Ring Nitrogen In The Additional Hetero Ring Patents (Class 546/208)
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Publication number: 20110046106Abstract: The present invention relates to compounds of general formula I wherein A, B, R1, R2 and R3 are defined as in claim 1, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: February 5, 2009Publication date: February 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Patent number: 7888384Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: GrantFiled: April 16, 2009Date of Patent: February 15, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Andreas Termin, Esther Martinborough, Nicole Zimmerman, Charles Cohen, Corey Gutierrez
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Publication number: 20110034417Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: ApplicationFiled: October 5, 2010Publication date: February 10, 2011Applicant: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland E. Dolle
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Publication number: 20110021489Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: May 27, 2010Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Dirk HEIMBACH, Susanne Röhrig, Yolanda Cancho Grande, Eckhard Bender, Katja Zimmermann, Anja Buchmüller, Christoph Gerdes, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
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Publication number: 20110021565Abstract: The invention relates to a compound of formula wherein Ar1, Ar2, R1, R2, R3, R4, R5, and R5? or to a pharmaceutically active salt thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 4, 2010Publication date: January 27, 2011Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian, Xihan Wu
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Publication number: 20110014226Abstract: A method to identify small molecules useful as therapeutics and/or vaccines to prevent, alleviate or ameliorate a pathogenic infection or an autoimmune disorder. The method can be used to screen small molecule test compounds for the ability to disrupt particular antigen-antibody interactions of interest. In one embodiment, the antigen is a pathogen-derived antigen and the antibody decreases or inhibits virulence of the pathogen when bound to the antigen (e.g., a neutralizing antibody, antibody with serum bactericidal activity, etc.). In another embodiment, the antigen is a self-antigen (autoantigen) and the antibody is an autoantibody that is known to be associated with a pathological condition (e.g., autoimmune disorder). Compounds that bind to the antigen or antibody disrupt binding can be used as therapeutics to decrease or inhibit the autoimmune disorder.Type: ApplicationFiled: March 17, 2009Publication date: January 20, 2011Inventors: Michael J. Caulfield, Michael D. Miller, Joseph G. Joyce, Paul D. Zuck, Krista L. Getty, Vadim Dudkin, Elizabeth A. Ottinger
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20100331375Abstract: 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: September 13, 2010Publication date: December 30, 2010Applicant: THERAVANCE, INC.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu
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Patent number: 7858624Abstract: Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.Type: GrantFiled: April 5, 2007Date of Patent: December 28, 2010Assignee: Vitae Pharmaceuticals, Inc.Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh
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Patent number: 7858797Abstract: 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: November 17, 2008Date of Patent: December 28, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu
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Patent number: 7851631Abstract: 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: July 19, 2007Date of Patent: December 14, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Eric L. Stangeland, Aaron Kushner, Craig Husfeld
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Patent number: 7851632Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 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: December 14, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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Publication number: 20100311794Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: June 7, 2010Publication date: December 9, 2010Applicant: Gilead Sciences, Inc.Inventor: Chandrasekar Venkataramani
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Publication number: 20100311792Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: September 26, 2008Publication date: December 9, 2010Inventors: Bin Shao, Jiangchao Yao
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Publication number: 20100311753Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.Type: ApplicationFiled: June 24, 2010Publication date: December 9, 2010Applicant: ChemoCentryx, Inc.Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
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Publication number: 20100305090Abstract: The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.Type: ApplicationFiled: March 5, 2008Publication date: December 2, 2010Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke
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Publication number: 20100298299Abstract: The present invention relates to new non-peptide derivatives of formula (I), wherein R1-R5, Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: October 27, 2007Publication date: November 25, 2010Inventors: Istvan Vago, Sandor Farkas, Katalin Hornok, Gyula Beke, Eva Bozo, Monika Vastag, Eva Szentirmay, Gyorgy Keseru, Eva Schmidt
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Patent number: 7834031Abstract: The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.Type: GrantFiled: September 25, 2006Date of Patent: November 16, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: H. Donald Burns, Terence G. Hamill, Craig W. Lindsley
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Patent number: 7834182Abstract: 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 diseasType: GrantFiled: March 6, 2009Date of Patent: November 16, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Norikazu Ohtake, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani, Sayaka Mizutani
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Publication number: 20100280005Abstract: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: November 4, 2010Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, John Gleason, Alexey V. Ishchenko, Brian Lawhorn, Gerard McGeehan, Jaclyn R. Patterson, Simon F. Semus, Robert D. Simpson, Suresh B. Singh, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Wei Zhao
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Patent number: 7825139Abstract: Compounds that selectively inhibit dipeptidyl peptidase-IV over closely related dipeptidyl peptidases are those of Formula (I): as well as pharmaceutically acceptable salts thereof, cyclic isomers thereof, prodrugs thereof, and solvates thereof, where all the variables are defined herein. These compounds can be used, alone or in combination with other drugs, for the treatment of diabetes and related diseases.Type: GrantFiled: May 25, 2006Date of Patent: November 2, 2010Inventors: David Alan Campbell, David T. Winn, Juan Manuel Betancort
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Publication number: 20100273782Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Baaum
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Publication number: 20100267696Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). 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, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: ApplicationFiled: December 11, 2008Publication date: October 21, 2010Applicant: THE UNIVERSITY OF EDINBURGHInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Patent number: 7816349Abstract: The present invention discloses novel compounds of Formula I: (I) possessing 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, cognitive disorders, and other conditions associated with 11?-HSD type 1 activity.Type: GrantFiled: April 23, 2007Date of Patent: October 19, 2010Assignee: Eli Lilly and CompanyInventors: John Gordon Allen, Alexei Pavlovych Krasutsky, Owen Brendan Wallace, Yanping Xu, Jeremy Schulenburg York
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Patent number: 7812021Abstract: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: August 21, 2008Date of Patent: October 12, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
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Publication number: 20100256130Abstract: The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.Type: ApplicationFiled: May 19, 2010Publication date: October 7, 2010Inventors: Krista B. Goodman, Michael J. Neeb, Clark A. Sehon, Andrew Q. Viet, Gren Z. Wang
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Publication number: 20100256144Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: ApplicationFiled: June 26, 2008Publication date: October 7, 2010Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Adreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Patent number: 7807669Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: GrantFiled: November 6, 2008Date of Patent: October 5, 2010Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
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Publication number: 20100249096Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.Type: ApplicationFiled: May 5, 2010Publication date: September 30, 2010Applicant: EXELIXIS, INC.Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
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Publication number: 20100249089Abstract: The present invention relates to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The invention provides an acrylonitrile derivative represented by formula (1): (wherein A represents an optionally substituted 3- to 8-membered heterocyclic ring) or a salt thereof.Type: ApplicationFiled: December 2, 2008Publication date: September 30, 2010Applicant: KABUSHIKI KAISHA YAKULT HONSHAInventors: Ryuta Yamazaki, Hiroshi Hatano, Takashi Yaegashi, Yoshiaki Igarashi, Oh Yoshida, Yoshikazu Sugimoto
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Publication number: 20100240139Abstract: The present invention relates to a free radical initiator and a method for peptide sequencing using the same. Compared with diazo or peroxy functionalized precursors, the precursors using the present compounds are chemically more robust and can generate radical species by homolytic cleavage upon thermal activation, enabling sequencing of more various peptides. In addition, the present invention makes it feasible to sequence peptides carrying disulfide bonds.Type: ApplicationFiled: October 14, 2009Publication date: September 23, 2010Applicant: University-Industry Cooperation Foundation Sogang UniversityInventors: Han-Bin Oh, Bong-Jin Moon, Min-Hyuck Kang, Min-Hee Lee
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Publication number: 20100240653Abstract: The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.Type: ApplicationFiled: October 16, 2007Publication date: September 23, 2010Inventors: Vincent J. Santora, Ryan M. Hart, Jason B. Ibarra, Douglas M. Park, Albert S. Ren, Graeme Semple, Jeffrey A. Schultz, Brian M. Smith, Jeffrey Smith
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Publication number: 20100234426Abstract: The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R1, R2, R3, R4 and R5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the activation of opioid receptors, particularly ?-opioid receptors. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: October 31, 2007Publication date: September 16, 2010Applicant: Purdue Pharma L.P.Inventor: Xiaoming Zhou
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Publication number: 20100234395Abstract: Discloses is a pharmaceutical agent comprising an ureide derivative represented by the formula: or a pharmaceutically acceptable salt thereof as an active ingredient. The ureide derivative or the pharmaceutically acceptable salt thereof is useful for the relief of a pain or the treatment or prevention of neurogenic pain.Type: ApplicationFiled: March 27, 2007Publication date: September 16, 2010Applicant: TORAY INDUSTRIES, INC.Inventors: Yuji Sugawara, Naoki Izumimoto, Hideyuki Tsutsui
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Publication number: 20100234356Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer, and osteolytic bone disorders.Type: ApplicationFiled: October 13, 2009Publication date: September 16, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Gerard Rosse, Linli Wei, Kenneth G. Carson
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Publication number: 20100226918Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: December 16, 2009Publication date: September 9, 2010Applicant: SANOFI-AVENTISInventors: Otmar KLINGLER, Joerg CZECH, Werngard CZECHTIZKY, Tilo WEISS, Melitta JUST
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Patent number: 7790725Abstract: A thiazolidine derivative represented by the formula (I) wherein each symbol is as defined in the specification, and a pharmaceutically acceptable salt thereof exhibit a potent DPP-IV inhibitory activity, and can be provided as an agent for the prophylaxis or treatment of diabetes, an agent for the prophylaxis or treatment of obesity and the like.Type: GrantFiled: July 9, 2007Date of Patent: September 7, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Sakashita, Tomohiro Yoshida, Hiroshi Kitajima, Masahiro Takeuchi, Yoshihito Tanaka, Takuya Yoshimura, Fumihiko Akahoshi, Yoshiharu Hayashi
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Publication number: 20100216748Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: May 7, 2010Publication date: August 26, 2010Applicant: ABBOTT LABORATORIESInventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li
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Publication number: 20100210618Abstract: The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRX—C(?O)—; —Z—C(?O)—; —Z—NRX—C(?O)—; —C(?O)—Z—; —NRX—C(?O)—Z—; —C(?S)—; —NRX—C(?S)—; —Z—C(?S)—; —Z—NRX—C(?S)—; —C(?S)—Z—; —NRX—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRX— or —NRX—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein saiType: ApplicationFiled: June 6, 2008Publication date: August 19, 2010Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Mieerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaret, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
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Patent number: 7776876Abstract: Embodiments of this invention provide methods for thereapeutic use of cyclic G-2-Allyl Proline to treat disorders of dopaminergic neurons, including Parkinson's disease. Cyclic G-2Allyl P is neuroprotective and has utility as a therapeutic agent for treatment of diseases and other conditions characterised by degeneration and/or death of dopaminergic neurons and the adverse symptoms of such degeneration and/or death. Such symptoms include loss of cognition and motor function. Compounds are also useful for manufacture of medicaments including tablets, capsules and injectable solutions that are useful for treatment of such conditions.Type: GrantFiled: April 7, 2006Date of Patent: August 17, 2010Assignee: Neuren Pharmaceuticals, Ltd.Inventors: Margaret Anne Brimble, Jian Guan
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Publication number: 20100204228Abstract: In one embodiment, compounds of the following structure are described, wherein R1 to R7 are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.Type: ApplicationFiled: April 15, 2010Publication date: August 12, 2010Applicant: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome, Michael Anthony Marella
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Publication number: 20100197715Abstract: The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.Type: ApplicationFiled: January 20, 2010Publication date: August 5, 2010Inventors: Sabine Kolczewski, Emmanuel Pinard, Henri Stalder
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Publication number: 20100197672Abstract: The present invention relates to a compound having the general formula (3): synthesis, intermediates and uses thereof.Type: ApplicationFiled: September 25, 2008Publication date: August 5, 2010Applicants: UNIVERSITA DEGLI STUDI DI ROMA "LA SAPIENZA", UNIVERSITA DEGLI STUDI DI SIENAInventors: Mariangela Biava, Giulio Cesare Porretta, Raffaello Pompei, Maurizio Botta, Fabrizio Manetti, Alessandro De Logu
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Publication number: 20100190762Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: April 2, 2010Publication date: July 29, 2010Applicant: CHEMOCENTRYX, INC.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
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Publication number: 20100190822Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: March 19, 2010Publication date: July 29, 2010Applicant: ABBOTT LABORATORIESInventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
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Publication number: 20100184764Abstract: The present invention discloses compounds of Formula I: (I) having 11beta-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 the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Applicant: ELI LILLY AND COMPANYInventors: Thomas Daniel AICHER, Mark Joseph CHICARELLI, Ronald Jay HINKLIN, Hongqi TIAN, Owen Brendan WALLACE, John Gordon ALLEN, Zhaogen CHEN, Thomas Edward MABRY, Jefferson Ray MCCOWAN, Nancy June SNYDER, Leonard Larry WINNEROSKI, JR.
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Publication number: 20100184805Abstract: Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. The present invention is also directed to pharmaceutical compositions comprising a compound described herein or enantiomers, diastereomers, or salts thereof and a pharmaceutically acceptable carrier or excipient.Type: ApplicationFiled: June 20, 2008Publication date: July 22, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishchenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao
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Publication number: 20100179118Abstract: The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or —C(R6)(R7)—, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.Type: ApplicationFiled: September 7, 2007Publication date: July 15, 2010Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Michinori Ozawa, Tomoya Shiro, Takaaki Sumiyoshi, Mari Itoh