Nitrogen Attached Directly At 2-position By Nonionic Bonding Patents (Class 544/320)
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Patent number: 7022650Abstract: A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of formula (I) and of their use as herbicides. In this formula (I) R1, R2, R3 and R4 are various radicals, A is an aromatic or heteroaromatic radical, and Z is a nitrogen or carbon atom.Type: GrantFiled: July 24, 2003Date of Patent: April 4, 2006Assignee: Bayer CropScience GmbHInventors: Michael Gerhard Hoffmann, Hendrik Helmke, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
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Patent number: 7015228Abstract: Compounds of formula wherein R1 and R2 are each independently of the other hydrogen; unsubstituted or mono- or poly-halo-substituted C1–C20alkyl, C1–C20alkoxy, C2–C20alkenyl, C2–C20alkynyl, C3–C18cycloalkyl, C3–C7cycloalkyl-C1–C20alkyl; hydroxy; C1–C6alkoxy-C1–C20alkyl; carboxy; C1–C6alkyloxycarbonyl; cyano; mono- or di-C1–C20alkylamino; C1–C6alkylamino-C1–C20alkyl; halogen; phenyl; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted phenyl-C1–C20alkyl, phenoxy or phenyl-C1–C20alkoxy; or R1 and R2 form a polymethylene chain of formula —(CH2)m— wherein m=2–12; R3 is unsubstituted C7–C20alkyl; or amino-, hydroxy-, carboxy- or C1–C6alkyloxycarbonyl-substituted C2–C20alkyl; C8–C18cycloalkyl; C8–C20alkenyl; C8–C20alkynyl; C3–C7cycloalkyl-C8–C20alkyl; C1–C4alkoxy-C8–C20alkyl; R7R8N—C7–C20alkyl; phenyl; phenyl-C1–C4alkyl; or phenyl-C1–C4alkoxy; R4 is hydrogen; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted C1–C20alkyl, C2–C20alkenyl, C2–C20alkynyl, C3–C20cycloalkyl, C3–C7cycloalkyl-C1–C20alkyType: GrantFiled: April 17, 2002Date of Patent: March 21, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Wolfgang Haap, Werner Hölzl, Karin Petzold
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Patent number: 6958332Abstract: This invention features pyrimidine compounds of formula (I): each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.Type: GrantFiled: September 5, 2003Date of Patent: October 25, 2005Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostik, Yumiko Wada
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Patent number: 6927193Abstract: Substituted aryl ether derived compounds represented by the general structure (I) are described. X and Y are independent of each other and are represented by hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, or (C1-4)haloalkoxy; Z is oxygen or sulfur; Q is selected form Q1 to Q6; Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants.Type: GrantFiled: March 3, 2003Date of Patent: August 9, 2005Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Sandeep Gupta, Masamitsu Tsukamoto, Mark Read
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Patent number: 6919347Abstract: Bradykinin B1-receptor antagonists of formula are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesia, asthma, rhinitis, septic shock, atherosclerosis and multiple sclerosis. Pyrimidines, triazines, and anilines in which Q is imidazolyl or pyrrolyl are particularly preferred.Type: GrantFiled: January 14, 2002Date of Patent: July 19, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Michael H. J. Ohlmeyer, John J. Baldwin, Roland E. Dolle, III, Vidyadhar Paradkar, Jorge Gabriel Quintero, Gonghua Pan
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Patent number: 6908924Abstract: The present invention is directed to a compound, method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the administration of N4-acylcytosine-1,3-dioxolane and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.Type: GrantFiled: December 16, 2002Date of Patent: June 21, 2005Assignee: Pharmasset, Inc.Inventors: Kyoichi A. Watanabe, Junxing Shi, Michael J. Otto
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Patent number: 6903213Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C16alkyloxy-carbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7Type: GrantFiled: June 28, 2002Date of Patent: June 7, 2005Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6900222Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is aType: GrantFiled: May 23, 2000Date of Patent: May 31, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 6897302Abstract: The invention provides a method of synthesizing ?-L-5-fluoro-2?,3?-dideoxy-2?,3?-didehydrocytidine (?-L-FD4C). The method allows for large-scale production of ?-L-FD4C in an efficient, cost-effective, and environmentally sound manner.Type: GrantFiled: April 11, 2003Date of Patent: May 24, 2005Assignee: Achillion Pharmaceuticals, Inc.Inventors: Bo Kowalczyk, Zhao Lei, Ralph M. Schure, Lisa Dunkle
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Patent number: 6872729Abstract: A pyrimidinylbenzimidazole or triazinylbenzimidazole derivative represented by the general formula (I): wherein A is N or CR3, and R1, R2, R3, X, Y and n are as defined in the disclosure.Type: GrantFiled: March 10, 2003Date of Patent: March 29, 2005Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masaru Shibata, Kiyoshi Kawai, Takechi Makihara, Norihisa Yonekura, Takehiro Kawashima, Junetsu Sakai, Norimichi Muramatsu
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Patent number: 6864368Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: April 12, 2002Date of Patent: March 8, 2005Assignees: Berlax Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6858606Abstract: This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g.Type: GrantFiled: November 26, 2002Date of Patent: February 22, 2005Assignee: Synta Pharmaceutical Corp.Inventors: Lijun Sun, Mitsunori Ono, Elena Kostik, Yumiko Wada
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Patent number: 6846829Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: April 12, 2002Date of Patent: January 25, 2005Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6844335Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted.Type: GrantFiled: March 22, 2001Date of Patent: January 18, 2005Assignees: Sanofi-Synthelabo, Mitsubishi Pharma CorporationInventors: Antonio Almario Garcia, Ryoichi Ando, Keiichi Arimoto, Fumiaki Uehara, Adrien Tak Li, Aya Shoda, Jonathan Reid Frost, Kazutoshi Watanabe
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Patent number: 6838414Abstract: The invention relates to novel substituted arylsulphonyl(thio)ureas in which A represents nitrogen or a CH grouping, Q represents oxygen or sulphur, R1 represents hydrogen, halogen or respectively optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy or heterocyclyloxy, R2 represents hydrogen, halogen or respectively optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy or heterocyclyloxy, R3 represents hydrogen or optionally substituted alkyl, R4 represents respectively optionally substituted alkyl, alkoxy, alkenyl, alkinyl, alkenyloxy, alkinyloxy, cycloalkyl, cycloalkyloxy or cycloalkylalkyl, and R5 represents hydrogen, formyl or respectively optionally substituted alkyl, alkylcarbonyl, alkoxycarbonyl, alkylsulphonyl, alkenyl, alkinyl, cycloalkyl, cycloalkylcarbonyl, cycloalkylsulphonyl or heterocyclyl, and to salts of compounds of the formula (I), except for the compound N-(4,6-dimethyl-pyrimidin-2-yl)-N?-[Type: GrantFiled: July 16, 2002Date of Patent: January 4, 2005Assignee: Bayer AktiengesellschaftInventors: Ernst Rudolf F. Gesing, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Müller, Mark Wilhelm Drewes, Johannes Rudolf Jansen, Ulrich Philipp, Hans-Jochem Riebel, Otto Schallner, Markus Dollinger, Hans-Joachim Santel
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Patent number: 6838463Abstract: Pyrimidine compounds of formula (1): wherein R1 is C3-C7 alkynyl optionally substituted with halogen; R2 and R3 are independently hydrogen or the like; and R4 is C3-C7 alkynyloxy optionally substituted with halogen, optionally substituted phenyl, or the like have an excellent pesticidal effect.Type: GrantFiled: September 7, 2001Date of Patent: January 4, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Hajime Mizuno, Noriyasu Sakamoto, Yoshiharu Kinoshita
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Publication number: 20040259865Abstract: The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.Type: ApplicationFiled: April 14, 2004Publication date: December 23, 2004Inventors: Hitoshi Harada, Osamu Asano, Masato Ueda, Shuhei Miyazawa, Yoshihiko Kotake, Yasuhiro Kabasawa, Masahiro Yasuda, Nobuyuki Yasuda
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Publication number: 20040224966Abstract: This invention relates to pyrimidine derivatives of general formula I 1Type: ApplicationFiled: May 11, 2004Publication date: November 11, 2004Inventors: Thomas Brumby, Rolf Jautelat, Olaf Prien, Martina Schafer, Gerhard Siemeister, Ulrich Lucking, Christoph Huwe
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Patent number: 6806229Abstract: The present invention relates to pyridine sulfonyl urea derivatives, salts or stereochemical isomers thereof showing an effective herbicidal activity in pre- and/or post-emergence treatment in rice farming, or to a method to use thereof, a method for the preparation thereof, an intermediate used for the preparation thereof, and a herbicidal composition comprising same.Type: GrantFiled: January 8, 2003Date of Patent: October 19, 2004Assignee: LG Life SciencesInventors: Suk-Jin Koo, Jin-Ho Cho, Jeong-Su Kim, Seung-Hun Kang, Kyung-Goo Kang, Dae-Whang Kim, Hae-Sung Chang, Young-Kwan Ko, Jae-Wook Ryoo
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Publication number: 20040204386Abstract: The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor-cells.Type: ApplicationFiled: September 24, 2003Publication date: October 14, 2004Applicant: Cell Therapeutics, Inc.Inventors: Rama Bhatt, Baoqing Gong, Feng Hong, Scott A. Jenkins, J. Peter Klein, Cory T. Kohm, John Tulinsky
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Publication number: 20040192910Abstract: Compounds of Formula I (I) wherein the substituents are as defined in claim 1, and the agrochemically tolerable salts and all stereoisomers and tautomers of the compounds of formula I, are suitable for use as herbicides.Type: ApplicationFiled: February 26, 2004Publication date: September 30, 2004Inventors: Christoph Luthy, Andrew Edmunds
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Publication number: 20040186118Abstract: This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseasesType: ApplicationFiled: November 28, 2003Publication date: September 23, 2004Inventors: Judi Bryant, Monica J. Kochanny, Shendong Yuan, Seock-Kyu Khim, Brad O. Buckman, Damian O. Arnaiz, Ulf Bomer, Hans Briem, Peter Esperling, Christoph Huwe, Joachim Kuhnke, Martina Schafer, Lars Wortmann, Dirk Kosemund, Emil Eckle, Richard J. Feldman, Gary B. Phillips
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Publication number: 20040167140Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or 5-fluoro]-2′,3′-dideoxy-2′,3′-didehydro-pyrimidine nucleoside or a [5-carboxamido or 5-fluoro]-3′-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.Type: ApplicationFiled: January 16, 2004Publication date: August 26, 2004Applicant: Emory UniversityInventors: Raymond F. Schinazi, Dennis C. Liotts
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Patent number: 6777420Abstract: The invention provides heterocyclic organic compounds that inhibit bacterial DNA polymerase IIIC and type II bacterial topoisomerase. The invention further provides compounds that are useful as intermediates in the synthesis of such heterocyclic organic compounds. Syntheses and uses of such heterocyclic organic molecules are also described.Type: GrantFiled: June 17, 2002Date of Patent: August 17, 2004Assignee: Microbiotix, Inc.Inventors: Chengxin Zhi, George E. Wright
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Publication number: 20040132718Abstract: The present application describes monocyclic or bicyclic carbocycles and heterocycles and derivatives thereof of Formula I: 1Type: ApplicationFiled: December 8, 2003Publication date: July 8, 2004Inventors: Irina C. Jacobson, Ruth R. Wexler, Suanne Nakajima, Mimi L. Quan, Shuaige Wang, Joanne M. Smallheer, Jennifer X. Qiao
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Publication number: 20040122031Abstract: The present invention relates to a thiazolidinedione derivative, represented in formula (1) below, pharmaceutically acceptable salts thereof, and/or pharmaceutically acceptable solvates thereof.Type: ApplicationFiled: July 3, 2003Publication date: June 24, 2004Inventors: Chung-ll Hong, Soon-Kil Ahn, Bok-Young Kim, Joong-Bok Ahn, Do-Young Lee, Hong-Woo Lee, Jae-Soon Shin
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Publication number: 20040101892Abstract: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.Type: ApplicationFiled: August 15, 2003Publication date: May 27, 2004Applicant: Affymetrix, INC.Inventors: Glenn H. McGall, Anthony D. Barone
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Publication number: 20040097525Abstract: Pyrimidone compounds of formula (I): 1Type: ApplicationFiled: October 27, 2003Publication date: May 20, 2004Applicant: SmithKline Beecham plcInventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
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Publication number: 20040092538Abstract: The present invention relates to a class of compounds represented by the Formula I 1Type: ApplicationFiled: December 20, 2002Publication date: May 13, 2004Inventors: Srinivasan R. Nagarajan, Ish Kumar Khanna, Michael Clare, Alan Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu, Yu Yi, Renee M. Huff, Bipinchandra N. Desai, Balekudru Devadas, Mihir D. Parikh, Thomas Penning
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Publication number: 20040087601Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed.Type: ApplicationFiled: January 10, 2003Publication date: May 6, 2004Inventors: Shawn David Erickson, John J. Baldwin, Roland Ellwood Dolle, James Inglese, Michael H.J. Ohlmeyer, Koc-Kan Ho, Adolph C. Bohnstedt, Steven G. Kultgen, Paolo Giovanni Martino Conti, Dirk Leysen, Jaap van der Louw
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Publication number: 20040082475Abstract: A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of the formula (I) and of their use as herbicides.Type: ApplicationFiled: July 24, 2003Publication date: April 29, 2004Inventors: Michael Gerhard Hoffman, Hendrik Helmke, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
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Publication number: 20040077669Abstract: Pyrimidine compounds of formula (1): 1Type: ApplicationFiled: February 11, 2003Publication date: April 22, 2004Inventors: Hajime Mizuno, Noriyasu Sakamoto, Yoshiharu Kinoshita
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Publication number: 20040077662Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: ApplicationFiled: May 2, 2003Publication date: April 22, 2004Applicant: Cytokinetics, Inc.Inventors: Han-Jie Zhou, David J. Morgans, Gustave Bergnes, Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Nicholas D. Adams
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Publication number: 20040072692Abstract: A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of formula (I) and of their use as herbicides.Type: ApplicationFiled: July 24, 2003Publication date: April 15, 2004Inventors: Michael Gerhard Hoffmann, Hendrik Helmke, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
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Patent number: 6716981Abstract: A process for the preparation of a 2,5-diamino-4,6-dihalopyrimidine of the formula: in which X is a halogen atom, comprising reacting 2,5-diamino-4,6-dihydroxypyrimidine or its salt of the formula: with a phosphorus oxyhalide and a quaternary ammonium halide or an amine in a halogenated hydrocarbon as a solvent.Type: GrantFiled: May 31, 2001Date of Patent: April 6, 2004Assignee: Lonza AGInventors: Elie Saikali, Walter Brieden
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Patent number: 6716838Abstract: The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: February 19, 2002Date of Patent: April 6, 2004Assignee: Pharmacia CorporationInventors: Michael S. South, Darin E. Jones, Melvin L. Rueppel
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Publication number: 20040063936Abstract: A pyrimidine derivative compound of formula (I) or a salt thereof and a method for the preparation thereof.Type: ApplicationFiled: June 25, 2003Publication date: April 1, 2004Inventors: Tsuneyuki Sugiura, Toshihide Horiuchi, Toru Miyazaki, Tsutomu Kojima, Shinsuke Hashimoto
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Publication number: 20040048884Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: February 6, 2003Publication date: March 11, 2004Applicant: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
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Patent number: 6693196Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein Y is CH or N and Z is H, OCH3, NH2 and alkyl of from 1 to 4 carbon atoms, with the proviso that when Y is N the 2,4-diaminophenoxy moieties are positioned at the 4 and 6 positions on the pyrimidine ring.Type: GrantFiled: January 18, 2002Date of Patent: February 17, 2004Assignee: The Procter & Gamble CompanyInventors: Mu-III Lim, Yuh-Guo Pan, James S. Anderson
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Publication number: 20040023966Abstract: A pyrimidinylbenzimidazole or triazinylbenzimidazole derivative represented by the general formula (I): 1Type: ApplicationFiled: March 10, 2003Publication date: February 5, 2004Applicant: KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Masaru Shibata, Kiyoshi Kawai, Takechi Makihara, Norihisa Yonekura, Takehiro Kawashima, Junetsu Sakai, Norimichi Muramatsu
