The Additional Five-membered Hetero Ring Consists Of Three Ring Carbons, And Of Nitrogen And Chalcogen In Adjacent Ring Positions (e.g., Isoxazolyl, Isothiazolyl, Etc.) Patents (Class 514/254.04)
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Publication number: 20110237596Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: November 24, 2009Publication date: September 29, 2011Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Seierstad
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Publication number: 20110237602Abstract: The invention relates to a method for treating schizophrenia and/or related diseases comprising administering lurasidone and a mGluR2 ligand to a mammal in need thereof.Type: ApplicationFiled: March 28, 2011Publication date: September 29, 2011Applicants: Vanderbilt University, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Herbert Y. MELTZER, Masakuni Horiguchi
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Publication number: 20110212975Abstract: Compounds which exhibit antiviral activity, particularly against influenza virus, and methods of making and using thereof are described herein. In one embodiment, the compounds are heterocyclic amides containing piperazine and isozazole rings and optionally substituted with one or more substituents. The compounds can be formulated with one or more pharmaceutically acceptable excipients to form compositions suitable for enteral or parenteral administration. The compounds are preferably used to treat or prevent Influenza A infections, such as H1N1, H2N2, H3N2, H5N1, H7N7, H1N2, H9N2, H7N2, H7N3, and H10N7.Type: ApplicationFiled: August 5, 2010Publication date: September 1, 2011Inventors: Yi Tsun Richard Kao, Dan Yang, Kwok-Yung Yuen
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Patent number: 8008300Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: GrantFiled: July 8, 2009Date of Patent: August 30, 2011Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Patent number: 8003637Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.Type: GrantFiled: March 28, 2011Date of Patent: August 23, 2011Assignee: Handa Pharmaceuticals, LLCInventors: Fang-yu Liu, Zhi-qun Shen
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Patent number: 7994338Abstract: The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof.Type: GrantFiled: August 16, 2007Date of Patent: August 9, 2011Assignees: The J. David Gladstone Institutes, University Of Maryland, BaltimoreInventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Publication number: 20110183993Abstract: The present invention relates to a novel cycloalkane derivative which has an excellent psychotropic action.Type: ApplicationFiled: January 28, 2011Publication date: July 28, 2011Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Ryu Nagata, Mayumi Oda, Norihiko Tanno, Masayuki Muto, Ikutaro Saji
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Publication number: 20110182947Abstract: A controlled release dosage form has a coated core with the core comprising a drug-containing composition and a water-swellable composition, each occupying separate regions within the core. The drug-containing composition comprises a low-solubility drug and a drug-entraining agent. The coating around the core is water-permeable, water-insoluble and has at least one delivery port therethrough. A variety of formulations having specific drug release profiles are disclosed.Type: ApplicationFiled: December 27, 2010Publication date: July 28, 2011Inventors: Leah E. Appel, Ronald A. Beyerinck, Mark B. Chidlaw, William J. Curatolo, Dwayne T. Friesen, Kelly L. Smith, Avinash G. Thombre
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Publication number: 20110178091Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.Type: ApplicationFiled: September 23, 2009Publication date: July 21, 2011Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
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Patent number: 7981883Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.Type: GrantFiled: May 17, 2006Date of Patent: July 19, 2011Assignee: Gruenenthal GmbHInventors: Robert Frank, Ruth Jostock, Melanie Reich, Gregor Bahrenberg, Hans Schick, Helmut Sonnenschein
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Publication number: 20110166156Abstract: Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed.Type: ApplicationFiled: December 23, 2010Publication date: July 7, 2011Applicant: Alkermes, Inc.Inventors: Laura Cook Blumberg, Örn Almarsson
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Publication number: 20110165188Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Inventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Way Tsun Yue
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Publication number: 20110160199Abstract: The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.Type: ApplicationFiled: July 28, 2008Publication date: June 30, 2011Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD., SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jianqi Li, Shaoping Peng, Wangping Cai, Kai Gao
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Publication number: 20110152272Abstract: The present invention relates to the use of agonists of 5-HT2C receptors for the treatment of urinary incontinence, preferably mixed incontinence or stress urinary incontinence. The invention also relates to the use of antagonists of 5-HT2C receptors for the treatment of urine retention. The present invention also relates to a method of treatment of incontinence, to assays to screen for compounds useful in the treatment of incontinence, and to methods of preparing compositions for the treatment of urinary incontinence.Type: ApplicationFiled: November 5, 2010Publication date: June 23, 2011Inventors: Gordon McMurray, Wesley Dennis Miner
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Publication number: 20110152251Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.Type: ApplicationFiled: November 17, 2010Publication date: June 23, 2011Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
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Publication number: 20110124659Abstract: The present invention relates to a novel cycloalkane derivative which has a useful psychotropic action with less side effect.Type: ApplicationFiled: November 12, 2010Publication date: May 26, 2011Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventor: Hironori KINOSHITA
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Publication number: 20110118264Abstract: The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammalType: ApplicationFiled: January 28, 2011Publication date: May 19, 2011Inventors: Yonggil Kim, Nahmryune Cho, Yunhee Kim, Joon Heo, Seonmin Dong, Mi Kyung Ji, Man-Young Cha, Kiho Lee
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Publication number: 20110112074Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: August 18, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Markus FOLLMANN, Volkmar WEHNER, Jean-Michel ALTENBURGER, Gilbert LASSALLE, Jean-Pascal HERAULT
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Patent number: 7939535Abstract: The present invention provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.Type: GrantFiled: September 16, 2009Date of Patent: May 10, 2011Assignee: Hoffman-La Roche Inc.Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Publication number: 20110105467Abstract: 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 SULT4A1-1 haplotype are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the haplotype status.Type: ApplicationFiled: August 18, 2010Publication date: May 5, 2011Inventors: TIMOTHY L. RAMSEY, MARK D. BRENNAN
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Publication number: 20110105519Abstract: The invention relates to new pharmaceutical compositions for the treatment of sexual disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment of sexual disorders and methods for the preparation thereof.Type: ApplicationFiled: January 10, 2011Publication date: May 5, 2011Inventors: Klaus Mendla, Thomas Friedl, Wolfram Eisenreich, Robert Pyke
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Patent number: 7915405Abstract: Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: September 30, 2009Date of Patent: March 29, 2011Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Taeho Lee, Moon-Kook Jeon, Heeyeong Cho, Jae Yang Kong, Gildon Choi, Dae Young Jeong, Soon-Hee Hwang
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Publication number: 20110046142Abstract: Methods for identifying prodrug antibiotic compounds and direct inhibitory antibiotic compounds utilizing various screens are provided. Also provided are methods for treating infections using these compounds.Type: ApplicationFiled: June 11, 2008Publication date: February 24, 2011Applicant: Northeastern UniversityInventors: Kim Lewis, Gabriele Casadei
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Publication number: 20110046134Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: October 29, 2010Publication date: February 24, 2011Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
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Publication number: 20110028482Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: ApplicationFiled: May 18, 2010Publication date: February 3, 2011Applicant: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20110008435Abstract: The present invention provides a composition comprising ziprasidone useful in the treatment and prevention of schizophrenia and similar psychiatric disorders. In one embodiment, the composition comprises nanoparticulate particles comprising ziprasidone and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. In another embodiment, the composition comprises a modified release composition that, upon administration to a patient, delivers ziprasidone in a bimodal, multimodal or continuous manner. The invention also relates to dosage forms containing such compositions, and to methods for the treatment and prevention of schizophrenia and similar psychiatric disorders.Type: ApplicationFiled: February 7, 2007Publication date: January 13, 2011Applicant: Elan Corporation plcInventors: John G. Devane, Paul Stark, Niall M.M. Fanning, Gurvinder Singh Rekhi, Scott A. Jenkins, Gary Liversidge
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Publication number: 20110003828Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.Type: ApplicationFiled: June 24, 2010Publication date: January 6, 2011Inventors: Laura Cook Blumberg, Julius F. Remenar, Örn Almarsson, Tarek A. Zeidan
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Publication number: 20110002989Abstract: The present invention provides methods, dosage forms and kits for treating with an effective amount of ziprasidone a CNS disorder in a human when the human is in a fasted state. In one embodiment, the invention relates to a method for treating a CNS disorder in a human, which method comprises administering to the human in a fasted state, a solid oral dosage form comprising an amount of ziprasidone effective to treat said CNS disorder, wherein the area under the serum concentration versus time curve (AUC0-inf) of the ziprasidone in the human subsequent to said administering is from 70% to 140% of the mean area under the ziprasidone serum concentration versus time curve (AUC0-inf) resulting from administration of a control ziprasidone immediate release oral capsule containing the same amount of ziprasidone to a cohort of humans in a fed state.Type: ApplicationFiled: March 4, 2009Publication date: January 6, 2011Inventors: William John Curatolo, Scott Max Herbig, Avinash Govind Thombre, Jaymin Chandrakant Shah, Sheri L. Shamblin, Timothy Lukas, William Brett Caldwell, Dwayne Thomas Friesen, David Keith Lyon, Christopher Donovan Craig
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Patent number: 7863277Abstract: A transdermal composition that contains an antipsychotic is provided for the treatment of neuropsychiatric disorders. Also, provided are methods for preparing a topical antipsychotic composition. Methods for treating neuropsychiatric disorders, including schizophrenia, are further disclosed. The transdermal composition includes a therapeutically effective amount of an antipsychotic in an amount sufficient to treat neuropsychiatric disorders in a pharmaceutically acceptable carrier.Type: GrantFiled: March 7, 2006Date of Patent: January 4, 2011Assignee: Medcara, L.L.C.Inventor: Craig Herman
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Patent number: 7858630Abstract: The present invention provides compounds of the general formula (I) wherein X, n and R1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, methods for their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, useful in the treatment and/or the prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.Type: GrantFiled: September 16, 2009Date of Patent: December 28, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Publication number: 20100324020Abstract: The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R1-R5 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Stanton F. McHardy, John A. Lowe, III
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Publication number: 20100324044Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: August 26, 2010Publication date: December 23, 2010Inventors: Joseph Cacciola, James Empfield, James Folmer, Angela M Hunter, Scott Throner
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Publication number: 20100317662Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: August 20, 2010Publication date: December 16, 2010Inventors: Joseph Cacciola, James Empfield, James Folmer, Angela M. Hunter, Scott Throner
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Patent number: 7851473Abstract: There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I0): wherein Z is oxygen or sulfur; R1 is aryl which may be substituted, or a heterocyclic group which may be substituted; R1a is a hydrogen atom, a hydrocarbon group which may be substituted, hydroxyl, etc.; R2 is piperidin-1,4-diyl which may be substituted, or piperazin-1,4-diyl which may be substituted; R3 is a group formed by eliminating two hydrogen atoms from a 5-membered aromatic heterocyclic group having 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, which may be further substituted, —CO—, etc.; and R4 is a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; or a salt thereof.Type: GrantFiled: November 17, 2005Date of Patent: December 14, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Matsumoto, Masakuni Kori, Junichi Miyazaki, Yoshihiro Kiyota
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Publication number: 20100310681Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.Type: ApplicationFiled: June 3, 2010Publication date: December 9, 2010Applicant: MARQUETTE UNIVERSITYInventor: Mohammadhossein Behnam Ghasemzadeh
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Publication number: 20100298313Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: ApplicationFiled: August 4, 2010Publication date: November 25, 2010Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Publication number: 20100292211Abstract: The present invention relates to the prediction of antipsychotic treatment efficacy based on a patient's genotype at one or more single nucleotide polymorphism (SNP) loci and to the treatment of a patient based on such prediction.Type: ApplicationFiled: September 10, 2008Publication date: November 18, 2010Inventor: Christian LAVEDAN
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Patent number: 7834017Abstract: There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.Type: GrantFiled: August 10, 2007Date of Patent: November 16, 2010Assignee: Palatin Technologies, Inc.Inventors: Kevin Burris, Yi-Qun Shi, Shubh D. Sharma, Yadi Reddy Bonuga, Papireddy Purma
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Publication number: 20100280045Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Pl3-kinase activity.Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Inventors: Julie Nicole HAMBLIN, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Nigel James Parr
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Publication number: 20100273795Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Jared Andrew Forrester
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Publication number: 20100240676Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, K, G, E and WType: ApplicationFiled: September 19, 2008Publication date: September 23, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober, Wolfgang Staehle
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Publication number: 20100240619Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1 N-oxides, and salts thereof, wherein R1, R2, A, G, W, Z1, X, J, and n are as defined in the disclosure, and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of the aforesaid composition. Also disclosed is a composition comprising component (a) of aforesaid composition and at least one insecticide. Also disclosed are compounds of Formula 1A, 1B and 1C, wherein R1, R2, A, G, W, Z1, X, J, n, Z3, M and J1 are as defined in the disclosure.Type: ApplicationFiled: October 23, 2008Publication date: September 23, 2010Inventors: Vann Gregory, Robert James Pasteris
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Publication number: 20100234389Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.Type: ApplicationFiled: October 9, 2008Publication date: September 16, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni Kori, Mitsunori Kouno
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Publication number: 20100234288Abstract: Sustained release pharmaceutical composition comprising at least one poorly soluble active agent(s), at least one solubilizer, a release rate controlling polymer system consisting of an acid-soluble polymer and a pH-dependent polymer, and optionally other pharmaceutically acceptable excipients. The present invention also describes a process for preparation of such compositions and method of using such compositions. The sustained release compositions are useful in providing therapeutically effective levels of active agent(s) for extended periods of time.Type: ApplicationFiled: March 19, 2007Publication date: September 16, 2010Applicant: PANACEA BIOTEC LTDInventors: Rajesh Jain, Kour Chand Jindal, Sampath Kumar Devarajan
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Publication number: 20100234391Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: DOW AGROSCIENCES LLCInventors: Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster
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Publication number: 20100234349Abstract: This invention relates to novel pharmaceutical compositions comprising therapeutically effective combination of a positive allosteric modulator of nicotine receptors; and a cognitive enhancer selected from the group consisting of a nicotine acetylcholine receptor agonist, an acetylcholine esterase inhibitor, a positive AMPA receptor modulator, an antipsychotic drug, an antidepressant drug and an anti Parkinson drug. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating cognitive disorders.Type: ApplicationFiled: September 4, 2007Publication date: September 16, 2010Inventors: Gunnar M. Olsen, Dan Peters, Bjarne H. Dahl, Jeppe Kejser Christensen, Steven Charles Loechel, Daniel B. Timmermann
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Publication number: 20100222341Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.Type: ApplicationFiled: September 19, 2008Publication date: September 2, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HARTUNGInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Patent number: 7786110Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: GrantFiled: November 8, 2007Date of Patent: August 31, 2010Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Publication number: 20100216795Abstract: The present invention relates to Traf2- and Nck-interacting kinase (TNIK) inhibitors, pharmaceutical compositions, and methods for the treatment of cancer patients with TNIK inhibitors. And the present invention relates to a novel aminothiazole derivatives. The TNIK inhibitors are showed by a next formula (I). Wherein R1, R2, R3, R4, R5 and R6 represent independently a hydrogen atom or a substituent group.Type: ApplicationFiled: April 23, 2010Publication date: August 26, 2010Inventors: Tesshi Yamada, Miki Shitashige, Koichi Yokota, Masaaki Sawa, Hideki Moriyama