Abstract: The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.
Type:
Application
Filed:
February 28, 2013
Publication date:
January 1, 2015
Applicant:
Takeda Pharmaceutical Company Limited
Inventors:
Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
Abstract: The present invention relates to the field of pharmaceutical technology and in particular to novel dosage forms of medicaments containing as active ingredients simvastatin and ezetimibe, or pharmaceutically acceptable salts thereof. The present pharmaceutical compositions are characterized in that the contact of the compositions with oxygen is substantially reduced, such as by coating the composition, providing a medicament useful for the treatment and prevention of atherosclerosis and related conditions, in an environment having an essentially reduced oxygen or humidity, respectively, content.
Abstract: The invention relates to a formulation for delivering by oral transmucosal administration at least one lipid-lowering active principle, preferably from the statin family, said formulation including said active principle in the base or salt form, an aqueous alcohol solution titrating at least 30° alcohol, and optionally a pH correcting agent and/or an antioxidant, said active principle being in a stable and completely dissolved state in the aqueous alcohol solution. The invention also relates to a method of preparing said formulation and to the use thereof, preferably in single-dose packaging, for treating and preventing hyperlipemia and/or cardiovascular conditions.
Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
Type:
Application
Filed:
July 25, 2014
Publication date:
November 13, 2014
Inventors:
Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
Type:
Application
Filed:
March 12, 2014
Publication date:
October 23, 2014
Inventors:
Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
Type:
Grant
Filed:
September 22, 2009
Date of Patent:
October 14, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
Abstract: The present invention is an orally consumed fixed combination formulation of both rosuvastatin and ezetimibe in one tablet that is expected to have the same Area Under Curve as two active ingredients taken together individually orally, and pharmaceutically acceptable additives suitable for the preparation. In preferred embodiments of this invention, the rosuvastatin is in the form of rosuvastatin calcium and the pharmaceutically acceptable additives are selected from diluents, disintegrants, glidants, lubric ants, colorants and combinations thereof.
Abstract: Disclosed are compound of Formula (Ia), wherein R1, R2, and R3 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions, comprising one or more compounds of Formula (Ia).
Type:
Application
Filed:
March 13, 2014
Publication date:
September 18, 2014
Inventors:
Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Andrew J. Souers, Rajeev Goswami
Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment, particularly for reducing the risk of cardiovascular disease, especially coronary heart disease (such as myocardial infarction) and stroke. For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents and kits for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents and kits for their detection.
Abstract: The invention pertains to a method of determining a statin dosage for an individual in need of treatment with a statin, comprising determining a SLCO1B1 genotype from a nucleic acid sample of the individual, said genotype comprising the presence or absence of the SLCO1B1-056 polymorphism, and determining an ApoE genotype or phenotype identifying an ApoE polymorphism selected from the group consisting of ApoE2, ApoE3, ApoE4, and any combination thereof, wherein the combination of a SLCO1B1 genotype identifying the presence of the SLCO1B1-056 C polymorphism and the ApoE genotype or phenotype identifying one of the ApoE3/4 or ApoE4/4 genotypes indicates the statin dosage.
Abstract: Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C?N—O— has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.
Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
Type:
Application
Filed:
July 19, 2012
Publication date:
August 7, 2014
Inventors:
Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
Type:
Application
Filed:
April 3, 2014
Publication date:
August 7, 2014
Applicant:
Endo Pharmaceuticals Inc.
Inventors:
Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
Type:
Application
Filed:
August 20, 2012
Publication date:
July 31, 2014
Inventors:
Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
Abstract: The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
Type:
Application
Filed:
September 17, 2012
Publication date:
July 17, 2014
Inventors:
Giuseppe Giannini, Walter Cabri, Gianfranco Battistuzzi, Davide Vignola, Nicola Fanto', Claudio Pisano, Loredana Vesci
Abstract: One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers.
Type:
Application
Filed:
July 29, 2013
Publication date:
June 12, 2014
Applicant:
CITY OF HOPE
Inventors:
Samuel RAHBAR, James L. FIGAROLA, Christopher LINCOLN, David HORNE, Rachael MOONEY, Monika POLEWSKI, George SOMLO, Lixin YANG
Abstract: Provided is a crystalline composition comprising a mixture of a compound of formula 1 (Ezetimibe) and proline or proline derivatives, or a hydrate/solvate thereof, as well as a process for obtaining the same. And a process for the purification of Ezetimibe is also disclosed.
Type:
Application
Filed:
July 24, 2012
Publication date:
June 5, 2014
Applicant:
BASF SE
Inventors:
Andreas Hafner, Tobias Hintermann, Martin Szelagiewicz, Bernd Siebenhaar, Fritz Blatter
Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
Type:
Grant
Filed:
August 23, 2012
Date of Patent:
May 20, 2014
Assignee:
Endo Pharmaceuticals Inc.
Inventors:
Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.
Type:
Application
Filed:
December 12, 2013
Publication date:
May 15, 2014
Applicant:
PTC THERAPEUTICS, INC.
Inventors:
Sergey V. Paushkin, Charles Romfo, Ellen Welch, Nikolai Naryshkin
Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment (particularly for reducing the risk of venous thrombosis). For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents for their detection.
Type:
Application
Filed:
March 20, 2013
Publication date:
May 8, 2014
Applicant:
CELERA CORPORATION
Inventors:
Lance BARE, James J. DEVLIN, Frits R. ROSENDAAL, Pieter H. REITSMA, Irene D. BEZEMER
Abstract: The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
Type:
Application
Filed:
October 8, 2013
Publication date:
April 10, 2014
Applicant:
SANOFI
Inventors:
Lothar SCHWINK, Martin BOSSART, Heiner GLOMBIK, Matthias GOSSEL, Dieter KADEREIT, Thomas KLABUNDE, Thomas MAIER, Siegfried STENGELIN
Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
Abstract: The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
Type:
Application
Filed:
May 24, 2013
Publication date:
April 3, 2014
Applicant:
Catabasis Pharmaceuticals, Inc.
Inventors:
Jill C. Milne, Michael R. Jirousek, Chi B. Vu
Abstract: Disclosed is a personalized diagnostic and treatment solution for cardiovascular disease. The invention comprises an extended CVD risk assessment panel, combining tests for traditional and new important risk markers, and methods for devising a personalized treatment plan for a patient via the use of a CVD diagnosis and treatment protocol algorithm. The new important risk markers include HDL subpopulation profile by two-dimensional gel-electrophoresis, plasma sterols, direct measurement of sdLDL-C, determination of CRP molecular forms, glycated albumin as a percentile of total albumin, and other specialized testing pertaining to apolipoprotein E and Factor V Leiden genotyping, NT-proBNP and adiponectin. This solution provides a more complete risk assessment of an individual than merely measuring traditional CVD risk markers, and enables the healthcare practitioner to optimize therapy for patients with or without established CVD.
Abstract: The invention generally relates to methods for determining whether a patient should be administered a drug that inhibits cholesterol absorption. In certain aspects, methods of the invention involve obtaining a sample from a patient, conducting an assay on the sample to obtain a level of a cholesterol absorption marker, and comparing the level to a reference level, in which a level above the reference level indicates that the patient should be administered a drug that inhibits cholesterol absorption.
Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
Type:
Application
Filed:
October 28, 2013
Publication date:
March 20, 2014
Inventors:
Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
Abstract: The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom, and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(?O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)RB (RB is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.
Type:
Grant
Filed:
February 5, 2010
Date of Patent:
March 18, 2014
Assignee:
Nippon Shinyaku Co., Ltd.
Inventors:
Hidetaka Fujihara, Tetsuo Asaki, Katsutoshi Hori, Haruna Naito
Abstract: Provided herein are polycyclic ?-lactam compounds, compositions thereof and methods for the treatment and prevention of diseases such as cancer, including pancreatic cancer and pancreatic cancers resistant to mainline chemotherapeutic agents.
Type:
Application
Filed:
January 27, 2012
Publication date:
March 6, 2014
Applicant:
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Abstract: The present invention encompasses compounds of general formula (1) wherein B, R1 to R5, Rx, m and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use in such treatment.
Type:
Application
Filed:
October 23, 2013
Publication date:
February 20, 2014
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Ioannis SAPOUNTZIS, Daniel KUHN, Heinz STADTMUELLER
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Type:
Application
Filed:
July 31, 2013
Publication date:
February 13, 2014
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
William K. Hagmann, Ravi P. Nargund, Timothy A. Blizzard, Hubert Josien, Purakkattle Biju, Christopher W. Plummer, Qun Dang, Bing Li, Linus S. Lin, Mingxiang Cui, Bin Hu, Jinglai Hao, Zhengxia Chen
Abstract: Methods and compositions for the effect of Cholesteryl ester transfer protein (CETP) polymorphisms on mRNA splicing, statin treatment outcome, response to CETP inhibitor drugs, and myocardial infarction risk are described.
Abstract: The present invention inter alia provides a method, and uses thereof, of predicting statin-induced muscle toxicity or its complications, such as myalgia, myopathy and rhabdomyolysis, by detecting the lipid concentrations or lipid ratios of a biological sample and comparing it to a control. This method has identified lipid markers that are more specific and sensitive in detecting these statin-induced muscle toxicity than the currently utilized clinical markers. Also provided is an antibody towards said lipids, and the use thereof for predicting, diagnosing, statin-induced muscle toxicity. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of statin-induced muscle toxicity.
Type:
Application
Filed:
April 8, 2011
Publication date:
January 30, 2014
Applicant:
ZORA BIOSCIENCES OY
Inventors:
Reijo Laaksonen, Kim Ekroos, Reini Hurme, Minna Janis, Riikka Katainen, Kirill Tarasov
Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
Type:
Application
Filed:
April 4, 2012
Publication date:
January 16, 2014
Inventors:
Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
Type:
Application
Filed:
July 12, 2013
Publication date:
January 16, 2014
Inventors:
Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
Abstract: Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
Type:
Application
Filed:
March 16, 2012
Publication date:
January 9, 2014
Inventors:
Stephen T. Wrobleski, Gregory D. Brown, Lidia M. Doweyko, Jingwu Duan, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Zhonghui Lu, Steven H. Spergel, John S. Tokarski, Hong Wu, Bingwei Vera Yang
Abstract: Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R1, R2, R3, R4, R5 and R6 are defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention.
Abstract: Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
Type:
Application
Filed:
March 16, 2012
Publication date:
January 2, 2014
Inventors:
Stephen T. Wrobleski, Jagabandhu Das, Lidia M. Doweyko, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Steven H. Spergel, John S. Tokarski, Hong Wu, Bingwei Vera Yang
Abstract: The present invention relates to a tablet composition comprising a particle and a pharmaceutically acceptable carrier, wherein the particle comprises an amorphous structure and a submicron domain, and wherein the amorphous structure is a molecular solid dispersion of a drug in a polymeric matrix and the submicron domain is a submicron drug particle. The tablet may further comprise a micronized drug particle. The pharmaceutically acceptable carrier comprises a binder, a filler, a lubricant, and optionally a gelling agent, a glidant and an anti-sticking agent.
Type:
Application
Filed:
November 18, 2012
Publication date:
December 26, 2013
Applicant:
Magnifica Inc.
Inventors:
David Wong, James Aiping Lee, Peter Pingfan Yang
Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing a pharmaceutical composition comprising a pharmaceutically active ingredient (API) that is poorly soluble in water, a pharmaceutical composition obtained according to said process, to a dosage form comprising said pharmaceutical composition and to the use of said dosage forms for the treatment of hypercholesterolemia.
Type:
Application
Filed:
December 21, 2011
Publication date:
December 19, 2013
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Rok Staric, Simon Skubin, Miha Homar, Bostjan Markun, Sandra Berglez, Petra Kralj, Marija Boskovic
Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
Type:
Application
Filed:
August 8, 2013
Publication date:
December 12, 2013
Applicant:
Novartis AG
Inventors:
Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
Type:
Application
Filed:
August 7, 2013
Publication date:
November 28, 2013
Applicant:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed.
Type:
Application
Filed:
June 24, 2013
Publication date:
October 31, 2013
Inventors:
Qun Kevin FANG, Frank Xinhe Wu, Paul T. Grover, Seth C. Hopkins, Una Campbell, Milan Chytil, Kerry L. Spear
Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
Type:
Application
Filed:
June 7, 2013
Publication date:
October 24, 2013
Inventors:
Arnab K. Chatterjee, Advait S. Nagle, Tao Wu, David C. Tully, Kelli L. Kuhen
Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
Type:
Grant
Filed:
July 9, 2010
Date of Patent:
October 15, 2013
Assignee:
IRM LLC
Inventors:
Arnab K. Chatterjee, Advait S. Nagle, Tao Wu, David C. Tully, Kelli L. Kuhen
Abstract: A compressed formulation comprising an ordered mesoporous silica loaded with an active ingredient, a combination of microcrystalline cellulose (MCC) and croscarmellose sodium, and optional further excipients.
Type:
Application
Filed:
November 28, 2011
Publication date:
September 19, 2013
Applicant:
FORMAC PHARMACEUTICALS N.V.
Inventors:
Monica Vialpando, Johan Martens, Guy Van Den Mooter, Filip Kiekens