Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/318)
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Patent number: 6124306Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R.sub.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; andR.sub.6 is --S--C.sub.1-6 alkyl (preferably --SCH.sub.3);The compounds of Formula I are useful in the treatment of individuals who are HIV positive.Type: GrantFiled: September 21, 1998Date of Patent: September 26, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Joel Morris, Wade J. Adams, Janice M. Friis, Donn G. Wishka
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Patent number: 6121201Abstract: A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: ##STR1## wherein X, Y are independently hydrogen, halogen, cyano, nitro, or (C.sub.Type: GrantFiled: September 23, 1998Date of Patent: September 19, 2000Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Masamitsu Tsukamoto, Takahiro Haga
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Patent number: 6103898Abstract: Cyclic urea derivatives of the formula I ##STR1## in which X, X', Y, Y' and Z can have various meanings, are prepared by a) reacting a urea derivative of the formula II ##STR2## with a diketone of the formula III ##STR3## and b) hydrogenating the product from step a) in the presence of a metal-containing catalyst.Type: GrantFiled: September 28, 1998Date of Patent: August 15, 2000Assignee: BASF AktiengesellschaftInventors: Andreas Kramer, Wolfgang Siegel
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Patent number: 6083951Abstract: Pyrimidine sulphonamide compounds of the following formula, ##STR1## wherein Q is a naphthyl or biphenyl group either unsubstituted or substituted with A.sup.1, and where A.sup.1, R.sup.1 and R.sup.2 are a variety of alkyl, aryl and cyclic moieties, as described in the specification hereof, which compounds are useful for the treatment of diseases or medical conditions such as hypertension, pulmonary hypertension, cardiac or cerebral circulatory disease and renal disease.Type: GrantFiled: December 14, 1998Date of Patent: July 4, 2000Assignee: Zeneca LimitedInventor: Robert Hugh Bradbury
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Patent number: 6066734Abstract: Chloropyrimidine compounds, such as 4,6-dichloro-2-ethoxypyrimidine, were prepared in good yield and good purity from the corresponding hydroxypyrimidine compounds in the absence of organic solvents and with a reduced amount of phosphorus oxychloride by carrying out the reaction in the presence of a trialkylamine compound and phosphorus trichloride. The additions of hydroxypyrimidine compound and trialkylamine compound could be made in segments. The chloropyrimidine compounds produced were recovered in an improved manner by adding chlorine to convert the chlorophosphoric acid by-products and phosphorus trichloride to phosphorus oxychloride, diluting the mixture with additional chloropyrimidine compound and removing the phosphorus oxychloride by distillation, combining the residue with water and a base, distilling the trialkylamine compound from the resulting mixture, and removing the aqueous phase.Type: GrantFiled: December 18, 1998Date of Patent: May 23, 2000Assignee: Dow AgroSciences LLCInventors: Ronald B. Leng, Julie L. Maurer, James W. Ringer
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Patent number: 6051709Abstract: The invention relates to a diastereoselective process for the preparation of compounds of formula (I), wherein W is S, S.dbd.O, SO.sub.2 or O; X is S, S.dbd.O, SO.sub.2 or O; R.sub.1 is hydrogen or acyl, and R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof.Type: GrantFiled: December 24, 1996Date of Patent: April 18, 2000Assignee: Glaxo Group LimitedInventors: Michael David Goodyear, P. Owen Dwyer, Malcolm Leithead Hill, Andrew Jonathan Whitehead, Roy Hornby, Peter Hallett
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Patent number: 6043248Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sub.4 is selected from the group consisitng of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase.Type: GrantFiled: October 17, 1997Date of Patent: March 28, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Gary J. Cleek, David R. Graber
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Patent number: 6039683Abstract: Compounds of the following formula useful for inhibiting Ras function and therefore inhibiting or treating the abnormal growth of cells are disclosed: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R and R.sup.2 are halo;R.sup.1 and R.sup.3 are H and halo, provided that at least one is H;W is N, CH or C when the double bond is present at the C-11 position;R.sup.4 is --(CH.sub.2).sub.n --R.sup.5 or ##STR2## R.sup.5 is ##STR3## R.sup.6 is R.sup.5 or ##STR4## Z.sup.1 and Z.sup.2 are independently selected from the group consisting of .dbd.O and .dbd.S;n is 1-6; andn.sub.1 is 0 or 1.Type: GrantFiled: September 29, 1998Date of Patent: March 21, 2000Assignee: Schering CorporationInventors: F. George Njoroge, Bancha Vibulbhan, Patrick A. Pinto, Viyyoor M. Girijavallabhan
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Patent number: 6025491Abstract: Onium salts of taxo-diterpenoid-C.sup.n, 2-0-aza-arenes are employed as water soluble prodrugs. For example, taxol-2'-methylpyridiniumtosylate (MPT) is characterized by an elevated aqueous solubility, rapid activation by serum protein, good stability in most other aqueous solutions, formation of a protein:taxol intermediate and good retension within the circulatory system. The toxicity of the activated form is comparable or greater than underivatized taxol. Furthermore, taxol-2'-MPT can be synthesized by a simple one step reaction between taxol and 2-fluoro-1-MPT. The invention is applicable to taxol and taxol mimetics having hydroxyls that are reactive with onium salts of 2-halogenated-aza-arenes. For example, taxol, C-2 substituted analogs of taxol, and Taxotere each have reactive hydroxyls at the 2' and 7 positions. The invention is also applicable to a wide array of 2-halogenated-aza-arenes.Type: GrantFiled: December 14, 1998Date of Patent: February 15, 2000Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Wolfgang Wrasidlo, Rodney K. Guy, Emmanuel Pitsinos
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Patent number: 6022968Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)3,4,5,6 tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.Type: GrantFiled: August 18, 1997Date of Patent: February 8, 2000Assignee: Pfizer IncInventors: Thomas G. LaCour, Charles William Murtiashaw, III
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Patent number: 6020491Abstract: Cyclic amine monomers and polymers and N-halamine biocidal polymer compounds are provided. Representative monomers have the structure: ##STR1## wherein R.sup.1 is selected from the group consisting of hydrogen and from C.sub.1 to C.sub.4 alkyl; R.sup.10 is a bond or parasubstituted phenyl; and R.sup.11 is cyclic amine unit of a 5- to 6-membered heterocyclic ring selected from the group consisting of: (a) 1,3,5-triazine-2,4-dione; (b) 3,4,5,6-tetrahydro(1H)pyrimidin-2-one; and (c) 2-oxazolidinone; R.sup.10 is attached to a linkage carbon of R.sup.11, wherein said linkage carbon of R.sup.11 is a carbon located on the ring of R.sup.11 and is substituted with a substituent selected from the group consisting of C.sub.1 -C.sub.4 alkyl, benzyl, and alkyl-substituted benzyl; from 0 to 2 non-linkage carbon members are a carbonyl group; and from 0 to 1 non-linkage carbon member is substituted with a moiety selected from the group consisting of C.sub.1 -C.sub.Type: GrantFiled: July 7, 1998Date of Patent: February 1, 2000Assignee: Auburn UniversityInventors: Shelby D. Wonley, Gang Sun, Wanying Sun, Tay-Yuan Chen
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Patent number: 6017923Type: GrantFiled: May 31, 1996Date of Patent: January 25, 2000Assignee: Hoechst Marion Roussel, Inc.Inventors: Jeffrey S. Sabol, Sai P. Sunkara, Shawn C. Miller
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Patent number: 6013651Abstract: The present invention is directed to compounds of the formula ##STR1## and pharmaceutically acceptable salts and isomers thereof.Type: GrantFiled: March 4, 1998Date of Patent: January 11, 2000Assignee: G. D. Searle & Co.Inventors: Thomas E. Rogers, Peter G. Ruminski
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Patent number: 6005096Abstract: A compound having the structure ##STR1## wherein R.sup.1 is H or a linker group; R.sup.24 is independently halo or C.sub.1 -C.sub.2 haloalkyl;R.sup.25 is independently --SH, --OH, .dbd.S or .dbd.O;A is independently N or C; andM, taken together with the radical --A--C(--R.sup.25), completes an aryl or heteroaryl ring structure comprising 5 or 6 ring atoms wherein the heteroaryl ring comprises a single O ring heteroatom, a single N ring heteroatom, a single S ring heteroatom, a single O and a single N ring heteroatom separated by a carbon atom, a single S and a single N ring heteroatom separated by a carbon atom, 2 N ring heteroatoms separated by a carbon atom, or 3 N ring heteroatoms at least two of which are separated by a carbon atom, and wherein the aryl or heteroaryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R.sup.6 ;R.sup.6 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, NO.sub.Type: GrantFiled: May 8, 1995Date of Patent: December 21, 1999Assignee: Gilead Sciences, Inc.Inventors: Mark Matteucci, Robert J. Jones, Kuei-Ying Lin
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Patent number: 5981537Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sup.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.Type: GrantFiled: May 9, 1996Date of Patent: November 9, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Fritz Reusser, Gary J. Cleek, Irene W. Althaus
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Patent number: 5977367Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.Type: GrantFiled: January 9, 1998Date of Patent: November 2, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5972949Abstract: There are disclosed novel ether compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen or the like; A is a group of the general formula: ##STR2## B is a group of the general formula: ##STR3## and X is oxygen or sulfur; and harmful-organism controlling agents containing them as active ingredients.Type: GrantFiled: October 16, 1998Date of Patent: October 26, 1999Assignee: Sumito Chemical Co., Ltd.Inventors: Akira Shuto, Hirosi Kisida, Toru Tsuchiya, Yoji Takada, Hiroaki Fujimoto
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Patent number: 5945406Abstract: Compounds of formula (I): ##STR1## wherein: R is halogen;Y is hydrogen, NH.sub.2, SH or OH;X is: ##STR2## wherein: either R.sub.1 or R.sub.2 is a bond, with the other being hydrogen;either R.sub.3 or R.sub.4 is hydrogen, with the other being hydrogen, OH, OAc or NHAc;R.sub.5 is OH or OAc;either R.sub.7 or R.sub.8 is hydrogen, with the other being OH or OAc;R.sub.9 is hydrogen, CH.sub.2 OH or CH.sub.2 OAc;with the proviso that when R.sub.4 is OH, OAc or NHAc then R.sub.8 is hydrogen;and enantiomers of such compounds, are disclosed. Pharmaceutical formulations comprising such compounds, their use in the treatment of various disease states, and methods of treatment employing the compounds are also provided.Type: GrantFiled: December 23, 1997Date of Patent: August 31, 1999Assignee: Oxford Glycosciences (UK) Ltd.Inventor: Stephen Martin Courtney
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Patent number: 5942516Abstract: Novel pyridines, pyrimidines, pyrazines, pyridazines and triazines, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: GrantFiled: September 27, 1996Date of Patent: August 24, 1999Inventors: John Duncan Elliott, Deborah Lynne Bryan
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Patent number: 5935968Abstract: The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: ##STR1## to the subject. The present invention further provides for a method for improving fertility and the response to in vitro fertilization (I.V.F.), comprising administration of therapeutically effective amount of compound of structural formula I to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating polycystic ovary syndrome or for improving fertility or the response to in vitro fertilization (I.V.F.).Type: GrantFiled: March 12, 1998Date of Patent: August 10, 1999Assignee: Merck & Co., Inc.Inventors: Joanne Waldstreicher, Georgianna S. Harris
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Patent number: 5932730Abstract: Carboxylic acid derivatives ##STR1## where R-R.sup.6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: March 27, 1997Date of Patent: August 3, 1999Assignee: BASF AktiengesellschaftInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: 5929082Abstract: The invention provides novel sulphonylurea, sulphonylthiourea and sulphonylguanidine compounds which have the ability to block potassium ion channels regulated by intracellular concentrations of ATP. Methods of synthesis, pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes, cardiac arrhythmias, ischaemic and hypoxic cardiovascular incidents, and cancers are also claimed.Type: GrantFiled: January 23, 1998Date of Patent: July 27, 1999Assignees: Polychip Pharmaceuticals Pty Ltd, The University of SydneyInventors: Noel John Chambers, Graham Allen Ross Johnston
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5877312Abstract: This invention relates to methods for preparing alkylating agents and use of the agents prepared. In particular, this invention relates to preparation methods for hydroxy halide and organooxy halide alkylating agents and their use for alkylating cyclic urea compounds.Type: GrantFiled: December 31, 1996Date of Patent: March 2, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Prabhakar Kondaji Jadhav, George Clautice Emmett, Michael Ernest Pierce
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Patent number: 5866036Abstract: Chiral nonracemic molecules which are useful as high tilt, high polarization and/or high birefringence FLC materials or are useful as components of such FLC materials and which have the following general structure are provided:RO--(Ph.sub.1).sub.m --(A).sub.a --(Ph.sub.2).sub.n --(B).sub.b --(Ph.sub.3).sub.p --Twhere Ph.sub.1, Ph.sub.2 and Ph.sub.Type: GrantFiled: February 2, 1994Date of Patent: February 2, 1999Assignee: Displaytech, Inc.Inventors: Michael D. Wand, Rohini T. Vohra, David M. Walba, Sean D. Monahan
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Patent number: 5861421Abstract: This invention relates to derivatives of 4,4-(disubstituted)cyclohexan-1-ones and related compounds which are useful for treating allergic and inflammatory diseases.Type: GrantFiled: June 23, 1997Date of Patent: January 19, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5846906Abstract: Herbicidally active phenyldiketone compounds of the formula I ##STR1## in which the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.4 -alkoxy, it being possible for these groups to be unsubstituted or substituted by one to five halogen atoms or C.sub.1 -C.sub.4 -alkoxy, or halogen, cyano, nitro, a group --(Y).sub.n --S(O).sub.m R.sup.7 or a group --(Y).sub.n --CO--R.sup.8,Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical which has one to three hetero atoms selected from the group consisting of oxygen, sulfur or nitrogen and which is unsubstituted or substituted by halogen, cyano, nitro, a group --CO--R.sup.8, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, di-C.sub.1 -C.sub.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 5846907Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
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Patent number: 5847149Abstract: Thiadiazole derivatives of the formula (I)X-B-A.sup.1 -(M.sup.1 -A.sup.2 -).sub.m (M.sup.2 -A.sup.3).sub.n -R.sup.1(I )in which the symbols and indices have the following meanings:X is Cl, Br or I;B is 1,3,4-thiadiazole-2,5-diyl;A.sup.1, A.sup.2 and A.sup.3 are identical or different and are substituted or unsubstituted 1,4-phenylene, pyrazine-2,5-diyl, pyridazine-3,6-diyl, pyridine-2,5-diyl, pyrimidine-2,5-diyl, trans-1,4-cyclohexylene, 1,3,4-thiadiazole-2,5-diyl, 1,3-dioxane-2,5-diyl, 1,3-dithiane-2,5-diyl, 1,3-thiazole-2,4-diyl, 1,3-thiazole-2,5-diyl, thiophene-2,4-diyl, thiophene-2,5-diyl, piperazine-1,4-diyl, piperazine-2,5-diyl, naphthalene-2,6-diyl, bicyclo?2.2.2!octane-1,4-diyl, or 1,3-dioxaborinane-2,5-diyl;M.sup.1 and M.sup.2 are identical or different and are --CO--O--, --O--CO--, --O--CO--O--, --O--CS--O--, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or a single bond;R.sup.Type: GrantFiled: July 16, 1996Date of Patent: December 8, 1998Assignee: Hoechst AktiengesellschaftInventors: Robert Walter Fuss, Javier Manero, Hubert Schlosser, Rainer Wingen
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Patent number: 5840892Abstract: A novel process for the preparation of substituted pyrimidine derivatives of the general formula: ##STR1## in which a halopyrimidine is reacted in the presence of a sulfinate with a compound selected from the series: ##STR2## The compounds of the general formula I are precursors of, for example, compounds with herbicidal activity.Type: GrantFiled: April 8, 1997Date of Patent: November 24, 1998Assignee: Lonza AGInventors: Yves Bessard, Gerhard Stucky
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Patent number: 5834468Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.Type: GrantFiled: July 2, 1996Date of Patent: November 10, 1998Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5792868Abstract: Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar.Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.Type: GrantFiled: March 18, 1994Date of Patent: August 11, 1998Assignee: Ajinomoto Co., Inc.Inventors: Kunisuke Izawa, Yoshihito Koguchi, Hiroshi Shiragami
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Patent number: 5786472Abstract: The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a .beta.-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu.sub.2 O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.Type: GrantFiled: December 12, 1996Date of Patent: July 28, 1998Assignee: Merck & Co., Inc.Inventors: Essa Hsinyi Hu, Daniel R. Sidler, Ulf H. Dolling, Michael A. Patane
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Patent number: 5777118Abstract: Cyclic acetals of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 and R.sup.2 are hydrogen, unsubstituted or substituted alkyl or phenyl; additionally R.sup.1 and R.sup.2 together are an unsubstituted or substituted C.sub.2 -C.sub.6 -alkylene chain;Y is oxygen or sulfur;A has the meaning as given in claim 1;a process for preparing the acetals I and their use for the production of crop protection compositions are described.Type: GrantFiled: July 12, 1996Date of Patent: July 7, 1998Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Hartmann Konig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5753594Abstract: 3-Halo-3-hetarylcarboxylic acid derivatives having the formula I ##STR1## in which R is a formyl group, a group CO.sub.2 H or a radical which can be hydrolyzed to COOH, and the remaining substituents have the following meanings:R.sup.2 and R.sup.3 are halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy or C.sub.1 -C.sub.4 -alkylthio;X is nitrogen or CR.sup.13, where R.sup.13 is hydrogen or together with R.sup.3 forms an alkylene or alkenylene chain in which in each case one methylene group is replaced by oxygen;R.sup.4 is an unsubstituted or substituted five- or six-membered heteroaromatic ring which contains one to three nitrogen atoms and/or one sulfur or oxygen atom;R.sup.5 is hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl or phenyl;Y is sulfur, oxygen or a single bond; andZ is halogen.The derivatives I having herbicidal and plant-growth regulating properties.Type: GrantFiled: December 1, 1995Date of Patent: May 19, 1998Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Albrecht Harreus, Matthias Bratz, Joachim Rheinheimer, Uwe Josef Vogelbacher, Hans Theobald, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen, Wilhelm Rademacher
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Patent number: 5746946Abstract: The invention relates to imidazolidinone derivatives formed from the reaction of (1) a substituted-ethyl imidazolidinone; (2) substituted ethyl/propyl propylene urea or (3) a cyclic propylene urea with: (a) a C.sub.1 -C.sub.24 alkyl or a C.sub.3 -C.sub.24 alkenyl substituted anhydride or, (b) a C.sub.3 -C.sub.24 carboxylic acid or corresponding ester; their compositions and use as corrosion inhibitors and/or surfactants.Type: GrantFiled: December 26, 1996Date of Patent: May 5, 1998Assignee: King Idustries, Inc.Inventors: Zhigiang Alex He, Werner Joseph Blank
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Patent number: 5747423Abstract: The novel 6-thienyl pyridines and 4-thienyl pyrimidines of formula I: ##STR1## (A, R.sub.1 to R.sub.5 and Z are defined in the specification) show selective herbicidal activity.The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.Type: GrantFiled: July 15, 1996Date of Patent: May 5, 1998Assignee: American Cyanamid CompanyInventors: Stefan Scheiblich, Thomas Maier, Helmut Siegfried Baltruschat, Joseph Luke Pont
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Patent number: 5733920Abstract: The invention provides novel inhibitors of cyclin-dependent kinases, in particular inhibitors of the CDK/cyclin complexes such as CDK4/cyclin D1. The novel compounds are analogs of chromones. These compounds can be used for inhibiting excessive or abnormal cell proliferation. Thus, the novel compounds are useful for treating a subject with a disorder associated with excessive cell proliferation, such as cancer.Type: GrantFiled: October 31, 1995Date of Patent: March 31, 1998Assignee: Mitotix, Inc.Inventors: Muzammil M. Mansuri, Krishna K. Murthi, Kollol Pal
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Patent number: 5728706Abstract: A benzenesulfonamide derivative of the formula ?I!: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.Type: GrantFiled: April 24, 1996Date of Patent: March 17, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
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Patent number: 5723610Abstract: Disclosed in this invention are the phenylpyrimidine derivatives represented by the general formula I: ##STR1## the alcohols represented by the formula: ##STR2## usable as starting material for the preparation of the phenylpyrimidine derivatives, and the processes for preparing such derivatives. The phenylpyrimidine derivatives of the formula I according to the present invention have very excellent properties as a liquid crystal compound and can be utilized effectively for the production of liquid crystal elements.Type: GrantFiled: April 12, 1996Date of Patent: March 3, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Takayuki Higashii, Masayoshi Minai, Isao Kurimoto, Shoji Toda, Takeshi Tani, Chizu Sekine, Koichi Fujisawa
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Patent number: 5723473Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.Type: GrantFiled: April 11, 1995Date of Patent: March 3, 1998Assignee: Zeneca LimitedInventor: Brian Leslie Pilkington
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Patent number: 5719158Abstract: Compounds of the Formula I ##STR1## are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: June 5, 1995Date of Patent: February 17, 1998Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek von Langen
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Patent number: 5698137Abstract: A 2H-5,6-optically active dihydropyran derivative represented by the general formula (I) or (I'): ##STR1## wherein Rf represents a fluoroalkyl group having 1 or 2 carbon atoms; a liquid crystal composition and a liquid crystal device comprising the derivative; and a racemic mixture comprising at least one type of the derivative. The derivative is a novel compound which exhibits the liquid crystal property by itself or can be used as an excellent dopant providing a high speed response to a composition comprising it even when the compound does not exhibit the liquid crystal property by itself. The derivative also exhibits a large spontaneous polarization.Type: GrantFiled: April 15, 1996Date of Patent: December 16, 1997Assignee: Kashima Oil CompanyInventors: Tatsushi Ishizuka, Mitsunori Takeda, Masaaki Namekawa, Keizou Itoh
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Patent number: 5696265Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.Type: GrantFiled: June 7, 1995Date of Patent: December 9, 1997Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.Inventors: Choung Un Kim, John C. Martin, Bing Uh Luh, Peter F. Misco
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Patent number: 5693798Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.Type: GrantFiled: June 7, 1995Date of Patent: December 2, 1997Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.wInventors: Choung Un Kim, John C. Martin, Bing Uh Luh, Peter F. Misco
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Patent number: 5691369Abstract: The cyclic ureas, and the pharmaceutically-acceptable salts and esters thereof, of the present invention are useful as antiarrhythmic and antifibrillatory agents and have the following general structure: ##STR1## wherein X, Y, A, L, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are defined as in the Specification.Type: GrantFiled: June 7, 1995Date of Patent: November 25, 1997Assignee: The Proctor & Gamble CompanyInventors: Stanford Salvatore Pelosi, Jr., Chia-Nien Yu
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Patent number: 5686611Abstract: Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A compound of formula (VI) ##STR2## wherein X is halogen, Y is S-phenyl, Se-phenyl or halogen and B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, 2-acetamido-6-diphenylcarbamoylpurine, 6-N-dimethylamino-methyladenine or 6-N-pivaloyladenine.Type: GrantFiled: June 7, 1995Date of Patent: November 11, 1997Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.Inventors: Choung Un Kim, John C. Martin, Bing Uh Luh, Peter F. Misco
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Patent number: 5684198Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.Type: GrantFiled: August 23, 1996Date of Patent: November 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
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Patent number: 5679792Abstract: Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are, for example, an alkyl chain,A is a mesogenic group, andM is a spacer group,are highly suitable as components of liquid-crystal mixtures.Type: GrantFiled: June 1, 1995Date of Patent: October 21, 1997Assignee: Hoechst AktiengesellschaftInventors: Claus Escher, Gerhard Illian, Hubert Schlosser, Rainer Wingen
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Patent number: 5672710Type: GrantFiled: November 3, 1995Date of Patent: September 30, 1997Assignee: AllerganInventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna