Hetero Ring Is Seven-membered Consisting Of Two Nitrogens And Five Carbon Atoms Patents (Class 514/218)
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Publication number: 20140179688Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that modulate the PLOD-2 enzyme in the skin. Also provided are methods for screening for substances which modulate PLOD-2 enzyme levels and the methods of using active agents identified by the screening protocol in the treatment of skin.Type: ApplicationFiled: December 20, 2012Publication date: June 26, 2014Applicant: AVON PRODUCTS, INC.Inventors: Uma Santhanam, Permanan Raaj Khusial
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Publication number: 20140179642Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ cosmetic composition comprising novel active agents that enhance collagen production in the skin.Type: ApplicationFiled: December 20, 2012Publication date: June 26, 2014Applicant: AVON PRODUCTS, INC.Inventors: Uma Santhanam, Permanan Raaj Khusial
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Publication number: 20140171418Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: ApplicationFiled: August 10, 2012Publication date: June 19, 2014Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans
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Publication number: 20140171421Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: February 21, 2014Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: Gurdip Bhalay, Emma Budd, Graham Charles Bloomfield, Stephen Paul Collingwood, Andrew Dunstan, Lee Edwards, Peter Gedeck, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt, Paul Oakley, Nichola Smith
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Publication number: 20140163010Abstract: New pyrazolo[3,4-d]pyrimidine compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for preparing these compounds, to compositions comprising them and to their use as medicaments.Type: ApplicationFiled: July 13, 2012Publication date: June 12, 2014Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Maria Rosa Cuberes-Altisent, Jordi Corbera-Arjona, Jose Luis Diaz-Fernanadez, Carmen Almansa-Rosales
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Publication number: 20140163000Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: June 12, 2014Inventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Publication number: 20140163005Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163001Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.Type: ApplicationFiled: July 27, 2012Publication date: June 12, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
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Publication number: 20140163006Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163004Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163003Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163007Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Patent number: 8748412Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: GrantFiled: February 2, 2011Date of Patent: June 10, 2014Assignee: Argusina Bioscience Inc.Inventors: Jiayu Liao, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Publication number: 20140148444Abstract: Described herein are compounds that activate pyruvate kinase, for use in a method for increasing lifetime of the red blood cells, for regulating 2,3-diphosphoglycerate levels in blood and for treating sickle cell anemia.Type: ApplicationFiled: May 3, 2012Publication date: May 29, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventor: Shin-San M. Su
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Publication number: 20140148443Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.Type: ApplicationFiled: November 20, 2013Publication date: May 29, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Patent number: 8735383Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT-1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: March 21, 2012Date of Patent: May 27, 2014Assignee: Amgen Inc.Inventors: Hitchcock Stephen, Albert Amegadzie, Wenyuan Qian, Xiaoyang Xia, Scott S. Harried
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Patent number: 8729079Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.Type: GrantFiled: August 23, 2012Date of Patent: May 20, 2014Assignee: Endo Pharmaceuticals Inc.Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
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Publication number: 20140135312Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicants: Astex Therapeutics Ltd., Novartis AGInventors: Gilbert BESONG, Christopher Thomas Brain, Clinton A. Brooks, Miles Stuart Congreve, Claudio Dagostin, Guo He, Ying Huo, Steven Howard, Yue Ll, Yipin Lu, Paul Mortenston, Troy Smith, Moo Je Sung, Steven Woodhead, Wojciech Wrona, Bharat Lagu
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Publication number: 20140135305Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.Type: ApplicationFiled: December 12, 2013Publication date: May 15, 2014Applicant: PTC THERAPEUTICS, INC.Inventors: Sergey V. Paushkin, Charles Romfo, Ellen Welch, Nikolai Naryshkin
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Publication number: 20140135308Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, 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: ApplicationFiled: January 23, 2014Publication date: May 15, 2014Applicant: Genentech, Inc.Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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Publication number: 20140135304Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors.Type: ApplicationFiled: June 7, 2011Publication date: May 15, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Amol Dinakar Deshpande, Adi Reddy Dwarampudi, Narasimhareddy Gangadasari, Sangram Keshari Saraf, Vishwottam Nagaraj Kandikere, Pradeep Jayarajan, Ishtiyaque Ahmad, Mohmadsadik Abdulhamid Mulla, Venkateswarlu Jasti
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Patent number: 8722663Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: GrantFiled: January 28, 2011Date of Patent: May 13, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Publication number: 20140128380Abstract: The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: Mimetica Pty LtdInventors: Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
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Publication number: 20140128361Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: ApplicationFiled: January 6, 2014Publication date: May 8, 2014Applicants: Pharmacopeia Drug Discovery, Inc., Merck Sharp & Dohme Corp.Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey H. Lowrie, Kurt W. Salonz, Suresh D. Babu
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Patent number: 8716312Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: November 17, 2009Date of Patent: May 6, 2014Assignee: Merck Sharp & Dohme CorporationInventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
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Publication number: 20140121200Abstract: Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.Type: ApplicationFiled: June 7, 2012Publication date: May 1, 2014Applicant: HUTCHISON MEDIPHARMA LIMITEDInventors: Wei-Guo Su, Wei Deng, Jianguo Ji
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Patent number: 8710028Abstract: A powder composition for intranasal delivery includes a benzodiazepine drug and chitosan, a salt of chitosan, a derivative of chitosan or a salt of a derivative of chitosan.Type: GrantFiled: August 29, 2008Date of Patent: April 29, 2014Assignee: Archimedes Development LimitedInventors: Peter James Watts, Yu-Hui Cheng, Alan Smith, Jonathan Castile
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Publication number: 20140113005Abstract: The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.Type: ApplicationFiled: January 16, 2013Publication date: April 24, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20140113882Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: September 27, 2013Publication date: April 24, 2014Applicants: Cancer Research Technology Limited, Cephalon, Inc.Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Katherine M. Fowler, Robert L. Hudkins, Eugen F. Mesaros, Nathaniel J.T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
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Publication number: 20140107105Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
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Patent number: 8697687Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: September 13, 2012Date of Patent: April 15, 2014Assignee: Novartis AGInventors: Gurdip Bhalay, Emma Budd, Graham Charles Bloomfield, Stephen Paul Collingwood, Andrew Dunstan, Lee Edwards, Peter Gedeck, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt, Paul Oakley, Nichola Smith
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1H-benzimidazole-4-carboxamides substituted with phenyl at the 2-position are potent PARP inhibitors
Patent number: 8697736Abstract: Compound having formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds having formula (I), methods of treatment comprising compounds having formula (I), and methods of inhibiting the PARP enzyme comprising compounds having formula (I).Type: GrantFiled: September 29, 2006Date of Patent: April 15, 2014Assignee: AbbVie Inc.Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda -
Publication number: 20140100215Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.Type: ApplicationFiled: December 7, 2013Publication date: April 10, 2014Applicant: Exelixis, Inc.Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
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Patent number: 8691810Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, B, R1, R2, R3, R4a, R5, and Z are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora.Type: GrantFiled: May 12, 2011Date of Patent: April 8, 2014Assignee: AbbVie Inc.Inventors: Michael R. Michaelides, Andrew S. Judd, Shannon R. Fix-Stenzel, Richard F. Clark, Bryan K. Sorensen, Zhiqin Ji
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Patent number: 8691184Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.Type: GrantFiled: January 24, 2012Date of Patent: April 8, 2014Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
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Publication number: 20140094450Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure 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 19, 2013Publication date: April 3, 2014Applicant: SANOFIInventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
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Publication number: 20140094448Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.Type: ApplicationFiled: September 13, 2013Publication date: April 3, 2014Applicant: SENHWA BIOSCIENCES, INC.Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas Raffaele, Suchitra Ravula, David M. Ryckman
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Publication number: 20140094451Abstract: There is provided a preventive for glaucoma or a preventive or a remedy for ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. A preventive or a remedy for glaucoma comprising a Rho kinase inhibitor and an ?1 blocker in combination.Type: ApplicationFiled: December 6, 2013Publication date: April 3, 2014Applicant: Kowa Co., Ltd.Inventors: Ken MIZUNO, Jiro MATSUMOTO
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Patent number: 8685981Abstract: Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: wherein A is selected from among a 3- to 10-membered heterocyclyl group, B is selected from among an amino group, and X is selected from N and CH.Type: GrantFiled: July 14, 2011Date of Patent: April 1, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Daigo Asano
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Patent number: 8685961Abstract: The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.Type: GrantFiled: March 27, 2007Date of Patent: April 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Karen M. Brashear, Paul J. Coleman, Christopher D. Cox, Anthony M. Smith, David B. Whitman
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Publication number: 20140086839Abstract: Provided are methods of treating autoimmune diseases by administering to the subject a therapeutically effective amount of a quinolone compound such as 2-(4-methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide (CX-5461). Also provided are methods of monitoring efficiency of treatment of the quinolone compound by determining the expression level of at least one gene of the RNA polymerase I pathway.Type: ApplicationFiled: February 26, 2012Publication date: March 27, 2014Applicant: Tel HaShomer Medical Research Infrastructure and Services Ltd.Inventors: Anat Achiron, Michael Gurevich
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Publication number: 20140088088Abstract: 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, Formulas (I), (II), (III) and (IV) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent proliferative disorders and their use to manufacture a medicine to treat or prevent proliferative disorders, particularly cancer such as leukemia. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent proliferative disorders. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of proliferative disorders and pathologic conditions such as, but not limited to, cancer such as leukemia.Type: ApplicationFiled: September 8, 2011Publication date: March 27, 2014Applicant: Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Jean Herman, Thierry Louat
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Publication number: 20140088029Abstract: Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.Type: ApplicationFiled: April 11, 2012Publication date: March 27, 2014Applicant: PHARMA EIGHT CO., LTD.Inventors: Hachiro Sugimoto, Michiaki Okuda, Takashi Takahashi, Ichiro Hijikuro, Hidetaka Suzuki, Shinichi Nakayama
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Patent number: 8680076Abstract: 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 scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.Type: GrantFiled: October 20, 2011Date of Patent: March 25, 2014Assignee: Signal Pharmaceuticals, LLCInventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
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Patent number: 8680089Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: GrantFiled: January 17, 2011Date of Patent: March 25, 2014Assignee: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Publication number: 20140080799Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: ApplicationFiled: September 20, 2013Publication date: March 20, 2014Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Publication number: 20140080801Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. 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: November 18, 2013Publication date: March 20, 2014Applicant: Genentech, Inc.Inventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
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Publication number: 20140080780Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.Type: ApplicationFiled: May 21, 2012Publication date: March 20, 2014Inventor: Benjamin WOLOZIN
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Patent number: 8673920Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: GrantFiled: April 27, 2010Date of Patent: March 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
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Publication number: 20140073627Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.Type: ApplicationFiled: November 7, 2013Publication date: March 13, 2014Applicant: EVOTEC AGInventors: James MADDEN, David James HALLETT, Alastair PARKES, Ali RAOOF, Xiaolu WANG