Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
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Publication number: 20130224257Abstract: The present invention relates to a method for preparing microsphere and microspheres produced thereby. The method comprises: mixing a water-insoluble organic solvent with a dispersion solvent; mixing a polymer compound, a drug and a water-insoluble organic solvent to prepare a dispersed phase; mixing the dispersed phase with the dispersion solvent mixed with the water-insoluble organic solvent to prepare an emulsion; and adding a base or an acid to the prepared emulsion. With the method, it is possible to prepare a drug-containing polymeric microsphere cost-effectively and conveniently.Type: ApplicationFiled: January 18, 2013Publication date: August 29, 2013Applicants: Ewha University - Industry Collaboration Foundation, SK Chemicals Co., Ltd.Inventors: SK Chemicals Co., Ltd., Ewha University - Industry Collaboration Foundation
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Publication number: 20130217673Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of mixed monoamine reuptake inhibitor locally at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least thirty days. In some embodiments, the relief can be for at least at least fifty days, at least one hundred days, at least one hundred and twenty days, at least one hundred and thirty, at least one hundred fifty days or at least one hundred and eighty days.Type: ApplicationFiled: February 22, 2012Publication date: August 22, 2013Applicant: Warsaw Orthopedic, IncInventor: Jared T. Wilsey
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Publication number: 20130217620Abstract: The present invention relates to ionic silicone hydrogel contact lenses which comprise at least one pharmaceutical or nutriceutical component and are formed from reaction mixtures comprising a mixture of slow-reacting hydrophilic monomers, including at least one slow-reacting ionic monomer, at least one silicone-containing component and at least one hydroxyl-containing component, wherein the ratio of the slow-reacting hydrophilic component half lives to the silicone-containing component half life is at least 2.Type: ApplicationFiled: March 14, 2013Publication date: August 22, 2013Applicant: Johnson & Johnson Vision Care, Inc.Inventor: Johnson & Johnson Vision Care, Inc.
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Publication number: 20130217681Abstract: Presented herein is a methodology for reducing weight in obese subjects and in patients receiving various medical treatments that are accompanied with weight gain. The methodology allows for management of weight gain, management of triglyceride levels and weight reduction in obese subjects.Type: ApplicationFiled: November 22, 2011Publication date: August 22, 2013Applicants: TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD., RAMOT AT TEL-AVIV UNIVERSITY LTD.Inventors: Avraham Weizman, Michael Poyurovsky
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Patent number: 8513238Abstract: The present invention provides heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: GrantFiled: May 5, 2011Date of Patent: August 20, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Cosimo Dolente, Patrick Schnider
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Publication number: 20130210806Abstract: The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.Type: ApplicationFiled: February 14, 2013Publication date: August 15, 2013Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20130210813Abstract: The invention relates to compositions and methods for effecting male contraception.Type: ApplicationFiled: May 16, 2011Publication date: August 15, 2013Inventors: James Elliott Bradner, Martin Matzuk, Jun Qi
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Publication number: 20130210804Abstract: The present invention is directed to tricyclic compounds which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: October 20, 2011Publication date: August 15, 2013Inventors: Neville J. Anthony, Robert P. Gomez, Jing Li, Swati P. Mercer, Anthony J. Roecker, Craig A. Stump, Theresa M. Williams
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Patent number: 8501750Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.Type: GrantFiled: May 20, 2008Date of Patent: August 6, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
