Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/278)
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Publication number: 20120202828Abstract: A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1, R2 and Rx are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: July 21, 2010Publication date: August 9, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Jose Luis Castro Pineiro, Adrian Hall, Andrew Madin, Ngoc-Tri Vo
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Publication number: 20120202785Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I 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: February 8, 2012Publication date: August 9, 2012Inventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
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Publication number: 20120202825Abstract: The present invention is directed to novel salts of thieno[2,3-d]pyrimidine derivatives, including 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine salts. The present invention is also directed to compositions including such polymorphs and methods for using such salts, e.g., in the treatment of gastrointestinal and/or genitourinary disorders.Type: ApplicationFiled: February 4, 2011Publication date: August 9, 2012Inventors: Martin Ian Cooper, Christopher Stephen Frampton
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Publication number: 20120196845Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
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Patent number: 8211900Abstract: Compounds of formula (I) or (II) are dihydrofolate reductase inhibitors, useful for the treatment of, for example, cell proliferative diseases: wherein A and D are independently —CHR7— or —NR7—; E and G are independently ?CR7— or ?N—; each R6 independently represents hydrogen or —OR7; R7 is hydrogen or C1-C6 alkyl; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid which does not contain a carboxyl, or carboxyl ester group; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, and Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—, —NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein RType: GrantFiled: April 24, 2007Date of Patent: July 3, 2012Assignee: Chroma Therapeutics Ltd.Inventor: Alan Hornsby Davidson
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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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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: 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: 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: 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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Patent number: 8193199Abstract: Substituted bicyclic heteroaryls having the structures: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid LeukemiType: GrantFiled: March 24, 2008Date of Patent: June 5, 2012Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20120136150Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.Type: ApplicationFiled: July 15, 2010Publication date: May 31, 2012Applicant: SDS BIOTECH K.K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
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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: 8183249Abstract: The subject invention concerns materials and methods for inhibiting the Akt/PKB pathway. In one embodiment, a compound of the invention inhibits kinase activity and/or phosphorylation levels of Akt proteins. The subject invention also concerns methods for inhibiting or killing a cancer cell or other cell in which expression of an Akt protein is elevated or constitutively active, comprising contacting the cell with an effective amount of a compound of formula I. The subject invention also concerns methods for treating cancer or a tumor in a person or animal comprising administering all effective amount of a compound of formula I to the person or animal.Type: GrantFiled: July 14, 2008Date of Patent: May 22, 2012Assignee: University of South FloridaInventors: Jin Q. Cheng, Mei Sun, Said M. Sebti
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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: 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: 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: 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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Publication number: 20120122679Abstract: Disclosed are compounds of Formula 1, N-oxides and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, EC(?X1); a is 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: August 3, 2010Publication date: May 17, 2012Applicant: E. I. Du Pont De Nemours and CompanyInventors: Wenming Zhang, Caleb William Holyoke, JR., Kenneth Andrew Hughes, George Philip Lahm, Thomas Francis Pahutski, JR., My-Hanh Thi Tong, Stephen Frederick McCann
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Publication number: 20120108576Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: November 30, 2011Publication date: May 3, 2012Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
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Publication number: 20120108813Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. 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 TRPV3.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Inventors: Prasada Rao V.S. LINGAM, Sachin Sundarlal CHAUDHARI, Abraham THOMAS, Neelima KHAIRATKAR-JOSHI, Vidya Ganapati KATTIGE
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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: 8158825Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 21, 2006Date of Patent: April 17, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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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: 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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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: 20120071489Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.Type: ApplicationFiled: April 16, 2010Publication date: March 22, 2012Inventors: Shizuo Kasai, Kevin Francis McGee, JR.
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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: 8133997Abstract: The invention relates to the dimeric compound of formula (II) wherein the two monomer-units are linked with each other either via R3 or via R4; the ring A is a five-or six-membered heteroaromatic ring, one of the groups R3 or R4 is an unsubstituted or substituted phenylene radical, the remaining group R3 or R4 is a C1-C4 alkyl, C5-C6 cycloalkyl, an unsubstituted or substituted phenyl, benzyl, benzanilide or naphthyl; or wherein the group NR4 together with the ring A constitutes a five-or six membered heterocycle that can be annelated with a benzene ring, and R3 is an unsubstituted or substituted phenylene radical. The inventive compounds can be used for pigmenting high-molecular organic materials.Type: GrantFiled: January 14, 2005Date of Patent: March 13, 2012Assignee: Clariant Produkte (Deutschland) GmbHInventors: Thomas Metz, Carsten Plueg
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Patent number: 8133898Abstract: The invention provides compounds, pharmaceutical compositions, kits, method of preparing, and method of using the compounds which exhibit renin and other S9 proteases activities and consist of the formula:—wherein the variables are as defined herein.Type: GrantFiled: March 11, 2008Date of Patent: March 13, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Stephen L. Gwaltney, Zhiyuan Zhang, Betty Lam
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Patent number: 8133998Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).Type: GrantFiled: May 9, 2008Date of Patent: March 13, 2012Assignee: Zalicus Pharmaceuticals, Ltd.Inventors: Hassan Pajouhesh, Hossein Pajouhesh, Yanbing Ding, Jason Tan, Mike Grimwood, Francesco Belardetti, Ramesh Kaul, Richard Holland, Navjot Chahal
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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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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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Publication number: 20120053345Abstract: Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.Type: ApplicationFiled: August 4, 2011Publication date: March 1, 2012Applicant: ABBOTT LABORATORIESInventors: Anna M. Ericson, Andrew Burchat, Kristine E. Frank, David J. Calderwood, Lily K. Abbott, Maria A. Argiriadi, David W. Borhani, Kevin P. Cusack, Richard W. Dixon, Thomas D. Gordon, Kelly D. Mullen, Robert V. Talanian, Xiaoyun Wu, Xiaolei Zhang, Lu Wang, Biqin Li, Claude E. Barberis, Neil Wishart
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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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Patent number: 8119647Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. 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 TRPV3.Type: GrantFiled: April 9, 2009Date of Patent: February 21, 2012Assignee: Glenmark Pharmaceuticals S.A.Inventors: Prasada Rao V. S. Lingam, Sachin Sundarlal Chaudhari, Abraham Thomas, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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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: 20120021907Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: January 6, 2010Publication date: January 26, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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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: 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: 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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Patent number: 8063070Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.Type: GrantFiled: May 4, 2010Date of Patent: November 22, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Publication number: 20110281861Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.Type: ApplicationFiled: July 2, 2009Publication date: November 17, 2011Inventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Thienthong, Nicholas Andrew Vandegraaff, Lisa Jane Winfield