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Patent number: 6683086Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.Type: GrantFiled: May 13, 2002Date of Patent: January 27, 2004Assignee: ARYx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
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Patent number: 6683151Abstract: The invention relates to a compound comprising a reaction product of (A) an isocyanate functional compound of which at least 40 wt. %, relative to the total amount of (A), has a molecular weight of at least about 500, and (B) a nitrogen-containing compound capable of reacting with said isocyanate functional compound (A). The reaction product has a molecular weight of less then about 20,000 and comprises an effective amount of groups that are able to form reversible intermolecular physical interactions such that a resulting compound shows polymeric mechanical properties at a temperature below a transition temperature. The nitrogen-containing compound is, for instance, melamine, urea, acetoguanamine, benzoguanamine, cyanamide, dicyanamide, thiourea, isocytosine, pyrimidone or aminopyridine. The supramolecular compound comprising a suitable amount of the reaction products exhibits a relatively high elongation at break.Type: GrantFiled: February 24, 2000Date of Patent: January 27, 2004Assignee: DSM N.V.Inventors: Jacobus A. Loontjens, Johan E. G. A. Jansen, Bartholomeus J. M. Plum
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Publication number: 20030232813Abstract: The present invention relates to novel amino substituted pyrimidinone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel amino substituted pyrimidinone derivatives of the general formula (I) and a method thereof.Type: ApplicationFiled: April 9, 2003Publication date: December 18, 2003Applicant: ORCHID CHEMICALS & PHARMACEUTICALS LIMITEDInventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
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Publication number: 20030220359Abstract: The invention relates to novel aryl-ethene-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: ApplicationFiled: January 3, 2003Publication date: November 27, 2003Inventors: Christoph Boss, Martin Bolli, Martine Clozel, Walter Fischli, Thomas Weller
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Patent number: 6653317Abstract: Hair growth-/hair loss-affecting cosmetic/therapeutic compositions contain an effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide having the structural formula (I): in which R1 is an alkyl radical having from 5 to 20 carbon atoms, and Z is either a hydrogen atom or a radical −OR2, wherein R2 is an alkyl radical having from 1 to 12 carbon atoms, or an acyl derivative or acid addition salt thereof.Type: GrantFiled: November 22, 2002Date of Patent: November 25, 2003Assignee: Societe l'Oreal S.A.Inventors: Yann Mahe, Jean-François Michelet, Patrick Pichaud, Jean-Baptiste Galey
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Patent number: 6653316Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: November 20, 2000Date of Patent: November 25, 2003Assignee: Pharmacia CorporationInventors: Michael S. South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones, Melvin L. Rueppel
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Publication number: 20030203851Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: ApplicationFiled: April 18, 2002Publication date: October 30, 2003Applicant: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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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: 6632821Abstract: Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or tri-alkyl-silyl, formyl or alkoxycarbonyl, wherein R1 groups are unsubstituted or substituted as defined in the specification; R2 represents phenyl, cycloalkyl or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which are unsubstituted or substituted; R3 represents hydrogen, halogen or alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; which are unsubstituted or substituted; R4 represents hydrogen or alkyl, alkenyl or alkynyl; which are unsubstituted or substituted; and X represents O, S, NR5 or a single bond, wherein R5 represents hydrogen or alkyl; or R1 and R5 together with the interjacent nitrogen atoType: GrantFiled: June 12, 2001Date of Patent: October 14, 2003Assignee: BASF AktiengesellschaftInventors: Klaus-Juergen Pees, Waldemar Pfrengle, Gavin Heffernan
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Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman