Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
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Patent number: 8299073Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.Type: GrantFiled: December 11, 2009Date of Patent: October 30, 2012Assignee: Respivert Ltd.Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
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Publication number: 20120270888Abstract: Disclosed are pharmaceutical compositions comprising HIV integrase strand transfer inhibitor. More particularly, oral pharmaceutical compositions of raltegravir or its pharmaceutically acceptable salts and process for preparing and use of the same are disclosed.Type: ApplicationFiled: April 13, 2012Publication date: October 25, 2012Inventors: Bandi PARTHASARADHI REDDY, Podili KHADGAPATHI, Goli KAMALAKAR REDDY
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Patent number: 8293748Abstract: There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.Type: GrantFiled: October 2, 2009Date of Patent: October 23, 2012Assignee: Respivert Ltd.Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
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Patent number: 8293729Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: GrantFiled: June 23, 2010Date of Patent: October 23, 2012Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences Inc.Inventors: Brian Dyck, Joe A. Tran, Junko Tamiya, Florence Jovic, Troy Vickers, Chen Chen, Nicole Harriott, Timothy Coon, Neil J. Ashweek
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Publication number: 20120263659Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 22, 2010Publication date: October 18, 2012Applicants: BASF SE, SYMRISE AGInventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
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Publication number: 20120264753Abstract: Disclosed is a novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative represented by general formula (I), which has both angiotensin II receptor antagonist activity and PPAR-? activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative. In general formula (I), ring A represents a group represented by formula (II) or (III); R1 represents a C1-6 alkyl group; R2 represents a C1-6 alkyl group which may be substituted by a hydroxy group, or a group represented by formula —CO—R4 (wherein R4 represents a hydroxy group, a C1-6 alkoxy group, an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group, a morpholino group, a piperidino group or a pyrrolidino group); R3 represents a halogen atom or a C1-6 alkoxy group; and X and Y may be the same or different and each represents a nitrogen atom or CH.Type: ApplicationFiled: December 22, 2010Publication date: October 18, 2012Applicant: KOWA COMPANY, LTD.Inventors: Toru Miura, Hajime Yamada, Junya Tagashira, Gen Watanabe, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
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Publication number: 20120264704Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: October 26, 2007Publication date: October 18, 2012Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
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Publication number: 20120264772Abstract: Provided is an antihypertensive pharmaceutical composition containing Fimasartan, a pharmaceutically acceptable salt thereof, a solvate thereof or a hydrate thereof as an angiotensin II receptor blocker, and Amlodipine, an isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof or a hydrate thereof as a calcium channel blocker.Type: ApplicationFiled: August 8, 2011Publication date: October 18, 2012Inventors: Seung Ho Kim, Ji Han Kim, Je Hak Kim, Kyung Wan Nam, Yong Ha Chi, Joo Han Lee, Soo Heui Paik, So Jeong Yi, Tae Eun Kim, Seo Hyun Yoon, Joo Youn Cho, Sang Goo Shin, In Jin Jang, Kyung Sang Yu
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Patent number: 8288401Abstract: Novel polymorphic forms of bosentan and processes for their preparation are disclosed. Further, pharmaceutical compositions comprising said polymorphic forms and the use of said compositions in the treatment of patients suffering from endothelin receptor mediated disorders, for example, cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris are disclosed.Type: GrantFiled: May 8, 2008Date of Patent: October 16, 2012Assignee: Generics [UK] LimitedInventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Dattaatraya Shinde, Prakash Bansode
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Patent number: 8288371Abstract: Compounds of the formula are disclosed. The compounds are CCR1 antagonists which are useful for the treatment and prevention of inflammatory and autoimmune diseases. Other embodiments are also disclosed.Type: GrantFiled: October 3, 2008Date of Patent: October 16, 2012Assignee: Pharmacopeia, LLCInventors: Vidyadhar M. Paradkar, Marc Brescia, Ray James, Jinqi Liu, Ruiyan Liu, James Robert Merritt, Michelle Morris, Michael J. Ohlmeyer, Chongwu Zhang, Rui Zhang
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Publication number: 20120258973Abstract: The invention relates to compound of the formula (I?) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: December 20, 2010Publication date: October 11, 2012Applicant: NOVARTIS AGInventors: Sangamesh Babiger, Dirk Behnke, Claudia Betschart, Vinod Chaudhari, Murali Chebrolu, Simona Cotesta, Samuel Hintermann, Arndt Meyer, Chetan Pandit
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Patent number: 8278331Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-? kinase, PDGFR-? kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.Type: GrantFiled: October 29, 2009Date of Patent: October 2, 2012Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20120244205Abstract: Nanoparticle (e.g., quantum dot) compositions and methods for delivery of substances (e.g., microbicies, fungicides, pesticides, therapeutic agents, biologics, diagnostic agents, dyes, marker substances or tags, etc.) to desired locations within plants or animals. In some embodiments, the quantum dot or naoparticle may be substantially free of cadmiun. In some embodiments, the methods may be employed to prevent to treat fungus or fungus-like infections in pains, such as agricultural crops.Type: ApplicationFiled: August 25, 2010Publication date: September 27, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Kathleen K. Treseder, Matthew D. Whiteside
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Publication number: 20120234219Abstract: The present inventions generally relate to compositions and methods for providing agricultural chemicals comprising active ingredients (A.I.s) combined with a top dressing for application to cultivated areas of turfgrass. Specifically, the compositions are in the form of moist formulations for providing top dressings comprising active ingredients. Further, the inventions relate to compositions and methods for delivering active ingredients simultaneously with a top dressing composition to golf course turf.Type: ApplicationFiled: May 15, 2012Publication date: September 20, 2012Inventors: A. Ronald Detweiler, Nancy M. Dykema, Joseph M. Vargas, JR.
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Patent number: 8269000Abstract: Substituted pyrimidine and triazine compounds corresponding to formula I wherein R1, R2, R3, R4a, R4b, R5a, R5b, R7, R8, R9a, R9b, R10, R11, A, a, b, s, t, V, W1, W2 and W3 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds, and the use of such compounds and compositions to treat or inhibit pain and/or other disorders or disease states.Type: GrantFiled: October 23, 2009Date of Patent: September 18, 2012Assignee: Gruenenthal GmbHInventors: Stefan Schunk, Melanie Reich, Kamila Hennig, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
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Patent number: 8268848Abstract: A cyclopropane compound represented by the following formula (A) or a pharmaceutically acceptable salt thereof has orexin receptor antagonism, and therefore has a potencial of usefulness for the treatment of sleep disorder for which orexin receptor antagonism is effective, for example, insomnia: wherein Q represents —CH— or a nitrogen atom, R1a and R1b each independently represent a C1-6 alkyl group and the like, R1c represents a hydrogen atom and the like, R2a, R2b, R2c and R2d each independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group and the like, R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom and the like, and R3d represents a hydrogen atom and the like.Type: GrantFiled: September 20, 2011Date of Patent: September 18, 2012Assignee: Eisai R&D Management Co., Ltd.Inventors: Taro Terauchi, Ayumi Takemura, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann, Yuji Kazuta
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Patent number: 8269002Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: GrantFiled: November 17, 2010Date of Patent: September 18, 2012Assignee: AstraZeneca ABInventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Patent number: 8268847Abstract: The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.Type: GrantFiled: August 28, 2007Date of Patent: September 18, 2012Assignee: Actelion Pharmaceuticals, Ltd.Inventor: Martine Clozel
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Publication number: 20120232049Abstract: A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen.Type: ApplicationFiled: February 22, 2008Publication date: September 13, 2012Applicant: Eisai R&D Management Co., Ltd.Inventors: Hiroshi Obaishi, Takayuki Nakagawa, Tomohiro Matsushima, Setsuo Funasaka, Shuji Shirotori, Keiko Takahashi
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Publication number: 20120232083Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.Type: ApplicationFiled: March 7, 2012Publication date: September 13, 2012Inventors: Usa REILLY, Michael MELNICK, Matthew F. BROWN, Mark S. PLUMMER, Justin MONTGOMERY, Ye CHE, Loren PRICE
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Publication number: 20120232101Abstract: The invention provides compounds of formula (I): wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds are useful as MMP inhibitors.Type: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Inventors: David Chapman, Balint Gabos, Magnus Munck af Rosenschöld
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Publication number: 20120232031Abstract: Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.Type: ApplicationFiled: October 19, 2010Publication date: September 13, 2012Applicant: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Petpiboon Peppi Prasit, Isabelle Marguerite Dearmond
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Patent number: 8263602Abstract: The present invention relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metallproteinase enzymes (MMPs).Type: GrantFiled: November 7, 2008Date of Patent: September 11, 2012Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
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Patent number: 8263588Abstract: 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: April 4, 2008Date of Patent: September 11, 2012Assignee: 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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Publication number: 20120225877Abstract: This invention relates provides novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1), wherein R1 is selected from phenethyl, 4,6-dimethoxypyrimidin-2-yl and (2-chloro-5-thiazolyl)methyl and R2 is selected from the group consisting of hydroxy, 4-bromo-2-chlorophenoxy, morpholin-4-yl, (2-chloro-5-thiazolyl)methyloxy, benzyloxy, phenylsulfanyl, benzotriazol-1-yl and 5-chloro-2-fluoroanilino. The present invention also relates to a process for the preparation of novel substituted 1,4-dioxa-8-azaspiro[4,5]decanes of general formula (1). The novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1) has fungicidal activity.Type: ApplicationFiled: March 23, 2010Publication date: September 6, 2012Inventors: Mukund Vinayak Deshpande, Sunita Ranjan Deshpande, Fazal Shirazi, Preeti Madhukar Chaudhary, Nelavelli Malleswara Rao, Baidyanath Mohanty, Nageshwar Nath Sharma, Anand Kumar Bachhawat, Ganesan Kaliannan, Sanjoy Paul, Raj Kumar, Bommena Vittal Rao, Bhimrao Bodhanrao Gawali, Vaddu Venkata Narayana Reddy, Jhillu Singh Yadav
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Publication number: 20120225895Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.Type: ApplicationFiled: November 9, 2010Publication date: September 6, 2012Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
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Publication number: 20120220609Abstract: The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by formula (1): [wherein, R1: formula (1A): [wherein, R4 and R5: H, halogen, or alkyl; R6: H, halogen, alkyl, or the like; R7: substitutable hydroxyalkyl, substitutable hydroxyhalo alkyl, substitutable alkoxyalkyl, or the like; substituent group ?: oxo, hydroxy, amino, or the like; ring Q1: a monocyclic heterocyclic group; ring Q2: a monocyclic hydrocarbon ring group, or a monocyclic heterocyclic group; ring Q3: a monocyclic hydrocarbon ring group, or a monocyclic heterocyclic group; X: a single bond, methylene, ethylene, or the like]; R2: alkyl, or methylsulfanyl; and R3: H, or methyl], or the like.Type: ApplicationFiled: October 20, 2010Publication date: August 30, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Takeshi Kuribayashi, Hideki Kubota, Naoki Tanaka, Takeshi Fukuda, Takashi Tsuji, Riki Goto
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Publication number: 20120214785Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
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Publication number: 20120214783Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre L. BEAULIEU, Pasquale FORGIONE, Alexandre GAGNON, Cedrickx GODBOUT, Marc-Andre JOLY, Montse LLINAS-BRUNET, Julie NAUD, Martin POIRIER, Jean RANCOURT
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Publication number: 20120213851Abstract: Compressed tablets for oral administration containing raltegravir in the form of a pharmaceutically acceptable salt are described. The tablets comprise: (A) an intragranular component comprising (i) an effective amount of an alkali metal salt of raltegravir, (ii) optionally a first superdisintegrant, and (iii) a binder; and (B) an extragranular component comprising (i) a second superdisintegrant, (ii) a filler, and (iii) a lubricant. Methods for preparing the tablets and the use of the tablets, optionally in combination with other anti-HIV agents, for the inhibition of HIV integrase, for the treatment or prophylaxis of HIV infection, or for the treatment, delay in the onset, or prophylaxis of AIDS are also described.Type: ApplicationFiled: October 21, 2010Publication date: August 23, 2012Inventors: Majid Mahjour, Feng Li, Decheng Ma, Sutthilug Sotthivirat
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Publication number: 20120208773Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.Type: ApplicationFiled: August 12, 2010Publication date: August 16, 2012Applicant: Valeant International (Barbados) SRLInventors: Andrew John Duffield, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
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Patent number: 8242125Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases.Type: GrantFiled: December 7, 2009Date of Patent: August 14, 2012Assignee: Novartis AGInventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
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Publication number: 20120202819Abstract: Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M2 antagonist. Such combination therapy provides improved efficacy and/or reduced side effects.Type: ApplicationFiled: September 27, 2010Publication date: August 9, 2012Applicant: Merck Sharp & Dohme CorporationInventors: Scott D. Edmondson, Mary Struthers SinhaRroy, Hiroshi Nagabukuro, William S. Denney, Tara F. Frenki
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Publication number: 20120202750Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: January 23, 2012Publication date: August 9, 2012Applicant: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20120202763Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.Type: ApplicationFiled: May 27, 2010Publication date: August 9, 2012Applicant: PTC THERAPEUTICS, INCInventors: Neil Almstead, Tamil Arasu, Soongyu Choi, Liangxian Cao, Jeffrey Allen Campbelll, Donald Corson, Thomas W. Davis, Jason D. Graci, Zhengxian Gu, Peter Seong Woo Hwang, William Lennox, Harry H. Miao, Langdon Miller, Young-Choon Moon, Hongyan Qi, Christopher Trotta, Marla L. Weetall
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Publication number: 20120196881Abstract: This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.Type: ApplicationFiled: December 5, 2011Publication date: August 2, 2012Applicant: Vivus, Inc.Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
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Publication number: 20120196882Abstract: The invention provides methods and compounds for the treatment and prevention of malaria infection and transmission in a mammal by administering compounds of the invention to a mammal having or suspected of having a malaria infection. The invention also provides pharmaceutical compositions that can kill or arrest the growth of Plasmodium organisms, and especially Plasmodium falciparum, thereby preventing or blocking transmission of malaria as well as treating malaria infection.Type: ApplicationFiled: August 27, 2010Publication date: August 2, 2012Inventors: Dipak Raj, Sittiporn Pattaradilokrat, Ron Johnson, Ruili Huang
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Patent number: 8232287Abstract: It is intended to provide a pyrimidyl indoline compound which structurally differs from compounds used as active ingredients in conventional oral hypoglycemic agents and has excellent hypoglycemic effect.Type: GrantFiled: October 15, 2008Date of Patent: July 31, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Toshio Kaneko, Takeshi Shida, Takayuki Baba, Koji Matsumoto, Kazumasa Aoki
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Publication number: 20120190543Abstract: The present invention concerns novel heteroaryl-N-aryl carbamates and their use in pest control, as insecticides and acaricides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: William T. Lambert, Gary D. Crouse, Thomas C. Sparks, Denise P. Cudworth
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Publication number: 20120190542Abstract: The present invention relates to pesticidal mixtures, compositions and uses thereof comprising a component (A) and a component (B), wherein components (A) and (B) are: (A) a carboxylic acid amide fungicide; and (B) a benzamide fungicide; with the proviso that the mixture does not comprise: 1). fluopicolide and mandipropamid and clothianidin; or 2). fluopicolide and mandipropamid and imidacloprid; or 3). fluopicolide and mandipropamid and thiamethoxam. The invention also relates to mixtures, compositions and uses thereof wherein component (A) is metalaxyl-M and component (B) is a benzamide fungicide.Type: ApplicationFiled: March 29, 2010Publication date: July 26, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Patrick John Doyle, Gilberto Olaya-Huertas, Paul John Kuhn, Allison Tally
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Publication number: 20120184572Abstract: Aryl GPR119 agonists are provided. These compounds are useful for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control.Type: ApplicationFiled: January 13, 2011Publication date: July 19, 2012Inventors: Jiangao Song, Jingyuan Ma, Christopher J. Rabbat, Imad Nashashibi, Xin Chen, Zuchun Zhao
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Patent number: 8222257Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.Type: GrantFiled: March 30, 2006Date of Patent: July 17, 2012Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
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Patent number: 8217063Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 15, 2008Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Publication number: 20120171183Abstract: This invention provides a composition comprising a biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure, and an effective amount of at least one fungicide.Type: ApplicationFiled: March 6, 2012Publication date: July 5, 2012Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20120172383Abstract: 1) Fungicidal compositions comprising: a) at least one pyridylmethylbenzamide derivative of Formula (I), in which the various radicals are as defined in the description; and b) at least one compound (II) capable of inhibiting the transport of electrons of the respiratory chain of mitochondrial ubiquinol:ferricytochrome-c oxidoreductase or complex III in phytopathogenic fungal organisms. 2) Process for curatively or preventively controlling the phytopathogenic fungi of crops, characterized in that an effective and nonphytotoxic quantity of one of these fungicidal compositions is applied to the aerial parts of plants.Type: ApplicationFiled: March 12, 2012Publication date: July 5, 2012Applicant: BAYER SASInventors: David Stanley HOLAH, Jane Elizabeth DANCER, Marie-Pascale LATORSE, Richard MERCER
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Publication number: 20120172382Abstract: Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.Type: ApplicationFiled: April 29, 2011Publication date: July 5, 2012Applicant: DECIPHERA PHARMACEUTICALS, LLC.Inventors: Daniel L. Flynn, Michael D. Kaufman
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Publication number: 20120165288Abstract: This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.Type: ApplicationFiled: March 2, 2012Publication date: June 28, 2012Inventors: Scott L. Harbeson, Roger D. Tung
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Publication number: 20120165353Abstract: Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPAR?-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound.Type: ApplicationFiled: September 29, 2010Publication date: June 28, 2012Applicant: KOWA COMPANY, LTD.Inventors: Toru Miura, Seiichi Sato, Hajime Yamada, Junya Tagashira, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
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Publication number: 20120157476Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 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: ApplicationFiled: December 8, 2011Publication date: June 21, 2012Inventors: Paul Hebeisen, Stephan Roever
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Patent number: RE43748Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.Type: GrantFiled: August 26, 2010Date of Patent: October 16, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura