The Additional Five-membered Hetero Ring Also Has Chalcogen As A Ring Member Patents (Class 514/254.02)
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Patent number: 7847101Abstract: Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R1, R2 and R3 at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R4 is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl.Type: GrantFiled: July 23, 2003Date of Patent: December 7, 2010Assignee: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
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Patent number: 7846951Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: July 31, 2008Date of Patent: December 7, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark T. Miller, Sarah S. Hadida Ruah, Peter D. J. Grootenhuis, Matthew Hamilton
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Publication number: 20100305139Abstract: The present invention provides a pharmaceutical agent for the treatment and/or prophylaxis of abnormal blood glucose and lipid metabolism associated with eating, for which a sufficient treatment method or a therapeutic drug has not been found.Type: ApplicationFiled: August 11, 2010Publication date: December 2, 2010Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Yuji ABE, Aki KUSUNOKI, Yoshiharu HAYASHI, Fumihiko AKAHOSHI
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Patent number: 7842693Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: December 9, 2003Date of Patent: November 30, 2010Assignee: ChemoCentryx, Inc.Inventors: Andrew M. K. Pennell, James B. Aggen, J. J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi, Valeri V. Martichonok
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Publication number: 20100298340Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: April 12, 2007Publication date: November 25, 2010Applicants: AstraZeneca AB, Astex Therapeutics Ltd.Inventors: Stefan Berg, Karin Kolmodin
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Publication number: 20100298316Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.Type: ApplicationFiled: March 22, 2007Publication date: November 25, 2010Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg, Inge Thoger Christensen, Jane Marie Lundbeck, Erik Knud Andersen
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Publication number: 20100298288Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moietyType: ApplicationFiled: June 16, 2008Publication date: November 25, 2010Applicant: MERCK & CO., INCInventors: Julianne A. HUNT, Ramzi F. Sweis, Dooseop Kim, Florida Kallashi, Peter J. Sinclair
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Publication number: 20100297035Abstract: Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: April 12, 2010Publication date: November 25, 2010Applicant: LIGAND PHARMACEUTICALS, INC.Inventors: Wallace C. Pringle, John M. Peterson, Linghong Xie, Ping Ge, Yang Gao, Joseph W. Ochterski, Jiong Lan
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Publication number: 20100297097Abstract: The present invention relates to substituted triazole compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming A?42 peptide such as Alzheimer's disease and the like.Type: ApplicationFiled: November 7, 2008Publication date: November 25, 2010Inventors: Anne Marie Jeanne Bouillot, Alain Laroze
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Publication number: 20100298301Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: May 9, 2008Publication date: November 25, 2010Applicant: SAREUM LIMITEDInventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
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Publication number: 20100292248Abstract: A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.Type: ApplicationFiled: July 27, 2010Publication date: November 18, 2010Applicant: Solvay Pharmaceuticals B.V.Inventors: Andrew C. McCreary, Gustaaf J.M. Van Scharrenburg, Martinus Th.M. Tulp
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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: 20100285006Abstract: The present invention relates to novel thiazole-substituted indolin-2-ones as inhibitors of CSCPK and related kinases; to methods of inhibiting cancer stem cells by using a kinase inhibitor; to pharmaceutical compositions containing such compounds; and to methods of using such compounds in the treatment of a protein kinase related disorder in a mammal; and to processes of making such compounds and intermediates thereof.Type: ApplicationFiled: September 5, 2008Publication date: November 11, 2010Inventors: Chiang Jia LI, Ji-Feng Liu, Youzhi Li, Wei Li, Harry Rogoff
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Publication number: 20100280030Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 8, 2008Publication date: November 4, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 7825112Abstract: The disclosure relates to 2-carbamide-4-phenylthiazole derivatives having the following general formula (I): wherein R1, R2, R3, Y and p are as defined in the disclosure. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: GrantFiled: June 26, 2008Date of Patent: November 2, 2010Assignee: sanofi-aventisInventors: Pierre Casellas, Daniel Floutard, Pierre Fraisse, Stephane Hourcade, Samir Jegham
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Patent number: 7825147Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.Type: GrantFiled: August 30, 2004Date of Patent: November 2, 2010Assignee: Ranbaxy Laboratories LimitedInventors: Venkata P. Palle, Sarala Balachandran, Mohammad Salman, Gagan Kukreja, Nidhi Gupta, Abhijit Ray, Sunanda G. Dastidar
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Publication number: 20100273766Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: ApplicationFiled: December 1, 2006Publication date: October 28, 2010Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Patent number: 7820657Abstract: 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: GrantFiled: March 16, 2007Date of Patent: October 26, 2010Assignee: Ambit Biosciences CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Publication number: 20100267685Abstract: The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases.Type: ApplicationFiled: April 23, 2010Publication date: October 21, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Röhrig, Karl-Heinz Schlemmer
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Publication number: 20100267708Abstract: The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient.Type: ApplicationFiled: December 22, 2008Publication date: October 21, 2010Applicant: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Sung Bae Lee, Seung Hyun Yoon, Mi Kyoung Cho, Kyoung Hee Kim, Heui Sul Park, Hyoung Jin Kim
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Patent number: 7816376Abstract: The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R1, R3, R4, R8, p, k, E, G, Z and Q are as defined in claim 1, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses.Type: GrantFiled: March 5, 2003Date of Patent: October 19, 2010Assignee: Merck Patent GmbHInventors: Oliver Schadt, Joachim Leibrock, Helmut Pruecher, Christoph Seyfried
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Patent number: 7816360Abstract: The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: GrantFiled: December 22, 2008Date of Patent: October 19, 2010Assignee: Janssen Pharmaceutica NVInventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Libuse Jaroskova, Peter Walter Maria Roevens, Louis Jozef Elisabeth Van Der Veken, Marcel Viellevoye, Joannes Theodorus Maria Linders
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Patent number: 7816354Abstract: The present invention is directed to compounds of Formula I: Wherein R1, R2, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: GrantFiled: December 6, 2006Date of Patent: October 19, 2010Assignee: AstraZeneca ABInventors: Abdelmalik Slassi, Methvin Isaac, Ian Egle, Fupeng Ma, Babu Joseph, Joshua Clayton, Krzysztof Swierczek
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Patent number: 7812021Abstract: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: August 21, 2008Date of Patent: October 12, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
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Patent number: 7807672Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: GrantFiled: February 13, 2007Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
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Publication number: 20100249188Abstract: The present invention relates to the prediction of QT prolongation following administration of a compound capable of increasing an individual's QT interval based on the individual'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: September 30, 2010Inventors: Christian Lavedan, Simona Volpi, Louis Licamele, Kendra Tomino Mack, Callie Michelle Heaton
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Publication number: 20100249030Abstract: The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment.Type: ApplicationFiled: July 28, 2008Publication date: September 30, 2010Inventor: Andrea Dawn Basso-Porcaro
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Patent number: 7799791Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms.Type: GrantFiled: January 8, 2009Date of Patent: September 21, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20100234390Abstract: The present invention provides novel compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The novel compounds are useful as antibacterial agents in the treatment of conditions such as nosocomial pneumonia, community acquired pneumonia, infections caused by vancomycin resistant enterococci (VRE), methicillin resistant Staphylococcus aureus (MRSA), Heamophilus influenzae (HI) and penicillin resistant Streptococcus pneumoniae (PRSP). The compounds of the present invention are effective against a number of human or animal pathogens including VRE, PRSP, HI and MRSA.Type: ApplicationFiled: June 20, 2008Publication date: September 16, 2010Inventors: Simi Pushpan, Uma Ramachandran, Mrinalkanti Kundu
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Publication number: 20100234365Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: December 12, 2007Publication date: September 16, 2010Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Publication number: 20100234395Abstract: Discloses is a pharmaceutical agent comprising an ureide derivative represented by the formula: or a pharmaceutically acceptable salt thereof as an active ingredient. The ureide derivative or the pharmaceutically acceptable salt thereof is useful for the relief of a pain or the treatment or prevention of neurogenic pain.Type: ApplicationFiled: March 27, 2007Publication date: September 16, 2010Applicant: TORAY INDUSTRIES, INC.Inventors: Yuji Sugawara, Naoki Izumimoto, Hideyuki Tsutsui
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Patent number: 7795288Abstract: The invention relates to thiazole and pyrazole derivatives of formula (I) wherein Q is S and X is C, or Q is CH and X is N; R1 is unsubstituted or substituted phenyl; and R2 is unsubstituted or substituted aryl or heteroaryl; or a salt of the said compounds, and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour disease, in particular such diseases which respond to an inhibition of the Flt-3 kinase.Type: GrantFiled: November 12, 2004Date of Patent: September 14, 2010Assignee: Novartis AGInventors: Guido Bold, Andreas Floersheimer, Pascal Furet, Vito Guagnano, Keiichi Masuya, Andrea Vaupel, Joseph Schoepfer
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Publication number: 20100227859Abstract: The present teachings relate to compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, R4, X, and Y are as defined herein. The present teachings also provide methods of making the compounds of formula I and methods of inhibiting matrix metalloproteinases, in particular, MMP-12, that may be involved in pathological disorders found in mammals, including a human.Type: ApplicationFiled: May 5, 2008Publication date: September 9, 2010Inventors: Wei LI, Jianchang Li, Yuchuan Wu, Junjun Wu, Rajeev Hotchandani, Steve Yikkai Tam, Tarek Suhayl, Joseph P. Sypek, Iain McFadyen
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100222329Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.Type: ApplicationFiled: November 10, 2009Publication date: September 2, 2010Applicant: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Susumu Watanuki, Yuji Koga, Hiroshi Nagata, Ryutaro Wakayama, Fukushi Hirayama, Ken-ichi Suzuki
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Patent number: 7786126Abstract: A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.Type: GrantFiled: June 13, 2007Date of Patent: August 31, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Andrew C. McCreary, Gustaaf J. M. Van Scharrenburg, Martinus Th. M. Tulp
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Publication number: 20100216787Abstract: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.Type: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Masakazu Sato, Yuko Matsunaga, Hajime Asanuma, Hideaki Amada, Takeshi Koami, Tetsuo Takayama, Tetsuya Yabuuchi, Fumiyasu Shiozawa, Hironori Katakai, Hiroki Umemiya, Akiko Ikeda
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Publication number: 20100216810Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: December 1, 2009Publication date: August 26, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masanori OKANIWA, Terufumi TAKAGI
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Patent number: 7781426Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.Type: GrantFiled: December 29, 2006Date of Patent: August 24, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Cameron J. Smith, Adrian A. Dowst, Yi-Heng Chen
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Publication number: 20100210635Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: March 23, 2007Publication date: August 19, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Benjamin Jones, Andre A. Kiryanov, Stephen W. Kaldor
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Publication number: 20100210647Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: ApplicationFiled: August 18, 2008Publication date: August 19, 2010Applicant: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Publication number: 20100210662Abstract: The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: February 9, 2010Publication date: August 19, 2010Applicant: SANOFI-AVENTISInventors: Marco BARONI, Letizia PULEO
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Publication number: 20100210618Abstract: The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRX—C(?O)—; —Z—C(?O)—; —Z—NRX—C(?O)—; —C(?O)—Z—; —NRX—C(?O)—Z—; —C(?S)—; —NRX—C(?S)—; —Z—C(?S)—; —Z—NRX—C(?S)—; —C(?S)—Z—; —NRX—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRX— or —NRX—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein saiType: ApplicationFiled: June 6, 2008Publication date: August 19, 2010Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Mieerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaret, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
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Patent number: 7776855Abstract: This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.Type: GrantFiled: July 9, 2007Date of Patent: August 17, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Mark J. Macielag, Manomi A. Tennakoon
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Publication number: 20100197703Abstract: This invention provides thiazolylpiperazine derivatives, and N-sulfonyl heterocyclic derivatives including phenyl- and benzyl-thiazolylpiperidine derivatives, and pharmaceutically acceptable salts thereof, which are useful active ingredients for administration in a method for the treatment of an ?-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides methods for making such derivatives, and pharmaceutical compositions including such derivatives together with pharmaceutically acceptable excipients.Type: ApplicationFiled: February 5, 2010Publication date: August 5, 2010Applicant: NV reMYNDInventors: Gerard GRIFFIOEN, Veronica ROJAS DE LA PARRA, Annick LAUWERS
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Patent number: 7767682Abstract: Methods of prevention or treatment of renal diseases or conditions associated with abnormal ion flux, in particular autosomal dominant polycystic kidney disease, with a modulator of human peroxisome proliferator activated receptor gamma.Type: GrantFiled: March 1, 2006Date of Patent: August 3, 2010Assignee: GlaxoSmithKline LLCInventors: Kathleen Keating Brown, Bonnie Blazer-Yost
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Patent number: 7767681Abstract: The disclosure concerns 2-carbamide-4-phenylthiazole derivatives of general formula (I). The disclosure also concerns pharmaceutical compositions containing a compound of general formula (I) and to processes for preparing and methods of using compounds of general formula (I).Type: GrantFiled: January 3, 2007Date of Patent: August 3, 2010Assignee: sanofi-aventisInventors: Pierre Casellas, Daniel Floutard, Pierre Fraisse, Samir Jegham
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Publication number: 20100189687Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: February 22, 2008Publication date: July 29, 2010Applicant: GILEAD SCIENCES, INC.Inventors: Manoj C. Desai, Allen Y. Hong, Hon Chung Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Publication number: 20100184766Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: January 18, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Aaron R. Kunzer, Steven W. Elmore, Laura A. Hexamer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Gary T. Wang, Xilu Wang, Michael D. Wendt