Benzene Ring Bonded Directly To The Diazole Ring Patents (Class 548/325.5)
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Patent number: 9156794Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: December 11, 2013Date of Patent: October 13, 2015Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Zhenjian Du, Kevin Paul Foley
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Patent number: 9034888Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R7, R6, R7, R8, R9, A, X and Y as defined herein are provided as useful for the treatment of cancer or for the manufacture of anti-cancer agents.Type: GrantFiled: February 16, 2011Date of Patent: May 19, 2015Assignee: Universite LavalInventors: René C. Gaudreault, Sébastien Fortin
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Patent number: 8889874Abstract: The present invention provides Chalcone linked Imidazolone compounds of formula A as anti cancer agent against fifty three human cancer cell lines.Type: GrantFiled: December 14, 2010Date of Patent: November 18, 2014Assignee: Council of Scientific and Industrial ResearchInventors: Kamal Ahmed, Ramakrishna Gadupudi, Balakishan Gorre, Raju Paidakula, Viswanath Arutla, Balakrishna Moku
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Publication number: 20140323519Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).Type: ApplicationFiled: April 20, 2012Publication date: October 30, 2014Applicant: MERCK SHARP & DOHME CORP.Inventors: M. Arshad Siddiqui, Lianyun Zhao, Amit K. Mandal
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Publication number: 20140315968Abstract: Compounds of formula (I) wherein R1, R4, R8, X and Y as defined herein are provided as useful for the inhibition of certain types of cancer cells, amongst others, breast cancer cells, or for the manufacture of anti-cancer agents.Type: ApplicationFiled: August 10, 2012Publication date: October 23, 2014Applicant: UNIVERSITE LAVALInventors: Rene C.-Gaudreault, Sebastien Fortin
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Publication number: 20140221383Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: April 14, 2014Publication date: August 7, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallet, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
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Patent number: 8629285Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: August 10, 2006Date of Patent: January 14, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
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Publication number: 20130210769Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Patent number: 8455530Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.Type: GrantFiled: March 2, 2012Date of Patent: June 4, 2013Assignee: Theravance, Inc.Inventors: Robert S. Chao, Weijiang Zhang
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Publication number: 20130123315Abstract: The present invention relates to compounds of the general structure shown in Formula (A): (A): and includes pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: July 8, 2011Publication date: May 16, 2013Inventors: Duane DeMong, Michael W. Miller, Xing Dai, Andrew Stamford
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Publication number: 20130066081Abstract: The present invention provides Chalcone linked Imidazolone compounds of formula A as anti cancer agent against fifty three human cancer cell lines.Type: ApplicationFiled: December 14, 2010Publication date: March 14, 2013Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Kamal Ahmed, Ramakrishna Gadupudi, Balakishan Gorre, Raju Paidakula, Viswanath Arutla, Balakrishna Moku
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Publication number: 20120309777Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R7, R6, R7, R8, R9, A, X and Y as defined herein are provided as useful for the treatment of cancer or for the manufacture of anti-cancer agents.Type: ApplicationFiled: February 16, 2011Publication date: December 6, 2012Applicant: UNIVERSITE LAVALInventors: René C. Gaudreault, Sébastien Fortin
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Publication number: 20120252699Abstract: The present invention relates to novel fluorophores and their use in combination with novel nucleic acid molecules, called aptamers, that bind specifically to the fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.Type: ApplicationFiled: February 18, 2010Publication date: October 4, 2012Applicant: CORNELL UNIVERSITYInventors: Samie R. Jaffrey, Jeremy S. Paige
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Patent number: 8158659Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: December 21, 2010Date of Patent: April 17, 2012Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Patent number: 8153675Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S) -2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2 -carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.Type: GrantFiled: November 11, 2010Date of Patent: April 10, 2012Assignee: Theravance, Inc.Inventors: Robert S. Chao, Weijiang Zhang
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Publication number: 20120083500Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Inventors: Li CHEN, Michael Patrick DILLON, Lichun FENG, Minmin YANG
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Patent number: 8129423Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.Type: GrantFiled: October 12, 2007Date of Patent: March 6, 2012Assignee: Hoffman-La Roche Inc.Inventors: Jean Ackermann, Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart, Tadakatsu Takahashi
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Patent number: 8124318Abstract: It is disclosed an over-coating agent for forming fine patterns which is applied to cover a substrate having thereon photoresist patterns and allowed to shrink under heat so that the spacing between adjacent photoresist patterns is lessened, with the applied film of the over-coating agent being removed substantially completely to form or define fine trace patterns, further characterized by containing either a water-soluble polymer and an amide group-containing monomer or a water-soluble polymer which contains at least (meth)acrylamide as a monomeric component. Also disclosed is a method of forming fine-line patterns using any one of said over-coating agents. According to the invention, the thermal shrinkage of the over-coating agent for forming fine patterns in the heat treatment can be extensively increased, and one can obtain fine-line patterns which exhibit good profiles while satisfying the characteristics required of semiconductor devices.Type: GrantFiled: August 24, 2010Date of Patent: February 28, 2012Assignee: Tokyo Ohka Kogyo Co., Ltd.Inventors: Yoshiki Sugeta, Fumitake Kaneko, Toshikazu Tachikawa
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Patent number: 8022617Abstract: An organic compound having excellent heat resistance, an excellent amorphous nature, an excellent ability to transport charges, highly excited singlet and triplet states, and excellent solubility in an organic solvent is an organic compound represented by Formula (I): wherein Ar1 represents an optionally-substituted aromatic hydrocarbon group, an optionally-substituted aromatic heterocyclic group, or an optionally-substituted alkyl group; Ar2 represents an optionally-substituted aromatic hydrocarbon group or an optionally-substituted aromatic heterocyclic group; R1 and R2 each represent a hydrogen atom or a substituent, and R1 and R2 may be bonded to each other to form a ring; and Q is represented by Formula (I-1) or (I-2): wherein Ar3 to Ar5 each represent an optionally-substituted aromatic hydrocarbon group or an optionally-substituted aromatic heterocyclic group, and Ar3 and Ar4 may be bonded to each other to form a ring.Type: GrantFiled: November 22, 2006Date of Patent: September 20, 2011Assignee: Mitsubishi Chemical CorporationInventors: Koichiro Iida, Yuichiro Kawamura, Tomoyuki Ogata, Masayoshi Yabe, Misako Okabe, Masako Takeuchi, Kazuki Okabe
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Publication number: 20110144160Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: July 2, 2009Publication date: June 16, 2011Applicant: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns
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Publication number: 20110130391Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.Type: ApplicationFiled: December 29, 2010Publication date: June 2, 2011Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
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Publication number: 20110039109Abstract: Activators for heat-curing epoxy resin compositions, as well as use thereof in heat-curing epoxy resin compositions. These activators are distinguished by a good activation effect as well as good storage stability.Type: ApplicationFiled: April 30, 2009Publication date: February 17, 2011Applicant: SIKA TECHNOLOGY AGInventors: Karsten Frick, Ulrich Gerber, Juergen Finter, Andreas Kramer
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Patent number: 7879896Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: April 23, 2008Date of Patent: February 1, 2011Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Patent number: 7855221Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.Type: GrantFiled: September 29, 2009Date of Patent: December 21, 2010Assignee: Theravance, Inc.Inventors: Robert S. Chao, Weijiang Zhang
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Patent number: 7790707Abstract: The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.Type: GrantFiled: March 21, 2007Date of Patent: September 7, 2010Assignee: EPIX Pharmaceuticals Inc.Inventors: Ashis Saha, Xiang Yu, Mercedes Lobera, Jian Lin, Srinivasa R. Cheruku, Oren Becker, Yael Marantz, Nili Schutz
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Patent number: 7745474Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and Y are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino, R3 may be alkoxy and Y may be a thioylamino- or methyl eneamino- linked substitutuent containing an aryl group.Type: GrantFiled: December 21, 2006Date of Patent: June 29, 2010Assignee: AstraZeneca ABInventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson, Maria Saxin
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Publication number: 20100004159Abstract: The present invention relates to polysubstituted imidazolone derivatives, to the pharmaceutical compositions comprising them and to the therapeutic uses thereof in the human and animal health fields. The present invention also relates to a process for preparing these derivatives.Type: ApplicationFiled: July 24, 2007Publication date: January 7, 2010Applicant: GENFITInventors: Edith Bouey, Christophe Masson, Karine Bertrand
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Publication number: 20090284134Abstract: An organic compound having excellent heat resistance, an excellent amorphous nature, an excellent ability to transport charges, highly excited singlet and triplet states, and excellent solubility in an organic solvent is an organic compound represented by Formula (I): wherein Ar1 represents an optionally-substituted aromatic hydrocarbon group, an optionally-substituted aromatic heterocyclic group, or an optionally-substituted alkyl group; Ar2 represents an optionally-substituted aromatic hydrocarbon group or an optionally-substituted aromatic heterocyclic group; R1 and R2 each represent a hydrogen atom or a substituent, and R1 and R2 may be bonded to each other to form a ring; and Q is represented by Formula (I-1) or (I-2): wherein Ar3 to Ar5 each represent an optionally-substituted aromatic hydrocarbon group or an optionally-substituted aromatic heterocyclic group, and Ar3 and Ar4 may be bonded to each other to form a ring.Type: ApplicationFiled: November 22, 2006Publication date: November 19, 2009Applicant: MITSUBISHI CHEMICAL CORPORATIONInventors: Koichiro IIDA, Yuichiro Kawamura, Tomoyuki Ogata, Masayoshi Yabe, Misako Okake, Masako Takeuchi, Kazuki Okabe
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Publication number: 20090209768Abstract: The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.Type: ApplicationFiled: May 14, 2007Publication date: August 20, 2009Inventors: Yasuhiro Saka, Akio Fujii, Kazumi Okuro, Masaru Mitsuda
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Publication number: 20090176773Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.Type: ApplicationFiled: May 18, 2006Publication date: July 9, 2009Applicant: FORSCHUNGSVERBUND BERLIN E.V.Inventors: Enno Klussmann, Walter Rosenthal, Jorg Rademann, Frank Christian, Sina Meyer
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Publication number: 20080275233Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.Type: ApplicationFiled: June 17, 2008Publication date: November 6, 2008Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
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Publication number: 20070292485Abstract: Disclosed are polyol esters comprising a polyol having at least one hydroxyl group esterified to at least one compound having a carboxyl group. Methods of making the polyol ester compounds are also disclosed. The invention also relates to feed compositions comprising polyol ester compounds.Type: ApplicationFiled: June 18, 2007Publication date: December 20, 2007Applicant: Novus International Inc.Inventors: Stephen J. Lorbert, Thomas Frederick Blackburn, Charles S. Schasteen
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Patent number: 7235345Abstract: It is disclosed an over-coating agent for forming fine patterns which is applied to cover a substrate having photoresist patterns thereon and allowed to shrink under heat so that the spacing between the adjacent photoresist patterns is lessened, further characterized by containing a water-soluble polymer and a surfactant. Also disclosed is a method of forming fine-line patterns using the over-coating agent. According to the invention, one can obtain fine-line patterns which exhibit good profiles while satisfying the characteristics required of semiconductor devices, being excellent in controlling the dimension of patterns.Type: GrantFiled: November 5, 2002Date of Patent: June 26, 2007Assignee: Tokyo Ohka Kogyo Co., Ltd.Inventors: Yoshiki Sugeta, Fumitake Kaneko, Toshikazu Tachikawa
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Patent number: 7018430Abstract: The present invention relates to a method of mass-coloring synthetic materials, which comprises using at least one pigment dye of formula (1) wherein R and R1 together form a phenyl or heteroaryl radical and R2 is hydrogen, or R1 and R2 together form a phenyl or heteroaryl radical and R is hydrogen, and the rings A and B may each independently of the other be substituted by C1-C4?alkyl, C1–C4alkoxy, halogen, —COOR3, —CONHR4 and/or by —SR5, wherein R3, R4 and R5 are each independently of the others hydrogen, C1–C4alkyl, C6–C12aryl or heteroaryl, to synthetic materials colored with such pigment dyes, and to novel pigment dyes of formula (3), wherein R6 is hydrogen or bromineType: GrantFiled: July 18, 2002Date of Patent: March 28, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Jean-Marie Adam, Jean-Pierre Bacher
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Patent number: 6858636Abstract: A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein each of R1, R2 and R3 is independently selected from hydrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R1, R2 and R3 must be a substituent other than hydrido, and with the further proviso that when each of R1 and R3 is hydrido, then R2 cannot be chloro; wherein R4 is hydrido; wherein R5 is alkyl; and wherein R6 is tetrazolyl; or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.Type: GrantFiled: August 27, 2003Date of Patent: February 22, 2005Assignee: G.D. Searle & Co.Inventors: David B. Reitz, Robert E. Manning
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Publication number: 20040214827Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: ApplicationFiled: June 5, 2003Publication date: October 28, 2004Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
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Patent number: 6683115Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: August 21, 2001Date of Patent: January 27, 2004Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 6635630Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15; is selected from the group consisting of X2 is —O—, —S— or —NR5—; Y is ═O, ═S or ═NR11; Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15; R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13Type: GrantFiled: June 6, 2002Date of Patent: October 21, 2003Assignee: Schering CorporationInventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
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Patent number: 6630497Abstract: A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein each of R1, R2 and R3 is independently selected from hydrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R1, R2 and R3 must be a substituent other than hydrido, and with the further proviso that when each of R1 and R3 is hydrido, then R2 cannot be chloro; wherein R4 is hydrido; wherein R5 is alkyl; and wherein R6 is tetrazolyl; or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.Type: GrantFiled: April 3, 2001Date of Patent: October 7, 2003Assignee: G.D. Searle & CoInventors: David B. Reitz, Robert E. Manning
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Patent number: 6613789Abstract: A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by Formula V: and pharmaceutically-acceptable salts thereof.Type: GrantFiled: December 5, 2001Date of Patent: September 2, 2003Assignee: G. D. Searle & Co.Inventors: Ish K. Khanna, Richard M. Weier, Paul W. Collins, Yi Yu, Xiangdong Xu, Richard A. Partis, Francis J. Koszyk, Renee M. Huff
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Patent number: 6593497Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: February 14, 2000Date of Patent: July 15, 2003Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Edmund J. Moran
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Patent number: 6562542Abstract: An image-forming material is described, comprising on an support an acid-generating agent selected from a sulfonic acid ester of a specific structure generating an acid by the action of heat and the polymer thereof, and a compound causing a light absorption change in the absorption region of from 350 to 700 nm by an intramolecular or intermolecular reaction by the action of an acid. The image-forming material has a high sensitivity and excellent storage stability and gives low haze and good images in the case of performing image formation using a high-output laser light.Type: GrantFiled: March 28, 2001Date of Patent: May 13, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Atsuhiro Ohkawa, Seiya Sakurai
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Patent number: 6541669Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: June 2, 1999Date of Patent: April 1, 2003Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 6455550Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: August 21, 1998Date of Patent: September 24, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6451736Abstract: There is disclosed substituted thiocarboxamides compounds of the formula (I): wherein R1, R2, R3 and Z are as defined in the specification. The compounds are useful as herbicides.Type: GrantFiled: September 25, 2001Date of Patent: September 17, 2002Assignee: Bayer AktiengesellschaftInventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger
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Patent number: 6426360Abstract: A class of compounds is described for treating inflammation and inflammation-related disorders.Type: GrantFiled: May 15, 2000Date of Patent: July 30, 2002Assignee: G D Searle & Co.Inventors: Richard M Weier, Paul W Collins, Michael A Stealey, Thomas E Barta, Renee M Huff
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Patent number: 6403805Abstract: The present invention describes compounds useful for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof.Type: GrantFiled: July 27, 1999Date of Patent: June 11, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy Jean Edgard Freyne, Gaston Stanislas Marcella Diels, José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea
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Publication number: 20020068830Abstract: The present invention describes the use of compounds for the manufacture of a medicament for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula 1Type: ApplicationFiled: July 27, 1999Publication date: June 6, 2002Inventors: EDDY JEAN EDGARD FREYNE, GASTON STANISLAS MARCELLA DIELS, JOSE IGNACIO ANDRES-GIL, FRANCISCO JAVIER FERNANDEZ-GADEA
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Patent number: 6353013Abstract: Novel compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-nitrophenyl)-5-methylimidazoline-2,4-dione; and, 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-cyanophenyl)-5-methylimidazoline-2,4-dione.Type: GrantFiled: June 28, 2000Date of Patent: March 5, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Ronald John Sorcek
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Patent number: 6335451Abstract: Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I in which the symbols have the meanings indicated in the claims, have outstanding antiarrhythmic properties and exhibit a cardioprotective component. They can preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias. Moreover, they have a potent inhibitory action on the proliferation of cells.Type: GrantFiled: January 21, 1998Date of Patent: January 1, 2002Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Sabine Faber, Hans-Willi Jansen