The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System [e.g., 2-(1-isothiochromanyl)-2-imidazoline Hydrochloride, Etc.] Patents (Class 548/311.4)
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Publication number: 20110172225Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: September 25, 2008Publication date: July 14, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Publication number: 20110168992Abstract: The present invention relates to a novel compound, a method for manufacturing the same, and an organic electronic device using the same, and the novel compound according to the present invention may act as a hole injection, hole transport, electron injection and transport, or light emitting material in an organic light emitting device and an organic electronic device, and the device according to the present invention shows excellent properties in terms of efficiency, a driving voltage, and stability.Type: ApplicationFiled: September 23, 2009Publication date: July 14, 2011Inventors: Jae-Soon Bae, Ji-Eun Kim, Jeung-Gon Kim, Jun-Gi Jang
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Publication number: 20110166142Abstract: 2-Substituted isoflavonoid compounds and pharmaceutical compositions containing same are useful as anti-inflammatory agents and antioxidants and for the treatment of related diseases and conditions.Type: ApplicationFiled: June 30, 2008Publication date: July 7, 2011Inventors: Eleanor Eiffe, Andrew Heaton, Catherine Walker, Alan James Husband
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Publication number: 20110166360Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral transition metal catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogen, halogen, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, the transition metal catalyst comprising a chiral ligand having the formula wherein each R and R? independently represents alkyl, aryl, aralkyl, alkenyl, alkynyl, alkoxy, aryloxy, alkylthio, arylthio, unsubstituted or substituted cyclic moiety selected from a group consisting of monocyclic or polycyclic saturated or partially saturated carbocyclic or heterocyclic, aromatic or heteroaromatic rings said rings comprising from 4 to 8 atoms and comprising from 0 to 3 heteroatoms, wherein: the term alkyl means hydrocarbon chains, straight or branched, conType: ApplicationFiled: March 13, 2009Publication date: July 7, 2011Applicant: BIAL - PORTELA & CA, S.A.Inventors: Alexander Beliaev, David Alexander Learmonth, Juan José Almena Perea, Gerhard Geib, Patrick Hitzel, Renat Kadyrov, David Voigtlaender
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Publication number: 20110152095Abstract: Pyrandione, thiopyrandione and cyclohexanetrione derivatives of formula (I), which are suitable for use as herbicides.Type: ApplicationFiled: June 4, 2009Publication date: June 23, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: James Nicholas Scutt, Christopher John Mathews, Michel Muehlebach
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Publication number: 20110152246Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, or V as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Publication number: 20110144174Abstract: The present application describes deuterium-enriched ondansetron, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: February 28, 2011Publication date: June 16, 2011Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20110144096Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or hetero-cycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: July 28, 2009Publication date: June 16, 2011Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20110136830Abstract: Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.Type: ApplicationFiled: February 15, 2011Publication date: June 9, 2011Inventors: Teresa MUJICA-FERNAUD, Herwig Buchholz, Wilfried Rautenberg, Christian Sirrenberg
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Publication number: 20110137633Abstract: Methods of identifying NS5A inhibitors are provided. Novel binding sites are identified on NS5A dimers, and these binding sites can be used to design and/or identify new NS5A inhibitors.Type: ApplicationFiled: December 3, 2010Publication date: June 9, 2011Applicant: ABBOTT LABORATORIESInventors: CHARLES W. HUTCHINS, DAVID A. DEGOEY, WARREN M. KATI, ALLAN C. KRUEGER, JOHN T. RANDOLPH, ROLF WAGNER, PAMELA L. DONNER
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Patent number: 7951822Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: March 30, 2009Date of Patent: May 31, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Koichi Yamazaki, Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Publication number: 20110124573Abstract: This invention relates to certain Aloesin derivatives with natural amino acids, peptides, and amino sugars (formula I).Type: ApplicationFiled: January 28, 2011Publication date: May 26, 2011Applicant: Island Kinetics Inc.Inventors: SHYAM K. GUPTA, Linda Walker
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Publication number: 20110118257Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: November 3, 2010Publication date: May 19, 2011Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
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Publication number: 20110098236Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: February 23, 2009Publication date: April 28, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Publication number: 20110098237Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: February 23, 2009Publication date: April 28, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan, Sergi Gulnik, John W. Erickson
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Publication number: 20110092553Abstract: The present invention provides azole derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and their use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.Type: ApplicationFiled: November 19, 2010Publication date: April 21, 2011Applicant: TransTech Pharma, Inc.Inventors: Adnan M.M. Mjalli, Dharma R. Polisetti, Govindan Subramanian, James C. Quada, JR., Murty N. Arimilli, Ravindra R. Yarragunta, Robert C. Andrews, Rongyuan Xie
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Publication number: 20110092700Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.Type: ApplicationFiled: December 3, 2010Publication date: April 21, 2011Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Patent number: 7919516Abstract: The present application describes deuterium-enriched ondansetron, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: GrantFiled: September 5, 2008Date of Patent: April 5, 2011Assignee: Protia, LLCInventor: Anthony W Czarnik
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Patent number: 7919509Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: February 27, 2009Date of Patent: April 5, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Hidefumi Ozawa, Ayako Tosaka, Koichi Yamazaki, Yuki Yamaguchi, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Publication number: 20110077399Abstract: This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.Type: ApplicationFiled: December 1, 2010Publication date: March 31, 2011Applicant: TRANSTECH PHARMA, INC.Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Ravindra R. Yarragunta, Rongyuan Xie, Govindan Subramanian, James C. Quada, JR., Murty N. Arimilli, Dharma R. Polisetti
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Publication number: 20110070297Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: December 1, 2010Publication date: March 24, 2011Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company LimitedInventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
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Publication number: 20110052643Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: January 7, 2009Publication date: March 3, 2011Applicant: Synta Pharmaceuticals Corp.Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen, Lijun Sun
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Publication number: 20110053997Abstract: The present invention relates to novel salts of the compound (R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione, polymorphs of the salts and methods of their preparation.Type: ApplicationFiled: December 5, 2008Publication date: March 3, 2011Inventors: Alexander Beliaev, David Alexander Learmonth, Melanie J. Roe, Petinka Vlahova, Eric Hagen, Valeriya Smolenskaya, Donglai Yang
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Publication number: 20110044938Abstract: Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.Type: ApplicationFiled: August 15, 2007Publication date: February 24, 2011Applicant: NYCOMED GMBHInventors: Bjorn Bartels, Mathias Schmidt, Klaus Pekari, Thomas Beckers, Astrid Zimmermann, Volker Gekeler
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Publication number: 20110039888Abstract: The present invention relates, generally, to asymmetric ?-functionalization and to asymmetric ?,?-bisfunctionalization of ketones and aldehydes and, in particular, to chiral auxiliaries suitable for use in effecting such functionalizations and to methods of using same.Type: ApplicationFiled: April 21, 2009Publication date: February 17, 2011Inventors: Don M. Coltart, Daniel Lim
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Publication number: 20110021590Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein each of Ring A, Ring B, T, R2, R2?, and RA is as defined and described herein and methods for treating subjects or patients with a disease, disorder, or condition.Type: ApplicationFiled: June 7, 2010Publication date: January 27, 2011Applicant: Link Medicine CorporationInventor: Mark E. Duggan
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Patent number: 7875645Abstract: The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.Type: GrantFiled: January 19, 2007Date of Patent: January 25, 2011Assignee: Hoffman-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Marius Hoener, Sabine Kolczewski, Roger Norcross, Henri Stalder
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Publication number: 20110009396Abstract: The present invention provides compounds represented by formula 1: wherein, R1 R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.Type: ApplicationFiled: July 25, 2008Publication date: January 13, 2011Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Rada Dalal, Sapna Parikh, Aditi Amol Tannu
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Publication number: 20110003861Abstract: 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives of formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.Type: ApplicationFiled: March 6, 2008Publication date: January 6, 2011Applicant: ROTTAPHARM S.P.A.Inventors: Antonio Giordani, Ilario Verpilio, Sabrina Pucci, Roberto Artusi, Gianfranco Caselli, Marco Lanza, Laura Mennuni, Francesco Makovec, Lucio Claudio Rovati
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Publication number: 20110002995Abstract: Provided is a pharmaceutical composition for the treatment and prevention of cardiac diseases, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.Type: ApplicationFiled: December 18, 2008Publication date: January 6, 2011Applicants: MAZENCE INC., KT & G CORPORATIONInventors: Taehwan Kwak, Myung-Gyu Park
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Patent number: 7858652Abstract: The present invention relates to a compound of formula I, wherein R1 is selected from the group consisting of hydrogen and lower alkyl; each R2 is independently selected from the group consisting of hydrogen and lower alkyl; each R3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; R4 is selected from the group consisting of hydrogen and lower alkyl; X is selected from the group consisting of —CH2—, —CH— and —O—; Y is selected from the group consisting of —CH2—, —CH2CH2—, —CH— and a bond; with the proviso that, when X is —O—, Y is —CH2—; Z is selected from the group consisting of —CH2— and —CH—; m is 1 or 2; and n is 1 or 2. The invention relates also to a pharmaceutically-acceptable acid-addition salt of such a compound, methods for making the compound, and a composition comprising such a compound.Type: GrantFiled: November 13, 2007Date of Patent: December 28, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20100310657Abstract: Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.Type: ApplicationFiled: December 18, 2008Publication date: December 9, 2010Applicants: MAZENCE INC., KT & G CORPORATIONInventors: Taehwan Kwak, Myung-Gyu Park, Kyoung Hoon Jung
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Publication number: 20100298301Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: May 9, 2008Publication date: November 25, 2010Applicant: SAREUM LIMITEDInventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
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Patent number: 7838545Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: GrantFiled: July 2, 2008Date of Patent: November 23, 2010Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gill, John E. Donello, Michael E. Garst, Larry A. Wheeler
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Publication number: 20100292190Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: February 14, 2006Publication date: November 18, 2010Applicant: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Patent number: 7834044Abstract: The present invention relates to compounds of formula I wherein R1 is selected from the group consisting of hydrogen and lower alkyl; each R2 is independently selected from the group consisting of hydrogen and lower alkyl; each R3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; X is selected from the group consisting of —CH2—, —CH— and —O—; Y is selected from the group consisting of —CH2—, —CH— and a bond with the proviso that, when X is —O—, Y may not be a bond; Z is selected from the group consisting of —CH2— and —CH—; m is 0, 1 or 2; and n is 0, 1 or 2; and to pharmaceutically-acceptable acid addition salts of such compounds.Type: GrantFiled: October 31, 2007Date of Patent: November 16, 2010Assignee: Hoffman-LaRoche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20100286219Abstract: A method comprising utilizing a compound of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X signifies CH2, oxygen atom or sulphur atom; n is 1, 2 or 3, with the proviso that when n is 1, X is not CH2; and the individual (R)- and (S)-enantiomers or mixtures of enantiomers and pharmaceutically acceptable salts thereof; wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; the term halogen means fluorine, chlorine, bromine or iodine, in the manufacture of a medicament for the treatment of one or more of the following indications: congestive heart failure, anginaType: ApplicationFiled: January 10, 2008Publication date: November 11, 2010Applicant: BIAL - PORTELA & CA S.A.Inventor: Patricio Manuel Vieira Araújo Soares Da Silva
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Patent number: 7829726Abstract: The invention relates to a method for manufacturing sertaconazole mononitrate. The invention also relates teserta-conazole mononitrate that is characterized by it: particle size and to sertaconazole mononitrate monohydrate.Type: GrantFiled: September 13, 2005Date of Patent: November 9, 2010Assignee: Ferrer Internacional, S.AInventors: Inés Petschen, Xavier Camps, Juan Sallarés
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Patent number: 7812026Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.Type: GrantFiled: December 21, 2006Date of Patent: October 12, 2010Assignee: AstraZeneca ABInventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson
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Publication number: 20100240725Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.Type: ApplicationFiled: October 31, 2008Publication date: September 23, 2010Applicant: DONG-A PHARMACEUTICAL. CO., LTDInventors: Yeong Geon Lee, Soo-Jung Choi, Tae-Kyung Kang, Mi-Jeong Seo, Chang-Yong Shin, Kyung-Seok Lee, Gook-Jun Ahn, Seul-Min Choi, Yong-Duck Kim, Dong-Hwan Kim, Kyung-Koo Kang, Hyun-Joo Shim, Dong-Sung Kim, Byoung-Ok Ahn, Moo-Hi Yoo
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Publication number: 20100204233Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.Type: ApplicationFiled: April 23, 2010Publication date: August 12, 2010Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7772230Abstract: The present invention provides a chroman compound of formula (I) and its pharmaceutical salt, methods of its preparation and its pharmaceutical applications. Wherein: X is O or S; n is for 2, 3 or 4; R1 is 6-substituted or 7-substituted halogen, C1-4alkyl, C1-4alkoxyl, benzyloxy, carbamoyl; R2 is nitrogen-containing five-membered or six-membered substituted heterocyclic ring selected from piperidinyl, morpholinyl, N-methyl-piperazinyl, N-(2-ethoxyl)piperazinyl, pyrrolyl, pyrazolyl or imidazolyl. The compounds are useful to prepare medicaments for treating cardiovascular diseases, their preparation employs mild reaction conditions, the raw material are plenty and easy to be obtained, and the operation and post-treatment in the preparation are simple.Type: GrantFiled: October 25, 2007Date of Patent: August 10, 2010Assignee: China Pharmaceutical UniversityInventors: Qidong You, Lvpei Du, Minyong Li, Lin Xia
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Publication number: 20100168195Abstract: In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: February 11, 2008Publication date: July 1, 2010Inventors: Junying Zheng, Kevin D. McCormick, Jianhua Chao, Christopher W. Boyce, Robert G. Aslanian, Younong Yu
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Patent number: 7732617Abstract: Tocopherol derivatives having the general formula: wherein n is an integer of 6 to 13, R1 is hydrogen, a silyl ether or acetate, R2 is an optionally substituted nitrogen-containing heterocycle or a polycyclic nitrogen-containing heterocycle; and pharmaceutically acceptable salts thereof are provided. A method for synthesizing the compounds is also provided. The tocopherol derivatives are capable of inhibiting the primary enzyme responsible for the metabolism of the tocopherols and tocotrienols compounds of vitamin E, namely tocopherol-?-hydroxylase, and thus increase the amount and prolong the availability of these compounds in plasma and tissue.Type: GrantFiled: May 25, 2007Date of Patent: June 8, 2010Assignees: Brock University, Cornell UniversityInventors: Jeffrey Atkinson, Robert S. Parker, Stephan Ohnmacht, Phillip John Nava, Ryan West
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Publication number: 20100137390Abstract: Compounds of formula I and a method for their preparation are described, where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or alkyl heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.Type: ApplicationFiled: May 6, 2008Publication date: June 3, 2010Applicant: BIAL - PORTELA & CA S.A.Inventors: Patricio Manuel Vieira Araüjo Soares Da Silva, David Alexander Learmonth, Alexander Beliaev
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Publication number: 20100121073Abstract: A process for making (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione and pharmaceutically acceptable salts thereof, and for making intermediates useful in the formation of said compound.Type: ApplicationFiled: January 31, 2008Publication date: May 13, 2010Applicant: BIAL - PORTELA & CA S.A.Inventors: Patrício Manuel Vieira Araújo Soares Da Silva, Alexander Beliaev, David Alexander Learmonth
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Publication number: 20100119623Abstract: The present invention relates to new imidazolyl modulators of 5-HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 16, 2009Publication date: May 13, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100113550Abstract: Polymorphs of (R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione hydrochloride and methods of their preparation.Type: ApplicationFiled: May 31, 2007Publication date: May 6, 2010Applicant: BIAL - PORTELA AND CA, S.A.Inventors: Alexander Beliaev, David Learmonth, Valeriya Smolenskaya
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Publication number: 20100113799Abstract: A process for making (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione and pharmaceutically acceptable salts thereof, and for making intermediates useful in the formation of said compound.Type: ApplicationFiled: January 31, 2008Publication date: May 6, 2010Applicant: BIAL - PORTELA & CA S.A.Inventors: Patricio Manuel Vieira Araújo Soares Da Silva, Alexander Beliaev, David Alexander Learmonth
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Publication number: 20100105726Abstract: The present invention relates to a pharmaceutical composition comprising compound for induction of apoptosis, a method for inducing cancer cell apoptosis, a method to suppress lymphocyte activation, a method to improve intracellular trafficking of misfolded mutants and a screening method to identify additional compounds useful for inducing apoptosis, and more specifically, it relates to pharmaceutical compositions comprising imidazole derivatives as active gradients for induction of apoptosis to treat various diseases including cancers and immune-related diseases, the method of inducing apoptosis by treating cancer cells with the said pharmaceutical composition, the method of inactivating human lymphocytes by treating lymphocytes with the said pharmaceutical composition, the method of improving intracellular trafficking of misfolded mutants by treating cells containing the mutants with the said pharmaceutical composition, and the screening method for identifying additional compound useful for inducing apoptosType: ApplicationFiled: February 26, 2007Publication date: April 29, 2010Applicant: Industry-Academic Cooperation Foundation, Yonsei UniversityInventors: In-Jae Shin, Myung-ryul Lee, Darren Williams