Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
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Patent number: 8735386Abstract: Compounds of general formula (I) wherein the groups R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.Type: GrantFiled: July 20, 2011Date of Patent: May 27, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Matthias Treu
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Patent number: 8729090Abstract: Embodiments of the invention include compositions effective for inhibiting collagen production and related methods. A preferred method comprises contacting at least one cell capable of producing collagen with a composition effective for inhibiting collagen production thereby. The composition comprises one or more of the compounds effective for inhibiting collagen production disclosed herein.Type: GrantFiled: October 5, 2012Date of Patent: May 20, 2014Assignee: The Florida State University Research Foundation, Inc.Inventor: Branko Stefanovic
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Patent number: 8722708Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.Type: GrantFiled: June 12, 2006Date of Patent: May 13, 2014Assignees: Merck Sharp & Dohme Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X. H. Le, Gang Qian, Yuefei Shao
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Publication number: 20140128390Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.Type: ApplicationFiled: September 5, 2013Publication date: May 8, 2014Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
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Publication number: 20140121204Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.Type: ApplicationFiled: January 6, 2014Publication date: May 1, 2014Applicant: GALAPAGOS NVInventors: Frédéric Gilbert Labéguère, Gregory John Robert NEWSOME, Luke Jonathan ALVEY, Laurent Raymond Maurice Sanière, Stephen Robert FLETCHER
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Publication number: 20140121198Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: October 31, 2013Publication date: May 1, 2014Applicant: Incyte CorporationInventors: Yun-Long Li, Wenyu Zhu, Song Mei, Joseph Glenn
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Patent number: 8709993Abstract: The present invention relates to novel quinazoline compounds and their use in perfume compositions. The novel quinazoline compounds of the present invention are represented by the following formula: an isomer or a mixture of isomers thereof, wherein the broken line represents a single or double bond.Type: GrantFiled: February 15, 2011Date of Patent: April 29, 2014Assignee: International Flavors & Fragrances Inc.Inventors: Michael G. Monteleone, Robert P. Belko, Franc T. Schiet, Paul D. Jones, Anthony T. Levorse, Jr.
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Patent number: 8710065Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 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: GrantFiled: February 28, 2012Date of Patent: April 29, 2014Assignee: AbbVie Inc.Inventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
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Publication number: 20140113896Abstract: The present invention relates to substituted phenoxypyridine compounds of general formula (I); in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: November 8, 2011Publication date: April 24, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: William Johnston Scott, Orlin Pertov, Manfred Möwes, Ningshu Liu, Ulf Bömer
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Publication number: 20140113920Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: July 2, 2012Publication date: April 24, 2014Applicant: MERCK SHARP & DOHME CORP.Inventor: Wen-Lian Wu
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Patent number: 8703769Abstract: Methods of treating or preventing obesity or obesity related disorders in a subject are provided, comprising administering to the subject a treatment effective in reducing one or more activities of an epidermal growth factor receptor (EGFR) in the subject. Methods of screening for compositions that can modulate one or more EGFR activities are also provided.Type: GrantFiled: July 14, 2006Date of Patent: April 22, 2014Assignee: The University of North Carolina at Chapel HillInventors: David Threadgill, Cordelia Johnson Barrick
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Patent number: 8703784Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.Type: GrantFiled: August 22, 2011Date of Patent: April 22, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyun Zhao, Andrew McRiner
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Patent number: 8703783Abstract: The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.Type: GrantFiled: October 17, 2011Date of Patent: April 22, 2014Assignee: Incyte CorporationInventors: Changsheng Zheng, Chu-Biao Xue, Ganfeng Cao, Michael Xia, Anlai Wang, Hai Fen Ye, Brian Metcalf
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Publication number: 20140100228Abstract: Antiviral compositions and methods are contemplated that are especially effective in the treatment and prevention of influenza A viruses. Also presented are cellular assays to identify small molecule compounds having antiviral properties, particularly as it relates to detection of influenza A RNA-dependent RNA polymerase activity in a mammalian cell independent of other influenza A components. Preferred assays allow for identification of viral replication inhibitors that do not disrupt normal cellular activity.Type: ApplicationFiled: December 11, 2013Publication date: April 10, 2014Applicant: Nant Holdings IP, LLCInventors: Kayvan Niazi, Shahrooz Rabizadeh, Anne-Laure LeNy, Oleksandr Buzko, Justin Golovato, Patrick Soon-Shiong
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Patent number: 8691832Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: December 1, 2011Date of Patent: April 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Duane A. Burnett, Zhiqiang Zhao, David Cole, Hubert Josien, Dmitri A. Pissarnitski, Thavalakulamgar Sasikumar, Wen-Lian Wu, Martin Domalski
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Patent number: 8691831Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula I are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: March 9, 2012Date of Patent: April 8, 2014Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20140093490Abstract: The present invention investigate the two modes of glutamate release and the releasing rate of glutamate, and thus can provide a useful technique for neuron protection and acceleration of neurotransmission by controlling the glutamate release in astroctye. Thus, the present invention provides an inhibitor of the fast-mode release and/or the slow-mode release of astrocytic glutamate, a screening method of the inhibitor and a pharmaceutical composition or method of ameliorating, preventing and/or treating the disease associated with the over-release of glutamate via the Ca2+-activated anion channel, with the inhibition of fast-mode glutamate release.Type: ApplicationFiled: July 23, 2013Publication date: April 3, 2014Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Changjoon Justin LEE, Soo Jin OH, Eun Mi HWANG, Dong Ho WOO
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Patent number: 8680110Abstract: A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein each of R11 and R12 is hydrogen, C1-8 alkyl or the like; R13 is hydrogen, C1-8 alkyl or the like; R14 is C1-8 alkoxy, hydroxyl, cyano, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene ring or the like.Type: GrantFiled: July 27, 2011Date of Patent: March 25, 2014Assignee: Nippon Chemiphar Co., Ltd.Inventors: Masatoshi Ushioda, Shogo Sakuma, Toshiyasu Imai, Kazuhide Inoue
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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: 8673923Abstract: Methods and compositions relating to TIC10 are described according to aspects of the present invention. The compositions and methods have utility in treating disease, particularly cancer in a subject in need thereof, including a human subject as well as subjects of other species. The compositions have utility in treating brain cancer in a subject in need thereof.Type: GrantFiled: April 30, 2012Date of Patent: March 18, 2014Assignee: The Penn State Research FoundationInventors: Wafik S. El-Deiry, Joshua E. Allen, Gen Sheng Wu
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Publication number: 20140073642Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.Type: ApplicationFiled: May 18, 2012Publication date: March 13, 2014Applicant: Janssen R&D IrelandInventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
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Publication number: 20140066466Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.Type: ApplicationFiled: March 12, 2012Publication date: March 6, 2014Applicant: President and Fellows of Harvard CollegeInventor: Junying Yuan
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Patent number: 8664207Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.Type: GrantFiled: December 7, 2009Date of Patent: March 4, 2014Assignee: Intra-Cellular Therapies, Inc.Inventors: Peng Li, Jun Zhao, Hailin Zheng, Lawrence Wennogle
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Patent number: 8664233Abstract: The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.Type: GrantFiled: December 21, 2007Date of Patent: March 4, 2014Assignee: The Medicines Company (Leipzig) GmbHInventors: Claudia Reichelt, Alexander Schulze, Mohammed Daghish, Friedrich-Alexander Ludwig, Jochen Heinicke, Konrad Herrmann, Maj Schuster, Sven Letschert, Kenneth Mugridge, Joseph DeAngelo
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Patent number: 8664234Abstract: The present invention is directed to dihydrobenzoquinazilinone 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: GrantFiled: September 29, 2011Date of Patent: March 4, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Patent number: 8664387Abstract: 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: GrantFiled: December 9, 2010Date of Patent: March 4, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Publication number: 20140057900Abstract: Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: August 23, 2013Publication date: February 27, 2014Applicant: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Enrique Fernandez
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Publication number: 20140057899Abstract: The present invention provides a new compound that has an inhibitory action against EGFR and that has cell growth inhibitory effects. The present invention further provides a pharmaceutical preparation useful for preventing and/or treating cancer, based on the EGFR inhibitory effect of the compound. A compound represented by the following Formula (I) or a salt thereof.Type: ApplicationFiled: February 22, 2013Publication date: February 27, 2014Applicant: Taiho Pharmaceutical Co., Ltd.Inventors: Takeshi Sagara, Satoru Ito, Sachie Otsuki, Katsumasa Nonoshita
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Publication number: 20140051689Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.Type: ApplicationFiled: October 24, 2013Publication date: February 20, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Alistair George Draffan, Roland Henry Nearn, Jeffrey Peter Mitchell
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Publication number: 20140051685Abstract: The present invention is directed to a method for treating a patient suffering from a metabolic disorder such as the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, and the metabolic sequale of these diseases including cardiovascular, cerebrovascular, renal and hepatic diseases, comprising the step of: administering to a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes a pharmaceutical composition comprising (1) at least one compound that stimulates an increase in central dopaminergic neuronal activity level in the subject, and (2) at least one compound that stimulates a decrease in central noradrenergic neuronal activity level in the subject.Type: ApplicationFiled: November 21, 2011Publication date: February 20, 2014Inventor: Anthony H. Cincotta
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Patent number: 8653097Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: October 15, 2009Date of Patent: February 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Lars Van Der Veen, Darryl McConnell, Tobias Wunberg
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Publication number: 20140045836Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: October 16, 2013Publication date: February 13, 2014Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Elena Casale, Francesco Casuscelli, Claudio Dalvit, Paolo Polucci, Fabio Zuccotto
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Publication number: 20140045833Abstract: The present invention relates to a novel family of inhibitors of protein kinases of Formula (1) wherein X is selected from CH2, O, S(0)n, or NR6; and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src, Btk and Lck protein kinase families.Type: ApplicationFiled: April 3, 2012Publication date: February 13, 2014Applicant: PHARMASCIENCE INC.Inventors: Alain Laurent, Yannick Rose, Stephen Morris, James Jaquith
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Publication number: 20140037547Abstract: The present invention relates to cGMP protein kinase (PKG) and regulatory domains and methods of use thereof. The structural determination of PKG domains is also described. cGMP independent PKG activators and uses thereof are also described.Type: ApplicationFiled: March 13, 2013Publication date: February 6, 2014Applicant: The University of Vermont and State Agricultural CollegeInventors: Wolfgang Dostmann, Brent W. Osborne, Thomas M. Moon
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Publication number: 20140038922Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.Type: ApplicationFiled: May 1, 2013Publication date: February 6, 2014Inventors: Lawrence LUM, Michael G. ROTH, Baozhi CHEN, Chuo CHEN, Michael E. DODGE, Wei TANG
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Publication number: 20140038988Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Franz VON NUSSBAUM, Dagmar KARTHAUS, SONJA ANLAUF, Martina DELBECK, Volkhart Min-Jian LI, Daniel MEIBOM, Klemens LUSTIG
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Patent number: 8637528Abstract: A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.Type: GrantFiled: May 4, 2009Date of Patent: January 28, 2014Assignee: Omeros CorporationInventors: John E Bergmann, Neil S Cutshall, Gregory A Demopulos, Vincent A Florio, George Gaitanaris, Patrick Gray, John Hohmann, Rene Onrust, Hongkui Zeng
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Publication number: 20140024654Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.Type: ApplicationFiled: September 18, 2013Publication date: January 23, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Jason W. Brown, Anthony R. Gangloff, Andre K. Kiryanov
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Publication number: 20140024657Abstract: 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 (1)-(7), (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: September 20, 2013Publication date: January 23, 2014Applicant: President and Fellows of Harvard CollegeInventors: Junying YUAN, Emily S. Hsu
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Publication number: 20140024662Abstract: The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associate with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described.Type: ApplicationFiled: September 25, 2013Publication date: January 23, 2014Applicants: Shanghai Institute of Organic Chemistry, President and Fellows of Harvard CollegeInventors: Junying YUAN, Chengye Yuan, Alexei Degterev
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Publication number: 20140023614Abstract: The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity.Type: ApplicationFiled: March 21, 2012Publication date: January 23, 2014Inventors: Dinesh Barawkar, Tanushree Bende, Robert Zahler, Anish Bandyopadhyay, Robindro Singh Sarangthem, Jignesh Doshi, Yogesh Waman, Rushikesh Jadhav, Umesh Prasad Singh
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Patent number: 8633212Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.Type: GrantFiled: March 12, 2010Date of Patent: January 21, 2014Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbHInventors: Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian McKeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
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Publication number: 20140018361Abstract: The present invention provides furano- and pyrrolo-pyrimidine and pyridine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Geraldine C. Harriman, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Publication number: 20140018343Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Patent number: 8629272Abstract: The present invention relates to compounds having the general formula (I) with the definitions of X1-X3, Y1, Y2, L1, R1 and R2 given below and/or solvates, hydrates, esters and pharmaceutically acceptable salts thereof. Furthermore, the invention relates to the use of said compounds for modulating of the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.Type: GrantFiled: June 25, 2010Date of Patent: January 14, 2014Assignee: Deutsches KrebsforschungszentrumInventors: Florian Fuchs, Daniel Gilbert, Corinna Koch, Rajendra-Prasad Maskey, Sandra Steinbrink, Michael Boutros
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Patent number: 8629155Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: March 15, 2012Date of Patent: January 14, 2014Assignee: Merck Sharp & Dohme, Corp.Inventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
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Patent number: 8629154Abstract: The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors. In general formulas 1 and 2 R1 represents hydrogen or C1-C3 alkyl; R2 represents C1-C3 alkyl; R3 represents hydrogen, one or more optionally identical halogens, C1-C3 alkyl or hydroxyl optionally substituted with C1-C3 alkyl; n represents the whole numbers 1, 2 or 3.Type: GrantFiled: January 23, 2009Date of Patent: January 14, 2014Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Nikolay Filippovich Savchuk
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Patent number: 8623885Abstract: Compounds of Formula I are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula I have the following structure: where R1 is a group of Formula IA, Formula IB, Formula IC, or Formula ID and the definitions of the other variables are provided herein.Type: GrantFiled: March 21, 2012Date of Patent: January 7, 2014Assignee: Amgen Inc.Inventors: Xiaoqi Chen, Kang Dai, Jason Duquette, Michael W. Gribble, Jr., Justin N. Huard, Kathleen S. Keegan, Zhihong Li, Sarah E. Lively, Lawrence R. McGee, Mark L. Ragains, Xianghong Wang, Margaret F. Weidner, Jian Zhang
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Publication number: 20140005182Abstract: The present invention is directed to benzoquinazilinone 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: August 29, 2013Publication date: January 2, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng Di Marco, Thomas J. Greshock
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Patent number: 8618121Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4?,3?:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: GrantFiled: July 1, 2008Date of Patent: December 31, 2013Assignee: Cancer Research Technology LimitedInventors: Ian Collins, John Charles Reader, Suki Klair, Jane Scanlon, Glynn Addison, Michael Cherry