Plural Piperidine Rings Patents (Class 514/316)
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Publication number: 20090264418Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: June 29, 2009Publication date: October 22, 2009Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20090264407Abstract: Substituted sulfonamide compounds corresponding to formula I: a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment of pain or other disorders or diseases that are mediated at least in part by B1R receptors.Type: ApplicationFiled: April 8, 2009Publication date: October 22, 2009Applicant: GRUENENTHAL GmbHInventors: Stefan OBERBOERSCH, Melanie REICH, Stefan SCHUNK, Michael ENGELS, Ruth JOSTOCK, Tieno GERMANN, Sabine HEES
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Publication number: 20090253709Abstract: An series of 2,7-disubstituted anthraquinone derivatives including a formula I are provided. R is a first substituted group selected from a group consisting of a hydrogen, an amino group, a nitro group, a hydroxyl group, a C1-C12 alkyl group, a C1-C12 alkyl halide group (—(CH2)nX), a C3-C12 cycloalkyl group, a benzyl group, a C1-C12 alkylamino group, a C5-C12 nitrocycloalkyl group and a heterocyclic group, n satisfies 1?n?12 and X is an atom selected from a group consisting of a fluoride (F), a chloride (Cl), a bromide (Br) and an iodine (I). The preparation method of the 2,7-disubstituted anthraquinone derivatives includes the steps of acetylating 2,7-diaminoanthraquinone to be one 2,7-disubstituted anthraquinone derivative, which can be further aminated to be another 2,7-disubstituted anthraquinone derivative.Type: ApplicationFiled: August 15, 2008Publication date: October 8, 2009Applicant: NATIONAL DEFENSE MEDICAL CENTERInventor: Hsu-Shan HUANG
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Publication number: 20090247509Abstract: 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 17, 2009Publication date: October 1, 2009Applicant: AVENTIS PHARMACEUTICALS 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: 20090226379Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 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: ApplicationFiled: May 8, 2009Publication date: September 10, 2009Applicant: THERAVANCE, INC.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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Patent number: 7585879Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 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: July 19, 2007Date of Patent: September 8, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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Patent number: 7585866Abstract: The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: wherein n is an integer, preferably n is 1; wherein R1 and R2 are independently selected from the group consisting of:Type: GrantFiled: July 31, 2003Date of Patent: September 8, 2009Assignee: Critical Outcome Technologies, Inc.Inventors: Wayne R. Danter, Martyn Brown, George Ma, Ghenadie Rusu, Jianhua Zhong, Natalie Lazarowych, Stephen Houldsworth
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Patent number: 7582655Abstract: The present invention relates to 4-piperidone derivatives represented by the following formula (I) and the acid addition salts thereof. The method of preparation and antineoplastic activity of the said compounds are disclosed. A number of the compounds possess submicromolar IC50 and CC50 values and have a selective toxicity for colon cancers and leukemic cells. In addition, many of the compounds are able to reverse multidrug resistance.Type: GrantFiled: November 22, 2006Date of Patent: September 1, 2009Assignee: University of SaskatchewanInventors: Jonathan R. Dimmock, Umashankar Das
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Publication number: 20090209582Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds. The invention further relates to crystalline forms of a compound of formula (I).Type: ApplicationFiled: May 24, 2006Publication date: August 20, 2009Inventors: Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seok-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess, Sean Dalziel, Kirsten M. Phizackerley
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Publication number: 20090209578Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, Het and m are as defined in the description. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors.Type: ApplicationFiled: November 27, 2006Publication date: August 20, 2009Inventors: Christopher Gordon Barber, David Clive Blakemore
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Patent number: 7576101Abstract: The application provides for methods and compositions for inhibiting demyelination, promoting remyelination and/or treating paralysis in a subject in need thereof. Preferably, such compositions include immunoglobulins (e.g., antibodies, antibody fragments, and recombinantly produced antibodies or fragments), polypeptides (e.g., soluble forms of the ligand proteins for integrins) and small molecules, which when administered in an effective amount inhibits demyelination and/or promotes remyelination in a patient. The compositions and methods described herein can also utilize other anti-inflammatory agents used to palliate conditions and diseases associated with demyelination.Type: GrantFiled: January 26, 2004Date of Patent: August 18, 2009Assignee: Elan Pharmaceuticals, Inc.Inventors: Stephen J. Karlik, Michael A. Pleiss, Andrei W. Konradi, Francine S. Farouz, Christopher M. Semko, Darren B. Dressen, Elizabeth Messersmith, Stephen Freedman, Ted Yednock
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Publication number: 20090203710Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's diseaseType: ApplicationFiled: March 6, 2009Publication date: August 13, 2009Inventors: Norikazu Ohtake, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani, Sayaka Mizutani
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Publication number: 20090203696Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: ApplicationFiled: December 15, 2008Publication date: August 13, 2009Applicant: SANOFI-AVENTISInventors: Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
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Publication number: 20090203736Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.Type: ApplicationFiled: February 5, 2009Publication date: August 13, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Patent number: 7569585Abstract: Substituted 1,5-diaminopentan-3-ol compounds and methods of making the same. Pharmaceutical compositions containing these compounds and methods of treatment using these pharmaceutical compositions.Type: GrantFiled: June 14, 2004Date of Patent: August 4, 2009Assignee: Gruenenthal GmbHInventors: Heinz Uragg, Corinna Maul, Helmut Buschmann, Bernd Sundermann, Werner Englberger
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Patent number: 7569586Abstract: 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: GrantFiled: August 15, 2005Date of Patent: August 4, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Trevor Mischki, Adam Hughes, Yu-Hua Ji
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Patent number: 7569604Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: GrantFiled: June 22, 2005Date of Patent: August 4, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Andreas Termin, Esther Martinborough, Nicole Zimmerman, Charles Cohen, Corey Gutierrez
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Publication number: 20090192139Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: ApplicationFiled: April 3, 2009Publication date: July 30, 2009Inventors: Daniel V. Paone, Anthony W. Shaw
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Publication number: 20090186874Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B and ring C are each an aromatic ring optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), Z is an optionally halogenated C1-6 alkyl group, Y is a methylene group optionally having substituent(s), m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof. The compound of the present invention has a superior tachykinin receptor antagonistic action, particularly an SP receptor antagonistic action, and is useful as a pharmaceutical agent, for example, a tachykinin receptor antagonist, an agent for the prophylaxis or treatment of an abnormality of lower urinary tract functions, a digestive organ disease or a central nerve disease, and the like.Type: ApplicationFiled: January 13, 2005Publication date: July 23, 2009Inventors: Yoshinori Ikeura, Junya Shirai
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Publication number: 20090186894Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: December 21, 2007Publication date: July 23, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Publication number: 20090176767Abstract: 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: ApplicationFiled: March 12, 2009Publication date: July 9, 2009Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Viengkham Malathong
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Publication number: 20090170864Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: May 1, 2008Publication date: July 2, 2009Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Lee Apostle McDermott, Yimin Qian, Jenny Tan, Weiya Yun
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Publication number: 20090170829Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: November 17, 2008Publication date: July 2, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Hui Hong, Xiang Xu, Jiaxin Yu, Rajinder Singh, Ihab S. Darwish, Sambaiah Thota
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Publication number: 20090163544Abstract: This invention relates to the treatment or prevention of nausea and/or vomiting by the administration of a NK-3 receptor antagonist.Type: ApplicationFiled: March 31, 2006Publication date: June 25, 2009Inventors: Michael Rigby, Frederick David
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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: 20090156638Abstract: Provided herein are methods for inhibiting proliferation of a microbe associated with a sexually transmitted disease (STD) or infection and for preventing transmission of one or more sexually transmitted diseases in a subject at-risk for acquiring the same, including an HIV positive subject at risk for acquiring another sexually transmitted disease. The methods comprise contacting a microbe or cell thereof associated with the STD or administering to the subject nordihydroguaiaretic acid or a derivative or analog thereof. In HIV positive at-risk subjects one or more anti-retroviral drugs are co-administered.Type: ApplicationFiled: May 12, 2008Publication date: June 18, 2009Inventor: Niharika Khanna
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Publication number: 20090156572Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.Type: ApplicationFiled: December 2, 2008Publication date: June 18, 2009Inventors: Yoshinori Ikeura, Junya Shirai, Hideyuki Sugiyama, Yuji Nishikimi, Taku Kamei, Nobuki Sakauchi
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Publication number: 20090156574Abstract: The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.Type: ApplicationFiled: January 27, 2009Publication date: June 18, 2009Applicant: SANOFI-AVENTISInventors: Pierre CARAYON, Pierre CASELLAS, Daniel FLOUTARD, Pierre FRAISSE, Samir JEGHAM, Bernard LABEEUW
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Patent number: 7547693Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnnia, repetitive hypersomnnia, true hypersomnnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder, and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disType: GrantFiled: September 21, 2004Date of Patent: June 16, 2009Assignee: Banyu Pharmaceutical Co. Ltd.Inventors: Norikazu Ohtake, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani, Sayaka Mizutani
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Publication number: 20090143372Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 31, 2007Publication date: June 4, 2009Inventors: Jianghe Deng, Jeffrey K. Kerns, Qi Jin, Guoliang Lin, Xichen Lin, Michael Lindenmuth, Christopher Neipp, Hong Nie, Sonia M. Thomas, Katherine L. Widdowson
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Patent number: 7541369Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: March 11, 2003Date of Patent: June 2, 2009Assignee: Janssen Pharmaceutica, NVInventors: Patrick René Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Publication number: 20090137576Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.Type: ApplicationFiled: May 29, 2006Publication date: May 28, 2009Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
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Patent number: 7534788Abstract: The present invention relates to compounds of formula I wherein X, A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: July 16, 2008Date of Patent: May 19, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Peter Mohr, Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Tadakatsu Takahashi, Sven Taylor
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Publication number: 20090124635Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, m and n are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.Type: ApplicationFiled: January 12, 2006Publication date: May 14, 2009Applicant: PFIZER INC.Inventors: Christopher Gordon Barber, David Clive Blakemore, David Cameron Pryde, James Welsh Auld Kinnaird
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Publication number: 20090118267Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, and q have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: February 13, 2006Publication date: May 7, 2009Inventors: Dirk Finsinger, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Kai Schiemann, Wolfgang Staehle, Christiane Amendt, Nina Heiss, Frank Zenke
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Publication number: 20090111803Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: April 30, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankat
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Publication number: 20090111808Abstract: The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.Type: ApplicationFiled: April 25, 2006Publication date: April 30, 2009Inventors: Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz, Olivier Labeeuw
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Publication number: 20090111809Abstract: The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-HSD type 1 activity.Type: ApplicationFiled: April 23, 2007Publication date: April 30, 2009Inventors: Julie Kay Bush, Marvin Martin Hansen, Renhua Li, Thomas Edward Mabry, Nancy June Snyder, Owen Brendan Wallace, Yanping Xu
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Patent number: 7524962Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W 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: April 28, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu
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Patent number: 7521445Abstract: 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: GrantFiled: March 5, 2007Date of Patent: April 21, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: James Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M Shutske, Joseph T Strupczewski, Kenneth J Bordeau, John G Jurcak, Thaddeus Nieduzak, Sharon A. Jackson, Paul Angell, James P Carey, George Lee, David Fink, Jean-Francois Sabuco, Yulin Chiang, Nicola Collar
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Patent number: 7521041Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 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: October 12, 2007Date of Patent: April 21, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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Publication number: 20090099182Abstract: The present invention discloses novel compounds of Formula I: having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 24, 2007Publication date: April 16, 2009Inventors: Renhua Li, Thomas Edward Mabry, Owen Brendan Wallace, Leonard Larry Winneroski, JR., Yanping Xu
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Patent number: 7514431Abstract: The present invention is directed to compounds of the formula I: I (wherein R1, R2, R3, R4, R5, R6, X, Z and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: GrantFiled: October 24, 2003Date of Patent: April 7, 2009Assignee: Merck & Co., Inc.Inventors: Changyou Zhou, Alexander Pasternak, Lihu Yang
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Publication number: 20090088430Abstract: The present invention discloses novel compounds of Formula I: having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 27, 2007Publication date: April 2, 2009Inventors: Owen Brendan Wallace, Yanping Xu, Jeremy Schulenburg York
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Publication number: 20090088453Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W 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: ApplicationFiled: December 4, 2008Publication date: April 2, 2009Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu
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Publication number: 20090082397Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W 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: ApplicationFiled: November 17, 2008Publication date: March 26, 2009Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu
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Publication number: 20090076078Abstract: Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R2, R3, X, m and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: September 8, 2008Publication date: March 19, 2009Applicant: ASTRAZENECA ABInventors: Yun-Xing Cheng, Xuehong Luo, Vijayaratnam Santhakumar, Miroslaw Jerzy Tomaszewski
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Publication number: 20090076026Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 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: ApplicationFiled: November 5, 2008Publication date: March 19, 2009Inventors: Yu-Hua JI, Craig Husfeld, Mathai Mammen, YongQi Mu, Eric L. Stangeland