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Publication number: 20130190299Abstract: Methods and formulations for the treatment of multiple sclerosis with drugs with affinity for both serotonergic 5-HT2 and dopaminergic receptors such as the D2 receptor are herein disclosed. According to one embodiment, a method includes delivering a therapeutic dosage of drugs with affinity for both serotonergic 5-HT2 and dopaminergic receptors such as the D2 receptors to a subject exhibiting symptoms of multiple sclerosis to alleviate the symptoms.Type: ApplicationFiled: June 28, 2011Publication date: July 25, 2013Applicant: Victoria Link Ltd.Inventors: Anne Camille La Flamme, Bronwen Jane Connor, David O'Sullivan
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Patent number: 8492376Abstract: The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: GrantFiled: April 14, 2011Date of Patent: July 23, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Cosimo Dolente, Patrick Schnider
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Publication number: 20130184265Abstract: The present invention relates to compounds of Formula I:Type: ApplicationFiled: December 14, 2012Publication date: July 18, 2013Applicant: Alkermes Pharma Ireland LimitedInventor: Alkermes Pharma Ireland Limited
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Publication number: 20130184264Abstract: The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).Type: ApplicationFiled: May 16, 2011Publication date: July 18, 2013Inventors: James Elliott Bradner, Jun Qi
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Publication number: 20130177603Abstract: Injectable depot compositions, comprising a biocompatible polymer which is a polymer or copolymer based on lactic acid and/or lactic acid plus glycolic acid having a monomer ratio of lactic to glycolic acid in the range from 48:52 to 100:0, a water-miscible solvent having a dipole moment of about 3.7-4.5 D and a dielectric constant of between 30 and 50, and a drug, were found suitable for forming in-situ biodegradable implants which can evoke therapeutic drug plasma levels from the first day and for at least 14 days.Type: ApplicationFiled: November 30, 2012Publication date: July 11, 2013Applicant: LABORATORIOS FARMACEUTICOS ROVI, S.A.Inventor: LABORATORIOS FARMACEUTICOS ROVI, S.A.
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Patent number: 8481528Abstract: The present invention relates to heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: GrantFiled: April 19, 2011Date of Patent: July 9, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Cosimo Dolente, Patrick Schnider
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Patent number: 8481042Abstract: The present invention relates to pyrrolo[1,4]benzodiazepine (PBD) dimer conjugates, to the compositions comprising them and to their therapeutic application, in particular as anticancer agents. The invention also relates to the process for the preparation of the conjugates, to their application as anticancer agents and to the dimers themselves.Type: GrantFiled: February 24, 2012Date of Patent: July 9, 2013Assignee: SanofiInventors: Alain Commercon, Laurence Gauzy-Lazo
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Publication number: 20130171268Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.Type: ApplicationFiled: June 5, 2012Publication date: July 4, 2013Inventors: Francisco Villarreal, Alan Maisel, George Schreiner, Guillermo M. Ceballos Reyes, Pam Taub
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Publication number: 20130172328Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: CROSSWING INC.Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
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Patent number: 8476260Abstract: The present invention relates to a novel antitumor agent containing a compound that inhibits binding between acetylated histone and a bromodomain-containing protein, preferably a thienotriazolodiazepine compound represented by the following formula (I) wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof or a hydrate or solvate as an active ingredient.Type: GrantFiled: December 26, 2008Date of Patent: July 2, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Shinji Miyoshi, Shinsuke Ooike, Kazunori Iwata, Hidemasa Hikawa, Kunio Sugahara
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Patent number: 8470814Abstract: A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.Type: GrantFiled: February 15, 2010Date of Patent: June 25, 2013Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shogo Sakuma, Toshihiro Takahashi, Masatoshi Ushioda, Toshiyasu Imai, Kazuhide Inoue
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Patent number: 8470813Abstract: The invention relates to a series of thiazoline and oxazoline derivatives, compositions thereof, and methods of treating conditions and disorders using such compounds.Type: GrantFiled: January 28, 2010Date of Patent: June 25, 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, Kathy A. Sarris, Melissa J. Michmerhuizen, Ying Wang
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Publication number: 20130157990Abstract: A method of detoxifying a patient addicted to at least one drug comprises the step of administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient. The method further comprises the step of administering an anesthetic component to the patient for putting the patient in a sedated state. The method further comprises the step of administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state. The detoxification component can comprise naloxone. The method further comprises the step of administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state. The second-medication component can comprise naltrexone. The method further comprises the step of terminating administration of the anesthetic component to the patient for reviving the patient from the sedated state.Type: ApplicationFiled: February 20, 2013Publication date: June 20, 2013Applicant: EAGLE ADVANCEMENT INSTITUTE LLCInventor: EAGLE ADVANCEMENT INSTITUTE LLC
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Publication number: 20130158016Abstract: The present invention relates to a new association of active ingredients working as anesthetic and pre-anesthetic formulated in a composition containing anesthetics and analgesics suitable for use in surgical and pre-surgical procedures and others which require sedation, tranquilization, chemical restraint and pre-anesthetic medication. More specifically the present invention relates to a new association comprising the active ingredients ketamine, preferably the isomer S-ketamine(+), midazolam and tramadol, formulated in true solution for parenteral use. The present invention also contemplates an anesthetic drug for veterinary use for parenteral use.Type: ApplicationFiled: September 5, 2011Publication date: June 20, 2013Applicant: Ouro Fino Participacoes e Empreendimentsos S/AInventor: Carlos Enrique Enrique
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Patent number: 8466144Abstract: The present invention relates to generally to the cytoprotective activity of mixed muscarinic inhibition/PARP modulation and in particular to the use of dual inhibitors of M1 muscarinic receptor and poly(ADP-ribose) polymerase (PARP) as neuroprotective medicaments, particularly as medicaments for the prevention and/or treatment of neurological diseases. Particularly preferred compounds are condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine.Type: GrantFiled: July 18, 2005Date of Patent: June 18, 2013Assignee: Proteosys AGInventor: André Schrattenholz
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Publication number: 20130150311Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible composition, useful as a pharmaceutical excipient, which composition comprises a mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers, and which possesses a Carr index of less than about 20. In other aspects, the present invention is directed a pharmaceutical composition comprising such adjuvant and a pharmaceutically active ingredient; as well as to a method of making the compositions.Type: ApplicationFiled: December 13, 2011Publication date: June 13, 2013Inventors: Grzegorz Pietrzynski, Valery Alakhov, Kishore Patel
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Publication number: 20130150350Abstract: Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: February 9, 2011Publication date: June 13, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Bruno Simoneau, Patrick Deroy, Lee Fader, Anne-Marie Faucher, Alexander Gagnon, Chantal Grand-Maitre, Stephen Kawai, Serge Landry, Jean-Francois Mercier, Jean Rancourt
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Publication number: 20130150351Abstract: Methods for treating a central nervous system (CNS) injury in a subject are provided. As of the methods include administering to the subject an effective amount of gamma aminobutyric acid (GABA) receptor signaling inhibitor to treat the subject for the CNS injury. Also provided are compositions useful in embodiments of the methods. Methods and compositions of the invention find use in the treatment of a variety of different CNS injuries, including but not limited to, treating a subject for CNS injury associated with the occurrence of stroke.Type: ApplicationFiled: June 2, 2011Publication date: June 13, 2013Inventors: Stanley T. Carmichael, Istvan Mody, Ben Huang, Andrew N. Clarkson
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Publication number: 20130150310Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.Type: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Applicant: ARQULE, INC.Inventor: ARQULE, INC.
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Publication number: 20130149380Abstract: The present invention is related to solid pharmaceutical preparations containing diatomaceous earth (diatomite) or a natural mineral mixture containing diatomaceous earth as filler besides the active ingredient and optional other auxiliary agents. A further object of the invention is a method for manufacturing such pharmaceutical preparations.Type: ApplicationFiled: May 27, 2011Publication date: June 13, 2013Applicants: ONP HOLDINGS SE, EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAGInventors: Endre Mikulásik, Ottó Albrecht
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Patent number: 8461152Abstract: The present invention is concerned with arylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. arylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein, their manufacture, and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: GrantFiled: May 15, 2012Date of Patent: June 11, 2013Assignee: Hoffmann-La Roche Inc.Inventor: Patrick Schnider
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Patent number: 8461149Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: August 15, 2008Date of Patent: June 11, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francoise Pierard, Jean-Damien Charrier
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Patent number: 8461150Abstract: The present invention relates to chalcone linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids and a process for the preparation there of. More particularly it relates to 7-Methoxy-8-{n[4-1-(2 or 4-substituted phenyl)-3-(4-hydroxy-3-methoxyphenyl)-2-propen-1-one]alkyl}-oxy}-(11aS)-1,2,3,11a-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one and 7-Methoxy-8-{n-[-3-(4-hydroxy-3-methoxyphenyl)-1-(2,4-alkyl-3-quinolyl)-2-propen-1-one]alkyl}-oxy-(11aS)-1,2,3,11a-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one with aliphatic chain length variations useful as anticancer (antitumor) agent. The general structural formula of these chalcone linked pyrrolo[2,1-c][1,4]benzodiazepines hybrids is given below. wherein R1=OH, methyl, ethyl or phenyl; R2=H, OH or F; R=H or methyl; x=c or N; n=1-4.Type: GrantFiled: October 31, 2008Date of Patent: June 11, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Ahmed Kamal, Bandari Rajendra Prasad, Adla Malla Reddy
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Patent number: 8461151Abstract: The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The invention further provides methods for the manufacture of such compounds and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: GrantFiled: April 4, 2011Date of Patent: June 11, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Cosimo Dolente, Patrick Schnider
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Patent number: 8461148Abstract: The present invention relates to the treatment of compulsive, impulsive and pervasive developmental disorders. More particularly, the methods described herein comprise administration of memantine to an individual suffering from such a disorder in an amount effective to relieve one or more symptoms of said disorder. In particularly preferred aspects, the invention is directed to the use of memantine for the treatment of autism.Type: GrantFiled: September 19, 2005Date of Patent: June 11, 2013Assignee: Icahn School of Medicine at Mount SinaiInventor: Eric Hollander
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Publication number: 20130143867Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.Type: ApplicationFiled: January 18, 2013Publication date: June 6, 2013Applicant: SYCHRONEURON INC.Inventor: SYCHRONEURON INC.
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Publication number: 20130143872Abstract: This invention relates to a composition formulated into a parenteral or injectable dosage form for the treatment of cancer, more particularly, this invention relates to a composition formulated into a parenteral dosage form suitable for administration in and around cancerous tissue, the composition including: a pharmaceutically acceptable solvent including from 20% to 100% ethanol (V/V); and a reverse transcriptase inhibitor exhibiting an anti-cancer effect, dissolved in the solvent.Type: ApplicationFiled: May 31, 2011Publication date: June 6, 2013Inventors: Nicole Stieger, Wilna Liebenberg, Melgardt Melvin De Villiers, Mino Rodolfo Caira
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Patent number: 8455479Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).Type: GrantFiled: January 23, 2009Date of Patent: June 4, 2013Assignee: Panacea Biotec LimitedInventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Publication number: 20130137680Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 1, 2010Publication date: May 30, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephen James Boyer, Jennifer Burke, Xin Guo, Thomas Martin Kirrane, JR., Roger John Snow, Yunlong Zhang
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Publication number: 20130137659Abstract: Provided herein are compounds of formula (I):Type: ApplicationFiled: January 25, 2013Publication date: May 30, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130131048Abstract: The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.Type: ApplicationFiled: January 24, 2013Publication date: May 23, 2013Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTD.Inventor: RAMOT AT TEL-AVIV UNIVERSITY LTD.
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Publication number: 20130129677Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: December 7, 2012Publication date: May 23, 2013Applicant: Siga Technologies, Inc.Inventor: Siga Technologies, Inc.
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Patent number: 8440655Abstract: The present invention provides methods of treating, reducing, preventing, or inhibiting symptoms of diabetes and/or lowering plasma levels of HbA1c by co-administration of therapeutic or subtherapeutic doses of telenzepine and sertraline to a subject in need thereof.Type: GrantFiled: June 21, 2011Date of Patent: May 14, 2013Assignee: Theracos, Inc.Inventors: Brian Seed, Jordan Mechanic
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Publication number: 20130109679Abstract: Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention.Type: ApplicationFiled: November 30, 2010Publication date: May 2, 2013Inventors: Stephen James Boyer, Donghong Amy Gao, Xin Guo, Thomas Martin Kirrane, JR., Christopher Ronald Sarko, Roger John Snow, Fariba Soleymanzadeh, Yunlong Zhang
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Publication number: 20130108693Abstract: A dosage form that provides a controlled release of at least two different active agents is provided. Particular embodiments include a dosage form that provides therapeutically effective levels of a first active agent and a second active agent in a mammal for an extended period of time following oral administration. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. The layers of the core are in stacked, substantially concentric or substantially eccentric arrangement.Type: ApplicationFiled: September 24, 2012Publication date: May 2, 2013Applicant: OSMOTICA KERESKEDELMI ES SZOLGALTATO KFTInventors: Juan A. VERGEZ, Marcelo A. RICCI
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Publication number: 20130095156Abstract: The invention provides disintegratable films containing a mixture of high molecular weight and low molecular weight water soluble components; and a pharmaceutically or cosmetically active ingredient. Optionally, the films contain a starch component, a glucose component, a filler, a plasticizer and/or humectant. The films are preferably in the form of a mucoadhesive monolayer having a thickness sufficient to rapidly disintegrate in the oral environment and release the active ingredient without undue discomfort to the oral mucosa. The monolayer can be cut to any desired size or shape to provide conveniently useable unit dosage forms for administration to oral or other mucosal surfaces for human pharmaceutical, cosmetic, or veterinary applications. The invention further provides methods of administering the film compositions by placing the composition into, for example, the oral cavity for a sufficient period of time to permit the film to disintegrate and release the active ingredient.Type: ApplicationFiled: December 10, 2012Publication date: April 18, 2013Applicant: Adhesives Research, Inc.Inventor: Adhesives Research, Inc.
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Publication number: 20130095176Abstract: A controlled release delivery composition comprising: a housing adapted for oral administration; and a plurality of discrete vehicles assembled within the housing, each of the vehicles are not compressed together, each of the vehicles being a bead, a pellet, a tablet, and/or granules compressed into a preselect shape, wherein each of the vehicles comprise a different combination and/or amount of an active agent, an amino acid, a buffer, and a polymer, such that each of the vehicles comprises a different active agent and/or release property from each other, wherein each of the vehicles releases the active agent independently of each other, and wherein each of the vehicles remains independent from each other and intact within the housing prior to oral administration of the delivery composition.Type: ApplicationFiled: September 25, 2012Publication date: April 18, 2013Applicant: Intellipharmaceutics Corp.Inventor: Intellipharmaceutics Corp.
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Patent number: 8420633Abstract: The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The invention further provides methods for the manufacture of such compounds and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists. The compounds are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: GrantFiled: March 24, 2011Date of Patent: April 16, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Cosimo Dolente, Patrick Schnider
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Publication number: 20130090329Abstract: Methods and compositions relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a OPRP genetic signature are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the genetic signature.Type: ApplicationFiled: October 7, 2011Publication date: April 11, 2013Applicant: SUREGENE, LLCInventors: Timothy L. Ramsey, Bharat Mehrotra, Mark D. Brennan
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Publication number: 20130085136Abstract: The present invention concerns novel compounds of Formula (I): wherein R1, R2, R3, R4, R5 and R6 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: June 1, 2011Publication date: April 4, 2013Inventors: Lieven Meerpoel, Louis Jules Roger Marie Maes, Kelly de Wit
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Publication number: 20130078256Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: November 20, 2012Publication date: March 28, 2013Applicant: Korea Research Institute of Chemical TechnologyInventor: Korea Research Institute of Chemical Technology