Benzothiazoles (including Hydrogenated) Patents (Class 544/135)
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Publication number: 20110263593Abstract: The disclosure concerns imidazo[1,2-a]pyrimidine derivatives of formula (I) and isomers and pharmaceutically acceptable salts thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.Type: ApplicationFiled: January 17, 2011Publication date: October 27, 2011Applicant: sanofi-aventisInventors: Eric Bacque, Dominique Damour, Conception Nemecek, Patrick Nemecek, Laurent Schio, Sylvie Wentzler
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Publication number: 20110257153Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: ApplicationFiled: April 21, 2011Publication date: October 20, 2011Inventors: Genesis M. Bacani, Scott D. Bembenek, Wendy Eccles, James P. Edwards, Matthew T. Epperson, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Kelly J. Mcclure, Taraneh Mirzadegan, Alexandro Santillan, JR.
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Publication number: 20110251386Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.Type: ApplicationFiled: October 15, 2009Publication date: October 13, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Koji Masuda, Shiro Kida, Kyohei Hayashi, Manabu Katou, Naoki Yoshikawa, Akira Kugimiya, Mado Nakajima, Nobuyuki Tanaka
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Publication number: 20110251193Abstract: Novel classes of 1,2-benzisothiazolinone and isoindolinone compounds and compositions are disclosed. These compounds and compositions are useful in treating, preventing, and/or ameliorating viral, yeast, and fungal infections such as, for example, Hepatitis C Virus, Flavivirus infections, Aspergillus fumigatus, and candidiasis.Type: ApplicationFiled: September 23, 2009Publication date: October 13, 2011Applicants: WICHITA STATE UNIVERSITY, GEORGETOWN UNIVERSITYInventors: Richard A. Calderone, William C. Groutas, Brent E. Korba
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Publication number: 20110201604Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.Type: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
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Patent number: 7985749Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.Type: GrantFiled: April 29, 2005Date of Patent: July 26, 2011Assignee: Novartis AGInventors: Hong Liu, David C. Tully, Arnab Chatterjee, Phillip B. Alper, David H. Woodmansee, Daniel Mutnick
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Publication number: 20110178083Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: July 9, 2009Publication date: July 21, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Patent number: 7951954Abstract: The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.Type: GrantFiled: March 12, 2007Date of Patent: May 31, 2011Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Andrew Lister, Garry Pairaudeau
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Patent number: 7928133Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: July 24, 2007Date of Patent: April 19, 2011Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
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Publication number: 20100324039Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Michael Jones, David Gunn, John Howard Jones, Michael Van Zandt
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Publication number: 20100317842Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.Type: ApplicationFiled: August 25, 2010Publication date: December 16, 2010Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Dhanalakshmi Kasi, Vani P. Mocharla, Bing Wang, Umesh B. Gangadharmath, Brian A. Duclos, Kai Chen, Wei Zhang, Gang Chen, Henry Clifton Padgett, Farhad Karimi, Peter J.H. Scott, Zhiyong Gao, Qianwa Liang, Thomas Lee Collier, Tieming Zhao, Chunfang Xia
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Publication number: 20100311741Abstract: This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-? Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-?, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in the inhibition of TACE, and in the treatment of conditions that are ameliorated by the inhibition of TACE.Type: ApplicationFiled: May 16, 2008Publication date: December 9, 2010Applicant: INHIBOX LTD.Inventors: Aigars Jirgensons, Gundars Leitis, Ivars Kalvinsh, Daniel Robinson, Paul Finn, Nagma Khan
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Patent number: 7847101Abstract: Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R1, R2 and R3 at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R4 is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl.Type: GrantFiled: July 23, 2003Date of Patent: December 7, 2010Assignee: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
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Publication number: 20100305067Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2Jalkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic raType: ApplicationFiled: December 12, 2008Publication date: December 2, 2010Applicant: BIOTA EUROPE LTDInventors: David John Haydon, Lloyd George Czaplewski
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Publication number: 20100292208Abstract: Compounds with two fused bicyclic heteroaryl moieties and their pharmaceutical compositions, and methods of using them as leukotriene A4 hydrolase (LTA4H) modulators and for the treatment of diseases, disorders and conditions mediated by LTA4H.Type: ApplicationFiled: May 12, 2010Publication date: November 18, 2010Inventors: Genesis Bacani, Christa C. Chrovian, Wendy Eccles, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, JR., Virginia M. Tanis, John J. M. Wiener
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Publication number: 20100292232Abstract: Disclosed herein are antiviral agents, in particular non-nucleoside reverse transcriptase inhibitors (NNRTIs) of the formula Also disclosed are methods of making the NNRTIs, as well as compositions that include such NNRTIs and methods of their use for treating viral infections, in particular retroviral infections, such as HIV infection.Type: ApplicationFiled: November 5, 2008Publication date: November 18, 2010Inventors: Daniel Elleder, John A.T. Young, Thomas J. Baiga, Joseph P. Noel
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Publication number: 20100273793Abstract: The disclosure relates to compounds of formula (I): wherein A, W, R, R5, and R6 are as defined in the disclosure, or a salt thereof, and to their use as drugs, in particular as c-Met inhibitors.Type: ApplicationFiled: April 16, 2010Publication date: October 28, 2010Applicant: SANOFI-AVENTISInventors: Conception Nemecek, Sylvie Wentzler
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Publication number: 20100240889Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, Y and G have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 24, 2006Publication date: September 23, 2010Applicant: PROSKELIA SASInventors: Pierre DePrez, Hélène Jary, Taoues Temal
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Patent number: 7767811Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: June 5, 2006Date of Patent: August 3, 2010Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Publication number: 20100137301Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: February 8, 2010Publication date: June 3, 2010Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Publication number: 20100099671Abstract: A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a C3-C6 cycloalkylsulfanyl group, a C3-C6 cycloalkylsulfinyl group, or a C3-C6 cycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).Type: ApplicationFiled: March 6, 2008Publication date: April 22, 2010Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Kohei Ohata, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
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Patent number: 7659269Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: GrantFiled: December 4, 2007Date of Patent: February 9, 2010Assignee: The Institute for Pharmaceutical Discovery, LLCInventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
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Publication number: 20100016304Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 21, 2007Publication date: January 21, 2010Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Ayako Nakamura, Kenji Fujita, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
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Patent number: 7642274Abstract: The invention aims to provide a drug having an activity on inhibiting a decrease in pain threshold. Since a ?-opioid receptor agonist effectively inhibits the decrease in pain threshold, it is useful as an inhibitor of pain threshold decrease.Type: GrantFiled: July 2, 2004Date of Patent: January 5, 2010Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kyoichi Shimomura, Hiroyuki Aono, Yaeko Tsukahara, Taeko Hata
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Patent number: 7576110Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: September 8, 2006Date of Patent: August 18, 2009Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
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Publication number: 20090186870Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: October 9, 2008Publication date: July 23, 2009Applicant: AstraZeneca ABInventors: Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
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Publication number: 20090143376Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: March 3, 2006Publication date: June 4, 2009Applicant: Sitris Pharmaceuticals, Inc.Inventors: Michael Milburn, Jill Milne, Jean Bemis, Joseph J. Nunes, Roger Xie, Karl D. Nomington, Chi B. Vu
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Publication number: 20090137570Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: ApplicationFiled: January 28, 2009Publication date: May 28, 2009Applicant: IRM LLCInventors: Hong LIU, Arnab K. CHATTERJEE, David C. TULLY, Phillip B. ALPER, Badry BURSULAYA, Jianhua GUO, David H. WOODMANSEE, Daniel MUTNICK, Donald S. KARANEWSKY, Yun HE
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Publication number: 20090118272Abstract: A compound of Formula (I) an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein A is independently selected from: further wherein R1, R2, R3, R4, R5, R6, R7, and W are as described herein. Also disclosed is a compound of Formula (II) an enantiomer, diastereomer, or a pharmaceutically-acceptable salt thereof, wherein each of G, X and Y are independently CH or N, wherein at each occurrence at least one of G, X or Y is N and the other two of G, X or Y are CH; and B is independently selected from: further wherein R1, R2, R3, R4, R5, R8, R9 and Z are as described herein. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and Formula (II), and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: December 12, 2008Publication date: May 7, 2009Inventors: Chunjian Liu, Katerina Leftheris, James Lin
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Publication number: 20090069317Abstract: The invention relates to insecticidal methods using 3-amino-1,2-benzoisothiazole compounds of the formula (I) wherein the variables n and R1 to R6 are as defined in the description. The invention relates to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, and to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects.Type: ApplicationFiled: November 15, 2006Publication date: March 12, 2009Applicant: BASF SEInventors: Matthias Pohlman, Wolfgang von Deyn, Florian Kaiser, Michael Rack, Henricus Maria Martinus Bastiaans, Douglas D. Anspaugh, Deborah L. Culbertson, Henry Van Tuyl Cotter
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Publication number: 20090062259Abstract: The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.Type: ApplicationFiled: March 12, 2007Publication date: March 5, 2009Applicant: ASTRAZENECA ABInventors: Lilian Alcaraz, Andrew Lister, Garry Pairaudeau
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Publication number: 20080306060Abstract: A series of 5,6-dihydro-1,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: April 25, 2006Publication date: December 11, 2008Applicant: UCB PHARMA S.A.Inventors: Rikki Peter Alexander, Pavandeep Aujla, Mark James Batchelor, Daniel Christopher Brookings, George Martin Buckley, Karen Viviane Lucile Crepy, Claire Louise Kulisa, James Petrie Turner
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Publication number: 20080214540Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: December 4, 2007Publication date: September 4, 2008Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Publication number: 20080194555Abstract: This invention relates to benzimidazole and benzothiazole compounds of formula (I) to methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.Type: ApplicationFiled: March 25, 2008Publication date: August 14, 2008Applicant: AVENTIS PHARMA S.A.Inventors: Conception NEMECEK, Francois CLERC
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
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Patent number: 7371749Abstract: The present invention relates to compounds of formulae IA and IB wherein R1 and R2 are each independently lower alkyl or —(CH2)m—O-lower alkyl, or together with the N atom to which they are attached form a heterocyclic ring; R3 is hydrogen or lower alkyl; R4 is lower alkyl; hetaryl is 3H-imidazole-2,4-diyl or 1H-pyrazole-1,4-diyl; n is 1 or 2; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used for the treatment of Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, ADHD, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or for the treatment of asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse, or for use as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for coronary artery disease and heart failure.Type: GrantFiled: July 18, 2005Date of Patent: May 13, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Claus Riemer
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Patent number: 7371748Abstract: This invention relates to compounds of formula I wherein R1 and R2 are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compounds of formula I are adenosine receptor ligands with good affinity to the A2A-receptor and a high selectivity to the A1- and A3 receptors. These compounds are useful, inter alia, in treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.Type: GrantFiled: May 17, 2004Date of Patent: May 13, 2008Assignee: Hoffman-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 7348347Abstract: Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions and/or treating or inhibiting various medical conditions such as, e.g., depression and pain.Type: GrantFiled: August 11, 2006Date of Patent: March 25, 2008Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Corinna Sundermann, Bernd Sundermann, Edward Bijsterveld
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Patent number: 7314872Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula I: wherein Q is morpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.Type: GrantFiled: August 18, 2004Date of Patent: January 1, 2008Assignee: IRM LLCInventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
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Patent number: 7304058Abstract: The present invention relates to a compound of formula I wherein R, X and n are defined hereinabove, and to a pharmaceutically acceptable salt thereof. The compound may be used for the treatment of diseases related to the A2A receptor.Type: GrantFiled: May 18, 2004Date of Patent: December 4, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 7285548Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are described herein, and their pharmaceutically acceptable salts thereof for the treatment of diseases, related to the A2A receptor.Type: GrantFiled: May 26, 2004Date of Patent: October 23, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 7226940Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel DiseaseType: GrantFiled: August 24, 2005Date of Patent: June 5, 2007Assignees: Incyte San Diego, Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P. M. Pleynet, Lyle W. Spruce
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Patent number: 7205312Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: November 2, 2004Date of Patent: April 17, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Patent number: 7141595Abstract: The present invention provides novel amino benzothiazole compounds, compositions comprising these compounds and methods of using these compounds as neuroprotectants. In particular, the compounds described in the present invention are useful for treating stroke and neuropathic pain.Type: GrantFiled: November 24, 2004Date of Patent: November 28, 2006Assignee: Neuraxon Inc.Inventors: Jailall Ramnauth, Suman Rakhit, Shawn Maddaford, Namrta Bhardwaj
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Patent number: 7122545Abstract: The invention relates to 2-imidazo-benzothiazoles of general formula wherein R1, R2, R3, R4, R5, R6, R7, R?, R?, X, R?? and n are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compound of formula I are adenosine receptor ligands with good affinity to the A1 and A3 receptors. These compounds have useful pharmaceutical activities.Type: GrantFiled: May 11, 2004Date of Patent: October 17, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 7105514Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: GrantFiled: April 27, 2004Date of Patent: September 12, 2006Assignee: The Institute for Dibetes Discovery LLCInventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Patent number: 7045518Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: October 3, 2003Date of Patent: May 16, 2006Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, Joseph J. McDonald
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Patent number: 7019001Abstract: A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula to a person in need of such treatment.Type: GrantFiled: October 23, 2003Date of Patent: March 28, 2006Assignee: Hoffman-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 6987184Abstract: Isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula: and pharmaceutically acceptable salts thereof, wherein R0 is —CH2—, —SO—, —O—, —SO2—, or —S—; compositions comprising the isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof; and methods for treating or preventing a disorder alleviated by inhibiting Jun N-terminal kinase (JNK) by administering the isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof are described herein.Type: GrantFiled: February 7, 2002Date of Patent: January 17, 2006Assignee: Signal Pharmaceuticals, LLCInventors: Steven T. Sakata, Heather K. Raymon
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Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley