Polycyclo Ring System Having The Additional 1,3-diazine Ring As One Of The Cyclos Patents (Class 514/252.16)
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Publication number: 20150038494Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&DInventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
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Patent number: 8946226Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.Type: GrantFiled: July 28, 2009Date of Patent: February 3, 2015Assignee: Nerviano Medical Sciences S.r.l.Inventors: Marina Ciomei, Francesco Fiorentini, Enrico Pesenti
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Publication number: 20150031672Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20150031704Abstract: The invention features a method of treating a peripheral vascular disease or a condition associated with a peripheral vascular disease by administering to a subject an effective amount of at least one phosphodiesterase type 5 inhibitor and at least one nitric oxide donor. The invention also features compositions formulated for topical or oral administration including at least one phosphodiesterase type 5 inhibitor, at least one nitric oxide donor, and a pharmaceutically acceptable carrier, as well as kits including these compositions. These methods, compositions, and kits can optionally include other therapeutic agents.Type: ApplicationFiled: October 3, 2014Publication date: January 29, 2015Inventors: Crist J. FRANGAKIS, Harry J. Leighton
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Publication number: 20150031674Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: July 25, 2014Publication date: January 29, 2015Applicant: GENENTECH, INC.Inventors: Joachim Rudolph, Lewis J. Gazzard, James J. Crawford, Chudi Ndubaku, Joy Drobnick, Wendy Lee
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Publication number: 20150031667Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: ApplicationFiled: July 1, 2014Publication date: January 29, 2015Inventors: Shelley Allen, Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Krecher, Jeongbeob Seo
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Publication number: 20150025084Abstract: Provided is a fast dissolving film composition comprising a medically active component as an active ingredient, in which the bitter taste of the active ingredient is masked and the fast dissolving film composition has a high content of 50% or higher. More particularly, provided is a pharmaceutical composition which comprises sildenafil or pharmaceutically acceptable salts thereof as an active ingredient, and which comprises a combination of a specific bitter taste masking agent to achieve masking of a bitter taste. Further, provided is a fast dissolving film composition which comprises a combination of a specific plasticizer to mask a bitter taste, and in which the physical properties of the high-content film are excellent.Type: ApplicationFiled: February 28, 2013Publication date: January 22, 2015Applicant: SEOUL PHARMA CO., LTDInventors: Hyun Jun Jeong, Ik Hyeon Chang, Dal Geun Kim, Jin Hoo Lee, Jin Hee Um, Hyun Soo Kim, Kyung Tae Jung, Kyu Jeong Yeon, Jin Gyu Park
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Publication number: 20150025008Abstract: The present invention generally relates to compositions, reagents and methods for detecting and treating a neural tube defect in a fetus. One aspect of the invention provides a method including administrating a composition containing noggin or LDN-193189 to the fetus in utero. In certain embodiments, the composition is administrated if the maternal blood or amniotic fluid contains an elevated amount of BMP4 and/or a reduced amount of noggin. In another aspect of the invention, the method includes administrating a composition containing GDC-0449 to the fetus in utero. In certain embodiments, the GDC-0449 is administrated if the maternal blood or amniotic fluid contains an elevated amount of sonic hedgehog.Type: ApplicationFiled: July 15, 2014Publication date: January 22, 2015Inventors: Chandra Shekhar Mayanil, Elise Allender, Takao Tsurubuchi, Norman Ginsberg, David G. McLone, Tadanori Tomita
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Publication number: 20150018349Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 27, 2014Publication date: January 15, 2015Applicant: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Publication number: 20150017267Abstract: The present invention relates to the prevention, reduction, inhibition and reversal of pain and inflammation in a non-human mammal by administration of an inhibitor of soluble epoxide hydrolase, as sole active agent or co-administered with other active agents.Type: ApplicationFiled: March 5, 2013Publication date: January 15, 2015Applicant: The Regents of the University of CaliforniaInventors: Alonso G.P. Guedes, Bruce D. Hammock, Christophe Morisseau
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Publication number: 20150018343Abstract: The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.Type: ApplicationFiled: November 30, 2012Publication date: January 15, 2015Inventors: Dominique Swinnen, Cyril Montagne, Vincent Pomel, Anna Quattropani, Jerome Molette, Patrick Gerber
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Patent number: 8933081Abstract: The invention relates to an orodispersible tablet comprising the components pharmaceutically acceptable sildenafil salt (a), polymeric adsorbent (b), in particular cation exchanger resin, sweetener (c), and flavoring (d) and, preferably, mucilage (e) and glidant (f). The invention furthermore relates to a process for the preparation of orodispersible tablets comprising a pharmaceutically acceptable sildenafil salt and to the use of a combination of cation exchanger resin and mucilage for masking the flavor of medicaments for treating erectile dysfunction.Type: GrantFiled: March 31, 2010Date of Patent: January 13, 2015Assignee: ratiopharm GmbHInventors: Sven Winter, Max-Werner Scheiwe
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Patent number: 8933085Abstract: The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: GrantFiled: November 18, 2011Date of Patent: January 13, 2015Assignee: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
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Publication number: 20150011542Abstract: Methods of treating adverse intestinal effects of a non-steroidal anti-inflammatory drugs (NSAID) in a subject by administering to the subject a therapeutically effective amount of a selective bacterial beta-glucuronidase inhibitor. The adverse intestinal effects to be treated include the formation or growth of an intestinal ulcer, increased intestinal permeability, the loss of intestinal villi, bleeding of the intestinal mucosa, and an increased intestinal inflammatory response. The methods are useful for treating the adverse effects of any NSAID such as propionic acid derivatives, carboxylic acid derivatives, enolic acid derivatives, fenamic acid derivatives, sulphonanilidies, and selective COX-2 inhibitors. The bacterial beta-glucuronidase inhibitors are selective for the inhibition of bacterial beta-glucuronidase enzymes and do not inhibit mammalian beta-glucuronidase.Type: ApplicationFiled: January 11, 2013Publication date: January 8, 2015Inventor: Urs A. Boelsterli
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Publication number: 20150005307Abstract: The invention provides a pharmaceutical composition for the transmucosal delivery of a PDE5 inhibitor, said composition comprising a PDE5 inhibitor and a carrier in which said PDE5 inhibitor is soluble or forms a suspension or emulsion. The invention also provides a pharmaceutical composition comprising a PDE5 inhibitor for use in inhibiting PDE activity in vivo, where in said use said composition is delivered by the transmucosal route.Type: ApplicationFiled: December 19, 2012Publication date: January 1, 2015Applicant: LondonPharma Ltd.Inventors: Martin James Sams, Juliet Victoria High, Paul Andrew Jamieson, Clive Booles
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Publication number: 20150005289Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.Type: ApplicationFiled: February 8, 2013Publication date: January 1, 2015Inventors: Hongyan Qi, Soongyu Choi, Amal Dakka, Gary Mitchell Karp, Jana Narasimhan, Nikolai Naryshkin, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Luke Green, Emmanuel Pinard, Hasane Ratni
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Patent number: 8921358Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: March 28, 2013Date of Patent: December 30, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Matthew H. McNeill, Tracy Duong, Angie Vassar, Takehiro Hirano, Yoshito Terao
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Publication number: 20140378452Abstract: Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are other wise delivered to the brain.Type: ApplicationFiled: September 10, 2014Publication date: December 25, 2014Inventor: Gabriela Chiosis
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Publication number: 20140371203Abstract: The present invention provides compounds of formula (I): (Formula (I); wherein A, R1, R2, R3I, V, X, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.Type: ApplicationFiled: November 15, 2012Publication date: December 18, 2014Inventors: David Madge, Fiona Chan, Derek Edward John, Simon D. Edwards, Richard Blunt, Basil Hartzoulakis, Lindsay Brown
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Publication number: 20140371219Abstract: Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases.Type: ApplicationFiled: December 27, 2012Publication date: December 18, 2014Applicant: HANMI PHARM. CO., LTDInventors: In Hwan Bae, Jung Beom Son, Sang Mi Han, Eun Joo Kwak, Ho Seok Kim, Ji Young Song, Eun Young Byun, Seung Ah Jun, Young Gil Ahn, Kwee Hyun Suh
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Patent number: 8912194Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor for use in the treatment of mesothelioma. The compound can be administered together with one or more cytotoxic or cytostatic agents.Type: GrantFiled: November 23, 2009Date of Patent: December 16, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Marina Ciomei, Angela Scaburri
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Publication number: 20140364420Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.Type: ApplicationFiled: January 13, 2014Publication date: December 11, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
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Publication number: 20140364395Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Publication number: 20140364410Abstract: The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 20, 2014Publication date: December 11, 2014Inventors: Tim OWENS, Erik VERNER
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Publication number: 20140364430Abstract: Provided herein are PAK inhibitors.Type: ApplicationFiled: August 14, 2014Publication date: December 11, 2014Inventors: Jay LICHTER, David CAMPBELL, Benedikt VOLLRATH, Sergio G. DURÓN
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Patent number: 8906867Abstract: The production method prepares a solid preparation by dissolving water-insoluble and/or water indissolvable alkaline active pharmaceutical ingredient in an acidifier-containing acid solution to obtain medicated acid liquid; homogeneously mixing alkalizer, adjuvants and the medicated acid liquid, and carrying out wet granulation. The alkalizer is a reagent to reduce the acidity of the mixture of the alkalizer and the medicated acid liquid relative to the acidity of the medicated acid liquid. The preparation method avoids the problems in mechanical pulverization, such as environmental pollution, great loss and serious security risks. This method is simply operated, has high safety coefficient and is convenient for industrialized production. Also disclosed is the solid preparation produced by the method. The solid preparation produced by the method has better dissolution performance than that produced by prior art, and has better or at least equivalent stability and content uniformity with prior art.Type: GrantFiled: December 28, 2010Date of Patent: December 9, 2014Assignees: Shanghai Zhongxi Pharmaceutical Company, Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.Inventors: Siji Zheng, Bo Tan
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Publication number: 20140357645Abstract: A method for healing a hard-to-heal wound including the steps of: topically administering a wound healing composition to a wounded area, wherein the wound healing composition includes, at least one of: (a) a medicament characterized as a calcium channel blocker or pharmaceutically acceptable salts or solvates thereof; (b) a medicament characterized as an alpha-adrenergic antagonist or pharmaceutically acceptable salts or solvates thereof; (c) a medicament characterized as a direct vasodilator or pharmaceutically acceptable salts or solvates thereof; and (d) a medicament characterized as a phosphodiesterase type five inhibitor or pharmaceutically acceptable salts or solvates thereof; and (e) a hemorrheologic agent or pharmaceutically acceptable salts or solvates thereof; (f) a primary dermal penetrating agent or pharmaceutically acceptable salts or solvates thereof: and (g) a topical stimulating agent or pharmaceutically acceptable salts or solvates thereof.Type: ApplicationFiled: August 19, 2014Publication date: December 4, 2014Inventors: Matthew H. Kopacki, Michael J. Torsiello
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Publication number: 20140357644Abstract: The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: August 12, 2014Publication date: December 4, 2014Inventors: Josef R. Bencsik, James F. Blake, Nicholas C. Kallan, Ian S. Mitchell, Keith Lee Spencer, Dengming Xiao, Rui Xu, Christine Chabot, Steven Do, Jun Liang, Brian Safina, Birong Zhang
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Publication number: 20140349996Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: August 11, 2014Publication date: November 27, 2014Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlacter, Anna L. Banka, Jun Liang, Brian Safina, Jun Li, Christine Chabot
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Publication number: 20140349998Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.Type: ApplicationFiled: November 30, 2012Publication date: November 27, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Sean P Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
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Publication number: 20140350021Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart.Type: ApplicationFiled: August 6, 2014Publication date: November 27, 2014Inventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
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Publication number: 20140349995Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: August 8, 2014Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian HURLEY, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
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Publication number: 20140349997Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: August 12, 2014Publication date: November 27, 2014Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlacter, Anna L. Banka, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
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Publication number: 20140343072Abstract: The invention relates to a process for the preparation of a pharmaceutical intermediate, comprising the steps of (i) mixing (a-i) sildenafil base, (b-i) wicking agent, (c-i) disintegrant, (d-i) optionally glidant; (ii) compacting the mixture; and (iii) milling the compacted material; and to an intermediate obtainable by that process. In addition, the invention relates to a process for the preparation of an orally dispersible tablet (hereinafter also referred to as an “orodispersible tablet”) comprising the intermediate of the invention, and to orodispersible tablets obtainable by that process.Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Inventors: Sven Winter, Max-Werner Scheiwe, Dieter Swatschek
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Publication number: 20140343071Abstract: The instant invention provides a method of treating a cancer, selected from the group consisting of breast cancer, melanoma, colorectal cancer, non-small cell lung cancer and ovarian cancer, by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is MK-1775 or a pharmaceutically acceptable salt thereof, or MK-3652 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is MK-8776 or a pharmaceutically acceptable salt thereof, or SCH900444 or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 11, 2012Publication date: November 20, 2014Inventors: Stuart Denham Shumway, Carlo Toniatti, Brian Scott Roberts, Melissa M. Martin
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Patent number: 8889684Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: GrantFiled: January 27, 2012Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Heinz Stadtmueller
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Patent number: 8889677Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.Type: GrantFiled: January 11, 2013Date of Patent: November 18, 2014Assignee: Boehringer Ingellheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Patent number: 8883791Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: GrantFiled: September 28, 2011Date of Patent: November 11, 2014Assignee: Intervet Inc.Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
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Patent number: 8883781Abstract: The present invention relates to compounds of formula IA-i useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: June 12, 2007Date of Patent: November 11, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lev T. D. Fanning, Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson, Yulian Zhang
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Publication number: 20140329800Abstract: The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.Type: ApplicationFiled: December 13, 2012Publication date: November 6, 2014Inventors: Daxin Gao, Heping Yang, Yajun Yu
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Publication number: 20140329827Abstract: The invention relates to the use of flibanserin for the preparation of a medicament for the treatment of pre-menopausal Sexual Desire Disorders.Type: ApplicationFiled: March 4, 2014Publication date: November 6, 2014Applicant: Sprout Pharmaceuticals, Inc.Inventors: Stephane Pollentier, Robert E. Pyke
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Patent number: 8877758Abstract: The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain at least one EP4 receptor antagonist (2), in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryl and wherein R1 and R2 have the meanings given in claim 1, the preparation thereof and the use thereof for the treatment of respiratory complaints.Type: GrantFiled: April 1, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Peter Nickolaus
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Publication number: 20140323438Abstract: The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal.Type: ApplicationFiled: December 17, 2012Publication date: October 30, 2014Inventors: Kevin Frankowski, Samarjit Patnaik, Sui Huang, Juan Jose Marugan, John Norton, Frank J. Schoenen, Noel Terrence Southall, Steven Titus, Wei Zheng
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Publication number: 20140323466Abstract: Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.Type: ApplicationFiled: October 23, 2012Publication date: October 30, 2014Inventors: Hong Liu, Jia Li, Jian Li, Jingya Li, Jiang Wang, Mingbo Su, Jie Lian, Hualiang Jiang, Kaixian Chen
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Publication number: 20140323441Abstract: The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.Type: ApplicationFiled: November 8, 2012Publication date: October 30, 2014Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig Mc Gowan, Philippe Muller, Piere Jean-Marie Bernand Raboisson
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Publication number: 20140323435Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: May 22, 2014Publication date: October 30, 2014Applicants: Cancer Research Technology Limited, Cephalon, Inc.Inventors: Bruce D. Dorsey, Keith S. Learn, Emma L. Morris, Gregory R. Ott, Jonathan R.A. Roffey, Christelle N. Soudy, Jason C. Wagner
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Publication number: 20140315885Abstract: A series of thiazolo[5,4-d]pyrimidine derivatives of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: (I) Q represents a group of formula (Qa), (Qb), (Qc), (Qd) or (Qe) are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.Type: ApplicationFiled: November 8, 2012Publication date: October 23, 2014Inventors: Daniel Christopher Brookings, Daniel James Ford, Richard Jeremy Franklin, Anant Ramrao Ghawalkar, Claire Louise Kulisa, Judi Charlotte Neuss, James Thomas Reuberson
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Publication number: 20140315888Abstract: The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.Type: ApplicationFiled: September 28, 2012Publication date: October 23, 2014Applicant: C&C RESEARCH LABORATORIESInventors: Pil Su Ho, Dong Oh Yoon, Sun Young Han, Won Il Lee, Jung Sook Kim, Woul Seong Park, Sung Oh Ahn, Hye Jung Kim
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Publication number: 20140315902Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: April 18, 2014Publication date: October 23, 2014Inventors: Yaping Sun, Liang Lu, Wenqing Yao, Jincong Zhuo, Liangxing Wu, Meizhong Xu, Ding-Quan Qian, Chunhong He, Fenglei Zhang
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Publication number: 20140315887Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Inventors: Josef R. Bencsik, James F. Blake, Nicholas C. Kallan, Ian S. Mitchell, Keith L. Spencer, Dengming Xiao, Rui Xu, Christine Chabot, Jun Liang, Brian S. Safina