Nitrogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 514/331)
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Publication number: 20090298883Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).Type: ApplicationFiled: April 8, 2009Publication date: December 3, 2009Inventors: Hassan PAJOUHESH, Ramesh KAUL, Yanbing DING, Yongbao ZHU, Lingyun ZHANG, Nagasree CHAKKA, Mike GRIMWOOD, Jason TAN, Yuanxi ZHOU
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Publication number: 20090298745Abstract: The invention provides a method of treatment of diabetes, particularly type II diabetes, or a diabetes related condition, comprising night time dosing of an inhibitor of glycogen phosphorylase, optionally in combination another anti-diabetic therapy.Type: ApplicationFiled: December 2, 2005Publication date: December 3, 2009Inventors: Gerard Hugh Thomas, Mikael Thomsen
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Publication number: 20090286833Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.Type: ApplicationFiled: June 20, 2008Publication date: November 19, 2009Applicant: GRUENENTHAL GmbHInventors: Stefan OBERBOERSCH, Beatrix MERLA, Bernd SUNDERMANN, Werner ENGLBERGER, Hagen-Heinrich HENNIES, Achim KLESS, Petra BLOMS-FUNKE, Babette-Yvonne KOEGEL, Heinze GRAUBAUM
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Publication number: 20090286765Abstract: A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.Type: ApplicationFiled: June 13, 2006Publication date: November 19, 2009Inventors: Wesley Peter Blackaby, Ian Thomas Huscroft, Linda Elizabeth Keown, Richard Thomas Lewis, Piotr Antoni Raubo, Leslie Joseph Street, Christopher George Thomson, Joanne Thomson
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Publication number: 20090270451Abstract: The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.Type: ApplicationFiled: October 27, 2006Publication date: October 29, 2009Applicants: MERCK & CO., INC., MERCK SHARP & DOHME LIMITEDInventors: David Hallett, Craig W. Lindsley, Elizabeth M. Naylor, Zhijian Zhao, Cory R. Theberge, Scott E. Wolkenberg, M. Brad Nolt
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Publication number: 20090253703Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: June 12, 2009Publication date: October 8, 2009Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, Holger Sellner
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Publication number: 20090252790Abstract: The present invention relates to a pharmaceutical fixed dose combination tablet comprising repaglinide and metformin. The present invention also provides a method of producing said tablet.Type: ApplicationFiled: May 10, 2007Publication date: October 8, 2009Applicant: NOVO NORDISK A/SInventors: Koichi Wada, Hikaru Fujita, Manabu Nakatani, Thomas Friedl
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Publication number: 20090253701Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: June 12, 2009Publication date: October 8, 2009Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, holger Sellner
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Publication number: 20090253670Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: ApplicationFiled: March 26, 2009Publication date: October 8, 2009Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
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Publication number: 20090247585Abstract: A subject-matter of the present invention is pharmaceutical compositions comprising, in combination, at least one active ingredient chosen from (S)-(?)-N-[4-(4-acetamido-4-phenylpiperidin-1-yl)-2-(3,4-dichlorophenyl)butyl]-N-methylbenzamide and pharmaceutically acceptable salts thereof and at least one second active ingredient chosen from (S)-(+)-1-[4-(3-(dimethylamino)propyl)]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: June 8, 2009Publication date: October 1, 2009Applicant: SANOFI-AVENTISInventors: Guy GRIEBEL, Caroline COHEN, Caroline LOUIS, Lisa Ann ARVANITIS
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Patent number: 7595331Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: December 8, 2004Date of Patent: September 29, 2009Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Publication number: 20090239841Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.Type: ApplicationFiled: October 24, 2005Publication date: September 24, 2009Inventors: Alan J. Hutchison, Jun Yuan
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Publication number: 20090239904Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: June 5, 2009Publication date: September 24, 2009Applicant: THERAVANCE, INC.Inventors: Mathai Mammen, Trevor Mischki, Adam Hughes, YuHua Ji
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Publication number: 20090233909Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.Type: ApplicationFiled: December 1, 2005Publication date: September 17, 2009Applicant: Virobay, Inc.Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
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Publication number: 20090227632Abstract: A subject-matter of the present invention is pharmaceutical compositions comprising, in combination, at least one active ingredient chosen from (S)-(?)-N-[4-(4-acetamido-4-phenylpiperidin-1-yl)-2-(3,4-dichlorophenyl)butyl]-N-methylbenzamide and pharmaceutically acceptable salts there and at least one second active ingredient chosen from selective serotonin reuptake inhibitors, serotonin/norepinephrine reuptake inhibitors and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: May 20, 2009Publication date: September 10, 2009Applicant: SANOFI-AVENTISInventors: Guy GRIEBEL, Caroline COHEN, Caroline LOUIS, Lisa Ann ARVANITIS
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Patent number: 7585858Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: May 26, 2005Date of Patent: September 8, 2009Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Milan Bruncko, Cheol-Min Park
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Patent number: 7582656Abstract: Compounds of the formula (I): in which the radicals R and R1 to R10 are as defined in the description, processes for the preparation of them, use thereof for the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: GrantFiled: June 28, 2005Date of Patent: September 1, 2009Assignee: Merck Patent GesellschaftInventors: Didier Roche, Bruno Roux, Isabelle Berard
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Publication number: 20090209586Abstract: HPV inhibitors with formula (I) where G1 represents a hydrocarbonated bond or chain possibly substituted by one or two alkyl groups, G2 represents a group (see formula Ia+Ib) or R represents a hydrogen, an alkyl, halogenoalkyl, or a prodrug radical such as carbamate, acetyl or dialkylaminomethyl, G represents a bond or a hydrocarbonated chain possibly substituted by one or two alkyls, W represents an oxygen or sulphur, R1 and R2 each represent a group chosen from among hydrogen, halogen, hydroxyl, thio, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, monoalkylamino, dialkylamino, cycloalkyl, alkyl or halogenoalkyl, R3 represents an acid or a prodrug radical of the acid function or a bioisostere of the acid function, A represents an aryl, cycloalkyl, cycloalkenyl or a heterocycle, each possibly substituted, and B represents an aryl or a heterocycle with 6 chains, each possibly substituted, and pharmaceutically acceptable salts.Type: ApplicationFiled: May 18, 2007Publication date: August 20, 2009Inventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
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Publication number: 20090209587Abstract: Processes for preparing solid pharmaceutical compositions comprising repaglinide or a derivative thereof, including a step of granulation. Embodiments include fluid bed granulation.Type: ApplicationFiled: January 13, 2009Publication date: August 20, 2009Inventors: Parag Prakash Borde, Praveen Kumar Bembaloor Subbappa, Ravinder Kodipyaka
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Publication number: 20090203740Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: March 21, 2005Publication date: August 13, 2009Applicant: Dompe' pha.r.ma S.p.AInventors: Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
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Publication number: 20090197918Abstract: The present invention relates to benzyloxy- and phenethyl-substituted phenyl-amidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.Type: ApplicationFiled: September 12, 2006Publication date: August 6, 2009Applicant: Bayer CropScience AGInventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Moradi, Thomas Seitz, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Mark Drewes, Ralf Dunkel, Ronald Ebbert, Olga Malsam, Eva Maria Franken
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Patent number: 7569588Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: August 4, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Viengkham Malathong
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Publication number: 20090191125Abstract: Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided.Type: ApplicationFiled: April 9, 2008Publication date: July 30, 2009Applicant: The General Hospital CorporationInventors: David R. Elmaleh, Choi Sungwoon, Alan J. Fischman
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Publication number: 20090186921Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.Type: ApplicationFiled: January 16, 2009Publication date: July 23, 2009Applicant: ACADIA PHARMACEUTICALS, INC.Inventors: Carl-Magnus A. Andersson, Glenn Croston, E. L. Hansen, Allan Kjaersgaard Uldam
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Publication number: 20090186884Abstract: Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.Type: ApplicationFiled: April 5, 2007Publication date: July 23, 2009Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty
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Publication number: 20090181943Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.Type: ApplicationFiled: April 9, 2008Publication date: July 16, 2009Applicant: METHYLGENE INC.Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
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Publication number: 20090176835Abstract: The present invention provides a pharmaceutical composition for suppression of the expression of ATP citrate lyase, which contains a compound that suppresses the expression of ATP citrate lyase by the in vivo administration. The compounds suppress the expression of ATP citrate lyase by the in vivo administration include insulin secretagogues such as nateglinide. This pharmaceutical composition is effective in preventing, improving and treating metabolic syndrome, in particular, liver disorders related to abnormal lipid metabolism such as fatty liver and NASH.Type: ApplicationFiled: March 5, 2009Publication date: July 9, 2009Applicant: Ajinomoto Co., Inc.Inventors: Yoshiro KITAHARA, Tomohisa OKUTSU, Akira MITSUI, Akira OKANO
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Publication number: 20090170899Abstract: The present invention relates to a novel combination of a serotonin selective re-uptake inhibitor (SSRI) and an agonist of the serotonin 4 (5-HT4) receptor to augment and/or provide faster onset of the therapeutic effect of the SSRI alone or administered with any other compound which causes an elevation in the level of extracellular serotonin (5-HT). The present invention also relates to a pharmaceutical formulation comprising said combination and to a method and use of said combination in the treatment of depression, anxiety, obsessive compulsive disorder (OCD) or other disease or disorder responsive to a SSRI.Type: ApplicationFiled: September 14, 2005Publication date: July 2, 2009Inventors: Guy Debonnel, Dominique Debonnel, Guillaume Lucas
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Patent number: 7550486Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.Type: GrantFiled: January 11, 2008Date of Patent: June 23, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, George V. Delucca
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Patent number: 7550485Abstract: The present invention is directed to substituted N-heterocycle derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: June 23, 2009Assignee: WyethInventors: Paige Erin Mahaney, Lori Krim Gavrin, Douglas John Jenkins
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Publication number: 20090156623Abstract: N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) 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.Type: ApplicationFiled: January 9, 2009Publication date: June 18, 2009Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Walter Maria Roevens
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Patent number: 7544716Abstract: This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.Type: GrantFiled: November 28, 2003Date of Patent: June 9, 2009Assignee: Xention LimitedInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20090137601Abstract: The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: November 22, 2006Publication date: May 28, 2009Applicant: ASTRAZENECA ABInventors: Simon Thomas Barry, Jason Grant Kettle, David Alan Rudge
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Publication number: 20090123387Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: January 9, 2009Publication date: May 14, 2009Inventor: Harry A. Dugger, III
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Publication number: 20090124664Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: ApplicationFiled: November 24, 2006Publication date: May 14, 2009Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
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Publication number: 20090118268Abstract: This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Publication number: 20090118306Abstract: The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.Type: ApplicationFiled: May 10, 2006Publication date: May 7, 2009Applicant: LABORATOIRE FOURNIER S.A. French Limited CompayInventors: Bernadette Husson, Pierre Broqua, Jean-Louis Junien
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Publication number: 20090105218Abstract: Compounds of formula (I) are useful in the treatment of disease responsive to modulation of CRTH2 receptor activity, wherein: A represents a carboxyl group —COOH, or a carboxyl bioisostere; L1 is a bond, —CH2—, —OCH2—, —CH2CH2— or —CH?CH—; L2 is CONH—, —NHCO—, SO2NR1—, —NR1SO2 wherein R1 is hydrogen or C1-C3 alkyl, or a divalent radical of formula (X) or (Y), wherein ring Q is a non aromatic heterocyclic ring containing 5 to 7 ring atoms, including the nitrogen shown; L3 is a divalent linker radical of formula -(Alk1)m-(Z)n-(Alk2)p as defined in the description; ring Ar1 is an optionally substituted divalent phenyl radical or divalent 5- or 6-membered monocyclic heteroaryl radical, in which L1 and the H[B]sL3L2Ar2CONH-radical are linked to adjacent ring carbon atoms; ring Ar2 is an optionally substituted 1,3-phenylene radical, or an optionally substituted divalent 5- or 6-membered monocyclic heteroaryl radical, in which AL1Ar1NHCO-radical and the H[B]sL3L2-radical are linked to ring carbon atoms which are notType: ApplicationFiled: May 30, 2005Publication date: April 23, 2009Applicant: 7TM PHARMA A/SInventors: Trond Ulven, Thomas Frimurer, Oystein Rist, Evi Kostenis, Thomas Hogberg
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Patent number: 7517892Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.Type: GrantFiled: September 12, 2001Date of Patent: April 14, 2009Assignee: Sepracor Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
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Publication number: 20090076083Abstract: The present application describes deuterium-enriched saredutant, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 15, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090076081Abstract: The invention relates to a compound of formula wherein Ar1, Ar2, R1, R2, R3, R4, R5, and R5? or to a pharmaceutically active salt 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: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian, Xihan Wu
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Publication number: 20090075985Abstract: Aryl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.Type: ApplicationFiled: November 3, 2008Publication date: March 19, 2009Applicant: DECODE GENETICS INC.Inventors: Jasbir Singh, Mark Gurney, Georgeta Hategan
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Publication number: 20090076082Abstract: The present application describes deuterium-enriched alvimopan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7504512Abstract: N-Benzoyl arylsulfonamides having the formula are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.Type: GrantFiled: April 7, 2004Date of Patent: March 17, 2009Assignee: Abbott LaboratoriesInventors: David J. Augeri, Steven A. Baumeister, Milan Bruncko, Daniel A. Dickman, Hong Ding, Jurgen Dinges, Stephen W. Fesik, Philip J. Hajduk, Aaron R. Kunzer, William McClellan, David G. Nettesheim, Thorsten Oost, Andrew M. Petros, Saul H. Rosenberg, Wang Shen, Sheela A. Thomas, Xilu Wang, Michael D. Wendt
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Publication number: 20090061031Abstract: The present invention relates to methods and pharmaceutical compositions for treating obesity or obesity-related disorders in a subject suffering from or predisposed to developing obesity or an obesity-related disorder, or for inhibiting the infectivity of HIV, by administering oleuropein, an analogue or derivative thereof, or the major metabolites of oleuropein including oleuropein aglycone, hydroxytyrosol, and elenolic acid or their analogues, or derivatives thereof, an iridoid glycoside, or a secoiridoid glycoside or analogues or derivatives thereof, or any combination of the foregoing including olive leave extract. The invention also relates to methods for screening/diagnosing a subject having, or predisposed to having obesity or a related disorder by measuring the expression profiles of an adipogenic gene selected from PPAR?2, LPL and ?P2 gene and gene product, or other adipogenic, lipogenic, or lipolytic genes and gene products in an individual.Type: ApplicationFiled: July 9, 2007Publication date: March 5, 2009Inventors: Sylvia Lee-Huang, Paul L. Huang, Philip Lin Huang, Dawei Zhang, John Z.H. Zhang, Young Tae Chang, Jae Wook Lee, Ju Bao, Yongtao Sun
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Publication number: 20090062296Abstract: Nitroderivatives of prostaglandin amides having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.Type: ApplicationFiled: June 28, 2006Publication date: March 5, 2009Inventors: Francesca Benedini, Valerio Chiroli, Wesley Kwan Mung Chong, Achim Hans-Peter Krauss, Michael Ross Niesman, Ennio Ongini
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Patent number: 7495105Abstract: The present invention describes a method of separation of the enantiomers of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide. Another object of the present invention refers to the enantiomeric manipulation of the enantiomers of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide, in order to achiever compounds and pharmaceutical compositions presenting diverse enantiomeric excesses of (S)-N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide, in order to quantify and determine the participation of (R)-N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide in the anesthetic and cardiotoxic effects. These compounds and compositions enantiomerically manipulated demonstrate to present a significant improvement in itsanesthetic properties, presenting a cardiotoxic profile equivalent to pure enantiomer, a (S)-N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide.Type: GrantFiled: October 8, 2002Date of Patent: February 24, 2009Assignee: Cristalia Produtos Quimicos Farmaceuticos Ltda.Inventors: Valter Freiro Torres Russo, Elisa Mannochio de Souza Russo, Ogari de Castro Pacheco
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Publication number: 20090048291Abstract: The present invention is directed to compounds of formula I compositions comprising them and their use.Type: ApplicationFiled: August 4, 2008Publication date: February 19, 2009Applicant: Euroscreen S.A.Inventors: Jacques Huck, Frederic Ooms, Julien Parcq, Regereau Yannick, Hamid R. Hoveyda, Guillaume Dutheuil
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Patent number: 7488738Abstract: There is provided an aminophenoxyacetic acid derivative of the following formula (I): wherein, R1, R2, R3 and R4 are, independent from each other, alkoxy group, alkyl group or aryl group, etc.; E1 and E2 are oxygen atom, sulfur atom, etc.; n is 0 to 5; X and Y are alkylene group, cycloalkylen group, or alkenylen group; Q is phenyl group which may be substituted or benzoyl group, etc, or a pharmaceutically acceptable salt thereof. These compounds have neuroprotective effects by inducing calbindin D28Kd, one of Ca2+-binding proteins.Type: GrantFiled: July 6, 2005Date of Patent: February 10, 2009Assignee: Asubio Pharma Co., Ltd.Inventors: Hirokazu Annoura, Naohiro Takemoto, Hiroshi Uramoto
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder