Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Four-membered Hetero Ring Patents (Class 514/210.17)
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Publication number: 20140235610Abstract: Use of an S1P receptor modulator in the treatment or prevention of a disease or condition dependent on brain-derived neurotrophic factor (BDNF) expression.Type: ApplicationFiled: December 5, 2013Publication date: August 21, 2014Inventors: Yves-Alain BARDE, Graeme BILBE, Ruben DEOGRACIAS, Rainer R. KUHN, Tomoya MATSUMOTO, Anis Khusro MIR, Anna Svenja SCHUBART
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Publication number: 20140235611Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.Type: ApplicationFiled: September 27, 2012Publication date: August 21, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Atsushi Naganawa, Kensuke Kusumi, Kazuhiro Otsuki, Tetsuya Sekiguchi, Akito Kakuuchi, Koji Shinozaki, Hiroshi Yamamoto, Shigeyuki Nonaka
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Patent number: 8809316Abstract: The present invention discloses various immunosuppressants, salts and polymorphs thereof useful in the treatment of various disorders, including peripheral neuropathy. The invention also discloses pharmaceutical formulations utilizing the immunosuppressants, alone or in combination with other compounds, useful in treating disorders such as peripheral neuropathy. The present invention also discloses a method of treating peripheral neuropathy with immunosuppressants disclosed herein.Type: GrantFiled: March 6, 2013Date of Patent: August 19, 2014Assignee: Novartis AGInventors: David Leppert, Erik Wallstroem, Barbara Nuesslein-Hildesheim
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Publication number: 20140228341Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 12, 2014Publication date: August 14, 2014Applicant: Allergan, Inc.Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
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Publication number: 20140228344Abstract: The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 6, 2014Publication date: August 14, 2014Applicant: Allergan, Inc.Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
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Patent number: 8802659Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: GrantFiled: August 5, 2010Date of Patent: August 12, 2014Assignee: Biogen Idec MA Inc.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Patent number: 8791100Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: January 28, 2011Date of Patent: July 29, 2014Assignee: Novartis AGInventors: Daniela Angst, Birgit Bollbuck, Philipp Janser, Jean Quancard, Nikolaus Johannes Stiefl
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Publication number: 20140187532Abstract: 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.Type: ApplicationFiled: March 7, 2014Publication date: July 3, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Jean-Guy BOITEAU, Karine BOUQUET, Sandrine TALANO, Corinne MILLOIS BARBUIS
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Publication number: 20140179665Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.Type: ApplicationFiled: December 9, 2013Publication date: June 26, 2014Inventors: George D. Hartman, Osvaldo A. Flores
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Publication number: 20140179636Abstract: Disclosed is a concentrate for dilution comprising a S1P receptor agonist or a pharmaceutically acceptable salt thereof, propylene glycol and optionally glycerin. This formulation is adapted for patients in a difficult condition to swallow.Type: ApplicationFiled: December 6, 2013Publication date: June 26, 2014Applicant: NOVARTIS AGInventors: Vivian Georgousis, Wei-Qin Tong
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Publication number: 20140171402Abstract: The present invention relates to an azetidine derivative or a pharmaceutically acceptable salt thereof, and an antidepressant agent or a composition for the prevention or treatment of psychiatric disorders including the same. The azetidine derivative is useful as a triple reuptake inhibitor capable of inhibiting reuptake of the neurotransmitters, dopamine, serotonin, and norepinephrine at the same time.Type: ApplicationFiled: September 4, 2012Publication date: June 19, 2014Inventors: Hoh-Gyu Hahn, Kee-Dal Nam, Min-soo Han, Young-Hue Han, Chi-Man Song, Dong-Yun Shin
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Patent number: 8697682Abstract: This invention relates to a hydrochloride, malate, oxalate and tartrate salt forms of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of each of these salts, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.Type: GrantFiled: April 3, 2013Date of Patent: April 15, 2014Assignee: Novartis AGInventors: Marilyn De La Cruz, Piotr H. Karpinski, Yugang Liu
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Publication number: 20140088074Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.Type: ApplicationFiled: May 29, 2012Publication date: March 27, 2014Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventor: Paolo Pevarello
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Publication number: 20140080802Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.Type: ApplicationFiled: October 28, 2013Publication date: March 20, 2014Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
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Publication number: 20140066420Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 16, 2013Publication date: March 6, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
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Patent number: 8653062Abstract: The present invention relates to novel cyclic amine and cycloalkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: November 22, 2010Date of Patent: February 18, 2014Assignee: Allergan, Inc.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
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Publication number: 20140023636Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.Type: ApplicationFiled: September 23, 2013Publication date: January 23, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Haruto KURATA, Shinji NAKADE
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Publication number: 20140011797Abstract: The present invention discloses various immunosuppressants, salts and polymorphs thereof useful in the treatment of various disorders, including peripheral neuropathy. The invention also discloses pharmaceutical formulations utilizing the immunosuppressants, alone or in combination with other compounds, useful in treating disorders such as peripheral neuropathy. The present invention also discloses a method of treating peripheral neuropathy with immunosuppressants disclosed herein.Type: ApplicationFiled: March 6, 2013Publication date: January 9, 2014Inventors: David LEPPERT, Erik WALLSTROEM, Barbara NUESSLEIN-HILDESHEIM
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Patent number: 8623856Abstract: The present invention relates to novel phenoxy-azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: February 20, 2013Date of Patent: January 7, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Publication number: 20140005162Abstract: This invention relates to a hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzylyazetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.Type: ApplicationFiled: June 12, 2013Publication date: January 2, 2014Inventors: Lech CISZEWSKI, Marilyn DE LA CRUZ, Piotr H. KARPINSKI, Michael MUTZ, Christian RIEGERT, Caspar VOGEL, Ricardo SCHNEEBERGER
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Publication number: 20130331371Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.Type: ApplicationFiled: April 19, 2013Publication date: December 12, 2013Applicant: Vernalis (R&D) Ltd.Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
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Publication number: 20130310359Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: June 24, 2013Publication date: November 21, 2013Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im, Wenkui K. Fang
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Publication number: 20130310360Abstract: The present invention relates to novel oxime azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: July 23, 2013Publication date: November 21, 2013Applicant: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Ken Chow, Evelyn G. Corpuz, Wha-Bin Im
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Patent number: 8586571Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: GrantFiled: October 17, 2008Date of Patent: November 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20130303515Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example inflammatory conditions, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.Type: ApplicationFiled: January 10, 2012Publication date: November 14, 2013Inventors: Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédicte Pourbaix-L'ebraly
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Publication number: 20130296245Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.Type: ApplicationFiled: November 14, 2011Publication date: November 7, 2013Inventors: Min Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
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Patent number: 8563714Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20130274240Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.Type: ApplicationFiled: November 5, 2012Publication date: October 17, 2013Inventor: JAPAN TOBACCO INC.
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Publication number: 20130244994Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: ApplicationFiled: February 15, 2013Publication date: September 19, 2013Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
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Publication number: 20130244995Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: September 19, 2013Applicant: LEO PHARMA A/SInventors: Per Vedsø, Lars Kristian Albert Blæhr
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Patent number: 8530461Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: GrantFiled: December 14, 2012Date of Patent: September 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
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Publication number: 20130225550Abstract: This invention relates to a hydrochloride, malate, oxalate and tartrate salt forms of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of each of these salts, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.Type: ApplicationFiled: April 3, 2013Publication date: August 29, 2013Inventors: Marilyn DE LA CRUZ, Piotr H. KARPINSKI, Yugang LIU
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Patent number: 8518932Abstract: The present invention relates to novel oxime azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: November 21, 2011Date of Patent: August 27, 2013Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Publication number: 20130217667Abstract: The present invention relates to novel phenoxy-azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 20, 2013Publication date: August 22, 2013Applicant: ALLERGAN, INC.Inventor: Allergan, Inc.
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Patent number: 8492561Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: November 28, 2011Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
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Patent number: 8486930Abstract: This invention relates to a hydrochloride, malate, oxalate and tartrate salt forms of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of each of these salts, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.Type: GrantFiled: December 17, 2009Date of Patent: July 16, 2013Assignee: Novartis AGInventors: Marilyn De La Cruz, Piotr H. Karpinski, Yugang Liu
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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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Publication number: 20130165422Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.Type: ApplicationFiled: November 29, 2012Publication date: June 27, 2013Applicant: SANOFIInventor: SANOFI
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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: 8450346Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.Type: GrantFiled: February 27, 2009Date of Patent: May 28, 2013Assignee: Vernalis (R&D) Ltd.Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
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Publication number: 20130123216Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.Type: ApplicationFiled: October 19, 2012Publication date: May 16, 2013Applicants: ALLIANT TECHSYSTEMS INC., RADIORX, INC., C/O INTERWEST VENTURE PARTNERSInventors: RADIORX, INC., C/O INTERWEST VENTURE PA, ALLIANT TECHSYSTEMS INC.
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Publication number: 20130095095Abstract: A method for treating thrombotic disorders using a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid. Also disclosed is a method of improving the efficacy of a blood thinning medication by co-administering a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid to a subject being treated with a blood thinning medication.Type: ApplicationFiled: October 13, 2011Publication date: April 18, 2013Inventor: Thomas Christian Lines
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Publication number: 20130040932Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 24, 2012Publication date: February 14, 2013Applicants: Neuromed Pharmaceuticals Ltd., Merck Sharp & Dohme Corp.Inventors: Merck Sharp & Dohme Corp., Neuromed Pharmaceuticals Ltd.
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Publication number: 20130023516Abstract: 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.Type: ApplicationFiled: September 12, 2012Publication date: January 24, 2013Applicant: Galderma Research & DevelopmentInventors: Jean-Guy BOITEAU, Karine Bouquet, Sandrine Talano, Corinne Millois Barbuis
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Publication number: 20120329773Abstract: This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: December 13, 2011Publication date: December 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Dieter HAMPRECHT, Barbara KISTLER, Iain LINGARD
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Patent number: 8334282Abstract: The present invention provides novel substituted amino-azetidines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.Type: GrantFiled: July 6, 2010Date of Patent: December 18, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20120295874Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.Type: ApplicationFiled: October 7, 2010Publication date: November 22, 2012Applicants: CORNELL UNIVERSITY, COFERON, INC., PURDUE RESEARCH FOUNDATIONInventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold
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Patent number: 8299053Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.Type: GrantFiled: March 4, 2009Date of Patent: October 30, 2012Assignees: RadioRx, Inc., Alliant Techsystems Inc.Inventors: Mark D. Bednarski, Lynn M. Oehler, legal representative, Susan Knox, Louis Cannizzo, Kirstin Warner, Robert Wardle, Stephen Velarde, Shoucheng Ning
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Patent number: 8299054Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.Type: GrantFiled: April 14, 2010Date of Patent: October 30, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Xiang-Yang Ye, Jeffrey A. Robl, Ronald L. Hanson, Zhiwei Guo, Ramesh N. Patel
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Publication number: 20120252776Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.Type: ApplicationFiled: March 12, 2012Publication date: October 4, 2012Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick