The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/194)
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7173137Abstract: Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.Type: GrantFiled: December 9, 2003Date of Patent: February 6, 2007Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Yun He, Sacha Ninkovic, Joaquin Pastor, Frank Roschangar, Francisco Sarabia, Hans Vallberg, Dionisios Vourloumis, Nicolas Winssinger, Zhen Yang, Nigel Paul King, Maurice Raymond Verschoyle Finlay
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Patent number: 7163952Abstract: The present invention relates to an azole compound represented by the formula [I] wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.Type: GrantFiled: December 3, 2002Date of Patent: January 16, 2007Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Tomoyuki Ikemoto, Shohei Sakata, Hiroshi Maegawa, Atsunori Kashiwagi
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Patent number: 7145017Abstract: The invention relates to a process for the synthesis of Aztreonam. Specifically, the process entails hydrolyzing [3S-[3?(Z),4?]]-3-[[(2-amino-4-thiazolyl)[(1-t-butoxycarbonyl-1-methylethoxy)imino]acetyl]amino]-4-methyl-2-oxo-1-azetidinesulfonic acid (t-Bu Aztreonam) to form Aztreonam.Type: GrantFiled: August 5, 2003Date of Patent: December 5, 2006Assignee: TEVA Gyógyszergyár Zártkörűen Működő RészvénytársaságInventors: Viktor Gyollai, Erzsebet Meszaros Sos, Csaba Szabo, Claude Singer, Szabolcs Salyi
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Patent number: 7125900Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 22, 2001Date of Patent: October 24, 2006Assignee: Biovitrum ABInventors: Tjeerd Barf, Marianne Nilsson, Jerk Vallgårda, Guido Kurz
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7091228Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: GrantFiled: May 6, 2004Date of Patent: August 15, 2006Assignee: Bayer Pharmaceuticals CorporationInventors: Roger Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
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Patent number: 7074794Abstract: The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the ?-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.Type: GrantFiled: August 10, 2001Date of Patent: July 11, 2006Assignee: Mitsubishi Pharma CorporationInventors: Hiroshi Kitajima, Hiroshi Sakashita, Fumihiko Akahoshi, Yoshiharu Hayashi
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Patent number: 6984735Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.Type: GrantFiled: November 26, 2003Date of Patent: January 10, 2006Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark, Wei Li
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Patent number: 6974830Abstract: The present invention relates to compounds according to the general formula (I) which bind to the NR1H4 receptor and act as agonists of the NR1H4 receptor. The invention further relates to the treatment of diseases and/or conditions through binding of the nuclear receptor by the compounds and the production of medicaments using the compounds.Type: GrantFiled: July 1, 2002Date of Patent: December 13, 2005Assignee: Phenix Pharmaceuticals AGInventors: Ulrike Bauer, Zach Cheruvallath, Ulrich Deuschle, Elena Dneprovskaia, Tim Gahman, Kristina Giegrich, Ronnie Hanecak, Normand Hébert, John Kiely, Ingo Kober, Manfred Kögl, Harald Kranz, Claus Kremoser, Matthew Lee, Kerstin Otte, Carlton Sage, Manish Sud
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Patent number: 6972297Abstract: 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infectionsType: GrantFiled: March 29, 2001Date of Patent: December 6, 2005Assignee: SmithKline Beecham p.l.c.Inventors: Gerald Brooks, Eric Hunt, Steven Howard
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Patent number: 6967212Abstract: Compounds are provided which have the structure wherein Q is C or N; R2a, R2b, R2c, X1 to X7, R1, R2, R3, R3a, R4, A, Y, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents. The present invention further provides a method for treating obesity and dyslipidemia in mammals including humans through simultaneous inhibition of peroxisome proliferator activated receptor-? (PPAR?) and stimulation of peroxisome proliferator activated receptor-? (PPAR?).Type: GrantFiled: November 14, 2002Date of Patent: November 22, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Hao Zhang
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Patent number: 6960664Abstract: Disclosed are compounds of formula: and pharmaceutically acceptable salts and esters thereof, useful in treating and/or preventing Alzheimer's disease and other similar diseases, wherein RN, RC, R1, R2 and R20 are defined herein. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: May 22, 2002Date of Patent: November 1, 2005Assignee: Pharmacia & UpJohn CompanyInventors: Heinrich Schostarez, Robert Alan Chrusciel, Rebecca S. Centko
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Patent number: 6924300Abstract: To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.Type: GrantFiled: December 27, 2002Date of Patent: August 2, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Hiroyuki Odaka, Hiroshi Imoto, Hiroyuki Kimura, Junichi Sakamoto
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Patent number: 6921770Abstract: 2-phenyliminothiazolines of the following formula I, their salts, their preparation method and their use for treating rice blast.Type: GrantFiled: July 28, 2001Date of Patent: July 26, 2005Assignee: Korea Institute of Science and TechnologyInventors: Hoh Gyu Hahn, Kee Dal Nam, Kee Hyuk Chang, Kwang Yun Cho, Heung Tae Kim
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Patent number: 6878827Abstract: This invention provides a novel industrial process for preparation of an anhydride of 2-(2-aminothiazole-4-yl)-2-hydroxy compound.Type: GrantFiled: November 28, 2001Date of Patent: April 12, 2005Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroki Ono, Masaru Hayashi, Masaru Ohnishi, Kazuo Ohkawa, Masato Kitayama
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Patent number: 6872730Abstract: The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (?v) integrins, for example ?v?3 and ?v?5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by ?v?3 and ?v?5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein.Type: GrantFiled: April 26, 2002Date of Patent: March 29, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Beth M. Anaclerio, Juan J. Marugan Sanchez, Victor J. Marder, David C. U'Prichard, Bruce E. Tomczuk
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Patent number: 6818634Abstract: Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline compounds are also included.Type: GrantFiled: March 30, 2001Date of Patent: November 16, 2004Assignees: Paratek Pharmaceuticals, Inc., Trustees of Tufts CollegeInventors: Mark L. Nelson, Stuart B. Levy, Roger Frechette, Todd E. Bowser, Mohamed Y. Ismail
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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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Patent number: 6797723Abstract: The invention relates to novel heterocycle substituted diphenyl leukotriene B4 (LTB4) antagonists, to compositions containing such compounds, and to methods of using such compounds for treatment of inflammatory diseases.Type: GrantFiled: April 24, 2002Date of Patent: September 28, 2004Assignee: Eli Lilly and CompanyInventors: Jason Scott Sawyer, Douglas Wade Beight, Edward C R Smith, William Thomas McMillen
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Publication number: 20040176431Abstract: Aminothiazole compounds substituted with sulfur-containing groups are represented by the Formula (I), and their pharmaceutically acceptable salts, prodrugs, active metabolites, and pharmaceutically acceptable salts of said metabolites are described.Type: ApplicationFiled: February 11, 2004Publication date: September 9, 2004Applicant: Pfizer, Inc.Inventors: Wesley K.M. Chong, Shao Song Chu, Rohit K. Duvadie, James Na, Lana Schaffer, Yi Yang, Lin Li
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Publication number: 20040167128Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.Type: ApplicationFiled: October 8, 2003Publication date: August 26, 2004Inventors: Kenneth M. Comess, Scott A. Erickson, Jack Henkin, Douglas M. Kalvin, Megumi Kawai, Ki H. Kim, Nwe Y. BaMaung, Chang Hoon Park, George S. Sheppard, Anil Vasudevan, Jieyi Wang, David M. Barnes, Steve D. Fidanze, Lawrence Kolaczkowski, Robert A. Mantei, David C. Park, William J. Sanders, Jason S. Tedrow, Gary T. Wang
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Publication number: 20040157836Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.Type: ApplicationFiled: September 23, 2003Publication date: August 12, 2004Inventors: Kenneth M. Comess, Scott A. Erickson, Jack Henkin, Douglas M. Kalvin, Megumi Kawai, Ki H. Kim, Nwe Y. BaMaung, Chang Hoon Park, George S. Sheppard, Anil Vasudevan, Jieyi Wang, David M. Barnes, Steve D. Fidanze, Lawrence Kolaczkowski, Robert A. Mantei, David C. Park, William J. Sanders, Jason S. Tedrow, Gary T. Wang
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Publication number: 20040082785Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.Type: ApplicationFiled: November 26, 2003Publication date: April 29, 2004Applicant: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark, Wei Li
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Patent number: 6720346Abstract: Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described. These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.Type: GrantFiled: July 5, 2002Date of Patent: April 13, 2004Assignee: Agouron Pharmaceuticals, Inc.Inventors: Shao Song Chu, Larry Andrew Alegria, Ted Michael Bleckman, Wesley Kwan Mung Chong, Rohit K. Duvadie, Lin Li, Siegfried Heinz Reich, William Henry Romines, III, Michael B. Wallace, Yi Yang
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Patent number: 6716881Abstract: The present invention provides carbanilides of formula (I), wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with methods of using the compounds to control microorganisms in crops and in the protection of materials. The compounds of the present invention also find use in controlling animal pests.Type: GrantFiled: May 30, 2002Date of Patent: April 6, 2004Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Bernd-Wieland Krüger, Robert Markert, Ralf Tiemann, Dietmar Kuhnt, Stefan Dutzmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Hans-Ulrich Buschhaus
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Publication number: 20040038990Abstract: Compounds of formula I 1Type: ApplicationFiled: August 5, 2003Publication date: February 26, 2004Inventors: Wolfgang Guba, Patrizio Mattei, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
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Publication number: 20040034233Abstract: This invention provides a novel industrial process for preparation of an anhydride of 2-(2-aminothiazole-4-yl)-2-hydroxy compound.Type: ApplicationFiled: June 3, 2003Publication date: February 19, 2004Inventors: Hiroki Ono, Masaru Hayashi, Masaru Ohnishi, Kazuo Ohkawa, Masato Kitayama
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Patent number: 6686381Abstract: Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, n, m and A have the significance disclosed in the specification, and can be used for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.Type: GrantFiled: February 26, 2003Date of Patent: February 3, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Patrizio Mattei, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger, Sven Taylor
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Patent number: 6653483Abstract: 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: April 17, 2000Date of Patent: November 25, 2003Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6642180Abstract: The present invention relates to novel biphenyl-substituted cyclic ketoenols of the formula (I) in which W represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or halogenoalkoxy, CKE represents one of the groups in which A, B, D, L, M, Q1, Q2, Q3, Q4, Q5 and Q6 are as defined in the description, to preparation and to their use as pesticides and herbicides.Type: GrantFiled: January 25, 2002Date of Patent: November 4, 2003Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
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Publication number: 20030203950Abstract: 2-phenyliminothiazolines of the following formula I, their salts, their preparation method and their use for treating rice blast. The phenyliminothiazolines and their salts of the present invention have low toxicity to environment or living organisms, and exert high activity at low concentration for treating rice blast through a new controlling mechanism, that is by inhibiting pentaketide synthesis and cyclization of the melanin sythesis process in formula I.Type: ApplicationFiled: May 30, 2003Publication date: October 30, 2003Inventors: Hoh Gyu Hahn, Kee Dal Nam, Kee Hyuk Chang, Kwang Yun Chio, Heung Tae Kim
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Publication number: 20030204085Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: July 30, 2002Publication date: October 30, 2003Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jonathan A. Pachter, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
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Patent number: 6610714Abstract: Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CR8R9)n— R8 and R9 are independently H, C1-C3 alkyl, OH or R8 and R9 together are ═O n is 1, 2 or 3 and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.Type: GrantFiled: March 5, 2002Date of Patent: August 26, 2003Assignee: Medivir ABInventors: Christer Sahlberg, Dmitry Antonov, Hans Wallberg, Rolf Noréen
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Patent number: 6605626Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6596746Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: April 13, 2000Date of Patent: July 22, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek J. Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
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Patent number: 6593327Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: December 14, 2001Date of Patent: July 15, 2003Assignee: Axys Pharmaceuticals, Inc.Inventors: Clifford M. Bryant, James T. Palmer, Robert M. Rydzewski, Eduardo L. Setti, Zong-Qiang Tian, Shankar Venkatraman, Dan-Xiong Wang
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Publication number: 20030130281Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: October 14, 2002Publication date: July 10, 2003Inventors: Markus Boehringer, Daniel Hunziker, Holger Kuehne, Bernd M. Loeffler, Ramakanth Sarabu, Hans P. Wessel
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Publication number: 20030105279Abstract: The present invention is directed to protected amino acid halide monomers and oligomers, and to their use in the efficient sythesis of polyamides. The present invention is further directed to the use of &agr;-haloenamine reagents, which may optionally be immobilized, for the preparation of the amino acid halides.Type: ApplicationFiled: August 30, 2002Publication date: June 5, 2003Applicant: Pharmacia CorporationInventor: Dennis P. Phillion
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Patent number: 6569878Abstract: Pharmaceutical compositions containing effective amounts of CDK-inhibiting diaminothiazole compounds of the following formula (where R1 and R2 are as defined in the specification) or their salts, or prodrugs or active metabolites of such compounds or salts, are useful for treating disorders and diseases such as cancer: In preferred embodiments, R1 and R2 are independently unsubstituted or substituted carbocyclic or heterocyclic aryl ring structures. Compounds where R2 is ortho-substituted aryl are especially potent inhibitors of CDKs such as CDK4.Type: GrantFiled: October 27, 1998Date of Patent: May 27, 2003Assignee: Agouron Pharmaceuticals Inc.Inventors: Wesley K. M. Chong, Shao Song Chu, Lin Li, Rohit K. Duvadie, Yi Yang, Wei Xiao
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Patent number: 6569874Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I: 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: November 17, 2000Date of Patent: May 27, 2003Assignee: Bristol-Myers Squibb CompanyInventors: James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
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Patent number: 6534532Abstract: The invention concerns novel carbanilides of formula (I), in which A, Q, R, X, Z and m have the meanings given in the description. The invention further concerns a plurality of processes for preparing these substances, in their use as microbiocides for controlling undesirable microorganisms both in crop protection and in the protection of materials. Additionally, they are suitable for controlling animal pests.Type: GrantFiled: September 18, 2001Date of Patent: March 18, 2003Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Bernd-Wieland Krüger, Robert Markert, Ralf Tiemann, Dietmar Kuhnt, Stefan Dutzmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Hans-Ulrich Buschhaus
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Patent number: 6515005Abstract: The present invention relates to thiazoles, oxazoles, imidazoles and pharmaceutical compositions comprising said compounds antagonizing the corticotropin releasing factor receptor (“CRF receptor”) and useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: September 17, 2001Date of Patent: February 4, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Gene M. Dubowchik, Dmitry S. Zuev
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Patent number: 6498174Abstract: The present invention discloses compounds of formula (I), and tautomeric forms, pharmaceutically acceptable salts, or solvates thereof. Preferably, the compounds of the invention are dual activators of hPPAR&ggr; and hPPAR{acute over (&agr;)}.Type: GrantFiled: February 22, 2001Date of Patent: December 24, 2002Assignee: SmithKline Beecham CorporationInventors: Jon Loren Collins, Milana Dezube, Jeffrey Alan Oplinger, Timothy Mark Willson
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Patent number: 6495581Abstract: A compound represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond, —CO—, —CH(OH)— or a group represented by —NR6— wherein R6 is a hydrogen atom or an optionally substituted alkyl group; n is an integer of 1 to 3; Y is an oxygen atom, a sulfur atom, —SO—, —SO2— or a group represented by —NR7— wherein R7 is a hydrogen atom or an optionally alkyl group; ring A is a benzene ring optionally having additional one to three substituents; p is an integer of 1 to 8; R2 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; q is an integer of 0 to 6; m is 0 or 1; R3 is a hydroxy group, OR8 (R8 is an optionally substituted hydrocarbon group.Type: GrantFiled: November 16, 2000Date of Patent: December 17, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Hiroyuki Odaka, Hiroshi Imoto, Hiroyuki Kimura, Junichi Sakamoto
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Publication number: 20020165259Abstract: Compounds of the formula 1Type: ApplicationFiled: March 29, 2002Publication date: November 7, 2002Inventors: David B. Rawlins, S. David Kimball, Kyoung S. Kim, Raj N. Misra, Kevin R. Webster
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Patent number: 6458959Abstract: This invention relates to methods for inhibiting herpes replication and for treating herpes infection in a mammal by inhibiting the herpes helicase-primase enzyme complex. This invention also relates to thiazolyphenyl derivatives that inhibit the herpes helicase-primase and to pharmaceutical compositions comprising the thiazolylphenyl derivatives, to methods of using and methods of producing the thiazolylphenyl derivatives.Type: GrantFiled: October 10, 2000Date of Patent: October 1, 2002Assignees: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim (Canada) Ltd.Inventors: James J. Crute, Anne-Marie Faucher, Christine A. Grygon, Karl D. Hargrave, Bruno Simoneau, Bounkham Thavonekham
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 6403535Abstract: The invention relates to novel substituted thiazol(in)ylidenaminosulphonyl-amino(thio)carbonyl-triazolinones of the formula (I) in which Q represents oxygen or sulphur, R1 represents hydrogen, amino, alkylideneamino or represents an in each case optionally substituted radical from the group consisting of alkyl, alkoxy, alkylamino, dialkylamino, alkanoylamino, alkenyl, alkinyl, alkenyloxy, cycloalkyl, cycloalkylalkyl, cycloalkylamino, aryl and arylalkyl, R2 represents hydrogen, cyano, halogen or represents an in each case optionally substituted radical from the group consisting of alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino, alkenyl, alkinyl, alkenyloxy, alkenylthio, alkenylamino, cycloalkyl, cycloalkylalkyl, cycloalkyloxy, cycloalkylthio, cycloalkylamino, aryl, aryloxy, arylthio, arylamino, arylalkyl, arylalkoxy, arylalkylthio and arylalkylamino, R3 represents an in each case optionally substituted radical from the group consisting of alkyl, alkoxy,Type: GrantFiled: April 27, 2001Date of Patent: June 11, 2002Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Klaus König, Johannes Rudolf Jansen, Ernst Rudolf F. Gesing, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky
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Patent number: RE38330Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.Type: GrantFiled: August 12, 1999Date of Patent: November 25, 2003Assignee: Alteon Inc.Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan