Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
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Patent number: 8461165Abstract: The invention relates to the compounds of formula I, their preparation and the pharmaceutical compositions containing the compounds. The invention also relates to the use of the compounds of formula I in preparing medicines, which can treat sexual dysfunction of animals including human (male and female), especially erectile dysfunction of male and the diseases in which the function of phospholipase 5 (cGMP PDE5) is involved.Type: GrantFiled: January 11, 2010Date of Patent: June 11, 2013Assignees: Yangtze River Pharmaceutical (Group) Co., Ltd, Tianjin North Pharma Sci-Tech Co., LtdInventors: Yongfeng Wang, Kejun Zhao
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Publication number: 20130143879Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: January 31, 2013Publication date: June 6, 2013Applicant: GENKYOTEX SAInventor: Genkyotex Sa
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Patent number: 8455486Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: GrantFiled: September 22, 2009Date of Patent: June 4, 2013Assignee: Genkyotex SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Patent number: 8455485Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: GrantFiled: September 22, 2009Date of Patent: June 4, 2013Assignee: Genkyotex SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Publication number: 20130137681Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: January 30, 2013Publication date: May 30, 2013Applicant: INCYTE CORPORATIONInventor: INCYTE CORPORATION
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Publication number: 20130137676Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 19, 2012Publication date: May 30, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130137685Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2 and R3 are defined as stated in the claims. The compounds of formula (I) are suitable, for example, for wound healing.Type: ApplicationFiled: January 12, 2011Publication date: May 30, 2013Applicant: SANOFIInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
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Patent number: 8450314Abstract: A compound formula (IA) or (IB), or a pharmaceutically acceptable thereof; wherein the substituents are defined as in the claims, and their use as P38 MAP kinase.Type: GrantFiled: February 16, 2010Date of Patent: May 28, 2013Assignee: Chiesi Farmaceutici S.p.A.Inventors: Amanda Beswick, Bohdan Waszkowycz
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Publication number: 20130131058Abstract: Compounds according to Formula (I), as well salts thereof: wherein R1 and R2 are as defined herein, are useful as antiproliferative agents and kinase inhibitors. Synthetic methods for preparing the compounds of Formula (I) are also provided.Type: ApplicationFiled: July 21, 2011Publication date: May 23, 2013Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Publication number: 20130129820Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d 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: January 10, 2013Publication date: May 23, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Patent number: 8445487Abstract: Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. 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: GrantFiled: February 9, 2012Date of Patent: May 21, 2013Assignee: Genentech, Inc.Inventors: Georgette Castanedo, Irina Chuckowree, Adrian Folkes, Daniel P. Sutherlin, Nan Chi Wan
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Publication number: 20130123231Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.Type: ApplicationFiled: November 9, 2012Publication date: May 16, 2013Applicant: Nimbus Apollo, Inc.Inventor: Nimbus Apollo, Inc.
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Publication number: 20130123237Abstract: Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: February 23, 2012Publication date: May 16, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: Rajan Anand, James M. Apgar, Tesfaye Biftu, Ping Chen, Lin Chu, Vincent J. Colandrea, Guizhen Dong, James F. Dropinski, Danqing Feng, Jacqueline D. Hicks, Jinlong Jiang, Alexander J. Kim, Kenneth J. Leavitt, Bing Li, Xiaoxia Qian, Iyassu Sebhat, Lan Wei, Robert R. Wilkening, Zhicai Wu
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Publication number: 20130123256Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: GENKYOTEX SAInventor: Genkyotex Sa
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Publication number: 20130123255Abstract: The invention relates to a method for the treatment of a patient with a proliferative disease including solid tumors, hematological malignancies and hyperplasia comprising administering a therapeutic combination to said patient wherein the therapeutic combination comprises a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of a compound of formula (II) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 6, 2012Publication date: May 16, 2013Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventor: CHUGAI SEIYAKU KABUSHIKI KAISHA
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Patent number: 8440651Abstract: 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: GrantFiled: February 18, 2011Date of Patent: May 14, 2013Assignee: F. Hoffmann-La Roche AGInventors: Georgette Castanedo, Bryan Chan, Matthew C. Lucas, Brian Safina, Daniel P. Sutherlin, Zachary Sweeney
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Patent number: 8440661Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: GrantFiled: May 13, 2010Date of Patent: May 14, 2013Assignee: Signal Pharmaceuticals, LLCInventors: Brydon L. Bennett, Kate Northcote, Brian Edwin Cathers
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Publication number: 20130116213Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.Type: ApplicationFiled: June 20, 2011Publication date: May 9, 2013Applicant: HANMI SCIENCE CO., LTD.Inventors: Mi Young Cha, Seok Jong Kang, Mi Ra Kim, Ju Yeon Lee, Ji Young Jeon, Myoung Gi Jo, Eun Joo Kwak, Kwang Ok Lee, Tae Hee Ha, Kwee Hyun Suh, Maeng Sup Kim
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Publication number: 20130116241Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: October 25, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130116236Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 6, 2012Publication date: May 9, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8435987Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: August 3, 2011Date of Patent: May 7, 2013Assignee: Amgen Inc.Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
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Patent number: 8436012Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.Type: GrantFiled: November 24, 2010Date of Patent: May 7, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
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Patent number: 8435986Abstract: Compounds of the formula (I), in which X1, X2, X3, X4, X5, R1, R2, R3, R3?, R4, R6 and R7 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: July 16, 2009Date of Patent: May 7, 2013Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Patent number: 8431572Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: July 6, 2011Date of Patent: April 30, 2013Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20130102587Abstract: Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.Type: ApplicationFiled: March 14, 2011Publication date: April 25, 2013Applicant: PROXIMAGEN LIMITEDInventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
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Publication number: 20130102601Abstract: The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBHInventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
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Publication number: 20130102590Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicant: AbbVie IncInventor: AbbVie Inc.
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Publication number: 20130102586Abstract: Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.Type: ApplicationFiled: March 30, 2012Publication date: April 25, 2013Applicant: ARRIEN PHARMACEUTICALS LLCInventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
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Publication number: 20130102600Abstract: The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBHInventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
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Publication number: 20130102595Abstract: The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.Type: ApplicationFiled: October 15, 2012Publication date: April 25, 2013Inventor: Curis, Inc.
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Publication number: 20130096115Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from autism.Type: ApplicationFiled: December 21, 2010Publication date: April 18, 2013Applicant: AFRAXIS, INC.Inventors: Jay Lichter, David Campbell, Benedikt Vollrath, Sergio G. Durón
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Publication number: 20130096104Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as an inhibitor of TYK2 kinase and conditions related, such as inflammatory illnesses, inflammatory bowel disease or psoriasis.Type: ApplicationFiled: March 15, 2011Publication date: April 18, 2013Applicant: GENENTECH, INC.Inventors: Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Vickie H. Tsui, Birong Zhang, Aihe Zhou
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Publication number: 20130096116Abstract: Changes in gastric pH due to oral co-administration of acid-reducing agents, such as proton pump inhibitors, and oncology drugs can have a marked impact on the absorption and oral bioavailability of the oncology drug if the pH decreases the maximal absorbable dose. Moreover, there is a potential for specific drug-drug interactions between some of the acid-reducing agents and these drugs. Methods are described for treating patients on gastric acid-reducing therapy with orally-administered PI3K inhibitor compound GDC-0941. Treatment with a re-acidification compound during treatment with GDC-0941 improves bioavailability of GDC-0941.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Genentech, Inc.Inventor: Genentech, Inc.
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Publication number: 20130096114Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof.Type: ApplicationFiled: December 7, 2012Publication date: April 18, 2013Applicant: SURFACE LOGIX, INC.Inventor: SURFACE LOGIX, INC.
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Publication number: 20130096113Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Ambit Biosciences CorporationInventor: Ambit Biosciences Corporation
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Publication number: 20130096110Abstract: Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: February 11, 2011Publication date: April 18, 2013Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
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Patent number: 8420636Abstract: The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA) wherein the variables are as defined herein, to their preparation and to their therapeutic use as CCR3 receptor ligands.Type: GrantFiled: January 26, 2011Date of Patent: April 16, 2013Assignee: SanofiInventors: Agnes Behr, Sandor Batori, Veronika Bartane Bodor, Zoltan Szlavik, Imre Bata, Katalin Urban-Szabo, Zoltan Kapui, Endre Mikus
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Publication number: 20130090335Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: ApplicationFiled: March 30, 2012Publication date: April 11, 2013Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian, Rudi Bao
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N3-HETEROARYL SUBSTITUTED TRIAZOLES AND N5-HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20130090330Abstract: N3-Heteroaryl substituted triazoles and N5-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: October 4, 2012Publication date: April 11, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: RIGEL PHARMACEUTICALS, INC. -
Publication number: 20130090336Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: December 5, 2012Publication date: April 11, 2013Applicant: YM BIOSCIENCES AUSTRALIA PTY LTDInventor: YM Biosciences Australia Pty Ltd
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Publication number: 20130085128Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 27, 2012Publication date: April 4, 2013Applicant: SANOFIInventor: SANOFI
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Patent number: 8410095Abstract: This invention relates to novel compounds of formula (I): and derivatives thereof useful for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?.Type: GrantFiled: May 20, 2010Date of Patent: April 2, 2013Assignee: GlaxoSmithKline LLCInventors: Hong Lin, Juan I. Luengo, Ralph A. Rivero, Mark James Schulz, Ren Xie, Jin Zeng
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Publication number: 20130079341Abstract: The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.Type: ApplicationFiled: May 23, 2011Publication date: March 28, 2013Inventors: Brigitte Johanna Bernita Folmer, de Adrianus Petrus Antonius Man, Elisabeth Sophia Gernette, Rita Corte Real Goncalves Azevedo, Hemen Ibrahim
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Publication number: 20130079303Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: ApplicationFiled: November 19, 2012Publication date: March 28, 2013Applicant: AMGEN INC.Inventor: Amgen Inc.
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Publication number: 20130079342Abstract: Substituted bicyclic heteroaryls of the following formulae 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 LeukemiaType: ApplicationFiled: June 30, 2011Publication date: March 28, 2013Inventors: Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Vatee Pattaropong, Jillian L. Simard
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Publication number: 20130079330Abstract: A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, 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: November 20, 2012Publication date: March 28, 2013Applicant: UCB Pharma, S.A.Inventor: UCB Pharma, S.A.
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Publication number: 20130079324Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Hengmiao Cheng, Theodore Otto Johnson, JR., John Charles Kath, Kevin Kun-Chin Liu, Elizabeth Ann Lunney, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken, Scott Channing Sutton
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Patent number: 8404682Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors.Type: GrantFiled: September 6, 2011Date of Patent: March 26, 2013Assignee: Cortex Pharmaceuticals, Inc.Inventors: Leslie Street, Rudolf Mueller, Steven Lee
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Patent number: 8404677Abstract: The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.Type: GrantFiled: October 29, 2010Date of Patent: March 26, 2013Assignees: Genosco, Oscotec, Inc.Inventors: Hong Woo Kim, Jong Sung Koh, Jaekyoo Lee, Ho-Juhn Song, Youngsam Kim, Hee Kyu Lee, Jang-Sik Choi, Sun-Hee Lim, Sunhwa Chang