Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Quinoline Ring System Patents (Class 546/168)
-
Publication number: 20110224242Abstract: The present disclosure concerns new substituted styrylquinolines, the process of their preparation and their therapeutic uses as integrase inhibitors and/or for the treatment and/or prevention of HIV.Type: ApplicationFiled: July 23, 2009Publication date: September 15, 2011Applicant: BIOALLIANCE PHARMAInventors: Bruno Giethlen, Mathieu Michaut, Claude Monneret, Emilienne Soma, Laurent Thibault, Camille Georges Wermuth
-
Publication number: 20110212941Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.Type: ApplicationFiled: November 3, 2009Publication date: September 1, 2011Inventors: Peter J. Manley, Kausik K. Nanda, B. Wesley Trotter
-
Publication number: 20110118262Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.Type: ApplicationFiled: June 24, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
-
Publication number: 20110015399Abstract: Disclosed is a vinamidinium salt represented by the formula (I): [wherein R1 represents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group or the like; R2 and R3 are the same or different and each represents a lower alkyl group, or alternatively R2 and R3 may combine together to form a ring; R4 and R5 are the same or different and each represents a lower alkyl group, or alternatively R4 and R5 may combine together to form a ring; X and Y are the same or different and each represents a bromine atom or a chlorine atom; n represents a number of not less than 2; and m represents 0 or n], which can be used as a general purpose reagent useful for synthesis of various nitrogen-containing heteroaromatic rings having a substituent. The vinamidinium salt has excellent storage stability and reaction selectivity. A method for synthesizing a nitrogen-containing heteroaromatic ring compound using the vinamidinium salt is also disclosed.Type: ApplicationFiled: March 27, 2009Publication date: January 20, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LTD.Inventors: Mitsuhisa Yamano, Yasuhiro Sawai, Masahiro Mizuno
-
Publication number: 20100298209Abstract: The invention which is the subject of the present application relates to a compound of structure I: A-B-C for use in the prophylaxis and/or treatment of a viral infection, and in particular for preventing and/or inhibiting viral replication, in which A is a quinoline or a quinoline-type group, B is a single amino acid or a peptide or polypeptide having a given amino acid sequence, C is an O-phenoxy group and the symbol “-” indicates that the entities A, B and C are chemically bonded within the compound I. According to a particular embodiment, said compound is a protease inhibitor, in particular a caspase inhibitor, and more particularly the inhibitor Q-VD-OPh (N-(2(quinolyl)valyl-aspartyl-(2,6-difluorophenoxy)methyl ketone), optionally in an O-methylated form.Type: ApplicationFiled: October 31, 2008Publication date: November 25, 2010Inventors: Jérôme Estaquier, Mireille Laforge, Anna Senik
-
Publication number: 20100261687Abstract: Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 19, 2010Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Marc GRUNDL, Horst DOLLINGER, Riccardo GIOVANNINI, Christoph HOENKE, Matthias HOFFMANN, Jan KRIEGL, Domnic MARTYRES, Georg RAST, Peter SEITHER
-
Publication number: 20100248313Abstract: The present invention relates to new optically active heteroaromatic ?-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.Type: ApplicationFiled: December 18, 2008Publication date: September 30, 2010Inventors: Johannes Platzek, Ludwig Zorn, Bernd Buchmann, Werner Skuballa, Orlin Petrov
-
Patent number: 7795437Abstract: The present invention relates to ether derivatives according to general formula I, and to their pharmaceutically-acceptable salts, which may be used in treating or preventing cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, or psychoses comprising paranoia and delusions.Type: GrantFiled: October 22, 2007Date of Patent: September 14, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Luca Claudio Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
-
Patent number: 7786137Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:Type: GrantFiled: May 8, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Aarti S. Kawatkar, Tara M. Whitney, Timothy D. Neubert, Nicole Zimmermann, Andreas Termin, Esther Martinborough
-
Publication number: 20100152192Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: December 11, 2009Publication date: June 17, 2010Applicant: Glenmark Pharmaceuticals S.AInventors: Sachin Sundarlal Chaudhari, Abraham Thomas, Ashok Bhausaheb Kadam, Sachin Vasantrao Dhone, Suresh Mahdadev Kadam, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
-
Publication number: 20100152184Abstract: The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C?O, (C?O)O, (C?O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C?O or (C?O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims.Type: ApplicationFiled: October 12, 2007Publication date: June 17, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Miles Stuart Congreve, Lynsey Helen Fazal, Martyn Frederickson, Christopher William Murray, Michael Alistair O'Brien, Andrew James Woodhead, John Francis Lyons, Neil Thomas Thompson
-
Publication number: 20100125091Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: November 12, 2009Publication date: May 20, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
-
Publication number: 20100120847Abstract: The present invention concerns new substituted styrylquinolines, their process of preparation and their therapeutic uses as integrase inhibitors and/or for the treatment and/or prevention of HIV.Type: ApplicationFiled: November 12, 2008Publication date: May 13, 2010Inventor: Laurent THIBAUT
-
Patent number: 7705153Abstract: The use of CCR3 antagonists of the formula I or a pharmaceutically acceptable salt thereof for the treatment of asthma is disclosed, as well as novel compounds of the formula II, pharmaceutical compositions comprising them, and their use in the treatment of asthma, wherein R, Ra, X, Xa, R1, R2, R2a, R14, R14a, R16 and n are as defined in the specification.Type: GrantFiled: February 2, 2005Date of Patent: April 27, 2010Assignee: Schering CorporationInventors: Pauline C. Ting, Jianhua Cao, Youhao Dong, Eric J. Gilbert, Ying Huang, Joseph M. Kelly, Stuart McCombie, Neng-Yang Shih
-
Publication number: 20100093707Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji NAKAMURA, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
-
Patent number: 7674909Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are H, Me; R3 is (2-6C)heterocycloalkyl(1-4C)alkyl, (2-5C)heteroaryl(1-4C)alkyl, (6C)aryl (1-4C)alkyl, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyl, (2-6C) heterocycloalkylcarbonylamino(2-4C)alkyl, R5-(2-4C)alkyl or R5-carbonyl(1-4C)alkyl; R4 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2-6C)heterocycloalkyl or (1-6C) alkyl and R5 is (di)(1-4C)alkylamino, (1-4C)alkoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alkenylamino, (2-5C)heteroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1-4C)alkoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino or (di)[hydroxy(2-4C)alkyl]amino. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.Type: GrantFiled: December 16, 2003Date of Patent: March 9, 2010Assignee: N.V. OrganonInventors: Cornelis Marius Timmers, Willem Frederik Karstens
-
Publication number: 20090324581Abstract: To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered. The invention provides a compound represented by general formula (I) (wherein A is a single bond, —O—, or —CH2—; R1 represents a hydrogen atom or a C1-C6 alkyl group, and V represents any one group selected from among the following groups (1) to (3): (1) -G1-, (2) -G2-N(R2)-G3-, and (3) a group represented by formula 2, wherein each of Z1 and Z2 represents a hydrogen atom or a C1-C6 alkyl group, Z3 represents a hydrogen or the like, Q represents —CH2—O— or the like, and Y represents a group represented by formula 3, a salt thereof, or a solvate thereof.Type: ApplicationFiled: May 9, 2007Publication date: December 31, 2009Applicant: Daiichi Sankyo company LimitedInventors: Nobuo Machinaga, Toshiharu Yoshino, Jun Chiba, Jun Watanabe, Takashi Suzuki, Youichi Kimura
-
Patent number: 7619091Abstract: The present invention relates to a method for the treatment, amelioration and/or prophylaxis of a neurological condition, in particular neurodegenerative disorders which comprises the administration of an effective amount of a compound of formula (I): to a subject in need thereof. The present invention also relates to a compound of formula (II) and processes for its preparation.Type: GrantFiled: July 16, 2003Date of Patent: November 17, 2009Assignee: Prana Biotechnology LimitedInventors: Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Gaik Beng Kok, Guy Krippner
-
Publication number: 20090264414Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: June 29, 2009Publication date: October 22, 2009Applicant: High Point Pharmaceuticals, LLCInventors: Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Inge Thoger Christensen, John Patrick Mogensen, Annette Rosendal Larsen, John Paul Kilburn
-
Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
-
Patent number: 7589114Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-sulfonyl]-azetidine-carboxylic acids, esters and amides which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: April 4, 2006Date of Patent: September 15, 2009Assignee: Boehringer Ingelheim International GmbHInventor: Steven Richard Brunette
-
Patent number: 7572916Abstract: A diastereoselective synthesis process for the preparation of (R)-(+)-6-[amino(4chlorophenyl)(1-methyl-1H-imidazol-5-yl) methyl]-4-(3-chlorophenyl)-1-methyl2(1H)-quinolinone which comprises the preparation of a compound of formula (XVII): and the stereochemically isomeric forms thereof wherein R is C1-6alkyl or C1-6alkylphenyl.Type: GrantFiled: April 28, 2005Date of Patent: August 11, 2009Assignee: Janssen Pharmaceutica NVInventors: Walter Ferdinand Maria Filliers, Rudy Laurent Maria Broeckx, Patrick René Angibaud
-
Publication number: 20090197914Abstract: The present invention provides a compound of a formula (I) wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.Type: ApplicationFiled: March 6, 2007Publication date: August 6, 2009Inventors: Peter Cage, Mark Furber, Matthew Perry, Brian Springthorpe
-
Publication number: 20090176775Abstract: The present invention is related to a compound of formula (I): wherein i, j, n, o, p, q, r, R1a, R1b, R1c, R1d, R2a, R2b, R2c, R2d, R3a, R3b and R4 are as defined herein, or an addition salt with an acid thereof, or a hydrate or solvate thereof, its preparation, pharmaceutical composition, and uses for treating a disease in which the enzyme 11?-HSD1 is involved.Type: ApplicationFiled: December 18, 2008Publication date: July 9, 2009Applicant: SANOFI-AVENTISInventors: Alain BRAUN, Patrick MOUGENOT, Claudie NAMANE, Eric NICOLAI, Francois PACQUET, Christophe PHILIPPO, Olivier VENIER, Olivier CRESPIN, Cecile PASCAL, Michel ALETRU, Stefan GUSSREGEN
-
Publication number: 20090170832Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted alkyl or the like, one of R2 and R4 is a group of formula: —Y—R5, wherein Y is —O— or the like, R5 is substituted alkyl (the substituent is optionally substituted cycloalkyl or the like), optionally substituted branched alkyl or the like, the other of R2 and R4 is hydrogen or optionally substituted alkyl, R3 is a group of formula: —C(?O)-Z-R6, wherein Z is —NR7— or —NR7—W—, R6 is optionally substituted cycloalkyl or the like, R7 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, X is ?N— or the like, with the proviso that compounds wherein R2 is 2-(morphorino)ethoxy, R3 is N-(1-adamantyl)carbamoyl and R1 is benzyl are excluded.Type: ApplicationFiled: November 20, 2006Publication date: July 2, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Noriyuki Kurose, Mikayo Hayashi, Tomoyuki Ogawa, Koji Masuda, Eiichi Kojima
-
Patent number: 7541466Abstract: Tetrahydroisoquinoline derivatives, pharmaceutical compositions comprising them and methods of treating disease are disclosed herein. The disclosed compounds are useful in the treatment and prevention of diseases mediated by chloride channel activity and/or protein trafficking, including, but not limited to, diseases associated with impaired mucociliary clearance such as cystic fibrosis, bronchitis, emphysema, and the like.Type: GrantFiled: December 7, 2004Date of Patent: June 2, 2009Assignee: Genzyme CorporationInventors: Marko J. Pregel, Bradford H. Hirth, John L. Kane, Jr., Shuang Qiao, Jill Gregory, Lisa Cuff
-
Patent number: 7524961Abstract: A diastereoselective synthesis process for the preparation of (R)-(+)-6-[amino(4-chlorophenyl) (1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2 (1H)-quinolinone which comprises the preparation of a compound of formula (VIII) and the stereochemically isomeric forms thereof wherein R is C1-6alkyl or C1-6alkylphenyl-.Type: GrantFiled: April 28, 2005Date of Patent: April 28, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Walter Ferdinand Maria Filliers, Rudy Laurent Maria Broeckx, Patrick René Angibaud
-
Publication number: 20090088441Abstract: The present invention relates to novel compounds of the general formula (I) wherein R1, R4, R5 and X are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).Type: ApplicationFiled: September 26, 2008Publication date: April 2, 2009Inventors: Leifeng Cheng, Michael Karle
-
Patent number: 7511063Abstract: Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.Type: GrantFiled: August 16, 2006Date of Patent: March 31, 2009Assignee: Schering CorporationInventors: Yongqi Deng, Patrick J. Curran, Gerald W. Shipps, Jr., Lianyun Zhao, M. Arshad Siddiqui, Janeta Popovici-Muller, Jose S. Duca, Alan W. Hruza, Thierry O. Fischmann, Vincent S. Madison, Rumin Zhang, Charles W. McNemar, Todd W. Mayhood, William T. Windsor, Emma M. Lees, David A. Parry
-
Publication number: 20090036442Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: October 29, 2007Publication date: February 5, 2009Inventors: Clive Leslie BRANCH, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
-
Publication number: 20090029986Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: October 29, 2007Publication date: January 29, 2009Inventors: Clive Leslie BRANCH, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
-
Patent number: 7482457Abstract: The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR?R? or C1-6 alkyl-NR?R? where R? and R? are independently chosen from hydrogen and C1-4 alkyl and where R? and R?, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR?R? as defined above or R2 is C1-6 alkoxy substituted by NR?R? as defined above; R3 is hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl or aryl C1-6 alkyl; R5 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl, aryl C1-6 alkyl or C1-6 alkoxycarbonyl; or R4 and R5, together with the nitrogen atom to which they are attached, form a C3-C10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF3, halogen and C1-4 alkyl; oType: GrantFiled: February 3, 2004Date of Patent: January 27, 2009Assignee: Merck Sharp & DohmeInventors: Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod
-
Publication number: 20090023772Abstract: This invention relates to novel substituted heteroaryloxy alkylamines useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: August 24, 2005Publication date: January 22, 2009Inventors: Birgitte L. Eriksen, Dan Peters, Elsebet Ostergaard Nielsen, Jorgen Scheel-Kruger, Gunnar M. Olsen
-
Publication number: 20090012083Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: October 29, 2007Publication date: January 8, 2009Inventors: Clive Leslie BRANCH, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth, Anne Stead, Geoffrey Stemp
-
Publication number: 20090012087Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.Type: ApplicationFiled: July 2, 2008Publication date: January 8, 2009Applicant: ASTRAZENECA ABInventors: Jonas Branalt, Ingemar Nilsson, Magnus Polla
-
Derivatives of [6,7-dihydro-5-imidazo[1,2-]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide
Patent number: 7462637Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: October 20, 2004Date of Patent: December 9, 2008Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence A. Kelly, Jin Mi Kim, René Marc Lemieux, Matt Aaron Tschantz -
Publication number: 20080300251Abstract: The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.Type: ApplicationFiled: September 1, 2006Publication date: December 4, 2008Inventors: Jitendra A. Sattigeri, Murugaiah M.S. Andappan, Kaushal Kishore, Sachin Sethi, Sachin Ramesh Kandalkar, Chanchal Kumar Pal, Dipak C. Mahajan, Shahadat Ahmed, Santhosh Sadashiv Parkale, T. Srinivasan, Lalima Sharma, Vinay S. Bansal, Anita Chugh, Joseph Alexanand Davis
-
Publication number: 20080269282Abstract: This invention is directed to inhibitors of copper-containing amine oxidases (E.C.1.4.3.6) including semicarbazide-sensitive amine oxidase (SSAO; also known as vascular adhesion protein-1, VAP-I), and their therapeutic use in inflammatory diseases, diabetes and its associated complications, atherosclerosis, neurodegenerative diseases, obesity, hypertension and cancer.Type: ApplicationFiled: August 2, 2005Publication date: October 30, 2008Applicant: GENMEDICA THERAPEUTICS SLInventors: Luc Marti Clauzel, Silvia Garcia Vicente, Francesc Yraola Font, Miriam Royo Exposito, Fernando Albericio Palomera, Antonio Zorzano Olarte
-
Publication number: 20080262230Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.Type: ApplicationFiled: March 29, 2006Publication date: October 23, 2008Applicant: Nippon Zoki Pharmaceutical Co., LTD.Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
-
Publication number: 20080255109Abstract: Compounds according to general formula 1, wherein A1-A3 are selected from A5 and A6 where A5 is either ?CR13— or ?N— and A6 is —NR14—, —O— or —S—; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1-A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1-A3 must be A5; R1 is selected from H, NHY? and COY2, in which case R2 is H, or R1 and R2 may both be methyl or together represent ?O; R3, R4 and R5 are each independently selected from H and lower alkyl groups; R6, R7, R8, R9, R10, R11 and R12 are each independently selected from H, lower alkyl groups, NH2, halogens (F, Cl and Br) O-alkyl, CH2NM2 and CF3; R13 is selected from H, F, Cl, Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF3; R14 is selected from H, methyl and ethyl; W is selected from ?CH— and ?N—; X is selected from CH2, O, S, SO2, NH and N-lower alkyl; Y1 is selected from CO-lower alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH2)bNHCOY3, where b is 1-3; Y2 is selected from OR15, NR16R17 and NH(CH2)cCOY3,Type: ApplicationFiled: April 28, 2008Publication date: October 16, 2008Inventors: Michael Bryan Roe, Andrzej Roman Batt, David Michael Evans, Gary Robert William Pitt, David Philip Rooker
-
Publication number: 20080200501Abstract: The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).Type: ApplicationFiled: November 2, 2007Publication date: August 21, 2008Applicant: Glenmark Pharmaceuticals S.A.Inventors: Meyyappan Muthuppalaniappan, Kumar Sukeerthi, Gopalan Balasubramanian, Srinivas Gullapalli, Neelima Khairatkar Joshi, Shridhar Narayanan, Pallavi V. Kamik
-
Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
-
Publication number: 20080146607Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: December 18, 2007Publication date: June 19, 2008Inventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
-
Patent number: 7342027Abstract: Provided are 1-phenylpiperidin-3-one derivatives and pharmaceutically acceptable salts thereof, having cysteine protease inhibitory activity, pharmaceutical compositions containing the same as an active ingredient, and processes for the preparation thereof.Type: GrantFiled: July 26, 2003Date of Patent: March 11, 2008Assignees: Yuhan Corporation, Dong-A Pharmaceutical Co., LtdInventors: Jong Wook Lee, Bong Yong Lee, Chun Ho Lee, Yun Hur, Tae Dong Han, Hyun Kyoung Ko, Suk Won Yun, Jae Young Shim, Joong In Lim, Moon Ho Son, Jae Sung Yang, Mi Kyung Kim
-
Patent number: 7294716Abstract: Synthetic methods for preparing isomerically pure N-arylsulfonyl derivatives of proton pump inhibitors which include a substituted benzimidazole nucleus are shown by the synthetic schemes and experimental description.Type: GrantFiled: July 13, 2004Date of Patent: November 13, 2007Assignee: Allergan, Inc.Inventors: Michael E. Garst, Lloyd Jay Dolby, Shervin Esfandiari, Vivian Rose MacKenzie, Alfred Arthur Avey, Jr., David Charles Muchmore, Geoffrey Kenneth Cooper, Thomas C. Malone
-
Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
-
Patent number: 7253168Abstract: Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: April 6, 2005Date of Patent: August 7, 2007Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Bertrand L. Chenard, James G. Tarrant, Guiying Li, Manuka Ghosh, George P. Luke, John M. Peterson, Wallace C. Pringle, Mary-Margaret E. O'Donnell, Kyungae Lee, Linda M. Gustavson, Dario Doller
-
Patent number: 7226929Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: GrantFiled: March 17, 2006Date of Patent: June 5, 2007Assignee: SmithKline Beecham CorporationInventors: Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
-
Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
-
Patent number: 7199265Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor ?, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.Type: GrantFiled: June 15, 2001Date of Patent: April 3, 2007Assignee: Karo Bio ABInventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg