The Additional Hetero Ring Is Five-membered Patents (Class 546/280.4)
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Publication number: 20090192175Abstract: Novel heteroaromatic compounds of formula (I): wherein A1, A2, A3, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: April 25, 2007Publication date: July 30, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Pierre Jung, Patricia Durieux, William Lutz, Peter Maienfisch, Thomas Pitterna, Peter Renold, Werner Zambach
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Patent number: 7560563Abstract: The present invention provides a method of producing a pyridine derivative having a substituent at the 2-position of a heterocyclic structure conveniently and with fine selectivity. The present invention relates to a production method of a pyridine derivative having a substituent at the 2-position of a heterocyclic structure, which is represented by the formula (III), which includes reacting a 2-sulfonylpyridine derivative of the formula (I) with an organometallic compound of the formula (II) and the like, and the like: wherein each symbol is as defined in the Description.Type: GrantFiled: July 23, 2003Date of Patent: July 14, 2009Assignee: Kuraray Co., Ltd.Inventors: Kenichi Koyakumaru, Yoshimi Fukunaga
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Patent number: 7553798Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: GrantFiled: June 21, 2005Date of Patent: June 30, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Clemens Lamberth, Camilla Corsi, Josef Ehrenfreund, Hans Tobler, Harald Walter
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Patent number: 7550481Abstract: The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: December 15, 2004Date of Patent: June 23, 2009Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Craig A. Coburn, Philippe G. Nantermet, Harold G. Selnick, Shawn J. Stachel, Matthew G. Stanton, Shaun R. Stauffer, Linghang Zhuang, Jennifer R. Davis
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Patent number: 7541472Abstract: Compounds of formula I are described: along with compositions thereof, methods of use thereof (particularly as fungicides), and methods of making the same.Type: GrantFiled: May 24, 2005Date of Patent: June 2, 2009Assignee: Cropsolution, Inc.Inventors: Richard Anderson, Shy-Fuy Lee, Vivian Du, Takeo Hokama, Rafael Oey, Patricia Arakaki
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Publication number: 20090131475Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B—C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.Type: ApplicationFiled: February 1, 2008Publication date: May 21, 2009Applicant: Baylor College of MedicineInventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Qian Mao, Shinji Kamisuki, Akira Kugimiya
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Patent number: 7531535Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: December 13, 2007Date of Patent: May 12, 2009Assignee: Bristol-Meyers Squibb CompanyInventors: Donald J. P. Pinto, Jennifer X. Qiao
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Patent number: 7531655Abstract: There are disclosed a large conductance calcium-activated K channel opener comprising a compound of the formula (I): wherein ring A is a 5-membered heterocyclic ring containing any one of O, N or S, which ring may be substituted by R4, R1 is aryl, heterocyclic or heterocycle-substituted carbonyl; R2 is hydrogen, halogen, carboxy, amino, alkyl, alkoxycarbonyl, alkenyl or cycloalkyl; R3 is aryl, heterocyclic or alkyl; and R4 is hydrogen or alkyl, each of substituents may be substituted, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: October 15, 2003Date of Patent: May 12, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Toshihiro Hosaka, Mari Kusama, Kiyomi Ohba, Rikako Kono, Shuntarou Kohnomi
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Publication number: 20090118286Abstract: Use of heterobicyclic acrylamides of the formula (I) in which A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description, for controlling pests, novel heterobicyclic acrylamides and processes for preparing these compounds, and also compounds of the formula (IA) in which A2, R1, R2, R5 and R6 are as defined in the description.Type: ApplicationFiled: February 27, 2006Publication date: May 7, 2009Applicant: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Jurgen Scherkenbeck, Graham Holmwood, Jurgen Wieschemeyer, Peter Losel, Olga Malsam, Mark Wilhelm Drewes, Karl-Heinz Kuck, Ulrike Wachendorf-Neumann, Christian Arnold, Vincent Lee Salgado, Thomas Bretschneider
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Publication number: 20090118506Abstract: The present invention discloses compounds of formula I, II or, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: September 17, 2008Publication date: May 7, 2009Inventors: IN JONG KIM, Tongzhu Liu, Yao-Ling Qiu, Guoqiang Wang, Jiang Long, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
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Publication number: 20090105280Abstract: Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning —X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: ApplicationFiled: September 20, 2006Publication date: April 23, 2009Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Ewald M. Aydt, Remo Kranich
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Publication number: 20090105279Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: April 23, 2009Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Patent number: 7521473Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.Type: GrantFiled: February 23, 2005Date of Patent: April 21, 2009Assignee: WyethInventors: Jinbo Lee, Zhao-Kui Wan, Douglas P. Wilson, Bruce C. Follows, Steven J. Kirincich, Michael J. Smith, Jun-Jun Wu, Kenneth W. Foreman, David V. Erbe, Yan-Ling Zhang, Weixin Xu, Steve Y. Tam
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Patent number: 7517893Abstract: Novel dicationic bichalcophene compounds are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.Type: GrantFiled: May 16, 2006Date of Patent: April 14, 2009Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: Richard R. Tidwell, David W. Boykin, Chad Stephens, Mohamed A. Ismail, W. David Wilson, Reto Brun, Karl Werbovetz
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Publication number: 20090069382Abstract: There is provided a compound of formula I, wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: ApplicationFiled: April 12, 2006Publication date: March 12, 2009Inventors: Mathias Alterman, Anders Hallberg, Murugaiah Andappan Murugaiah Subbaiah
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Publication number: 20090043096Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).Type: ApplicationFiled: February 2, 2007Publication date: February 12, 2009Applicants: SUMITOMO CHEMICAL COMPANY, LIMITED, OSAKA UNIVERSITYInventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
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Patent number: 7488824Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein the substituents are as defined in claim 1, by reaction of a compound of formula (II) wherein R3 is C1-C8alkyl or C3-C6cycloalkyl and R4 and R05 are as defined for formula (I), with a compound of formula (III) wherein R, R1, R2 and X1, are as defined for formula (I) in claim 1, in an inert solvent in the presence of a proton source.Type: GrantFiled: March 5, 2004Date of Patent: February 10, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: David Anthony Jackson, Martin Charles Bowden
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Patent number: 7482366Abstract: Compounds of the invention, such as compounds of formula (I): where n, m, A, B, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: GrantFiled: July 24, 2004Date of Patent: January 27, 2009Assignee: X-Ceptor Therapeutics, Inc.Inventors: Christopher D Bayne, Alan T Johnson, Shao-Po Lu, Raju Mohan, Michael C Nyman, Edwin J Schweiger, William C Stevens, Jr., Haixia Wang, Yinong Xie
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Publication number: 20090023781Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: December 1, 2005Publication date: January 22, 2009Applicant: Virobay, Inc.Inventor: Eduardo L. Setti
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Patent number: 7479500Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: June 1, 2005Date of Patent: January 20, 2009Assignee: WyethInventors: Michael Byron Webb, Gary Paul Stack, Magda Asselin, Deborah Ann Evrard
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Publication number: 20090018169Abstract: This present invention is related to sulfonamide derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of bacterial infections such as tuberculosis.Type: ApplicationFiled: February 9, 2007Publication date: January 15, 2009Applicant: Laboratoires Serono SAInventors: Jerome Gonzalez, Dominique Swinnen, Agnes Bombrun, Rob Hooft Van Huijsduijnen, Timothy Wells
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Publication number: 20090018168Abstract: Disclosed herein is a compound having a formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: April 29, 2008Publication date: January 15, 2009Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20090012127Abstract: Compounds of Formula (I) wherein E, A and R1 are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: June 26, 2006Publication date: January 8, 2009Applicant: ASTRAZENECA ABInventors: Thomas R. Simpson, Michael Balestra, Dean G. Brown, Cathy L. Dantzman, Glen E. Ernst, William Frietze, Christopher R. Holmquist, James Kang, Frances M. McLaren, Reed W. Smith, JR., James M. Woods
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Patent number: 7468360Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.Type: GrantFiled: August 8, 2007Date of Patent: December 23, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20080293716Abstract: There is provided a compound of Formula (I) or a salt, solvate, or physiologically functional derivative thereof:Type: ApplicationFiled: January 28, 2005Publication date: November 27, 2008Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: David Harold Drewry, Robert Neil Hunter, III, David Kendall Jung, James Andrew Linn, Clark Sehon, Robert A. Stavenger
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Patent number: 7446195Abstract: Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.Type: GrantFiled: August 16, 2006Date of Patent: November 4, 2008Assignee: Schering CorporationInventors: Yongqi Deng, Lianyun Zhao, Gerald W. Shipps, Jr., Patrick J. Curran, M. Arshad Siddiqui, Rumin Zhang, Charles W. McNemar, Todd W. Mayhood, William T. Windsor, Emma M. Lees, David A. Parry
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Publication number: 20080269283Abstract: Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: ApplicationFiled: June 27, 2008Publication date: October 30, 2008Inventors: Pingchen Fan, Hiroyuki Goto, Xiao He, Makoto Kukutani, Marc Labelle, Dustin L. McMinn, Jay P. Powers, Yosup Rew, Daqing Sun, Xuelei Yan
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Publication number: 20080269265Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: June 25, 2008Publication date: October 30, 2008Inventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, David Gunn, Martha Rodriguez, Ming Wang, Tiffany Turner, Catherine Brennan
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Patent number: 7442702Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: September 25, 2002Date of Patent: October 28, 2008Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Publication number: 20080261994Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: ApplicationFiled: January 18, 2008Publication date: October 23, 2008Inventors: Takashi INABA, Julia Hass, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Publication number: 20080255108Abstract: Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. Said compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are defined in the specification, as are A Z, Q, R1 and R2.Type: ApplicationFiled: April 3, 2008Publication date: October 16, 2008Inventors: Nalin L. Subasinghe, Shelley Ballentine, Jeremy M. Travins, Ehab M. Khalil, Farah Ali, Kristi A. Leonard, Joan M. Gushue, Michael Peter Winters, Heather Hufnagel, Maxwell David Cummings
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Publication number: 20080214394Abstract: N-(4-Pyridyl)methylsulfonamides for combating arthropodal pests The present invention relates to the use of N-(4-pyridyl)methylsulfonamides of the formula for combating arthropodal pests (harmful arthropodes) and for protecting materials against infestation and/or destruction by said pests: (I) where the substituents are as follows: R1 is hydrogen, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, C2-C4-alkynyl or benzyl; R2, R3, R4, R5 independently of one another are hydrogen, halogen, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkoxy or C1-C4-haloalkyl; R2 and R3 or R4 and R5 together with the carbon atoms to which they are attached may also form a condensed 5- or 6-membered hydro-carbon ring, it being possible for the hydrocarbon ring to carry one or two groups R2?, R3?, R2?, R3? independently of one another are halogen, C1-C4-alkyl, C1-C4-alkoxy, halomethoxy or halomethyl; X is a cyclic radical selected from phenyl, naphthyl and five- or six-membered saturated, partially unsaturated or aromatic heterocycles, the heterType: ApplicationFiled: March 15, 2006Publication date: September 4, 2008Applicant: BASF AktiengesellschaftInventors: Michael Puhl, Christopher Koradin, Joachim Rheinheimer, Wassilios Grammenos, Jan Klaas Lohmann, Ernst Baumann, Wolfgang von Deyn, Jurgen Langewald, Norbert Gotz, Douglas D. Anspaugh, Deborah L. Culbertson, Henry Van Tuyl Cotter, Hassan Olumi-Sadeghi
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Patent number: 7417150Abstract: The present application relates to novel heterocyclic compounds, to processes for their preparation, and to their use as crop protection agents, particularly for controlling animal pests.Type: GrantFiled: April 10, 2002Date of Patent: August 26, 2008Assignee: Bayer CropScience AGInventors: Peter Jeschke, Michael Beck, Wolfgang Krämer, Detlef Wollweber, Angelika Lubos-Erdelen, legal representative, Andreas Turberg, Olaf Hansen, Hans-Dieter Martin, Piet Sauer, Christoph Erdelen
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Publication number: 20080200513Abstract: The present invention relates to pyridinone derivatives of formula (I): wherein Z represents C2-6 alkynyl, aryl or heteroaryl, any of which groups may be optionally substituted, and R1 represents hydrogen, C1-6 alkyl, C3-7 heterocycloalkyl(C1-6)alkyl, di(C1-6)alkylamino(C1-6)alkyl, C2-6 alkylcarbonyloxy(C1-6)alkyl or C3-7 cycloalkoxycarbonyloxy(C1-6)alkyl, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C virus infections.Type: ApplicationFiled: June 1, 2004Publication date: August 21, 2008Applicant: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPAInventors: Stafania Colarusso, Frank Narjes
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Patent number: 7414060Abstract: The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.Type: GrantFiled: February 23, 2006Date of Patent: August 19, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Publication number: 20080188527Abstract: Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.Type: ApplicationFiled: December 10, 2004Publication date: August 7, 2008Inventor: John R. Cashman
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Patent number: 7396944Abstract: Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: June 13, 2005Date of Patent: July 8, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Georg Fertig, Frank Herting, Matthias Koerner, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Ulrich Tibes
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Patent number: 7393865Abstract: Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.Type: GrantFiled: June 17, 2005Date of Patent: July 1, 2008Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Wilna (Willy) J Moree, Florence Jovic, Timothy Coon, Jinghua Yu
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Patent number: 7388018Abstract: Sulfonamides of the formula I where the substituents are as follows: R1 is hydrogen, alkyl, alkoxy, alkenyl or alkynyl; and R2, R3, R4, R5 are hydrogen, halogen, alkyl, alkoxy or halomethyl; R2 and R3 together may also form a phenyl, cyclopentyl or cyclohexyl ring, it being possible for these rings to carry two groups R2, and R3, R2, R3, are hydrogen, halogen, alkyl, alkoxy or halomethyl; in case a), if R2, R3, R4 and R5 are hydrogen: X is phenyl substituted by a group —C(R6)?NOR7, where R6 is alkyl and R7 is alkyl, benzyl, alkenyl, haloalkyl, haloalkenyl, alkynyl or haloalkynyl; and in case b), if at least one of the groups R2, R3, R4 and R5 is not hydrogen: X is phenyl, naphthyl or a five- or six-membered saturated, or partially unsaturated or aromatic heterocycle which is attached via a carbon atom and contains one to four heteroatoms from the group consisting of O, N and S, where X may be substituted according to the description; Processes for preparing these compounds, compositions comprisiType: GrantFiled: September 10, 2004Date of Patent: June 17, 2008Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Carsten Blettner, Bernd Müller, Markus Gewehr, Jordi Tormo i Blasco, Thomas Grote, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Oliver Wagner, Norbert Götz, Siegfried Strathmann, Ulrich Schöfl, Maria Scherer, Reinhard Stierl
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Publication number: 20080119488Abstract: Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: July 24, 2005Publication date: May 22, 2008Applicant: EXELIXIS, INC.Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Haixia Wang, Yinong Xie, Lynne Canne Bannen, Diva Sze-Ming Chan, Ping Huang, Vasu Jammalamadaka, Richard G. Khoury, Morrison B. Mac, Jason Jevious Parks, Yong Wang, Wei Xu
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Publication number: 20080108665Abstract: Methods to control certain invertebrates including insects in agricultural, urban, animal health, and industrial systems by directly or systemically applying to a locus where control is desired an effective amount of a compound of N-substituted sulfoximines.Type: ApplicationFiled: February 9, 2007Publication date: May 8, 2008Inventors: Jim X. Huang, Yuanming Zhu, Richard B. Rogers, Michael R. Loso, Robert L. Hill, James D. Thomas, Thomas Meade, James M. Gifford, Joseph J. DeMark, Benjamin M. Nugent
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Patent number: 7365070Abstract: This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.Type: GrantFiled: December 4, 2003Date of Patent: April 29, 2008Assignee: Ore Pharmaceuticals Inc.Inventors: Tricia J. Vos, Michael Patane, Michael E. Solomon, Christopher Blackburn, Mihaela D. Danca
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Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Publication number: 20080064874Abstract: Novel 2-halofuryl/thienyl-3-carboxamides of the formula (I) in which A, Hal, R, M and Z are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: January 22, 2005Publication date: March 13, 2008Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jorg Nico Greul, Benoit Hartmann, Peter Dahmen, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann
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Publication number: 20080015231Abstract: A compound having a formula is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: July 10, 2007Publication date: January 17, 2008Inventors: David W. Old, Vinh X. Ngo
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Patent number: 7297797Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.Type: GrantFiled: September 8, 2003Date of Patent: November 20, 2007Assignee: Bayer CropScience AGInventors: Johannes Rudolf Jansen, Udo Kraatz, Hubertus Stakemeier, Thomas Seitz, Fritz Maurer, Martin Füsslein, Bernd Alig, Christian Funke, Werner Hallenbach, Jörg Konze, Udo Beckmann, Ulrich Görgens
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Patent number: 7279470Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.Type: GrantFiled: December 13, 2002Date of Patent: October 9, 2007Assignee: Novo Nordisk A/SInventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
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Patent number: 7259172Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 2, 2004Date of Patent: August 21, 2007Assignee: MethylGene Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 7256203Abstract: A compound of Formula (I): wherein: X is selected from the group consisting of O, S, and NR17, where R17 is hydrogen or lower alkyl; A and Y are CH, N, NR17, O, or S; C1 and C2 are each C or N, wherein C1 and C2 are the same or different; D1 and D2 are each C or N, wherein D1 and D2 are the same or different; B and Z are CH, N, or NR17, provided that B, Z, or both B and Z are not present when A, Y, or both A and Y are O, S, or NR17; R13, R14, R1 and R8 can be present or absent, and when present are selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R15 and Rare selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R3 and R6 are each independently selected from the group consisting of H, hydroxy, lower alkyl, cycloalkyl, aryl, aralkyl, alkoxyl, hydroxycycloalkyl, alkoxycycloalkyl, hydroxyalkyl, aminoalkyl, acyloxy, acetoxy, and alkylaminoalkyl; and R2, R4, R5 and R7 are each independently selected frType: GrantFiled: November 25, 2003Date of Patent: August 14, 2007Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, Richard R. Tidwell, Mohamed A. Ismail, Reto Brun