Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/245)
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Patent number: 6818775Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: December 9, 2003Date of Patent: November 16, 2004Assignee: Allergan, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Publication number: 20040106794Abstract: There are disclosed compounds of the formula 1Type: ApplicationFiled: September 11, 2002Publication date: June 3, 2004Applicant: Schering CorporationInventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Laura L. Rokosz
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Publication number: 20040059123Abstract: Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.Type: ApplicationFiled: August 12, 2003Publication date: March 25, 2004Inventors: Richard P. Polniaszek, Xuebao Wang, John K. Thottathil, Theodor Denzel
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Publication number: 20040058931Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1Type: ApplicationFiled: November 15, 2002Publication date: March 25, 2004Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
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Patent number: 6699904Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: GrantFiled: February 14, 2002Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Cheryl M. Hayward, David A. Perry
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Patent number: 6686382Abstract: Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazolyl)phenylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.Type: GrantFiled: December 29, 2000Date of Patent: February 3, 2004Assignee: Encysive Pharmaceuticals Inc.Inventors: Chengde Wu, Natalie Blok, George W. Holland
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Patent number: 6680317Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 17, 2002Date of Patent: January 20, 2004Assignee: SmithKline Beecham CorporationInventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030236287Abstract: The invention provides compounds of Formula I: 1Type: ApplicationFiled: April 25, 2003Publication date: December 25, 2003Inventors: David W. Piotrowski, Bruce N. Rogers, William W. McWhorter, Daniel Patrick Walker, Jeffrey W. Corbett, Vincent E. Groppi, Daniel G. Rudmann
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Patent number: 6649639Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: September 7, 2001Date of Patent: November 18, 2003Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
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Publication number: 20030207929Abstract: The 3-nitroisoxazoles of the formula (I) 1Type: ApplicationFiled: April 10, 2003Publication date: November 6, 2003Inventors: Hermann Uhr, Oliver Kretschik, Martin Kugler, Peter Wachtler
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Patent number: 6638937Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.Type: GrantFiled: December 14, 2000Date of Patent: October 28, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, John E. Tellew, John E. Macor, Zhengxiang Gu
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Publication number: 20030181482Abstract: This invention relates to novel heteroatom containing compounds and compositions thereof, and their use for the prevention and treatment of disease. The invention also provides for methods of making the compounds. The invention is based on the discovery that certain heteroatom containing compounds, 3-oxoacetamideindolyl compounds, have potent anticancer, cytotoxic, and anti-angiogenic activity.Type: ApplicationFiled: December 5, 2002Publication date: September 25, 2003Inventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
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Publication number: 20030181718Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: ApplicationFiled: February 10, 2003Publication date: September 25, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6624167Abstract: Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an ethylenic or acetylenic unit to an azabicyclic moiety.Type: GrantFiled: August 4, 2000Date of Patent: September 23, 2003Assignee: Targacept, Inc.Inventors: Thomas Jeffrey Clark, Balwinder Singh Bhatti
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Publication number: 20030176668Abstract: A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group.Type: ApplicationFiled: January 17, 2003Publication date: September 18, 2003Inventors: Jonathan S. Stamler, Eric J. Toone
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Patent number: 6608077Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 5, 2002Date of Patent: August 19, 2003Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Qi Jin
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Patent number: 6596747Abstract: Compounds having the formula (I), are effective as inhibitors of IMPDH enzyme and/or serine protease Factor VIIa, wherein B is a monocyclic or bicyclic carbocyclic or heterocyclic ring, D is a monocyclic or bicyclic carbocyclic or heterocyclic ring except when A is a heterocyclic ring, then D is a heterocyclic ring system, R is hydrogen or C1-4alkyl, and A, R1, R2 and R4 are as defined in the specification.Type: GrantFiled: November 29, 2001Date of Patent: July 22, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Chunjian Liu, T. G. Murali Dhar, Henry H. Gu, Edwin J. Iwanowicz, Katerina Leftheris, William J. Pitts, Timothy F. Herpin, Gregory S. Bisacchi
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Publication number: 20030130328Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: September 26, 2002Publication date: July 10, 2003Inventors: Steven W. Andrews, Julie A. Wurster
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Patent number: 6586433Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: July 1, 2003Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030114505Abstract: The present invention relates to novel isoxazole and thiazole compounds having an excellent lysophosphatidic acid (LPA) receptor antagonistic activity represented by general formula [1] or salts thereof: 1Type: ApplicationFiled: August 19, 2002Publication date: June 19, 2003Inventors: Akihiro Ueno, Rika Nagao, Tomoko Watanabe, Hideo Ohta, Mikio Yagi
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Patent number: 6576780Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: October 13, 2000Date of Patent: June 10, 2003Assignee: GD Searle & CompanyInventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
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Publication number: 20030100590Abstract: 1 The invention relates to 3-(4,5-dihydroisoxazole-5-yl)benzoylpyrazole of the formula (I), wherein the variables have the following meanings: R1, R1 represent hydrogen, nitro, halogen, cyano, alkyl, halogenalkyl, alkoxy, halogenalkoxy, alkylthio, halogenalkylthio, alkylsulfinyl, halogenalkylsulfinyl, alkylsulfonyl or halogenalkylsulfonyl; hydrogen, R3 represents halogen or alkyl; R4 represents hydrogen or alkyl; R5, R6 represent hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl R3 or carbonyl, wherein the latter six groups can be substituted; R7 represents halogen, cyano, hydroxy, alkyl, halogenalkyl, alkoxy, halogenalkoxy, alkylthio, halogenalkylthio, alkylsulfinyl, halogenalkylsulfinyl, alkylsulfonyl, halogenalkylsulfonyl, amino, alkylamino, dialkylamino, dialkoxymethyl, hydroxyiminoalkyl, alkoxyiminoalkyl or optionally substituted carbonyl; R11 represents optionally substituted pyrazole that is bound in the 4 position and that carries a hydroxy group or a derivative theType: ApplicationFiled: June 19, 2002Publication date: May 29, 2003Inventors: Ernst Baumann, Wolfgang von Deyn, Steffen Kudis, Klaus Langemann, Guido Mayer, Ulf Misslitz, Ulf neidlein, Helmut Walter, Karl-Otto Westphalen, Matthias Witschel
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Publication number: 20030092751Abstract: Disclosed is an anti-cancer compound represented by Structural Formula (I): 1Type: ApplicationFiled: August 29, 2002Publication date: May 15, 2003Applicant: SBR Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Mitsunori Ono, Guiqing Liang, David James, Hao Li, Zhi-Qiang Xia
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Patent number: 6544982Abstract: A thrombin receptor antagonist having the formula useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.Type: GrantFiled: October 27, 2000Date of Patent: April 8, 2003Assignee: Merck & Co., Inc.Inventors: Harold G. Selnick, Philippe G. Nantermet, James C. Barrow, Roger M. Freidinger, Thomas Connolly
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Publication number: 20020165400Abstract: The present invention relates to processes for the conversion of nitrites to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.Type: ApplicationFiled: April 25, 2002Publication date: November 7, 2002Inventors: Philip Ma, Pasquale N. Confalone, Hui-Yin Li
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Patent number: 6455561Abstract: The present invention pertains to compositions and methods for treating disease states which are capable of being modulated by inhibition of phosphodiesterase IV or Tumour Necrosis Factor, or that is a pathological condition associated with a function of phosphodiesterase IV, eosinophil accumulation or a function of the eosinophil, said method comprising administering to a person or animal in need of such treatment an effective amount of the compound of a formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is CH2OCH3 or 2 or 3-tetrahydrofuranyl; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) R4 is C 1-3 alkyl; and R5 and R6, which may be the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereofType: GrantFiled: October 12, 2001Date of Patent: September 24, 2002Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Christopher Lowe, John Gary Montana
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Patent number: 6432994Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, pharmaceutically-acceptable salts of sulfonamides, formulations of salts and the sulfonamides, and methods for modulating or altering the activity of the endothelin family of peptides using the formulations and sulfonamides are provided. In particular, formulations of sodium salts of N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides are provided. A process of preparing an alkali metal salt of a hydrophobic sulfonamide is provided. The process includes the step of dissolving a free sulfonamide in an organic solvent in the presence of a saturated alkali metal salt solution and recovering the formed sulfonamide salt from the organic phase.Type: GrantFiled: March 27, 2000Date of Patent: August 13, 2002Assignee: Texas Biotechnology CorporationInventors: Chengde Wu, Natalie Blok, Timothy Kogan, Karin Keller, Patricia Woodard
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Patent number: 6420567Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.Type: GrantFiled: September 26, 1997Date of Patent: July 16, 2002Assignee: Texas Biotechnology CorporationInventors: Chengde Wu, Bore Gowda Raju, Timothy Kogan, Natalie Blok
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Patent number: 6417214Abstract: This invention provides compounds of the formula 1: wherein: R1 and R2 are chosen independently from each other from H, OH; OAc; alkylaryl; alkylheteroaryl; 1-propynyl; 3-propynyl; and optionally substituted alkyl, O(alkyl); aryl; or heteroaryl groups; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2CMe2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is selected from optionally substituted benzene ring; a five or six membered heterocyclic ring; a 4 or 7-substituted indole or a substitutType: GrantFiled: April 19, 2000Date of Patent: July 9, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: John W. Ullrich, Andrew Fensome, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6395724Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.Type: GrantFiled: June 7, 1999Date of Patent: May 28, 2002Assignee: Advanced Medicine, Inc.Inventors: J. Kevin Judice, Deborah L. Higgins, John H. Griffin
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Publication number: 20010056183Abstract: Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazolyl)phenylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.Type: ApplicationFiled: December 29, 2000Publication date: December 27, 2001Applicant: Texas Biotechnology CorporationInventors: Chengde Wu, Natalie Blok, George W. Holland
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Patent number: 6331556Abstract: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is CH2OCH3 or 2 or 3-tetrahydrofuranyl; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) R4 is C1-3 alkyl; and R5 and R6, which may be the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 9, 2001Date of Patent: December 18, 2001Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Christopher Lowe, John Gary Montana
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Patent number: 6331637Abstract: N-alkyl, N-alkenyl, N-alkynyl, N-aryl and N-fused bicyclo or tricyclo thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, (phenyl) and (phenoxy)thienylsulfonamides, (phenyl) and (phenoxy)furylsulfonamides, and (phenyl) and (phenoxy)pyrrolylsulfonamides and methods of using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: March 22, 1999Date of Patent: December 18, 2001Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Adam Kois, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamoori, Vitukudi Narayanaiyengar Balaji
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Patent number: 6331554Abstract: Picornaviral 3C protease inhibitors of formula I, obtainable by chemical synthesis, that inhibit or block the biological activity of the picornaviral 3C protease are described. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: October 20, 1999Date of Patent: December 18, 2001Assignee: Agouron Pharmaceuticals, Inc.Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
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Patent number: 6313308Abstract: Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates therof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension, congestive heart failure and male erectile dysfunction.Type: GrantFiled: March 20, 2000Date of Patent: November 6, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Ambarish Singh, Chien-Kuang Chen, John A. Grosso, Edward J. Delaney, Xuebao Wang, Richard P. Polniaszek, John K. Thottathil
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Publication number: 20010021714Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides and N-(isoxazolyl)pyrrolyisulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prod rugs thereof that inhibit or increase the activity of endothelin are also provided.Type: ApplicationFiled: November 7, 1997Publication date: September 13, 2001Inventors: MING FAI CHAN, CHENGDE WU, BORE GOWDA RAJU, TIMOTHY KOGAN, ERIK JOEL VERNER, ROSARIO SILVESTRE CASTILLO, VENKATACHALAPATHI YALAMOORI, ADAM KOIS, VITUKUDI NARAYANAIYENGAR BALAJI
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Patent number: 6277790Abstract: Tetrazolinonecarboxamides of formula I wherein Het is oxetan-3-yl, thietan-3-yl, tetrahydrofuran-3-yl, furan-3-yl, tetrahydrothiophen-3-yl, thiophen-3-yl, tetrahydro-2H-pyran-3-yl, tetrahydro-2H-thiopyran-3-yl, tetrahydro-2H-pyran-4-yl or tetrahydro-2H-thiopyran-4-yl, in each case with or without substitution; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, or 3- to 7-membered heterocyclyl; R2 is hydrogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, or is optionally substituted cycloalkyl, cycloalkylalkyl, phenyl, phenylalkyl, 3- to 7-membered heterocyclyl, or 3- to 7-membered heterocyclylalkyl, their preparation and herbicidal compositions comprising them.Type: GrantFiled: February 1, 2000Date of Patent: August 21, 2001Assignee: BASF AktiengesellschaftInventors: Cyrill Zagar, Gerhard Hamprecht, Markus Menges, Olaf Menke, Robert Reinhard, Peter Schäfer, Karl-Otto Westphalen, Martina Otten, Helmut Walter
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Patent number: 6271248Abstract: Compounds of the formula wherein X, Y, R1, R2, R3, R4 and R5 are as described herein, inhibit the activity of endothelin.Type: GrantFiled: January 20, 2000Date of Patent: August 7, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, Joel C. Barrish, John Lloyd
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Patent number: 6248767Abstract: Formulations of pharmaceutically-acceptable salts of thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides using the formulations are provided. In particular, formulations of sodium salts of N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamide salts for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide salt are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamide salts or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: September 26, 1997Date of Patent: June 19, 2001Assignee: Texas Biotechnology Corp.Inventors: Natalie Blok, Chengde Wu, Patricia Woodard, Karin Keller, Timothy Kogan
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Patent number: 6248770Abstract: The present invention relates to new benzimidazoles of general formula wherein Ra to Rc, A, Ar and B are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof the prodrugs, the derivatives thereof which contain a group which is negatively charged under physiological conditions, instead of a carboxy group, and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein Rc denotes one of the amidino groups mentioned in claim 1 which have valuable pharmacological properties, particularly an antithrombotic activity.Type: GrantFiled: June 24, 1999Date of Patent: June 19, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Uwe Ries, Iris Kauffmann, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6197795Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g.Type: GrantFiled: June 11, 1999Date of Patent: March 6, 2001Assignee: American Cyanamid CompanyInventors: Jeremy Ian Levin, Frances Christy Nelson
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Patent number: 6187797Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: December 22, 1997Date of Patent: February 13, 2001Assignee: Dupont Pharmaceuticals CompanyInventors: James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
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Patent number: 6150303Abstract: Substituted 3-phenylisoxazolines I, and their salts and enol ethers, are described as herbicides ##STR1## where X.dbd.--O--, --S--, --N(R.sup.9)--;R.sup.1 .dbd.CN, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylsulfonyl;R.sup.2 .dbd.H or unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, (C.sub.1 -C.sub.6 -alkyl)carbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.2 -C.sub.6 -alkenyl, (C.sub.2 -C.sub.6 -alkenyl)carbonyl, C.sub.2 -C.sub.6 -alkynyl, (C.sub.2 -C.sub.6 -alkynyl)carbonyl;R.sup.3 .dbd.H, halogen;R.sup.4 .dbd.CN, halogen, C.sub.1 -C.sub.3 -haloalkyl;R.sup.5 .dbd.H, CN, halogen, C.sub.1 -C.sub.3 -haloalkyl;R.sup.6 .dbd.H, CN, halogen, C.sub.1 -C.sub.3 -haloalkyl or unsubstituted or substituted C.sub.1 -C.sub.6 -alkoxy;R.sup.7 .dbd.CN, halogen;R.sup.8 in position .alpha., R.sup.7 in this case being in position .beta., or in position .beta., R.sup.7 in this case being in position .alpha., is1) H, OH, SH, CN, NO.sub.2, halogen, C.sub.1 -C.sub.Type: GrantFiled: January 21, 2000Date of Patent: November 21, 2000Assignee: BASF AktiengesellschaftInventors: Olaf Menke, Markus Menges, Gerhard Hamprecht, Robert Reinhard, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Patent number: 6107320Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2 and R.sup.3 are each independently(a) hydrogen, except that R.sup.1 is other than hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.6 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.6 ;(i) --SH, --S(O).sub.n R.sup.6, --S(O).sub.m --OH, --S(O).sub.m --OR.sup.6, --O--S(O).sub.m --R.sup.6, --O--S(O).sub.m OH or --O--S(O).sub.m --OR.sup.6 ;(j) --Z.sup.4 --NR.sup.7 R.sup.8 ; or(k) --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ;and the remaining symbols are as defined in the specification.Type: GrantFiled: January 11, 1996Date of Patent: August 22, 2000Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, John T. Hunt
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Patent number: 6080774Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: ##STR2## R.sup.2 and R.sup.3 are each independently (a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.6 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.6 ;(i) --SH, --S(O).sub.n R.sup.6, --S(O).sub.m --OH, --S(O).sub.m --OR.sup.6, --O--S(O).sub.m --R.sup.6, --O--S(O).sub.m OH or --O--S(O).sub.m --OR.sup.6 ;(j) --Z.sup.4 --NR.sup.7 R.sup.8 ; or(k) --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ;and the remaining symbols are as defined in the specification.Type: GrantFiled: October 8, 1996Date of Patent: June 27, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, Joel C. Barrish, John Lloyd
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Patent number: 6022977Abstract: The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.Type: GrantFiled: March 25, 1998Date of Patent: February 8, 2000Assignee: DuPont Pharmaceuticals CompanyInventors: Lin-Hua Zhang, Luigi Anzalone, Jaan A. Pesti, Jianguo Yin
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Patent number: 6013805Abstract: The invention relates to intermediates to herbicidal compounds of formulae (Ia), (Ib) or (Ic): ##STR1##Type: GrantFiled: September 29, 1998Date of Patent: January 11, 2000Assignee: Rhone-Poulenc Agriculture LtdInventor: David William Hawkins
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Patent number: 6013655Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin pepuide are provided. The methods use compositions that contain compounds that include those of the formula: ##STR1## where X is selected from groups that include O, S, and NH; Y is selected from O.sup.+ and N, and R.sup.1 and R.sup.2 are each selected independently from among alkyl, lower allkenyl, lower alkynyl, lower haloalkyl, halide, pseudohalide or H, except that R.sup.2 is not halide. R.sup.3, R.sup.4 and R.sup.5 are selected from among groups that include hydrogen, halide, alkoxy, alkyl, haloalkyl; and R.sup.7 is selected from groups that include (CH.sub.2).sub.r R.sup.18, in which r is 0 to 6 and R.sup.18 is selected from groups that include aryl, particularly pyrimidinyl and phenyl.Type: GrantFiled: September 4, 1998Date of Patent: January 11, 2000Assignee: Texas Biotechnology CorporationInventor: Erik Joel Verner
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Patent number: 5981511Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: March 5, 1997Date of Patent: November 9, 1999Assignee: G.D. Searle & Co.Inventors: Rolando E. Gapud, Timothy J. Hagen, Ann E. Hallinan, Donald W. Hansen, Jr., Robert E. Manning, Suzanne Metz, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, R. Keith Webber