Ring Nitrogen In The Additional Hetero Ring Patents (Class 514/235.5)
  • Publication number: 20110319378
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: June 3, 2011
    Publication date: December 29, 2011
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
  • Patent number: 8084615
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: December 27, 2011
    Assignees: University of Washington, Novartis Vaccines and Diagnostics, Inc.
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Publication number: 20110312962
    Abstract: The present application discloses novel 2-morpholino-3-amido-pyhcline derivatives and their use as modulators of the voltage gated Kv7 (KCNQ) potassium ion channels in the treatment of pain, neurodegenerative disorders, urinary incontinence, etc. . . . . In other aspects the application discloses the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: November 26, 2009
    Publication date: December 22, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: William Dalby Brown, Carsten Jessen, Dorte Strøbaek
  • Patent number: 8080543
    Abstract: The present invention relates to pyridine substituted ethanol compounds and derivatives thereof having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: December 20, 2011
    Assignee: Merck Sharp & Dohme
    Inventors: B. Wesley Trotter, Kausik K. Nanda, Nathan R. Kett
  • Publication number: 20110306614
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Patent number: 8076329
    Abstract: The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
    Type: Grant
    Filed: April 25, 2006
    Date of Patent: December 13, 2011
    Assignee: Bioprojet
    Inventors: Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz, Olivier Labeeuw
  • Patent number: 8076330
    Abstract: 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: Grant
    Filed: January 13, 2011
    Date of Patent: December 13, 2011
    Assignee: Amgen Inc.
    Inventors: Heiko Kroth, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochgürtel, Fritz-Frieder Frickel, Arthur G. Taveras, Christoph Steeneck
  • Publication number: 20110301140
    Abstract: The present invention is directed to pyridyl carboxamide 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: Application
    Filed: August 4, 2011
    Publication date: December 8, 2011
    Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
  • Publication number: 20110301128
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Application
    Filed: August 22, 2011
    Publication date: December 8, 2011
    Applicant: EXELIXIS, INC.
    Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T. Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B. Mac, Larry W. Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C. Stevens, Tie-Lin Wang, Yong Wang, Jason H. Wu
  • Patent number: 8071594
    Abstract: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the notrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.
    Type: Grant
    Filed: June 22, 2004
    Date of Patent: December 6, 2011
    Assignee: Glaxo Group Limited
    Inventor: John Liddle
  • Patent number: 8071582
    Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
    Type: Grant
    Filed: January 13, 2010
    Date of Patent: December 6, 2011
    Assignee: UCB Pharma S.A.
    Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
  • Publication number: 20110294787
    Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.
    Type: Application
    Filed: July 28, 2011
    Publication date: December 1, 2011
    Applicant: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzèn, William Patrick Watson
  • Publication number: 20110288092
    Abstract: Disclosed are methods of treating hyperproliferative disorders, method of treating inflammatory disorders, and methods of inhibiting MEK activity in a mammal, comprising administering an effective amount of one or more compounds of the Formula V or pharmaceutically acceptable salts thereof, wherein R1, R2, R7, R8, R9 and W are as defined in the specification.
    Type: Application
    Filed: November 22, 2010
    Publication date: November 24, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Patent number: 8063043
    Abstract: Salts of N-[6-(cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4?-(trifluoromethoxy)[1,1?-biphenyl]-3-carboxamide are prepared and characterized.
    Type: Grant
    Filed: September 15, 2009
    Date of Patent: November 22, 2011
    Assignee: Novartis AG
    Inventors: Joginder Bajwa, Marilyn de la Cruz, Stephanie Kay Dodd, Liladhar Murlidhar Waykole, Raeann Wu
  • Patent number: 8063036
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Grant
    Filed: April 7, 2010
    Date of Patent: November 22, 2011
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
  • Publication number: 20110281871
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Application
    Filed: July 26, 2011
    Publication date: November 17, 2011
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20110281851
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Application
    Filed: July 29, 2011
    Publication date: November 17, 2011
    Applicant: THERAVANCE, INC.
    Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
  • Publication number: 20110281872
    Abstract: The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.
    Type: Application
    Filed: March 11, 2011
    Publication date: November 17, 2011
    Applicant: Kinex Pharmaceuticals, LLC
    Inventors: David G. Hangauer, JR., Michael J. Ciesielski, Robert A. Fenstermaker
  • Publication number: 20110281854
    Abstract: Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
    Type: Application
    Filed: May 10, 2011
    Publication date: November 17, 2011
    Inventors: Agustin Casimiro-Garcia, Kentaro Futatsugi, David W. Piotrowski
  • Publication number: 20110281850
    Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.
    Type: Application
    Filed: July 7, 2011
    Publication date: November 17, 2011
    Applicant: MANNKIND CORPORATION
    Inventors: Gary A. Flynn, Sandra Aeyoung Lee, Mary Faris, David William Brandt, Subrata Chakravarty
  • Publication number: 20110281837
    Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
    Type: Application
    Filed: January 3, 2011
    Publication date: November 17, 2011
    Inventors: Alan J. Hutchinson, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
  • Publication number: 20110280831
    Abstract: The present invention provides a combination which comprises (a) methotrexate and (b) a non-hepatotoxic DHODH inhibitor of formula (I): wherein: R1 is selected from the group consisting of hydrogen atoms, halogen atoms, C1-4 alkyl, C3-4 cycloalkyl, —CF3 and —OCF3, R2 is selected from the group consisting of hydrogen atoms, halogen atoms and C1-4 alkyl groups, R3 is selected from the group consisting of —COOR5, —CONHR5, tetrazolyl, —SO2NHR5 and —CONHSO2R5 groups, wherein R5 is selected from the group consisting of a hydrogen atom and linear or branched C1-4 alkyl groups, R4 is selected from the group consisting of a hydrogen atom and a C1-4 alkyl group, R9 is selected from the group consisting of a hydrogen atom and a phenyl group, G1 represents a group selected from N and CR6 wherein R6 is selected from the group consisting of hydrogen atoms, halogen atoms, C1-4 alkyl, C3-4 cycloalkyl, C1-4 alkoxy, —CF3, —OCF3, monocyclic N-containing C5-7 heteroaryl, monocyclic N— containing C3-7 heterocyclyl groups and C6-1
    Type: Application
    Filed: January 19, 2010
    Publication date: November 17, 2011
    Inventors: Nuria Godessart Marina, Maria Pilar Pizcueta Lalanza
  • Publication number: 20110275616
    Abstract: Methods of utilizing an opioid agonist in a mammalian subject in a manner that inhibits peripheral effects of the opioid agonist are described. The methods comprise administering the opioid agonist in an amount sufficient to confer analgesia the subject and co-administering a neutral opioid antagonist or pharmaceutically acceptable isomorph or pharmaceutically acceptable salt thereof in an amount sufficient to substantially inhibit peripheral effects and insufficient to block substantial central effects of the opioid agonist in the subject.
    Type: Application
    Filed: July 18, 2011
    Publication date: November 10, 2011
    Applicant: AIKO BIOTECHNOLOGY
    Inventors: Wolfgang Sadée, Edward Bilsky, Janet Yancey-Wrona
  • Publication number: 20110275615
    Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or un
    Type: Application
    Filed: October 29, 2010
    Publication date: November 10, 2011
    Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
  • Patent number: 8048898
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: (wherein Y1 represents a nitrogen atom or a group represented by CRA, Y2 represents a nitrogen atom or a group represented by CRB, Y3 represents a nitrogen atom or a group represented by CRC, RA, RB and RC, which may be the same or different, each represent a hydrogen atom, etc. (excluding the case where Y1 is CRA, Y2 is CRB and Y3 is CRC), X represents an oxygen atom, etc., R1 represents a C1-C6 alkyl group, etc., R2 represents a C1-C6 alkyl group, etc., R3 represents an optionally substituted phenyl group, etc., R4 represents a hydrogen atom, etc., and R5 represents an optionally substituted phenyl group, etc.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: November 1, 2011
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Naoya Ono, Fumiyasu Shiozawa, Tetsuya Yabuuchi, Hironori Katakai
  • Publication number: 20110263540
    Abstract: Small-molecule inhibitors of a protein synthesis inhibiting toxin, e.g., ricin, abrin, Shiga, and Shiga-like toxins, as well as methods of using the inhibitors are provided. Further provided are methods of identifying small-molecule inhibitors of a protein synthesis inhibiting toxin.
    Type: Application
    Filed: July 24, 2009
    Publication date: October 27, 2011
    Inventors: Yuan-Ping Pang, Nilgun Ereken Tumer, Charles B. Millard
  • Publication number: 20110263564
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 29, 2009
    Publication date: October 27, 2011
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Radha Narayan, Jeremy S. Disch, Robert B. Perni, Chi B. Vu
  • Publication number: 20110256064
    Abstract: 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: Application
    Filed: April 15, 2011
    Publication date: October 20, 2011
    Applicant: AC Immune, S.A.
    Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
  • Publication number: 20110257164
    Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.
    Type: Application
    Filed: January 7, 2010
    Publication date: October 20, 2011
    Applicant: ORCHID RESEARCH LABORATORIES LIMITED
    Inventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
  • Publication number: 20110251168
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Application
    Filed: June 16, 2011
    Publication date: October 13, 2011
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Publication number: 20110250197
    Abstract: This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof.
    Type: Application
    Filed: June 1, 2011
    Publication date: October 13, 2011
    Applicant: RANBAXY LABORATORIES
    Inventors: Jitendra A. SATTIGERI, Vinay S. BANSAL
  • Publication number: 20110245222
    Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.
    Type: Application
    Filed: March 31, 2011
    Publication date: October 6, 2011
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
  • Publication number: 20110237586
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: or a pharmaceutically acceptable salt thereof The compounds of the invention are useful for methods of protecting against or treating hearing loss, osteoporosis, cell proliferative disorders, obesity, diabetes, eye disease, stroke, atherosclerosis, neuropathic pain or hepatitis B.
    Type: Application
    Filed: June 3, 2011
    Publication date: September 29, 2011
    Applicant: Kinex Pharmaceuticals, LLC
    Inventor: David G. Hangauer, JR.
  • Publication number: 20110237573
    Abstract: The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.
    Type: Application
    Filed: March 1, 2010
    Publication date: September 29, 2011
    Applicant: IRM LLC
    Inventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
  • Patent number: 8026237
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Grant
    Filed: July 30, 2005
    Date of Patent: September 27, 2011
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B Mac, Larry W Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C Stevens, Tie-Lin Wang, Yong Wang, Jason H Wu
  • Publication number: 20110230467
    Abstract: [Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.
    Type: Application
    Filed: November 20, 2009
    Publication date: September 22, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Shohei Shirakami, Fumie Takahashi, Yutaka Nakajima, Hirofumi Omura, Naohiro Aoyama, Hiroshi Sasaki, Takeshi Hondo, Hiroaki Tominaga
  • Publication number: 20110224209
    Abstract: The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
    Type: Application
    Filed: March 9, 2011
    Publication date: September 15, 2011
    Inventors: Bart L. DeCorte, Renee L. DesJarlais, Yifang Huang, Michael H. Parker, Dennis J. Hlasta
  • Publication number: 20110224204
    Abstract: Di-substituted phenyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. The disclosure also relates to methods for treating neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.
    Type: Application
    Filed: June 25, 2009
    Publication date: September 15, 2011
    Inventors: Richard Chesworth, Gideon Shapiro, Amy Ripka
  • Publication number: 20110224192
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: May 20, 2011
    Publication date: September 15, 2011
    Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
  • Publication number: 20110224179
    Abstract: We disclose a diagnostic test to determine suitable therapeutic intervention of subjects suffering from subclinical Cushing's syndrome [SCS] and also agents that antagonise the action of cortisol or inhibit excess cortisol production in the treatment of conditions such as SCS in the presence of an adrenal incidentaloma.
    Type: Application
    Filed: November 7, 2008
    Publication date: September 15, 2011
    Inventor: John Newell-Price
  • Publication number: 20110224210
    Abstract: The invention relates to novel bis-amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.
    Type: Application
    Filed: November 18, 2009
    Publication date: September 15, 2011
    Inventors: Hamed Aissaoui, Christoph Boss, Olivier Corminboeuf, Marie-Celine Frantz, Corinna Grisostomi
  • Patent number: 8017607
    Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: September 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
  • Publication number: 20110218199
    Abstract: Compounds of formula I are disclosed. These compounds are useful in the control or prevention of cancer.
    Type: Application
    Filed: August 20, 2008
    Publication date: September 8, 2011
    Inventors: Guy Georges, Klaus Kaluza, Matthias Koerner, Ulrike Reiff, Stefan Scheiblich, Wolfgang Von Der Saal, Stefan Weigand
  • Publication number: 20110217383
    Abstract: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40 95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5 60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250 % by weight of a non-porous inert lubricant, 1 to 35 % by weight of a neutral cellulosic compound and 1 to 25 % by weight of an emulsifier, each calculated on dry weight of the polymer mixture.
    Type: Application
    Filed: September 24, 2008
    Publication date: September 8, 2011
    Inventors: Hans Bär, Thomas Fürst, Gerhard Renner, Michael Gottschalk
  • Publication number: 20110218160
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Application
    Filed: May 12, 2011
    Publication date: September 8, 2011
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8012970
    Abstract: The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: September 6, 2011
    Assignee: Universta' Degli Studi di Siena
    Inventors: Mariangela Biava, Fabrizio Manetti, Delia Deidda, Raffaello Pompei, Maurizio Botta, Giulio Cesare Porretta
  • Patent number: 8012969
    Abstract: The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radiopharmaceutical for positron emission tomography.
    Type: Grant
    Filed: January 11, 2006
    Date of Patent: September 6, 2011
    Assignee: GE Healthcare Limited
    Inventors: Christopher John Helal, Gunnar Antoni, Bengt Langstrom, Jia Zhi Sheng, Susan Beth Sobolov-Jaynes, Timothy James McCarthy
  • Patent number: 8012967
    Abstract: There is provided compounds of formula (I), wherein R1, R11, R12, Qa, X, Qb, Qc, A and D have meanings given in the description, or a pharmaceutically acceptable salt or solvate thereof, which compound, salt or solvate binds to the minor groove of DNA.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: September 6, 2011
    Assignee: University of Strathclyde
    Inventors: Abedawn Khalaf, Colin Suckling, Roger Waigh
  • Publication number: 20110212945
    Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
    Type: Application
    Filed: August 8, 2008
    Publication date: September 1, 2011
    Applicant: ALMIRALL, S.A.
    Inventors: Julio Cesar Castro Palomino Laria, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
  • Patent number: 8008296
    Abstract: The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. (Formula I).
    Type: Grant
    Filed: June 28, 2006
    Date of Patent: August 30, 2011
    Assignee: Eli Lilly and Company
    Inventors: Lisa Selsam Beavers, Don Richard Finley, Robert Alan Gadski, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Richard Todd Pickard, Takako Takakuwa, Grant Mathews Vaught