Chalcogen Bonded Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 514/428)
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Patent number: 8772290Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.Type: GrantFiled: April 21, 2011Date of Patent: July 8, 2014Assignee: Oscotech Inc.Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
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Patent number: 8754117Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.Type: GrantFiled: January 28, 2013Date of Patent: June 17, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: Liming Shao, Jianguo Ma
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Publication number: 20140161830Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.Type: ApplicationFiled: November 25, 2013Publication date: June 12, 2014Applicant: Massachusetts Institute of TechnologyInventors: Daniel Griffith Anderson, Kathryn Ann Whitehead, Joseph R. Dorkin, Arturo Jose Vegas, Yunlong Zhang
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Publication number: 20140148438Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: September 22, 2011Publication date: May 29, 2014Inventor: Michael Farber
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Publication number: 20140147517Abstract: Amisulpride is used in the therapy of nausea, vomiting or retches. The therapy may utilize a novel injectable formulation, in unit dosage form, comprising less than 50 mg amisulpride.Type: ApplicationFiled: February 4, 2014Publication date: May 29, 2014Inventors: Julian Clive Gilbert, Robert William Gristwood, Nicola Cooper, Gabriel Fox
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Patent number: 8735604Abstract: The present invention relates to compounds of the general formula: (I) wherein ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: GrantFiled: September 16, 2010Date of Patent: May 27, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Eric J. Gilbert, Michael W. Miller, Duane Eugene DeMong, Andrew W. Stamford, William J. Greenlee
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Patent number: 8735442Abstract: Disclosed are: a composition for alleviating ultraviolet irradiation-induced damage, which can be used on a daily based and is stable and safe; and a pharmaceutical preparation, a cosmetic and a food composition, each of which comprises the composition. The composition for alleviating ultraviolet irradiation-induced damage contains one or more compounds selected from the group consisting of D-glutamic acid, L-glutamic acid, D-proline, D-cystine, L-cystine, and derivatives and/or salts of the aforementioned compounds. The composition can be used as an external formulation for the skin, a cosmetic composition, an anti-wrinkle agent, a sunscreen agent, a pharmaceutical composition for treating and/or preventing skin diseases, a food composition, or a pharmaceutical composition for preventing or treating cataract.Type: GrantFiled: March 30, 2010Date of Patent: May 27, 2014Assignee: Shiseido Company, Ltd.Inventors: Yutaka Ashida, Yosuke Tojo, Masashi Mita, Chieko Mizumoto, Shoichiro Shimada, Kayo Matsumoto
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Patent number: 8729119Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: May 22, 2013Date of Patent: May 20, 2014Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
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Patent number: 8691977Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.Type: GrantFiled: August 22, 2011Date of Patent: April 8, 2014Assignee: Neupharma, Inc.Inventors: Xiangping Qian, Yong-Liang Zhu
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Patent number: 8686027Abstract: Administration of a loop diuretic in nebulized dry powder form directly to a patient's lungs for treating bronchial disease.Type: GrantFiled: December 7, 2011Date of Patent: April 1, 2014Assignee: Microdose Therapeutx, Inc.Inventor: Andrew Abrams
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Publication number: 20140080833Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: ApplicationFiled: November 11, 2013Publication date: March 20, 2014Applicant: MannKind CorporationInventors: Gary A. Flynn, Sandra A. Lee, Mary Faris, David W. Brandt, Subrata Chakravarty
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Patent number: 8669252Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: GrantFiled: May 12, 2011Date of Patent: March 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
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Patent number: 8658691Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.Type: GrantFiled: September 28, 2012Date of Patent: February 25, 2014Assignee: Theravance, Inc.Inventors: Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
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Publication number: 20140044774Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising an H1 antihistamine and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: December 29, 2011Publication date: February 13, 2014Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
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Publication number: 20140038949Abstract: The present invention provides methods of inducing differentiation of oligodendrocyte progenitor cells to a mature myelinating cell fate with a neurotransmitter receptor modulating agent. The present invention also provides methods of stimulating increased myelination in a subject in need thereof by administering said neurotransmitter receptor modulating agent. Methods of treating a subject having a demyelinating disease using a neurotransmitter receptor modulating agent are also provided.Type: ApplicationFiled: February 17, 2012Publication date: February 6, 2014Applicants: IRM LLC, The Scripps Research InstituteInventors: Peter Schultz, Luke Lairson, Vishal Deshmukh, Costas Lyssiotis
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Patent number: 8637568Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: July 8, 2013Date of Patent: January 28, 2014Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
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Publication number: 20140024680Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.Type: ApplicationFiled: January 9, 2013Publication date: January 23, 2014Applicant: Bayer Intellectual Property GmbHInventor: Bayer Intellectual Property GmbH
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Publication number: 20140018407Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.Type: ApplicationFiled: December 19, 2012Publication date: January 16, 2014Applicant: THERAVANCE, INCInventor: Daisuke Roland Saito
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Publication number: 20140018341Abstract: A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
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Patent number: 8623900Abstract: The present invention relates to amino alcohol derivatives of general formula I: These derivatives possess an interesting activity in that they block the secondary products of lipid oxidative stress, and are consequently suitable for therapeutic use in all disorders related with the presence of reactive carbonyl compounds.Type: GrantFiled: December 20, 2010Date of Patent: January 7, 2014Assignees: Flamma S.p.A., Universita degli Studi di MilanoInventors: Gianpaolo Negrisoli, Renato Canevotti, Massimo Previtali, Giancarlo Aldini, Marina Carini, Marica Orioli, Giulio Vistoli
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Publication number: 20140005222Abstract: The present invention provides a compound of the Formula II: wherein A is: R1 is CH3, CF3, or F; R2 is H, CH3, or F; R3 is CH3, OCH3, OH, F; R4 is OH or CH2OH; and X is CH or N; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 20, 2013Publication date: January 2, 2014Inventors: Maria-Jesus BLANCO-PILLADO, Matthew Joseph FISHER, Steven Lee KUKLISH, Tatiana Natali VETMAN
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Patent number: 8618143Abstract: Non-peptide, azole-substituted nitric oxide snythase inhibitor compounds, compositions and related methods, as can be used to enhance bioavailability and inhibit production of nitric oxide.Type: GrantFiled: October 18, 2011Date of Patent: December 31, 2013Assignee: Northwestern UniversityInventors: Richard B. Silverman, James M. Kraus
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Patent number: 8609713Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 7, 2010Date of Patent: December 17, 2013Assignee: AbbVie Inc.Inventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li
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Patent number: 8604038Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: August 24, 2010Date of Patent: December 10, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
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Publication number: 20130324540Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.Type: ApplicationFiled: August 7, 2013Publication date: December 5, 2013Applicant: Obschestvo Ogranichennoi Otvetstvennostyu "Pharmenterprises"Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
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Patent number: 8592453Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: October 6, 2010Date of Patent: November 26, 2013Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
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Publication number: 20130303525Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.Type: ApplicationFiled: July 19, 2011Publication date: November 14, 2013Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
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Publication number: 20130296279Abstract: The invention in one embodiment is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention is also directed to a composition comprising the compound of formula I or a pharmaceutically acceptable salt, and methods of treating the indications listed herein.Type: ApplicationFiled: May 10, 2013Publication date: November 7, 2013Inventor: Adam Morgan
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Publication number: 20130296322Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: July 8, 2013Publication date: November 7, 2013Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
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Patent number: 8545816Abstract: Benzoic acid ester compounds of formula (I): wherein R and R1-R5 have the meanings explained in the description, methods for producing them and use thereof in cosmetic, pharmaceutical, personal care and industrial preparations as sunscreens based on photochemical precursor properties of ultraviolet absorbers.Type: GrantFiled: March 20, 2006Date of Patent: October 1, 2013Assignee: Ferrer Internacional, S.A.Inventors: Ricardo Miralles, Santiago Nonell, Manuel M. Raga, Antonio Giuglietta, Jordi Teixidó
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Publication number: 20130251787Abstract: Pulmonary arterial hypertension (PAH) can be prevented in persons susceptible to the diseases and PAH patients can be treated by administering an effective dose of a leukotriene inhibitor. Suitable inhibitors include leukotriene A4 hydrolase (LTA4H) inhibitors, leukotriene B4 receptor (BLT1/BLT2) antagonists, 5-lipoxygenase (5-LO) inhibitors, and 5-lipoxgygenase activating protein (FLAP) inhibitors.Type: ApplicationFiled: March 15, 2013Publication date: September 26, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Mark R. Nicolls, Wen Tian, Jayakumar Rajadas
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Publication number: 20130253013Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 22, 2013Publication date: September 26, 2013Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
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Patent number: 8536201Abstract: The present invention relates to novel pesticidal arylpyrrolidine compounds (arylpyrrolidines) having the general formula (I) wherein A, X1, X2, X3, X4, R1, R2, R3, R4, and G are as defined in the application and their use as pesticide, in particular for combating animal pests which occur in the agricultural and/or the veterinary field, as well as to a preparation methods for preparing such compounds.Type: GrantFiled: December 23, 2010Date of Patent: September 17, 2013Assignee: Bayer Intellectual Property GmbHInventors: Jun Mihara, Mamoru Hatazawa, Daiei Yamazaki, Norio Sasaki, Tetsuya Murata, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Hidetoshi Kishikawa, Ulrich Görgens
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Publication number: 20130237542Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.Type: ApplicationFiled: October 17, 2011Publication date: September 12, 2013Applicants: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Kyeong Lee, Mi Sun Won, Hwan Mook Kim, Song Kyu Park, Kiho Lee, Ki Hoon Lee, Chang Woo Lee, Jung Joon Lee, Kyung Sook Chung, Bo Kyung Kim, Yinglan Jin, Seung-hee Lee
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Publication number: 20130237581Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: April 25, 2013Publication date: September 12, 2013Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam D. Hughes, Lori Jean Patterson
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Patent number: 8530465Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: GrantFiled: August 1, 2012Date of Patent: September 10, 2013Assignee: National Defense Medical CenterInventors: Hsu-Shan Huang, Chia-Chung Lee
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Publication number: 20130231319Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.Type: ApplicationFiled: November 16, 2011Publication date: September 5, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeup, Sylvaine Gren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein, Davide Pozzi
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Publication number: 20130225573Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.Type: ApplicationFiled: February 7, 2013Publication date: August 29, 2013Applicant: GENZYME CORPORATIONInventor: Genzyme Corporation
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Publication number: 20130217660Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: ApplicationFiled: May 12, 2011Publication date: August 22, 2013Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
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Publication number: 20130203815Abstract: The present invention provides compounds represented by general formula (I): wherein, R1, R2, R3, L and T are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, and prodrugs thereof. The invention also relates to processes for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful in the treatment of a condition or disorder mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-?) and interleukins such as IL-1, IL-6, and IL-8. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (I) or its pharmaceutical composition, to a mammal in need thereof.Type: ApplicationFiled: March 25, 2011Publication date: August 8, 2013Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Babasaheb Pandurang Bandgar, Jalindar Vasant Totre
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Patent number: 8501964Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: December 1, 2011Date of Patent: August 6, 2013Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
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Publication number: 20130184206Abstract: Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: ApplicationFiled: October 23, 2012Publication date: July 18, 2013Applicant: Ligand Pharmaceuticals IncorporatedInventor: Ligand Pharmaceuticals Incorporated
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Publication number: 20130178494Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.Type: ApplicationFiled: June 29, 2012Publication date: July 11, 2013Applicant: Academia SinicaInventors: Tsann-Long SU, Ting-Chao Chou, Te-Chuang Lee
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Publication number: 20130178509Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 27, 2012Publication date: July 11, 2013Applicant: THERAVANCE, INC.Inventors: Eric Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
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Patent number: 8470871Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.Type: GrantFiled: June 19, 2012Date of Patent: June 25, 2013Assignee: Galderma Research & DevelopmentInventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
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Patent number: 8471040Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: October 10, 2011Date of Patent: June 25, 2013Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
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Publication number: 20130143858Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.Type: ApplicationFiled: January 28, 2013Publication date: June 6, 2013Applicant: ASTRAZENECA ABInventor: AstraZeneca AB
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Publication number: 20130143924Abstract: The present invention is directed to a non-therapeutical process for deterring vermin, which is based on the usage of the largely known beta amino-alcohol derivatives of formula (I) as described herein. Further, the present invention is directed to corresponding vermin-deterring compositions which contain these substances as the active ingredient, compounds of the formula (I) for the preparation of vermin-deterring compositions, and the use of compounds of formula (I) in the defense against vermin.Type: ApplicationFiled: November 16, 2012Publication date: June 6, 2013Inventors: Pierre DUCRAY, Tania Cavaliero, Maike Lohrmann, Jacques Bouvier
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Patent number: 8455665Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: August 17, 2012Date of Patent: June 4, 2013Assignee: Theravance, Inc.Inventors: Eric Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam Hughes, Lori Jean Patterson
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Publication number: 20130137746Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: June 15, 2011Publication date: May 30, 2013Applicant: ARAGON PHARMACEUTICALS, INC.Inventors: Steven P. Govek, Nicholas D. Smith