Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
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Publication number: 20130231342Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).Type: ApplicationFiled: July 27, 2011Publication date: September 5, 2013Applicant: Oryzon Fenomics S.A.Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
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Publication number: 20130225643Abstract: It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) I2 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) I2 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.Type: ApplicationFiled: April 4, 2013Publication date: August 29, 2013Applicant: ONO PHARMACEUTICAL CO., LTD.Inventor: ONO PHARMACEUTICAL CO., LTD.
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Publication number: 20130225596Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 9, 2011Publication date: August 29, 2013Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
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Publication number: 20130224299Abstract: A method for the treatment of chronic obstructive pulmonary disease (COPD), including administering to a patient suffering from COPD, a therapeutically effective amount of roflumilast having a purity of greater than or equal to 99% by weight, and N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.Type: ApplicationFiled: April 10, 2013Publication date: August 29, 2013Applicant: NYCOMED GMBHInventors: Bernhard KOHL, Bernd MUELLER, Walter PALOSCH
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Patent number: 8518977Abstract: 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: GrantFiled: September 28, 2011Date of Patent: August 27, 2013Assignee: 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
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Patent number: 8518948Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: GrantFiled: March 10, 2011Date of Patent: August 27, 2013Assignee: Ingenium Pharmaceuticals GmbHInventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Patent number: 8519142Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: September 14, 2012Date of Patent: August 27, 2013Assignee: Novartis AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20130217706Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease; and other diseases.Type: ApplicationFiled: September 13, 2012Publication date: August 22, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Yoúng-Jun Shin, Pureza Vallar, Ning Zou -
Publication number: 20130210835Abstract: A composition of an antitussive, a decongestant, or an antihistamine to treat respiratory and oral pharyngeal congestion and related symptoms in a patient.Type: ApplicationFiled: June 13, 2011Publication date: August 15, 2013Applicant: GM PHARMACEUTICAL, INCInventor: Odes W. Mitchell
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Publication number: 20130210866Abstract: Disclosed herein is use of one or more aminopyridines in methods and compositions for treatment of impairments in gait or balance in patients with multiple sclerosis.Type: ApplicationFiled: February 13, 2013Publication date: August 15, 2013Applicant: Acorda Therapeutics, Inc.Inventor: Acorda Therapeutics, Inc.
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Patent number: 8507536Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: August 10, 2012Date of Patent: August 13, 2013Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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Patent number: 8501788Abstract: This invention is generally directed to a method for recovering flunixin and flunixin analogs from pharmaceutical compositions. The recovered flunixin and analogs can be, for example, reused to make new pharmaceutical compositions and thereby reduce the need and expense of manufacturing new flunixin and flunixin analogs.Type: GrantFiled: December 12, 2008Date of Patent: August 6, 2013Assignee: Intervet Inc.Inventors: James C. Towson, Donal Coveney
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Patent number: 8501943Abstract: The present disclosure is directed to the sodium salt of 5-cyclopropyl-2-{[2-(2,6-difluorophenyl)pyrimidin-5-yl]amino}benzoic acid, pharmaceutically acceptable solvates thereof, pharmaceutical combinations thereof, and methods of treatment.Type: GrantFiled: March 11, 2010Date of Patent: August 6, 2013Assignee: Almirall, S.A.Inventors: Nuria Garcia Gonzalez, Francesc Carrera Carrera, Monserrat Julia Jane, Laurent Debethune, Xavier Serra Masia
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Publication number: 20130196993Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: September 28, 2011Publication date: August 1, 2013Inventors: Michael Berger, Christopher Kern, Marko Eck
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Publication number: 20130197040Abstract: Provided are polymorphs I to VIII of a dalfampridine or of its solvates, a preparation method therefore, and applications thereof as an active component of a medicine. Said polymorphs Ito VIII of the dalfampridine or of its solvents can be used to prepare formulations for improving the walking speed of patients of multiple sclerosis and for alleviating other symptoms of multiple sclerosis.Type: ApplicationFiled: October 8, 2011Publication date: August 1, 2013Applicants: TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD., TIANJIN HEMAY BIO-TECH CO., LTD.Inventors: Hesheng Zhang, Xin Chen
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Patent number: 8492410Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: February 6, 2013Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Publication number: 20130184316Abstract: The invention provides methods for treating, suppressing, ameliorating and/or preventing the effects of disorders relating to concussion, including those associated with post-concussion syndrome. The methods comprise administering to a subject an effective amount of a compound that modulates neuronal ion channel function, or a pharmaceutically acceptable salt, solvate or hydrate thereof, or a composition comprising a compound that modulates neuronal ion channel function, or a pharmaceutically acceptable salt, solvate or hydrate thereof, and a pharmaceutically acceptable carrier. The invention also provides inventive methods relating to identifying, classifying and/or diagnosing conditions involving post-concussion syndrome and related concussive disorders.Type: ApplicationFiled: July 7, 2011Publication date: July 18, 2013Inventor: Andrew Hornstein
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Publication number: 20130184315Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: July 18, 2011Publication date: July 18, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbHInventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
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Publication number: 20130183289Abstract: The invention relates to compositions, methods, and kits for treating subjects infected by or at risk of infection with a DNA virus (e.g., a JC Virus or a BK virus). Aspects of the invention are useful to prevent or treat DNA virus associated conditions (e.g., PML) in subjects that are immunocompromised. Compositions are provided that inhibit intracellular replication of DNA viruses.Type: ApplicationFiled: September 13, 2008Publication date: July 18, 2013Applicant: Biogen Idec MA IncInventors: Leonid Gorelik, Margot Brickelmaier, Alexey Lugovskoy
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Publication number: 20130184314Abstract: The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: MERCK PATENT GMBHInventors: Andreas Goutopoulos, Henry YU, Benny C. Askew, JR., Lesley Liu-Bujalski
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Patent number: 8486950Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereof.Type: GrantFiled: June 10, 2010Date of Patent: July 16, 2013Assignee: F. Hoffmann-La Roche AGInventors: Simon Charles Goodacre, Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Mark S. Stanley, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang, Aihe Zhou
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Publication number: 20130178446Abstract: The present invention is directed to the topical application of the malonamide ACAT inhibitors described by Formula I. Other aspects of the invention are directed to topical formulations of these diamides, their use to treat sebaceous gland disorders and their use to alleviate oily skin.Type: ApplicationFiled: March 4, 2013Publication date: July 11, 2013Applicant: Medicis Pharmaceutical CorporationInventors: Catherine R. Kostlan, Raj Neil Raheja, Meera Tugnait, Kimberly Wade
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Patent number: 8481569Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1Dadrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: October 7, 2010Date of Patent: July 9, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Masato Yoshida, Nobuki Sakauchi, Ayumu Sato
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Publication number: 20130172310Abstract: 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: ApplicationFiled: September 12, 2012Publication date: July 4, 2013Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: 8476269Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: July 9, 2012Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
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Patent number: 8476249Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.Type: GrantFiled: May 6, 2010Date of Patent: July 2, 2013Assignee: GlaxoSmithKline LLCInventors: Connie L. Erickson-Miller, Michael Arning
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Patent number: 8470859Abstract: Provided are an iminopyridine derivative having a selective ?1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like, and a screening method for a compound having an ?1D adrenergic receptor antagonistic action. An ?1D adrenergic receptor antagonist containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof, and a method of screening for an agent having an ?1D adrenergic receptor antagonistic action for the prophylaxis or treatment of a lower urinary tract disease, which includes measuring the bladder smooth muscle tension of rats with bladder outlet obstruction.Type: GrantFiled: October 22, 2007Date of Patent: June 25, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Masato Yoshida, Tomohiko Suzaki, Yasuhisa Kohara, Haruhiko Kuno, Hiroshi Nagabukuro, Reiko Saikawa, Yuuichi Okabe, Shigemitsu Imai
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Publication number: 20130158070Abstract: Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and/or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis.Type: ApplicationFiled: September 6, 2011Publication date: June 20, 2013Inventor: Taher Nassar
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Publication number: 20130158035Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: August 23, 2011Publication date: June 20, 2013Applicant: Brigham Young UniversityInventor: Marc Hansen
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Publication number: 20130150410Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with ion channel modulators. In these methods, the ion channel modulator compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of the ion channel modulator compositions and formulations onto the auris interna target areas, or via perfusion into the auris interna structures.Type: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, OTONOMY, INC.Inventors: OTONOMY, INC., THE REGENTS OF THE UNIVERSITY OF CALIF
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Publication number: 20130150414Abstract: Specific amine derivatives have been found to possess excellent activities as pest control agents.Type: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Shinzo KAGABU, Masaaki MITOMI, Shigeki KITSUDA, Ryo HORIKOSHI, Masahiro NOMURA, Yasumichi ONOZAKI
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Publication number: 20130150368Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R2, R4, R5, R6, R7, R8, R9, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 22, 2011Publication date: June 13, 2013Applicant: CYTOKINETICS, INC.Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R. Muci, Xiangping Qian, Antonio Romero, Jeffrey Warrington, Zhe Yang
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Patent number: 8461183Abstract: The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.Type: GrantFiled: May 26, 2009Date of Patent: June 11, 2013Assignee: GenfitInventors: Christophe Masson, Karine Caumont-Bertrand
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Publication number: 20130143910Abstract: A method and composition for treating cancer cells that targets fructose-1,6-biphosphataseenzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways.Type: ApplicationFiled: November 14, 2012Publication date: June 6, 2013Inventor: Zhang Weihua
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Publication number: 20130143932Abstract: The present invention discloses optically pure (R) and (S) Phenyramidol enantiomers and their pharmaceutically acceptable salts, a process for synthesizing such enantiomers by means of a styrene oxide based synthesis, and also a clinical evaluation of (R) and (S) enantiomers of Phenyramidol, their salts and compositions thereof for enhanced/newer therapeutic benefits.Type: ApplicationFiled: January 28, 2013Publication date: June 6, 2013Applicant: FERMENTA BIOTECH (UK) LIMITEDInventor: FERMENTA BIOTECH (UK) LIMITED
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Publication number: 20130143861Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling.Type: ApplicationFiled: February 4, 2013Publication date: June 6, 2013Applicant: ARMETHEON, INC.Inventor: Armetheon, Inc.
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Patent number: 8455501Abstract: The present invention relates to compounds of the formula wherein R1 to R3 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: GrantFiled: September 10, 2012Date of Patent: June 4, 2013Assignee: Hoffmann-La Roche IncInventors: Uwe Grether, Stephan Roever
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Patent number: 8455688Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N, wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15, wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.Type: GrantFiled: March 21, 2012Date of Patent: June 4, 2013Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson
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Publication number: 20130137660Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: January 22, 2013Publication date: May 30, 2013Applicant: YM Biosciences Australia Pty LtdInventor: YM Biosciences Australia Pty Ltd
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Publication number: 20130136794Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.Type: ApplicationFiled: April 21, 2011Publication date: May 30, 2013Applicant: PEKING UNIVERSITYInventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
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Patent number: 8450348Abstract: The present invention provides derivatives of squaric acid, in particular derivatives of 3,4-diamino-cyclobut-3-ene-1,2-dione and tautomers and isomers thereof, as a single stereoisomer or a mixture of stereoisomers, or as a pharmaceutically acceptable salt thereof. These compounds show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: GrantFiled: February 21, 2007Date of Patent: May 28, 2013Assignee: Forma TM, LLCInventors: Krishna K. Murthi, Roland Köstler, Chase Smith, Tilman Brandstetter, Arthur F. Kluge
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Publication number: 20130131056Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.Type: ApplicationFiled: January 15, 2013Publication date: May 23, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130131123Abstract: An immediate release solid dosage form in tablet or pellet form for oral administration of a PDE 4 inhibitor, comprising a PDE 4 inhibitor that is N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide (roflumilast) or a salt thereof, and one or more suitable pharmaceutical excipients; wherein said dosage form contains 500 ?g of the roflumilast or salt thereof.Type: ApplicationFiled: January 11, 2013Publication date: May 23, 2013Applicant: Nycomed GmbHInventors: Rango DIETRICH, Hartmut NEY, Klaus EISTETTER
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Publication number: 20130131036Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: October 23, 2012Publication date: May 23, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Patent number: 8445520Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.Type: GrantFiled: December 21, 2011Date of Patent: May 21, 2013Assignee: Pfizer Inc.Inventors: Hengmiao Cheng, Xiao Hu, Kevin D. Jerome, Mark G. Obukowicz, Lisa Maria Olson, Paul V. Rucker, Ronald Keith Webber
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Publication number: 20130121919Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.Type: ApplicationFiled: June 11, 2012Publication date: May 16, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
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Patent number: 8440703Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at about 12 hours and the use of the composition to treat various neurological diseases, including multiple sclerosis. A method of selecting individuals based on responsiveness to a treatment, including, for example, identifying individuals who responded to treatment with a sustained release fampridine composition.Type: GrantFiled: November 18, 2011Date of Patent: May 14, 2013Assignee: Acorda Therapeutics, Inc.Inventors: Andrew R. Blight, Ron Cohen
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Patent number: 8440652Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: GrantFiled: March 2, 2012Date of Patent: May 14, 2013Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
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Publication number: 20130109725Abstract: Provided herein are methods and compositions for improving the dispersion properties in water of a pesticide-containing granule with a water soluble agglomeration suppressant.Type: ApplicationFiled: October 31, 2012Publication date: May 2, 2013Applicant: DOW AGROSCIENCES LLCInventor: DOW AGROSCIENCES LLC
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Publication number: 20130102617Abstract: Phenylacetamide compounds of the formula having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide have an excellent glucokinase activation action. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, as well as metabolic syndrome and obesity.Type: ApplicationFiled: April 18, 2012Publication date: April 25, 2013Applicant: ASTELLAS PHARMA INC.Inventors: Masahiko Hayakawa, Yoshiyuki Kido, Takahiro Nigawara, Mitsuaki Okumura, Akira Kanai, Keisuke Maki, Nobuaki Amino