The Additional Hetero Ring Is Five-membered Patents (Class 546/283.4)
-
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
-
Publication number: 20090176837Abstract: Disclosed herein are novel compounds with activity at RAR? 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.Type: ApplicationFiled: July 12, 2006Publication date: July 9, 2009Applicant: SONY CORPORATIONInventors: Roger Olsson, Fabrice Piu, Birgitte Lund
-
Publication number: 20090105306Abstract: The present invention relates compounds of formula (I) wherein A and R1 are as defined in the specification, pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions.Type: ApplicationFiled: October 7, 2008Publication date: April 23, 2009Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Jennifer Frost, Teodozyj Kolasa, Bo Liu, Steven P. Latshaw, Xueqing Wang
-
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
-
Patent number: 7507754Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: August 14, 2007Date of Patent: March 24, 2009Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
-
Patent number: 7498358Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.Type: GrantFiled: December 13, 2002Date of Patent: March 3, 2009Assignee: Exelixis, Inc.Inventors: S. David Brown, Lynne Canne-Bannen, Erick Wang Co, Vasu Jammalamadaka, Rickard George Khoury, Moon Hwan Kim, Donna T. Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, John M. Nuss, Michael P. Prisbylla, Wei Xu
-
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
-
Publication number: 20080280952Abstract: The present invention relates to novel pyridine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.Type: ApplicationFiled: February 1, 2005Publication date: November 13, 2008Inventors: Gerard Martin Paul Giblin, Karamjit Singh Jandu, William Leonard Mitchell, Ian David Wall
-
Publication number: 20080274891Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as herbicides.Type: ApplicationFiled: May 23, 2008Publication date: November 6, 2008Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Luthy, Jurgen Schaetzer
-
Patent number: 7446106Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.Type: GrantFiled: September 5, 2002Date of Patent: November 4, 2008Assignee: SmithKline Beecham plcInventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
-
Patent number: 7396936Abstract: In various aspects, the present invention relates to non-peptidic compounds, which modulate calcitonin and amylin receptor activity; to processes for the preparation of some such compounds; and to pharmaceutical compositions including such compounds. Compounds of the invention are useful as calcitonin and/or amylin agonists and in the treatment of bone diseases and metabolic diseases.Type: GrantFiled: November 9, 2005Date of Patent: July 8, 2008Assignee: Kemia, Inc.Inventors: Kent Pryor, Jan Urban, Lubomir Sebo, Stephen Miller, Nancy Delaet
-
Patent number: 7375105Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.Type: GrantFiled: September 5, 2002Date of Patent: May 20, 2008Assignee: SmithKline Beecham p.l.c.Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
-
Patent number: 7345059Abstract: The invention relates to 5,6-diphenylpyridine-3-carboxamide derivatives of general formula (I): where: R1 represents hydrogen or a (C1-C4)alkyl; R2 represents: a monoazo saturated heterocycle of 5 to 7 atoms, the nitrogen atom being substituted with a (C1-C4)alkanoyl; NR10R11; a nonaromatic (C3-C10) carbocycle more than tri-substituted with (C1-C4)alkyl; a nonaromatic (C11-C12) carbocycle unsubstituted or mono- or polysubstituted with (C1-C4)alkyl; a monooxygenated saturated heterocycle with 5 to 7 atoms, more than tri-substituted with (C1-C4)alkyl; or R1 and R2, together with the nitrogen atom to which the above are bonded, form a 4-disubstituted piperidin-1-yl group; the salts, solvates and hydrates thereof. The invention further relates to a method for production and therapeutic application thereof.Type: GrantFiled: December 22, 2005Date of Patent: March 18, 2008Assignee: Sanofi-AventisInventors: Francis Barth, Laurent Hortala, Murielle Rinaldi-Carmona
-
Patent number: 7332608Abstract: The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).Type: GrantFiled: November 9, 2006Date of Patent: February 19, 2008Assignee: SANOFI-AVENTIS Deutschland GmbHInventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
-
Publication number: 20080027056Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: ApplicationFiled: July 24, 2007Publication date: January 31, 2008Inventors: Michael F. Parker, Joanne J. Bronson, Mark V. Silva, Kevin W. Gillman
-
Patent number: 7297694Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.Type: GrantFiled: September 5, 2002Date of Patent: November 20, 2007Assignee: SmithKline Beechum P.L.C.Inventors: David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson
-
Patent number: 7235690Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).Type: GrantFiled: April 26, 2002Date of Patent: June 26, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
-
Patent number: 7214678Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 1, 2006Date of Patent: May 8, 2007Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
-
Patent number: 7205305Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: July 17, 2003Date of Patent: April 17, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W Bemis, Francesco G Salituro, John P Duffy, John E Cochran, Edmund M Harrington, Mark A Murcko, Keith P Wilson, Michael Su, Vincent P Galullo
-
Patent number: 7196089Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: January 29, 2004Date of Patent: March 27, 2007Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
-
Patent number: 7169798Abstract: The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described below. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: February 13, 2004Date of Patent: January 30, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Guy Bemis, Anne-Laure Grillot, Mark Ledeboer, Francesco G. Salituro, Edmund Harrington, Huai Gao, Christopher Baker, Jingrong Cao, Michael Hale
-
Patent number: 7109220Abstract: The present invention provides amino substituted pyridinyl methanone compounds; pharmaceutical compositions comprising the compounds and methods of synthesis thereof. The compounds, which are cyclin dependent kinase (CDK) inhibitors, can be used to treat or ameliorate CDK mediated disorders. The invention thus also provides the therapeutic or prophylactic use of the compounds and/or pharmaceutical compositions to treat such disorders.Type: GrantFiled: November 4, 2004Date of Patent: September 19, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Ronghui Lin, Steven K. Wetter, Yanhua Lu, Peter J. Connolly, Stuart Emanuel, Robert H. Gruninger, Steven A. Middleton
-
Patent number: 7087625Abstract: PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formulas I–III: wherein A, B, D, R1, R2, R3, R7, R8, R9, R10 and R6are as defined herein.Type: GrantFiled: November 19, 2003Date of Patent: August 8, 2006Assignee: Memory Pharmaceuticals CorporationInventors: Richard A. Schumacher, Elizabeth Doorly Graham, Allen T. Hopper, Ashok Tehim
-
Patent number: 7067540Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.Type: GrantFiled: February 14, 2003Date of Patent: June 27, 2006Assignee: Pharmacia CorporationInventors: Balekudru Devadas, John Walker, Shaun R. Selness, Terri L. Boehm, Richard C. Durley, Rajesh Devraj, Brian S. Hickory, Paul V. Rucker, Kevin D. Jerome, Heather M. Madsen, Edgardo Alvira, Michele A. Promo, Radhika M. Blevis-Bal, Laura D. Marruto, Jeff Hitchcock, Thomas Owen, Win Naing, Li Xing, Huey S. Shieh, Aruna Sambandam, Shuang Liu, Ian L. Scott, Kevin F. McGee
-
Patent number: 7041702Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 20, 1998Date of Patent: May 9, 2006Assignee: Scion Pharmaceuticals, Inc.Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
-
Patent number: 7015320Abstract: The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) process, comprising: contacting a compound of formula (II): with hydrogen under a suitable pressure in the presence of an iridium complex of the formula (R2)IrL+X? wherein L is a chelating diene, X is a non coordinating anion, and R2 is selected fromType: GrantFiled: March 18, 2003Date of Patent: March 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: William A. Nugent, Tai Yue
-
Patent number: 6995179Abstract: Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel such as encephalopathies caused by the ischemia in the acute phase after the onset of cerebral infarction, cerebral hemorrhage or the like, Alzheimer's disease, etc.Type: GrantFiled: December 13, 2001Date of Patent: February 7, 2006Assignee: Ajinomoto Co., Inc.Inventors: Hisayuki Uneyama, Seiji Niwa, Tomoyuki Onishi
-
Patent number: 6989397Abstract: The present invention provides 2-pyridylcarboxaldehyde isonicotinoyl hydrazone (PCIH) analogues suitable for use as an in vivo iron chelators, the PCIH analogue having Formula 1: wherein R1 is an aromatic or heterocyclic group and R2 is either H or OH; isomers thereof or salts thereof; pharmaceutical compositions containing the analogues; and uses of the analogues in the treatment of iron-overload diseases.Type: GrantFiled: September 4, 2000Date of Patent: January 24, 2006Assignees: University of Queensland, The Heart Research Institute Ltd.Inventors: Des Richardson, Paul Vincent Bernhardt, Erika Michelle Becker
-
Patent number: 6939867Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with ?-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseasesType: GrantFiled: February 28, 2002Date of Patent: September 6, 2005Assignee: Pfizer Inc.Inventors: Robert L. Dow, Ernest S. Paight
-
Patent number: 6927225Abstract: The present invention relates to compounds of Formula I: wherein: represents a 6-membered heterocyclic aromatic ring in which X1 is N, and X2, X3 and X4 are CR?; wherein R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORz in which Rz is H or C1-C3 alkyl; and c) A represents (i) C2-C14 alkenyl, or C2-C14 alkynyl, all of which may be branched or unbranched, unsubstituted or substituted with halogen, hydroxy, nitro, aroyl, aryloxy, C1-C8 acyloxy, C1-C6 alkylthio, arylthio, aryl, heteroaryl, heteroarylthio, heteroaryloxy, C1-C6 acyl, C1-C6 haloalkyl, C1-C6 alkoxy or C1-C6 haloalkoxy, and (ii) C3-C14 cycloalkyl, containing 0 heteroatoms and 0-2 unsaturations, substituted with aryloxy, heteroaryloxy, C1-C6 alkylthio, aType: GrantFiled: December 2, 2002Date of Patent: August 9, 2005Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison
-
Patent number: 6906089Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2 and R3 are various substituent groups; and one of X1 and X2 is N or CR?, and the other is NR? or CHR? wherein R? is hydrogen, OH, C1-6alkyl, or C3-7cycloalkyl; or when one of X1 and X2 is N or CR? then the other may be S or O; and their use as pharmaceuticals.Type: GrantFiled: March 26, 2001Date of Patent: June 14, 2005Assignee: SmithKline Beecham CorporationInventors: Laramie Mary Gaster, John David Harling
-
Patent number: 6903132Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.Type: GrantFiled: June 11, 2003Date of Patent: June 7, 2005Assignees: Agouron Pharmaceuticals, Inc., Pfizer Inc.Inventors: Mark B. Anderson, Lance Christopher Christie, Quyen-Quyen Thuy Do, Jun Feng, Yufeng Hong, Haitao Li, Ved P. Pathak, Ranjan Jagath Rajapakse, Eric T. Sun, Eileen Valenzuela Tompkins
-
Patent number: 6900210Abstract: The present invention provides novel heterocyclic amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A, B and Z are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said heterocyclic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: May 31, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Li-Qiang Sun, Jie Chen, Huan He
-
Patent number: 6875768Abstract: Heterocyclic amine derivatives represented by general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Q represents an optionally substituted heterocycle containing O, S or N; X represents halogeno, cyano, halo(C1-6)alkyl, etc.; n is from 1 to 4; and Z1 and Z2 represent each O or S; and intermediates thereof represented by the following general formula (IV?): Q?—NH2 wherein Q? represents a definite heterocycle selected from among those represented by Q. Agricultural/horticultural insecticides having a remarkable effect of controlling pest insects of crops such as rice, fruit trees and vegetables, as well as various agricultural, forestry, horticultural and stored grain pest insects.Type: GrantFiled: July 4, 2000Date of Patent: April 5, 2005Assignee: Nihon Nohyako Co., Ltd.Inventors: Kouzou Machiya, Kazuyoshi Endoh, Takashi Furuya, Hayami Nakao, Makoto Gotoh, Eiji Kohno, Masanori Tohnishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
-
Patent number: 6828332Abstract: The present invention provides compounds of formula (I) and a method of inhibiting the reuptake of serotonin and antagonizing the serotonin receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula (I).Type: GrantFiled: February 27, 2002Date of Patent: December 7, 2004Assignee: Eli Lilly and CompanyInventors: Daniel Timothy Kohlman, Sidney Xi Liang, Yao-Chang Xu
-
Publication number: 20040192689Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine or cardiac hypertrophy.Type: ApplicationFiled: March 4, 2004Publication date: September 30, 2004Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
-
Patent number: 6797712Abstract: Compounds of formula I, or a pharmaceutically acceptable salt thereof, The compounds of the present invention are suitable for the treatment of pain and migraine. Also disclosed are method for preparing the compounds, and pharmaceutical composition comprising the compounds as well as methods for treating pain and migraine using the pharmaceutical compositions.Type: GrantFiled: May 30, 2003Date of Patent: September 28, 2004Assignee: Gruenenthal GmbHInventors: Corinna Maul, Werner Englberger, Michael Przewosny
-
Patent number: 6784137Abstract: 4-Aminopicolinic acids having aryl or heteroaryl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: July 30, 2002Date of Patent: August 31, 2004Assignee: Dow AgroSciences LLCInventors: Terry William Balko, Ann Marie Buysse, Jeffrey Brian Epp, Stephen Craig Fields, Christian Thomas Lowe, Renee Joan Keese, John Sanders Richburg, III, James Melvin Ruiz, Monte Ray Weimer, Renard Antonio Green, Roger Eugene Gast, Kristy Bryan, Nicholas Martin Irvine, William Chi-Leung Lo, William Kirkland Brewster, Jeffery Dale Webster
-
Publication number: 20040157890Abstract: A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof, for the treatment of a hPPAR mediated disease or condition.Type: ApplicationFiled: March 23, 2004Publication date: August 12, 2004Inventors: Paul John Beswick, Christopher Charles Hamlett, Vipulkumar Patel, Michael Lawrence Sierra, Nigel Grahame Ramsden
-
Publication number: 20040127518Abstract: Fatty acid amide hydrolase inhibitors of the Formula: 1Type: ApplicationFiled: October 7, 2003Publication date: July 1, 2004Applicant: The Regents of the University of CaliforniaInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
-
Publication number: 20040073029Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I: 1Type: ApplicationFiled: April 9, 2003Publication date: April 15, 2004Inventors: James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
-
Patent number: 6716987Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z representsType: GrantFiled: December 20, 2001Date of Patent: April 6, 2004Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
-
Publication number: 20040029923Abstract: Disclosed are a novel organic acid salt of amlodipine with superb physicochemical properties, its preparation method, and a pharmaceutical composition containing the same as a therapeutically active ingredient.Type: ApplicationFiled: July 29, 2003Publication date: February 12, 2004Applicant: CJ CorporationInventors: Seong Hwan Cho, Yong Sik Youn, Yun Taek Jung, Choong Sil Park, Hyuk Koo Lee, Kwang Hyeg Lee, Eun Ju Jeong, Young Hoon Kim, Hae Tak Jin, Jun Hee Cheon, Sung Hak Lee, Sung Hak Jung, Dong Kwon Lim, Kyu Jeong Yeon, Yun Cheul Kim, Kyung Mi Park, Hyun Suk Kang
-
Publication number: 20040019217Abstract: This invention relates to dihydroxyhexanoic acid derivatives and their intermediates, as well as to methods of preparing such compounds. Additionally, present invention relates to removing a protecting group from a protected amine wherein the method comprises reacting the protected amine with phosphoric acid.Type: ApplicationFiled: May 7, 2003Publication date: January 29, 2004Applicant: Pfizer Inc.Inventors: John C. Kath, Zhengong B. Li, V. John Jasys, Frank J. Urban
-
Patent number: 6680329Abstract: Compounds of formula [I] in which: W may represent a —(CH2)2—, —(CH2)3—, —CH2—C≡C— or —CH2—CH═CH— group, R2 may in particular represent a piperidyl group, an optionally substituted 1,2,3,6-tetrahydropyridyl group, a hexahydro-1H-azepinyl group, an optionally substituted piperazinyl group or a morpholinyl group, R3 may in particular represent a group —COR1, A may in particular represent an optionally substituted phenyl group, a heterocycle or a cyclopentyl group, and B may in particular represent a pyridyl group, an aminopyrazinyl group, an aminopyridazinyl group, a pyrimidinyl group optionally substituted with an amino group, piperidyl group or an aminopyridyl group optionally substituted on the pyridine with a (C1-C4)alkyl or (C1-C4)alkoxy group, the amino group possibly also being substituted with a (C1-C4)alkyl group, their preparation and their therapeutic application.Type: GrantFiled: September 12, 2002Date of Patent: January 20, 2004Assignee: Sanofi-SynthelaboInventors: Jean-Michel Altenburger, Gérard Cremer, Gilbert Lassalle, Mostafa Matrougui
-
Patent number: 6653302Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted; R4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.Type: GrantFiled: December 13, 2002Date of Patent: November 25, 2003Assignee: Pfizer Inc.Inventor: David Nathan Abraham Fox
-
Patent number: 6649633Abstract: This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is —O—; or —S(═O)t—, where t is 0, 1, or 2; Y is —C(R1a); Q1 is phenyl or substituted phenyl; Q2 is biphenyl or substituted biphenyl; and the remaining variables are defined as set forth in the specification. This application is also directed to pharmaceutical compositions comprising those compounds and to methods of treating diseases regulated by the activation and degranulation of eosinophils, in particular asthma, chronic bronchitis and chronic obstructive pulmonary disease.Type: GrantFiled: January 31, 2002Date of Patent: November 18, 2003Assignee: Pfizer IncInventors: Robert J. Chambers, Anthony Marfat, Thomas V. Magee
-
Publication number: 20030203943Abstract: The present invention relates to a chemical composition comprising a pyridine carboxy derivative and an H2 histamine receptor antagonist and a pharmaceutical composition or a dietary supplement comprising a pyridine carboxy derivative and an H2 histamine receptor antagonist and to the use of such compositions for the preparation of a medicament or a dietary-supplement for immunomodulation in a mammal and the suppression of hypersensitivity and/or inflammatory reaction.Type: ApplicationFiled: May 5, 2003Publication date: October 30, 2003Applicant: Astion Development Aps.Inventor: Morten Sloth Weidner
-
Publication number: 20030191118Abstract: The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O— -(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur; W is oxygen, sulfur, —CH═CH—, —NH— or —N═CH—; R1, R2 and R3 are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl gorup, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl, etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.Type: ApplicationFiled: November 4, 2002Publication date: October 9, 2003Applicant: Tanabe Seiyaku Co., Ltd.Inventors: Ila Sircar, Kristjan S. Gudmundsson, Richard Martin
-
Publication number: 20030153602Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders.Type: ApplicationFiled: December 27, 2002Publication date: August 14, 2003Applicant: G.D. Searle & Co.Inventors: John J. Talley, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Roland S. Rogers