Polycyclo Ring System Having The Four-membered Hetero Ring As One Of The Cyclos Patents (Class 514/210.16)
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Publication number: 20100221211Abstract: The invention relates to a compound of general formula (I-0): wherein R1 means a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, or a C3-C6 cycloalkyl group; R2, R3, R4 and R5 mean a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo-C1-C6 alkoxy group; R6 means a hydrogen atom, or a C1-C6 alkyl group; R7a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxy-C1-C6 alkyl group, -Q2-N(R1c)R1d or a nitrogen-containing heterocyclic group; R8a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group or a hydroxy-C1-C6 alkyl group; or R7a and R8a form, as taken together, a C2-C6 alkylene group, or R7a and R8a and the ring atoms to which they bond may form a spiro ring or a bicyclo ring; and X and Y mean a methine group or a nitrogen atom.Type: ApplicationFiled: October 20, 2008Publication date: September 2, 2010Inventors: Hidetomo Furuyama, Mikako Kawamura, Toshihiro Sakamoto, Fuyuki Yamamoto, Takashi Yoshizumi
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Patent number: 7776885Abstract: This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.Type: GrantFiled: September 2, 2004Date of Patent: August 17, 2010Assignee: Pfizer, Inc.Inventors: Yasuhiro Katsu, Satoru Iguchi, Hiroki Sone, Chikara Uchida, Takashi Kojima
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Publication number: 20100204197Abstract: The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are polo-like kinase (PLKs) inhibitors useful for the treatment of disease states mediated by PLK, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumour growth, rheumatoid arthritis, restenosis and atherosclerosis.Type: ApplicationFiled: July 25, 2008Publication date: August 12, 2010Inventors: Gaston Stanislas Marcella Diels, Peter Ten Holte, Eddy Jean Edgard Freyne, Thierry Andre Regis Grand-Perret, Kristof Van Emelen, Werner Constant Johan Embrechts, Pascal Ghislain André Bonnet
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Publication number: 20100190688Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.Type: ApplicationFiled: July 12, 2005Publication date: July 29, 2010Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
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Publication number: 20100190763Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: January 21, 2010Publication date: July 29, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 7754708Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain.Type: GrantFiled: May 9, 2008Date of Patent: July 13, 2010Assignee: Targacept, Inc.Inventors: Balwinder Bhatti, Scott R. Breining, Philip S. Hammond, Jozef Klucik, Yun-De Xiao
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PRO-DRUGS OF NSAIAS WITH VERY HIGH SKIN AND MEMBRANES PENETRATION RATES AND THEIR NEW MEDICINAL USES
Publication number: 20100172960Abstract: The novel positively charged pro-drugs of NSAIAs in the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” were designed and synthesized. The compounds of the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” indicated above can be prepared from metal salts, organic base salts, or immobilized base salts of NSAIAs with suitable halide compounds. The positively charged amino groups in the pro-drugs in this invention largely increase the solubility of the drugs in water and will bond to the negative charge on the phosphate head group of membrane. Thus, the local concentration of the outside of the membrane or skin will be very high and will facilitate the passage of these pro-drugs from a region of high concentration to a region of low concentration. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the pro-drug.Type: ApplicationFiled: June 4, 2007Publication date: July 8, 2010Inventors: Chongxi Yu, Lina Xu -
Publication number: 20100152157Abstract: The invention relates to the 6-cycloamino-3-(pyridazin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.Type: ApplicationFiled: January 11, 2010Publication date: June 17, 2010Applicant: SANOFI-AVENTISInventors: Frederic PUECH, Yulin CHIANG, Sylvain COTE DES COMBES, Adrien Tak LI, Philippe BURNIER
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Publication number: 20100144700Abstract: A compound of Formula 1: A-C(O)-Cy, wherein A is a diazabicyclic core, containing 7, 8, or 9 ring atoms, and selected from the following: 2,6-diazabicyclo[3.2.0]heptane; 3,6-diazabicyclo[3.ZO]heptane; 2,7-diazabicyclo[4.2.0]octane; 3,7-diazabicyclo[4.2.0]octane; 3,8-diazabicyclo[4.2.0]octane; 2,7-diazabicyclo[3.3.0]octane; 2,7-diazbicyclo[4.3.0]nonane; 2,8-diazbicyclo[4.3.0]nonane; 3,7-diazabicyclo[4.3.0]nonane; 3,8-diazabicyclo[4.3.0]nonane; 3,9-diazabicyclo[4.3.0]nonane; 2,6-diazabicyclo[3.2.1]octane; 3,6-diazabicyclo[3.2.1]octane; wherein the diazabicycle is attached as a radical to the depicted carbonyl via either one of the two ring nitrogen atoms, such that the carbonyl forms an amide bond with the ring nitrogen; Cy is a heteroaryl group; The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?402 subtype in the central nervous system (CNS).Type: ApplicationFiled: March 12, 2008Publication date: June 10, 2010Applicant: TARGACEPT, INC.Inventors: Philip S. Hammond, Anatoly A. Mazurov, Lan Miao, Yun-De Xiao, Balwinder Singh Bhatti, Jon-Paul Strachan, V. Srinivasa Murthy, David C. Kombo, Srinivisa Rao Akireddy
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Publication number: 20100093691Abstract: There is provided topical pharmaceutical compositions comprising compounds of formula I wherein R1, R2, R3 and X have meanings given in the description. These compositions can be used to treat microbial infections and to kill clinically latent microorganisms.Type: ApplicationFiled: November 8, 2007Publication date: April 15, 2010Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Petra Helga BECK, Marc Barry Brown, Anthony Coates, Yanmin Hu, Gerlinda Stoddart
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Patent number: 7696191Abstract: A novel crystalline form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1-methylethyl)oxy]-N-1H-pyrazol-3-ylbenzamide is described in the specification. This compound is a glucokinase (GLK or GK) activator and useful as a pharmaceutical agent in the treatment or prevention of a disease or medical condition mediated through GLK, leading to a decreased glucose threshold for insulin secretion. Processes for the manufacture of the crystalline form, pharmaceutical compositions comprising the crystalline form and the use of the crystalline form in medical treatment are also described.Type: GrantFiled: December 21, 2007Date of Patent: April 13, 2010Assignee: AstraZeneca ABInventors: James McCabe, Gary Peter Tomkinson
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Publication number: 20100048531Abstract: The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their corresponding enantiomers and/or optical isomers thereof. Compounds of the invention are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.Type: ApplicationFiled: August 14, 2009Publication date: February 25, 2010Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
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Publication number: 20100016277Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: August 19, 2009Publication date: January 21, 2010Applicant: 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
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Publication number: 20100009958Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, X, Y, and Z are defined herein. It also discloses a method of treating cancer with one of these compounds.Type: ApplicationFiled: June 30, 2008Publication date: January 14, 2010Applicant: Hutchison MediPharma Enterprises LimitedInventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
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Publication number: 20100009959Abstract: The present invention relates to pentacyclic indole derivatives of formula (I): wherein A, Ar, R1, R2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: ApplicationFiled: May 4, 2007Publication date: January 14, 2010Applicant: Instituto di Ricerche di Biologia Molecolare P. Angeletti SPAInventors: Elena Capito, Joerg Habermann, Frank Narjes, Maria del Rosario Rico Ferreira, Ian Stansfield
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Publication number: 20090318406Abstract: The present invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, A, B and Y are as defined in claim 1, medicinal products containing them and use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.Type: ApplicationFiled: August 24, 2007Publication date: December 24, 2009Applicant: ABBOTT GMBH & CO. KGInventors: Herve Geneste, Thorsten Oost, Astrid Netz, Charles W. Hutchins, Wolfgang Wernet, Wolfgang Lubisch, Liliane Unger, Wilfried Hornberger
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Bioactive polymeric liquid formulations of absorbable, segmented aliphatic polyurethane compositions
Publication number: 20090291925Abstract: Bioactive liquid formulations are formed of combinations of absorbable, segmented aliphatic polyurethane compositions and liquid polyether for use as vehicles for the controlled release of at least one active agent for the conventional and unconventional treatment of different forms of cancer and the management of at least one type of bacterial, fungal, and viral infection.Type: ApplicationFiled: May 22, 2009Publication date: November 26, 2009Inventor: Shalaby W. Shalaby -
Publication number: 20090281073Abstract: This invention relates to compounds of Formula (I), and to pharmaceutically acceptable salts and solvates thereof, wherein Z, W, X, Y, V, R1, R2, and R3 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula (I) and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula (I). The invention also relates to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: December 15, 2005Publication date: November 12, 2009Inventors: Samit Kumar Bhattacharya, Donna G. Wishka, Gonghua Pan
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Publication number: 20090264403Abstract: The invention relates to azacyclyl-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the azacyclyl-substituted aryidihydroisoquinolinones of the invention and their derivatives as MCH antagonists.Type: ApplicationFiled: August 14, 2008Publication date: October 22, 2009Applicant: SANOFI-AVENTISInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Torsten HAACK, Petra LENNIG
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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
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Publication number: 20090203664Abstract: The present invention discloses (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane, salts thereof, and its use to treat pain and other disorders associated with the nicotinic acetylcholine receptor.Type: ApplicationFiled: April 20, 2009Publication date: August 13, 2009Applicant: ABBOTT LABORATORIESInventors: Michael J. Buckley, Jianguo Ji, Geoff G.Z. Zhang, Rodger F. Henry, Weili W. Wang, Gregory S. Wayne, Wenke Li, Timothy B. Towne, Steven J. Wittenberger, Steven M. Hannick, Brian J. Kotecki, Bryan S. Macri, Timothy A. Robbins
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Publication number: 20090197860Abstract: The invention relates biaryl substituted diazabicycloalkanes, and more particularly bicycloheteroaryl substituted fused diazabicycloalkane derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: November 20, 2008Publication date: August 6, 2009Applicant: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li, Kevin B. Sippy, Chih-Hung Lee, Murali Gopalakrishnan
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Publication number: 20090169567Abstract: A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac /vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.Type: ApplicationFiled: November 17, 2006Publication date: July 2, 2009Applicant: ONO PHARMACEUTICAL CO., LTD.,Inventors: Masaya Kokubo, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20090156575Abstract: The invention provides compounds of general formula wherein A, B, p, w, x, y, and z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: September 4, 2006Publication date: June 18, 2009Inventors: Lena Borjesson, Henrik Johansson, Anna Kristoffersson, Igor Shamovsky, Marco Skrinjar, Stephen Connolly, Tero Linnanen
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Patent number: 7547705Abstract: The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: GrantFiled: October 3, 2007Date of Patent: June 16, 2009Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Nathalie Chereze, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Publication number: 20090124595Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: November 7, 2008Publication date: May 14, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: MarK Adams, Qing Dong, Toufike Kanouni, Stephen W. Kaldor, Nicholas Scorah, Michael B. Wallace
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Publication number: 20090098218Abstract: The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.Type: ApplicationFiled: July 16, 2008Publication date: April 16, 2009Inventors: Achim Schlapbach, Laszlo Revesz, Guido Koch
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Publication number: 20090036422Abstract: The present invention relates to compounds of formula wherein Ar, R1, R2, R3, R4, R5, n, o, and p are as defined herein or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds of formula I can be used for the treatment of sleep disorders, such as sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.Type: ApplicationFiled: July 24, 2008Publication date: February 5, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20080299164Abstract: A coating formed of a substituted polycaprolactone and method of making and using the same are disclosed.Type: ApplicationFiled: May 30, 2007Publication date: December 4, 2008Inventor: Mikael O. Trollsas
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Publication number: 20080247964Abstract: Substituted azaspiro derivatives 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: May 7, 2007Publication date: October 9, 2008Inventors: Yuelian Xu, Timothy M. Caldwell, Linghong Xie, Bertrand L. Chenard
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Publication number: 20080188452Abstract: Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.Type: ApplicationFiled: September 28, 2007Publication date: August 7, 2008Inventors: Robert J. Altenbach, Huaqing Liu, Irene Drizin, Marlon D. Cowart, Neil Wishart, David J. Babinski, Robert J. Gregg, Arthur A. Hancock, Kathryn J. Hancock, Timothy A. Esbenshade, Gin C. Hsieh, Jorge D. Brioni, Marie P. Honore, Lawrence A. Black, Chen Zhao, Brian D. Wakefield
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Publication number: 20080167286Abstract: The invention relates to a composition comprising a neuronal nicotinic receptor ligand and an ?4?2 positive allosteric modulator, a method of using the same, and a related article of manufacture.Type: ApplicationFiled: December 10, 2007Publication date: July 10, 2008Applicant: Abbott LaboratoriesInventors: Murali Gopalakrishnan, Marie P. Honore, Chih-Hung Lee, John Malysz, Jianguo Ji, Tao Li, Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson
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Patent number: 7384929Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain.Type: GrantFiled: September 19, 2005Date of Patent: June 10, 2008Assignee: Targacept, Inc.Inventors: Balwinder Bhatti, Scott R. Breining, Philip S. Hammond, Jozef Klucik, Yun-De Xiao
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Publication number: 20080113957Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein, X is —C(R3R4)—; Y is —N(R5)—; Z is (—C(?N—R5?)—; and R1, R2, R3, and R4 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.Type: ApplicationFiled: June 12, 2006Publication date: May 15, 2008Inventors: Brian McKittrick, Zhaoning Zhu, Andrew Stamford
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Patent number: 7217705Abstract: The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the pharmaceutical compositions comprising them and to their use in the treatment of Parkinson's disease.Type: GrantFiled: February 25, 2004Date of Patent: May 15, 2007Assignee: Aventis Pharma S.A.Inventors: Jésus Benavides, Daniel Boccio, Yvette Henin, Odile Piot-Grosjean
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Patent number: 7105504Abstract: The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the pharmaceutical compositions comprising them and to their use in the treatment of Parkinson's disease.Type: GrantFiled: February 25, 2004Date of Patent: September 12, 2006Assignee: Aventis Pharma S.A.Inventors: Jésus Benavides, Daniel Boccio, Yvette Henin, Odile Piot-Grosjean
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Patent number: 6821964Abstract: Chemokine receptor antagonists, in particular, bicyclic diamine compounds of Formula (I) that act as antagonists of chemokine CCR2 and CCR3 receptors including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leucocyte accumulation are described herein.Type: GrantFiled: March 6, 2002Date of Patent: November 23, 2004Assignee: Pfizer IncInventors: Roberto Colon-Cruz, Mary T. Didiuk, Erin M. Duffy, Ravi Garigipati, Wan F. Lau, Wayne S. McDonald
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Publication number: 20040220173Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: ApplicationFiled: April 6, 2004Publication date: November 4, 2004Applicant: Aventis Pharmaceutical Inc.Inventors: James A. Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M. Shutske, Joseph T. Strupczewski, Kenneth J. Bordeau, John G. Jurcak, Thaddeus R. Nieduzak, Sharon A. Jackson, Paul Angell, James P. Carey, George Lee, David Fink, Jean-Francois Sabuco, Yulin Chiang, Nicola Collar
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Publication number: 20040204398Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: February 27, 2004Publication date: October 14, 2004Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
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Publication number: 20040186088Abstract: The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.Type: ApplicationFiled: December 19, 2003Publication date: September 23, 2004Inventors: Upul Bandarage, Jon H. Come, Emanuele Perola, Govinda Rao Bhisetti, Jeffrey O. Saundres
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Publication number: 20040162279Abstract: The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.Type: ApplicationFiled: October 2, 2003Publication date: August 19, 2004Inventors: Michael Robert Barbachyn, J. Craig Ruble, Arthur Glenn Romero, Lisa Marie Thomasco, Alexander Ross Hurd, John Raymond Palmer, Peter Laurence Toogood, Dennis Joseph McNamara, Debra Ann Sherry, Paul Joseph Dobrowolski
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Publication number: 20040142916Abstract: The invention provides novel compounds useful as kinase inhibitors or as starting materials And/or intermediates in the synthesis of compounds useful as kinase inhibitors.Type: ApplicationFiled: January 9, 2004Publication date: July 22, 2004Inventors: Paul A. Wender, Marc A. Scanio
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Publication number: 20040102474Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: October 24, 2003Publication date: May 27, 2004Inventors: Andrew W. Stamford, Ying Huang, Li Guoqing
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Publication number: 20040087569Abstract: Novel N-heterocyclic bicyclic lactone compounds of formula I and its novel hydroxyamide precursors of formula IV, 1Type: ApplicationFiled: October 28, 2003Publication date: May 6, 2004Inventors: Todd D. Nelson, Carl LeBlond, Michael H. Kress
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Publication number: 20040067930Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain.Type: ApplicationFiled: June 27, 2003Publication date: April 8, 2004Applicant: Targacept, Inc.Inventors: Balwinder S. Bhatti, Craig Harrison Miller, Jeffrey Daniel Schmitt
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Publication number: 20030229066Abstract: The invention relates to heterocyclic substituted urea derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: ApplicationFiled: February 19, 2002Publication date: December 11, 2003Inventors: James A. Hendrix, Joseph T. Strupczewski, Kenneth J. Bordeau, Sarah Brooks, Horst Hemmerle, Matthias Urmann, Xu-Yang Zhao, Paul J. Mueller
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Publication number: 20030195216Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: July 12, 2002Publication date: October 16, 2003Inventors: Solo Goldstein, Guillaume Poissonnet, Jean-Gilles Parmentier, Pierre Lestage, Brian Lockhart
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Publication number: 20030166628Abstract: The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds of Formula (I) including pharmaceutically acceptable salts thereof in which have affinity for 5-HT1A receptors and which inhibits neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snacking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such asType: ApplicationFiled: January 16, 2003Publication date: September 4, 2003Inventors: Kevin James Doyle, Frank Kerrigan, John Paul Watts
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Patent number: 6602864Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: June 3, 1998Date of Patent: August 5, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
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Publication number: 20030109516Abstract: The present invention relates to tetrahydroquinazoline-2,4-diones derivatives of the formula (I): 1Type: ApplicationFiled: January 10, 2003Publication date: June 12, 2003Applicant: Pfizer Inc.Inventors: Anton Franz Joseph Fliri, Todd William Butler, Randal James Gallaschun, John Anthony Ragan, Brian Patrick Jones