Additional Hetero Ring Attached Directly Or Indirectly To The Morpholines By Nonionic Bonding Patents (Class 514/232.2)
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Publication number: 20120288492Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.Type: ApplicationFiled: December 27, 2010Publication date: November 15, 2012Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Mann-Yan Kuo, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
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Publication number: 20120282252Abstract: The invention relates to the use of compounds of formula (I) or (II) in the treatment of mammalian target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.Type: ApplicationFiled: July 17, 2012Publication date: November 8, 2012Applicant: NOVARTIS AGInventor: Carlos Garcia-Echeverria
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Publication number: 20120283255Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, and Y have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 27, 2012Publication date: November 8, 2012Inventors: Pierre DEPREZ, Hélène Jary, Taoues Temal
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Publication number: 20120264749Abstract: The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: March 13, 2012Publication date: October 18, 2012Inventors: Sara Sabina Hadida-Ruah, Hayley Marie Binch, Michael Paul DeNinno, Lev Tyler Dewey Fanning, Bryan A. Frieman, Peter Diederik Jan Grootenhuis, Nicole Hilgraf, Pramod Joshi, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Alina Silina, Urvi Jagdishbhai Sheth, Dennis James Hurley, Vijayalaksmi Arumugam
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Publication number: 20120255502Abstract: A method of treatment and a package that is designed to accomplish this. The package provides the pet owner with a pack containing individual doses of topically applied medications pre-packaged with an oral taste treat. The topically applied medication contains at least one pharmaceutically active ingredient selected from the group of chemical families comprising phenylpyrazoles, macrocyclic lactones, neonicotinoids, synthetic pyrethroids, insect growth regulators, amidines, semicarbazones, spinosyns, octadepsipeptides, and pyrazinoisoquinolines, or any combination thereof. The treat can be administered either before the topically applied treatment is given so as to relax and distract the pet, or after the treatment is given so as to reward the pet and help it forget the stress of treatment. The treat can also be shaped to signify the type of animal to be treated.Type: ApplicationFiled: March 29, 2012Publication date: October 11, 2012Applicant: ALLEVA ANIMAL HEALTH LIMITEDInventor: Robert HOLMES
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Publication number: 20120258947Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2012Publication date: October 11, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Publication number: 20120252802Abstract: Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.Type: ApplicationFiled: March 27, 2012Publication date: October 4, 2012Applicant: Pathway Therapeutics Inc.Inventors: S. David Brown, David J. Matthews
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Publication number: 20120238540Abstract: The invention relates to certain amino-pyrimidine compounds that inhibit IKK epsilon and/or TBK1, methods of making such compounds, pharmaceutical compositions comprising such compounds, and the use of these compounds in treating a variety of diseases and disorders.Type: ApplicationFiled: April 12, 2012Publication date: September 20, 2012Applicant: Myrexis, Inc.Inventors: Ryan C. HOLCOMB, Kazuyuki Suzuki, Robert J. Halter, Paul R. Sebahar, Donald A. McLeod, Mark D. Shenderovich, Kraig M. Yager, Matthew Gregory Bursavich, Ashantai J. Yungai, Burt Richards, Paul L. Bartel, Daniel A. Wettstein
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Publication number: 20120225859Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Matthew BURGER, Zhi-Jie NI, Sabina PECCHI, Gordana ATALLAH, Sarah BARTULIS, Kelly FRAZIER, Aaron SMITH, Joelle VERHAGEN, Yanchen ZHANG, Allan WAGMAN, Simon NG, Keith PFISTER, Daniel POON, Alicia LOUIE, Teresa PICK, Paul BARSANTI, Edwin IWANOWICZ, Wendy FANTL, Thomas HENDRICKSON, Mark KNAPP, Hanne MERRITT, Charles VOLIVA, Marion WIESMANN, Xiaohua XIN
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Publication number: 20120225847Abstract: The present application discloses novel squaric acid derivatives of the formula A: from —C(?O)—, —S(?O)2—, —C(?S)— and —P(?O)(R5)—; B: -, —O—, —NR6— and —C(?O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylType: ApplicationFiled: June 24, 2009Publication date: September 6, 2012Inventors: Mette Knak Christensen, Fredrik Bjorkling
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Patent number: 8252789Abstract: The present invention provides compositions and methods for treating lysosomal disorders using a class of substituted imidazole derivatives or compounds.Type: GrantFiled: November 26, 2008Date of Patent: August 28, 2012Assignee: Neuraltus Pharmaceuticals, Inc.Inventors: Clifford A. Lingwood, Michael S. McGrath, Arasteh Ari Azhir
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Patent number: 8252308Abstract: The present invention provides a substantially clear gel designed to reduce itching discomfort when applied to the vulvar tissue. The gel includes at least one anesthetic, protectant, emulsifier, and pH modifier, such as a base. The gel has a pH adapted to vulvar use and may be applied to the vulvar tissues.Type: GrantFiled: January 27, 2005Date of Patent: August 28, 2012Assignee: C.B. Fleet Company Inc.Inventors: Nelson Ayala, Michael L. Caswell
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Publication number: 20120214788Abstract: The invention relates to novel heteroaryl-substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular diseases and tumour diseases.Type: ApplicationFiled: February 20, 2012Publication date: August 23, 2012Applicant: Bayer Pharma AktiengesellschaftInventors: Dirk Heimbach, Susanne Röhrig, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Yolanda Cancho Grande, Mario Jeske, Kersten Matthias Gericke
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Publication number: 20120202806Abstract: The present invention relates to new hepcidin antagonists, pharmaceutical compositions containing them and the use thereof as a drug, in particular for the treatment of iron metabolism disorders such as, in particular, iron deficiency diseases and anaemia, in particular anaemia associated with chronic inflammatory disease (ACD: anaemia of chronic disease and AI: anaemia of inflammation).Type: ApplicationFiled: August 31, 2010Publication date: August 9, 2012Applicant: VIFOR (INTERNATIONAL) AGInventors: Franz Dürrenberger, Susanna Burckhardt, Peter O. Geisser, Wilm Buhr, Felix Funk, Julia M. Bainbridge, Vincent A. Corden, Stephen M. Courtney, Tara Davenport, Stefan Jaeger, Mark P. Ridgill, Mark Slack, Christopher J. Yarnold, Wei Tsung Yau
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Patent number: 8236795Abstract: The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: March 24, 2010Date of Patent: August 7, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Elena Kostik, Teresa Przewloka, Howard P. Ng, Dinesh Chimmanamada, Zachary Demko
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Patent number: 8217036Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.Type: GrantFiled: August 26, 2011Date of Patent: July 10, 2012Assignee: Wyeth LLCInventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo Dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
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Patent number: 8217035Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: GrantFiled: January 22, 2007Date of Patent: July 10, 2012Assignee: Novartis AGInventors: Matthew Burger, Zhi-Jie Ni, Sabina Pecchi, Gordana Atallah, Sarah Bartulis, Kelly Frazier, Aaron Smith, Joelle Verhagen, Yanchen Zhang, Allan Wagman, Simon Ng, Keith Pfister, Daniel Poon, Alicia Louie, Teresa Pick, Paul Barsanti, Edwin Iwanowicz, Wendy Fantl, Thomas Hendrickson, Mark Knapp, Hanne Merritt, Charles Voliva, Marion Wiesmann, Xiaohua Xin
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Publication number: 20120149695Abstract: Disclosed are dihydropyrimidine compounds and preparation methods, pharmaceutical compositions and uses thereof. Specifically, the compounds described herein in general formula (I), or their isomers, pharmaceutically acceptable salts or hydrates are provided, wherein each variable has the meaning as defined in the description. Also provided are a process for preparing the compounds of the general formula (I), the use of the compounds, an isomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof as a medicament, in particular as a medicament for the treatment and/or prevention of Hepatitis B.Type: ApplicationFiled: May 27, 2010Publication date: June 14, 2012Applicant: INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A.Inventors: Song Li, Xiaoqian Xu, Guoming Zhao, Lili Wang, Hua Guan, Junhai Xiao, Wu Zhong, Zhibing Zheng, Yunde Xie, Xingzhou Li, Xiaokui Wang, Xinbo Zhou, Hongying Liu
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Publication number: 20120115855Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 2, 2009Publication date: May 10, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 8173647Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.Type: GrantFiled: February 6, 2008Date of Patent: May 8, 2012Inventors: Gordana Atallah, Sarah Bartulis, Matthew Burger, Hanne Merritt, Simon Ng, Zhi-Jie Ni, Sabina Pecchi, Keith B. Pfister, Aaron Smith, Charles Voliva, Allan Wagman, Yanchen Zhang
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Publication number: 20120108566Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: November 1, 2011Publication date: May 3, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Yonghong Song, Qing Xu, Jack W. Rose, Zhaozhong J. Jia, Brian Kane, Wolin Huang, Anjali Pandey, Mukund Mehrotra
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Publication number: 20120101079Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: October 19, 2011Publication date: April 26, 2012Applicant: Grunenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Publication number: 20120100227Abstract: The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating a variety of diseases and disorders, including cell proliferative disorders, especially cancer.Type: ApplicationFiled: March 4, 2010Publication date: April 26, 2012Applicant: University of Florida Research FoundationInventors: Vita Golubovskaya, David A. Ostrov, William G. Cance
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Publication number: 20120101072Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: December 21, 2011Publication date: April 26, 2012Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
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Patent number: 8148367Abstract: Disclosed are compounds, pharmaceutical compositions, kits, articles of manufacture, methods of using, and methods of preparing compounds having the formula: wherein the variables are as defined herein. The disclosed compounds are inhibitors of Renin.Type: GrantFiled: January 9, 2008Date of Patent: April 3, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Lily Kwok, Betty Lam, Zhe Li, Zhiyuan Zhang
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Publication number: 20120077807Abstract: Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.Type: ApplicationFiled: June 24, 2011Publication date: March 29, 2012Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-sen Lai, Daniel P. O'Connell, Wengen Wu, Christopher P. Kiritsy
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Publication number: 20120077808Abstract: Disclosed are heterocyclylalkyl-substituted and heteroaralkyl-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.Type: ApplicationFiled: June 24, 2011Publication date: March 29, 2012Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-sen Lai, Daniel P. O'Connell, Wengen Wu, Christopher P. Kiritsy
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Patent number: 8138177Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthmaType: GrantFiled: March 2, 2006Date of Patent: March 20, 2012Assignee: Pfizer Inc.Inventors: Kazuo Ando, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
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Publication number: 20120045454Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: November 3, 2011Publication date: February 23, 2012Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Publication number: 20120040977Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: February 22, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20120015941Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: ApplicationFiled: July 23, 2008Publication date: January 19, 2012Applicant: CRESTONE, INC.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20110319392Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: ApplicationFiled: March 10, 2010Publication date: December 29, 2011Inventors: George Adjabeng, Erich Baum, Neil Bifulco, JR., Ronda G. Davis-Ward, Scott Howard Dickerson, Kelly Horne Donaldson, Keith Hornberger, Kimberly Petrov, Tara Renae Reheault, Douglas McCord Sammond, Gregory M. Schaaf
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Publication number: 20110312955Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.Type: ApplicationFiled: August 26, 2011Publication date: December 22, 2011Inventors: Aranapakam Mudumbai VENKATESAN, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
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Publication number: 20110294798Abstract: The invention relates to cyclic hydrazone compounds, compositions including the cyclic hydrazone compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: ApplicationFiled: December 23, 2010Publication date: December 1, 2011Applicant: Synta Pharmaceuticals Corp.Inventors: Zachary Demko, Lijun Sun, Howard P. Ng
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Publication number: 20110294662Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.Type: ApplicationFiled: April 14, 2011Publication date: December 1, 2011Applicant: Bayer CropScience AGInventors: Thomas SEITZ, Jürgen Benting, Ulrike Wachendorff-Neumann
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Publication number: 20110294749Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: ApplicationFiled: June 28, 2011Publication date: December 1, 2011Applicant: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110274648Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: November 4, 2010Publication date: November 10, 2011Inventors: Rico Lavoie, John A. Bender, Zhong Yang, Makonen Belema, Omar D. Lopez, Qi Chen, Gan Wang, Piyasena Hewawasam
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Publication number: 20110256064Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 15, 2011Publication date: October 20, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
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Patent number: 8039469Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.Type: GrantFiled: May 22, 2009Date of Patent: October 18, 2011Assignee: Wyeth LLCInventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
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Publication number: 20110237579Abstract: The invention relates to non-macrocyclic, non-peptidic, substituted heterocyclic compounds useful for inhibiting hepatitis C virus (“HCV”) replication, particularly functions of the non-structural 5A (“NS5A”) protein of HCVType: ApplicationFiled: December 2, 2009Publication date: September 29, 2011Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 7994329Abstract: Compounds that are ligands for the growth hormone secretagogue receptor type 1A (GHS-R 1A), as well as pharmaceutically acceptable salts of such compounds, are useful for the manufacture of medicaments for the regulation of food intake.Type: GrantFiled: June 19, 2006Date of Patent: August 9, 2011Assignee: Helsinn Therapeutics (U.S.), Inc.Inventor: Michael Ankerson
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Publication number: 20110172215Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: ApplicationFiled: May 4, 2009Publication date: July 14, 2011Inventors: George Adjabeng, Jeffrey Leroy Adams, Scott Howard Dickerson, Keith Hornberger, Neil W. Johnson, Kevin Kuntz, Kimberly Petrov, Jeffrey M. Ralph, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, Xinrong Tian, David E. Uehling, Alex G. Waterson, Brian Wilson
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Publication number: 20110166129Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: April 9, 2009Publication date: July 7, 2011Inventors: Michelle R. Machacek, Andrew Haidle, Anna A. Zabierek, Kaleen M. Konrad, Michael D. Altman
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Publication number: 20110136799Abstract: Compounds of formula (I): wherein A, B, C, D, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, m, n, p, q, r, t, u, and v are defined herein. Also disclosed is a method for treating hepatitis C virus infection with these compounds.Type: ApplicationFiled: December 2, 2010Publication date: June 9, 2011Applicant: National Health Research InstitutesInventors: Jyh-Haur Chern, Yu-Sheng Chao
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Publication number: 20110135599Abstract: The present application includes novel inhibitors of HCV, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Applicant: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Mingzhe Ji, Choung U. Kim, Hyung-jung Pyun, Xiaoning C. Sheng, Qiaoyin Wu
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Publication number: 20110130386Abstract: A compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 and RN2 are selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms.Type: ApplicationFiled: April 24, 2009Publication date: June 2, 2011Inventors: Mark Frigerio, Heather Mary Ellen Duggan, Marc Geoffrey Hummersone, Keith Allan Menear, Niall Morrison Barr Martin, Celine Cano, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle
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Publication number: 20110112051Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.Type: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Applicant: Alantos Pharmaceuticals Holding, Inc.Inventors: Heiko KROTH, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
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Publication number: 20110112075Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: August 18, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Markus FOLLMANN, Volkmar WEHNER, Jerome MENEYROL, Jean-Michel ALTENBURGER, Frédéric PETIT, Gilbert LASSALLE, Jean-Pascal HERAULT
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Publication number: 20110105483Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperprolif erative disorders, such as cancer, in a subject in need thereof.Type: ApplicationFiled: February 8, 2008Publication date: May 5, 2011Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan Michael Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Przewloka
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Publication number: 20110105486Abstract: Wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.Type: ApplicationFiled: December 6, 2010Publication date: May 5, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Takao Nakajima, Masamori Sugawara, Shin-ichi Uchida, Tetsuji Ohno, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato