Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/244)
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Patent number: 9815803Abstract: The present invention relates to processes for the preparation of substituted cycloserine compounds of formula (I) wherein R1 is C1-C8alkyl, C1-C8haloalkyl, C3-C6 cycloalkyl, aryl or aryl substituted by one to five R11, or aryl-C1-C4alkylene or aryl-C1-C4alkylene substituted by one to five R11; and each R11 is independently C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy, cyano or halogen; The invention also relates to intermediates produced by the processes. Compounds of formula (I) are useful intermediates for the production of compounds in the agricultural and pharmaceutical fields.Type: GrantFiled: April 3, 2017Date of Patent: November 14, 2017Assignee: Syngenta Participations AGInventors: Tomas Smejkal, Helmars Smits, Christian Lothschuetz, Miroslav Terinek
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Patent number: 9643938Abstract: The present invention relates to processes for the preparation of substituted cycloserine compounds of formula (I) wherein R1 is C1-C8alkyl, C1-C8haloalkyl, C3-C6cycloalkyl, aryl or aryl substituted by one to five R11, or aryl-C1-C4alkylene or aryl-C1-C4alkylene substituted by one to five R11; and each R11 is independently C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy, cyano or halogen; The invention also relates to intermediates produced by the processes. Compounds of formula (I) are useful intermediates for the production of compounds in the agricultural and pharmaceutical fields.Type: GrantFiled: April 30, 2015Date of Patent: May 9, 2017Assignee: Syngenta Participations AGInventors: Tomas Smejkal, Helmars Smits, Christian Lothschuetz, Miroslav Terinek
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Publication number: 20140350261Abstract: There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an ?,?-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.Type: ApplicationFiled: November 8, 2012Publication date: November 27, 2014Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Ken-ichi Toyama, Yuji Moriyama, Kazutaka Matoba, Manabu Yaosaka, Eitatsu Ikeda
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Publication number: 20140343049Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: August 10, 2012Publication date: November 20, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Julie Clementine Toueg, Tomas Smejkal, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere, Nicolas Poirier
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Publication number: 20140256702Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: March 4, 2014Publication date: September 11, 2014Applicant: THERAVANCE, INC.Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
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Publication number: 20140228577Abstract: The present invention relates to compounds of formula (I): wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jerome Yves CASSAYRE, Peter RENOLD, Myriem EL QACEMI, Thomas PITTERNA, Julie Clementine TOUEG
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Patent number: 8802706Abstract: Provided is a therapeutic or prophylactic agent for generalized pain syndrome, for which no cause and therapies have been established. A therapeutic or prophylactic agent for generalized pain syndrome containing an LPA1 antagonist or autotaxin-inhibiting substance as an active ingredient. The pharmaceutical is preferably administered to the central nervous system. The generalized pain syndrome is preferably fibromyalgia, chronic fatigue syndrome or hypersensitivity colitis.Type: GrantFiled: August 7, 2009Date of Patent: August 12, 2014Assignees: Nagasaki University, Kabushiki Kaisha M.S.SInventor: Hiroshi Ueda
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Publication number: 20140121254Abstract: The invention provides a pharmaceutical composition, medical food, dietary supplement or micronutrient for the treatment of a movement disorder comprising an NMDAR agonist or partial agonist as active ingredient therein in combination with a pharmaceutically acceptable carrier.Type: ApplicationFiled: January 2, 2014Publication date: May 1, 2014Applicant: Sarah Herzog Memorial Hospital Ezrath Nashim AssociationInventors: Uriel Heresco-Levy, Daniel C. Javitt
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Publication number: 20140107056Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH-0- or —CH?C—CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C=0, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 aType: ApplicationFiled: May 30, 2012Publication date: April 17, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
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Publication number: 20140041062Abstract: The present disclosure relates to an ASD genetically engineered model carrying a deletion of Shank2 gene and having reduced NMDA receptor function. According to the present disclosure, genetically engineered mice that show the clinical features of ASD due to the deletion of the Shank2 gene can be obtained, and the genetically engineered mice can be effectively used to screen candidate therapeutic agents.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Applicants: Industry-Academic Cooperation Foundation, Yonsei University, Korea Advanced Institute of Science and Technology, Seoul National University R&DB FoundationInventors: Min Goo Lee, Bong Kiun Kaang, Eunjoon Kim
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Publication number: 20130096168Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: December 5, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventors: Yuki IWAKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI
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Patent number: 8383651Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 15, 2010Date of Patent: February 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Doris Riether, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Monika Ermann, Innocent Mushi, Robert John Scott
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Publication number: 20120129800Abstract: The present invention concerns an agent for prevention and treatment of pityriasis. The agent according to the present invention comprises at least one transaminase inhibitor effectively inhibiting the transamination process which is of pathogenetic relevance for the disease, prevents a recurrence of the disease and which protects the human skin flora. Upon release into the environment, no resistances are induced in other fungi.Type: ApplicationFiled: January 14, 2010Publication date: May 24, 2012Applicant: Justus-Liebig-Universitat GiessenInventor: Peter Mayser
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Patent number: 8183265Abstract: The present invention relates to 2-adamantyl-butyramide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.Type: GrantFiled: November 22, 2007Date of Patent: May 22, 2012Assignee: Merck Patent GmbHInventors: Didier Roche, Denis Carniato, Liliane Doare, Christine Charon, Caroline Leriche
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Patent number: 8048902Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: GrantFiled: December 15, 2009Date of Patent: November 1, 2011Assignee: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
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Publication number: 20110244486Abstract: Methods, assays and compositions for the diagnosis and treatment of diabetes, in which the glutamate transporters and/or receptors expressed in pancreatic islet cells are used as therapeutic targets or tools for the identification or treatment of individuals suffering from or susceptible to diabetes.Type: ApplicationFiled: November 20, 2009Publication date: October 6, 2011Inventors: Carla Perego, Eliana Sara Di Cairano, Alberto Davalli, Franco Folli
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Patent number: 7964624Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.Type: GrantFiled: February 27, 2007Date of Patent: June 21, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
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Publication number: 20110124695Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 16, 2010Publication date: May 26, 2011Inventors: Yuki IWAKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI
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Patent number: 7947718Abstract: Certain isoxazole compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: GrantFiled: September 15, 2009Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica NVInventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20100261665Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: ApplicationFiled: January 28, 2010Publication date: October 14, 2010Applicant: Xcovery, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Publication number: 20100113453Abstract: The invention provides methods and compositions for treating anxiety-related disorders in a subject. The methods include sublingually administering D-cycloserine to a subject with the anxiety-related disorder, either alone or in combination with extinction training.Type: ApplicationFiled: April 10, 2008Publication date: May 6, 2010Inventors: Jason P. McDevitt, Michael Davis, Kerry J. Ressler
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Patent number: 7557133Abstract: The present invention relates to an isoxazoline derivative as an inhibitor against various caspases, a process for preparing the same, and a therapeutic composition for preventing inflammation and apoptosis comprising the same.Type: GrantFiled: August 26, 2004Date of Patent: July 7, 2009Assignee: LG Life Sciences Ltd.Inventors: Hye-Kyung Chang, Yeong-Soo Oh, Cheol-Won Park, Yong-Jin Jang, Tae-Kyo Park, Sung-Sub Kim, Min-Jung Kim, Mi-Jeong Park, Jung-Gyu Park, Hee-Dong Park, Kyeong-Sik Min, Tae-Soo Lee, Sang-Kyun Lee, Soo-Hyeon Kim, Hee-Kyung Jeong, Sun-Hwa Lee, Hwa-Dong Kim, Ae-Ri Kim, Ki-Sook Park, Hyun-Ik Shin, Hyeong-Wook Choi, Kyu-Woong Lee, Jae-Hoon Lee, Tae-Ho Heo, Ho-Jun Kim, Tae-Sik Kwon, Jeong Hui Seong
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Publication number: 20090093640Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.Type: ApplicationFiled: October 11, 2007Publication date: April 9, 2009Inventors: Andrew G. Myers, Jason D. Brubaker
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Publication number: 20090076005Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: ApplicationFiled: December 28, 2007Publication date: March 19, 2009Applicant: Xcovery, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Publication number: 20080188472Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia, e.g. myocardial ischemia, or as cardioprotectants or inhibitors of abnormal cell growth.Type: ApplicationFiled: March 8, 2005Publication date: August 7, 2008Applicant: PROSIDION LIMITEDInventors: Stuart Edward Bradley, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Martin James Procter, Robert John Rowley, Gerard Hugh Thomas, Ana Valdes
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Patent number: 7202257Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: GrantFiled: July 6, 2004Date of Patent: April 10, 2007Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: 7084163Abstract: Compounds of general formula (I), in which Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with -P-Qi-T-Q2, -GZ and Y, such that the substituant -GZ is adjacent to both, the other substituants being as defined in the description, process for preparing this compound, fungicidal composition comprising this compound, method for treating plants by applying this compound or compositionType: GrantFiled: July 8, 2002Date of Patent: August 1, 2006Assignee: Bayer Cropscience S.A.Inventors: Stéphanie Gary, Tim Lange, Benoît Muller, Christopher Richard Steele, Geoffrey Gower Briggs, Joseph Perez, Alain Villier, Brian Hill
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Patent number: 7081538Abstract: Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, X is O, S or NH; HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are describedType: GrantFiled: November 28, 2000Date of Patent: July 25, 2006Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Michael John Betts
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Patent number: 6835842Abstract: The 3-nitroisoxazoles of the formula (I) in which R1 and R2 are each as defined in the description, some of which are known, are highly suitable for use as biocides for protecting industrial materials.Type: GrantFiled: April 10, 2003Date of Patent: December 28, 2004Assignee: Bayer AktiengesellschaftInventors: Hermann Uhr, Oliver Kretschik, Martin Kugler, Peter Wachtler
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Patent number: 6833370Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: April 26, 2000Date of Patent: December 21, 2004Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji
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Patent number: 6746989Abstract: The invention relates to novel substituted benzoylpyrazoles of the general formula (I), in which n represents the numbers 0, 1, 2 or 3, A represents a single bond or represents alkanediyl(alkylene), R1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkoxycarbonyl or cycloalkyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, Y represents hydrogen or represents in each case optionally substitutedType: GrantFiled: September 26, 2001Date of Patent: June 8, 2004Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
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Publication number: 20020188134Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.Type: ApplicationFiled: August 13, 2002Publication date: December 12, 2002Inventors: Michael Ambuhl, Barbara Luckel, Barbara Haberlin, Armin Meinzer
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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: 6387915Abstract: Isoxazole-sulfonamide endothelin antagonists of formula (I) below having good affinity for endothelin receptors and selectivity for ETA over ETB are described herein. Such compounds are useful in the treatment of conditions mediated by endothelin, in particular, conditions mediated by endothelin ETA.Type: GrantFiled: May 30, 2001Date of Patent: May 14, 2002Assignee: Pfizer Inc.Inventors: Bernard Joseph Banks, Nathan Anthony Logan Chubb, James John Eshelby, Michael Stephen Pacey, Darren John Schulz
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Patent number: 6384066Abstract: Novel sulphonyltriazole derivatives of the formula in which Hal represents fluorine, chlorine or bromine, R1 represents hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkylaminocarbonyl, optionally substituted phenyl, optionally substituted phenoxy or represents optionally substituted heterocyclyl and R2 represents alkyl or represents optionally substituted heterocyclyl or represents a radical of the formula in which R3 represents halogen, alkyl or phenyl, R4 represents hydrogen or alkyl and R5 represents alkyl or optionally substituted phenyl, or R4 and R5 together with the nitrogen atom to which they are attached form a heterocyclic ring which may be substituted and which may also contain an additional heteroatom, a process for preparing these substances and their use for controlling undesirable microorganisms.Type: GrantFiled: March 20, 2001Date of Patent: May 7, 2002Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Stefan Hillebrand, Klaus Stenzel, Ulrike Wachendorff-Neumann
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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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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: 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: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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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: 6020354Abstract: New halogenobenzimidazoles of the formula in whichA, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings given in the description,and their acid addition salts and metal salt complexes,a process for their preparation and their use as microbicides in crop protection and in the protection of materials.New intermediates of the formula ##STR1## in which R.sup.12 -R.sup.17 and X have the meanings given in the description,and processes for the preparation of these substances.Type: GrantFiled: January 28, 1998Date of Patent: February 1, 2000Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Albrecht Marhold, Ralf Tiemann, Klaus Stenzel
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Patent number: 5962490Abstract: 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)pyrrolylsulfonamides 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 or increase the activity of endothelin are also provided.Type: GrantFiled: September 27, 1996Date of Patent: October 5, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Adam Kois, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamorri, Vitukudi Narayanaiyengar Balaji
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Patent number: 5939418Abstract: Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: ##STR1## where X is O, S or NR.sup.15.Type: GrantFiled: December 17, 1996Date of Patent: August 17, 1999Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Mimi Lifen Quan, John Wityak, Robert Anthony Galemmo, Jr., Petrus F. W. Stouten, James Russell Pruitt, Donald J. P. Pinto
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5856507Abstract: 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: GrantFiled: January 21, 1997Date of Patent: January 5, 1999Assignee: Bristol-Myers Squibb Co.Inventors: Richard P. Polniaszek, Xuebao Wang, Jeffrey S. DePue, Chennagiri R. Pandit, Kumar G. Gadamasetti, Yadagiri Pendri, Eduardo J. Martinez
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Patent number: 5686434Abstract: This invention relates to 3-aryl-2-isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The 3-aryl-2-isoxazolines are useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.Type: GrantFiled: May 15, 1996Date of Patent: November 11, 1997Assignee: Pfizer Inc.Inventor: Edward Fox Kleinman
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Patent number: 5621109Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.Type: GrantFiled: May 31, 1995Date of Patent: April 15, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5599942Abstract: Taxoids having a 1,3-oxazole containing moiety at the 13-position of the taxane nucleus.Type: GrantFiled: June 7, 1995Date of Patent: February 4, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Herv e Bouchard, Jean-Dominique Bourzat, Alain Commercon
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Patent number: 5594021Abstract: 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)pyrrolylsulfonamides 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 or increase the activity of endothelin are also provided.Type: GrantFiled: June 6, 1995Date of Patent: January 14, 1997Assignee: Texas Biotechnology CorporationInventors: Ming F. Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji