Date of Patent: March 27, 2012Assignee: AstraZeneca ABInventors: Paul Andrew Willis, Roger Bonnert, Simon Fraser Hunt, Iain Alistair Stewart Walters
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Publication number: 20120071486Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.Type: ApplicationFiled: September 23, 2011Publication date: March 22, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Nobuo Cho, Takashi Imada, Takenori Hitaka, Kazuhiro Miwa, Masami Kusaka, Nobuhiro Suzuki
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Patent number: 8138194Abstract: Fused bicyclic pyrimidine compounds of formula (I): wherein R1, R3, R4, X1, X2, Y, Z, A, B, C, D, n, and the two bonds are defined herein. Also disclosed are a method for inhibiting Aurora kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: April 22, 2009Date of Patent: March 20, 2012Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Su-Ying Wu, Yu-Sheng Chao
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Publication number: 20120065200Abstract: Compounds are disclosed for the treatment, management and prevention of diseases and disorders affecting the bone. Particular compounds are potent inhibitors of Notum Pectinacetylesterase, and are of the formula: wherein E, G, Y, Z, R1, R2, and R3 are defined herein.Type: ApplicationFiled: September 13, 2011Publication date: March 15, 2012Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Wei HE, Victoria LOMBARDO, Praveen PABBA, James TARVER, JR.
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Publication number: 20120065162Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: ApplicationFiled: November 17, 2011Publication date: March 15, 2012Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
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Patent number: 8129397Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and learning and memory disorders such as Alzheimer's disease.Type: GrantFiled: November 12, 2008Date of Patent: March 6, 2012Assignee: MSD Oss B.V.Inventors: Michael Gerard Gallagher, Craig C. Jamieson, Amanda Jane Lyons, John Kinnaird Ferguson Maclean, Elizabeth Margaret Moir
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Patent number: 8129371Abstract: The invention relates to thienopyrimidine and pyrazolopyrimidine compounds of the Formulas (Ia) and (IIa), or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein compositions comprising the compounds, and methods for making and using the compounds.Type: GrantFiled: October 15, 2008Date of Patent: March 6, 2012Assignee: Wyeth LLCInventors: Arie Zask, Joshua Aaron Kaplan, Jeroen Cunera Verheijen, Kevin J. Curran, David James Richard, Semiramis Ayral-Kaloustian
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Publication number: 20120046278Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.Type: ApplicationFiled: March 15, 2010Publication date: February 23, 2012Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&DInventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
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Publication number: 20120046267Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.Type: ApplicationFiled: February 11, 2011Publication date: February 23, 2012Inventors: Keith R. Hornberger, Dan M. Berger, Xin Chen, Andrew P. Crew, Hanqing Dong, Andrew Kleinberg, An-Hu Li, Lifu Ma, Mark J. Mulvihill, Bijoy Panicker, Kam W. Siu, Arno G. Steinig, James G. Tarrant, Jing Wang, Qinghua Weng, Rajaram Sangem, Ramesh C. Gupta
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Publication number: 20120040981Abstract: The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.Type: ApplicationFiled: March 4, 2010Publication date: February 16, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yuya Oguro, Osamu Kurasawa
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Patent number: 8114878Abstract: The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2 and R3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: GrantFiled: April 18, 2007Date of Patent: February 14, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Pascale Pouzet, Christoph Hoenke, Rolf Goeggel, Birgit Jung, Peter Nickolaus, Dennis Fiegen, Thomas Fox
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Publication number: 20120035191Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives and pharmaceutically acceptable salts and methods of use thereof for the prevention and treatment of cancer including brain cancer, breast cancer, blood cancer, colorectal cancer, lung cancer, liver cancer, ovarian cancer, pancreas cancer, prostate cancer, stomach cancer, testicular cancer, uterus cancer, intestinal cancer, skin cancer, and other forms of cancer; tumor progression, metastasis and fibrosis in the neuroendocrine neoplasia, fibrotic processes associated with neuroendocrine cell dysregulation for example Crohn's disease, pulmonary arterial hypertension, pulmonary hypertension associated with chronic obstructive pulmonary disease (COPD), right ventricular hypertrophy, pulmonary vascular remodeling, asthma, cystic fibrosis, hypertension, ischemic stroke, angina pectoris, congestive heart failure, arrhythmia, arterial fibrillation, neurodenerative diseases, Alzheimer's disease, dementiType: ApplicationFiled: September 14, 2011Publication date: February 9, 2012Inventor: Daljit Singh Dhanoa
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Publication number: 20120035143Abstract: The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (=non-steroidal anti-inflammatory drug) (2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma. The invention particularly relates to those drug combinations which contain, in addition to one or more, preferably one PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.Type: ApplicationFiled: February 18, 2010Publication date: February 9, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter Nickolaus, Rolf Goeggel, Daniel Peter
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Publication number: 20120015962Abstract: Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.Type: ApplicationFiled: July 12, 2011Publication date: January 19, 2012Inventors: Nidhi Arora, Shaoqing Chen, Johannes Cornelius Hermann, Adreas Kuglstatter, Sharada Shenvi Labadie, Clara Jeou Jen Lin, Matthew C. Lucas, Amy Geraldine Moore, Eva Papp, Francisco Xavier Talamas, Jutta Wanner, Yansheng Zhai
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Publication number: 20120010223Abstract: The present invention is related to novel isothiazolo[3,4-d]pyrimidinedione and isothiazolo[5,4-d]pyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: ApplicationFiled: March 22, 2010Publication date: January 12, 2012Applicant: Glenmark Pharmaceuticals, S.A.Inventors: Sukeerthi Kumar, Abraham Thomas, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
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Publication number: 20120004245Abstract: The use of certain urea compounds, for the treatment of retinal disorders associated with pathologic ocular angiogenesis and/or neovascularization is disclosed.Type: ApplicationFiled: June 24, 2011Publication date: January 5, 2012Applicant: ALCON RESEARCH, LTD.Inventors: Jesse A. MAY, David P. BINGAMAN, Carmelo ROMANO
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Patent number: 8088780Abstract: There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.Type: GrantFiled: April 3, 2006Date of Patent: January 3, 2012Assignee: AstraZeneca ABInventors: Gunnar Nordvall, Colin Ray, Tobias Rein, Daniel Sohn
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Publication number: 20110312908Abstract: The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: ApplicationFiled: November 28, 2008Publication date: December 22, 2011Applicants: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang, Amy Wojciechowski
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Publication number: 20110306616Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1 and Rx are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: June 15, 2011Publication date: December 15, 2011Applicant: ABBOTT LABORATORIESInventors: Michael J. Dart, Teodozyj Kolasa
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Publication number: 20110301128Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.Type: ApplicationFiled: August 22, 2011Publication date: December 8, 2011Applicant: EXELIXIS, INC.Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T. Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B. Mac, Larry W. Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C. Stevens, Tie-Lin Wang, Yong Wang, Jason H. Wu
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Publication number: 20110293745Abstract: The present invention provides Compound 1, solid forms thereof, compositions thereof, as Aurora kinase inhibitor for use as an oncology agent. The present invention also provides synthetic methods of preparing Compound 1 and intermediates thereto.Type: ApplicationFiled: March 16, 2009Publication date: December 1, 2011Applicant: SUNESIS PHARMACEUTICALS, INC.Inventors: Ute Hoch, Jeffrey A. Silverman, Daniel C. Adelman
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Patent number: 8067591Abstract: Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: GrantFiled: December 28, 2005Date of Patent: November 29, 2011Assignees: Agouron Pharmaceuticals, Inc., Pfizer Inc.Inventors: Junhu Zhang, Chuangxing Guo, Djamal Bouzida, Liming Dong, Haitao Li, Joseph Timothy Marakovits, Anle Yang, Yufeng Hong
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BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20110281846Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20110281859Abstract: Compounds of the formula I, in which D, X, Y, Z, R and R1 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.Type: ApplicationFiled: December 22, 2009Publication date: November 17, 2011Applicant: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Timo Heinrich, Frank Zenke, Mireille Krier, Kai Schiemann
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Publication number: 20110281874Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Ronald Jay HINKLIN, Ajay SINGH
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Patent number: 8058280Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.Type: GrantFiled: August 31, 2007Date of Patent: November 15, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuo Cho, Takashi Imada, Takenori Hitaka, Kazuhiro Miwa, Masami Kusaka, Nobuhiro Suzuki
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Publication number: 20110275589Abstract: The invention is directed to 3,5-disubstituted and 3,5,7-trisubstituted-3H-oxazolo and 3H-thiazolo[4,5-d]pyrimidin-2-one compounds and prodrugs thereof that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and pharmaceutical compositions containing them, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds and prodrugs.Type: ApplicationFiled: July 1, 2009Publication date: November 10, 2011Applicant: Anadys Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Gregory J. Haley, Joseph R. Lennox, Alan X. Xiang, Erik J. Rueden