Unsubstituted Or Hydrocarbyl Substituted Only, Or Salt Thereof Patents (Class 546/348)
-
Patent number: 6399821Abstract: The invention concerns a method of sulphonation characterised in that it consists in contacting a nucleophile whose nucleophilic atom is a nitrogen atom with a reagent comprising by successive or simultaneous addition: a heavy sulphonyl halide (i.e. whose atomic number is not less than that of chlorine), advantageously suphonyl chloride; and an organic base both not capable of alkylation and lipid soluble; and the organic part of said sulphonyl is perfluorinated on the carbon carried by the sulphur. The invention is applicable to organic synthesis.Type: GrantFiled: August 7, 2001Date of Patent: June 4, 2002Assignee: Rhodia ChimieInventors: Virginie Pevere, Emmanuel Marx, Laurent Gilbert
-
Patent number: 6399820Abstract: The present invention relates to a process and a reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function. This persulphonylation process is characterized in that it comprises a step of placing a nucleophile, whose nucleophilic atom is a nitrogen, in contact with a reagent comprising, for successive or simultaneous addition, a heavy halide of sulphonyl, advantageously sulphonyl chloride, and an organic base comprising a trivalent atom from column V whose lone pair is conjugated directly or indirectly to a bond, and in that the organic part of the said sulphonyl is perhalogenated, advantageously perfluorinated, on the carbon borne by the sulphur. Application to the synthesis of intermediates for organic chemistry.Type: GrantFiled: May 15, 2001Date of Patent: June 4, 2002Assignee: Rhodia ChimieInventors: Jean-Roger Desmurs, Andr{dot over (e)} Millet, Virginie Pevere
-
Patent number: 6392050Abstract: The invention relates to a process for preparing substituted pyridines in a simple and cost-effective manner in good yields by reacting substituted 1,4-dihydropyridines with methyl nitrite in the presence of an acid that contains less than 20% by weight of oxidizing components.Type: GrantFiled: June 4, 2001Date of Patent: May 21, 2002Assignee: Bayer AktiengesellschaftInventors: Norbert Lui, Hans Panskus, Albert Schnatterer
-
Publication number: 20020058811Abstract: Compounds of formula (1) where R1 is of formulae (II), (III), or (IV), or (V); R2 is —R4, —O—R4, —O—S(O)2—R4, —NR4R5, R4—(CH2)b—NH(C═X)—(CH2)c—, R4—(CH2)b—O(C—O)NH—(CH2)c—(C═O)NH—, R4—(C═O)NH—(C═O)NH—, —(CH2)b—NH(C═X)—(CH2)c—R4, R4—(CH2)b—O(C═O)CH2)c—, —(CH2)b—O(C═O)—(CH2)c—R4, —NH(C═X)NH—R4, R4—O(C═O)O—, —O(C═O)NH—R4, R4—O(C═O)NH—, —(CH2)b—(C═O)—(CH2)c—R4, —NH—S(O)2—R4, —C(OH)R4R5, —CH(OH)—R4, —(C═O)—NR4, —CN, —NO2, substituted C1 to C6 alkyl, substituted or unsubstituted C1 to C6 alkenyl, or substituted or unsubstituted C1 to C6 alkynyl, said substituted moieties substituted with a moiety of the formulae —R4, —R4R5, &mdType: ApplicationFiled: December 3, 2001Publication date: May 16, 2002Inventors: Bertrand L. Chenard, John E. Macor, Barbara E. Segelstein
-
Patent number: 6365744Abstract: A process for producing a pyridine derivative, which comprises reacting an azametallacyclopentadiene represented by formula (1) with an alkyne in an organic solvent containing a complex of a transition metal such as Ni(II). (In formula (1), M represents an early transition metal, e.g., Zr, Ti or Hf; L represents cyclopentadienyl, indenyl, fluorenyl, hydrocarbon-oxy, amide, acetylacetonato, or carboxy group, a phosphine ligand, an amine ligand, an ether ligand, or a ligand comprising two or more these bonded to each other through appropriate crosslinking group; n is an integer of 1 to 4; and R1, R2, R3, R4 and R5 each represents C1-20 (substituted) alkyl, alkenyl, an aromatic group, silyl, alkoxy, or an ester group.Type: GrantFiled: November 9, 2000Date of Patent: April 2, 2002Assignee: Japan Science & Technology CorporationInventor: Tamotsu Takahashi
-
Patent number: 6362009Abstract: Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.Type: GrantFiled: November 21, 1997Date of Patent: March 26, 2002Assignee: Merck & Co., Inc.Inventors: Benito Munoz, Chixu Chen
-
Patent number: 6362193Abstract: Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.Type: GrantFiled: April 7, 2000Date of Patent: March 26, 2002Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ravi Garigipati
-
Publication number: 20020032211Abstract: Dihydronaphthalene compounds have excellent 17&agr;-hydroxylase/C17-20-lyase inhibiting activity, thromboxan A2 synthesis inhibiting activity, and aromatase inhibiting activity and are thereby are useful as preventive and/or therapeutic agents for various male sex hormone- and female sex hormone-dependent diseases such as prostate cancer, prostatomegaly, masculinization, breast cancer, mastopathy, uterine cancer, endometriosis, and ovarian cancer, as well as myocardial infarction, angina pectoris, and bronchial asthma.Type: ApplicationFiled: May 25, 2001Publication date: March 14, 2002Inventors: Rolf Wolfgang Hartmann, Bertil Wachall, Makoto Yoshihama, Masamichi Nakakoshi, Shin Nomoto, Yoshikazu Ikeda
-
Patent number: 6355806Abstract: Compounds of the formula wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.Type: GrantFiled: September 16, 1999Date of Patent: March 12, 2002Assignee: Allergen Sales, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
-
Patent number: 6352566Abstract: Ethers of polyalkyl or polyalkenyl N-hydroxyalkyl succinimides having the formula: or a fuel soluble salt thereof; wherein R is a polyalkyl or polyalkenyl group having an average molecular weight in the range of about 450 to about 5,000; n is an integer from 2 to 5; and Z is a moiety selected from the group consisting of wherein R1 is a hydroxy, nitro, cyano or —(CH2)x—NR3R4, wherein R3 and R4 are independently hydrogen or lower alkyl of 1 to 6 carbon atoms and x is 0 or 1; and R2 is hydrogen, hydroxy, nitro, cyano or —(CH2)y—NR5R6, wherein R5 and R6 are independently hydrogen or lower alkyl of 1 to 6 carbon atoms and y is 0 or 1. The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: September 1, 2000Date of Patent: March 5, 2002Assignee: Chevron Chemical Company LLCInventor: Richard E. Cherpeck
-
Patent number: 6313132Abstract: The invention relates to novel compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary tract incontinence, and methods for preparing the compounds of Formula (I).Type: GrantFiled: September 27, 1999Date of Patent: November 6, 2001Assignee: Pharmacia ABInventors: Rolf Johansson, Martin Haraldsson, Erik Ringberg, Ian Vagberg, Katarina Beierlein, Rikard Emond, Birger Sjoberg
-
Patent number: 6288009Abstract: The invention provides novel mepiquat plant growth regulator compositions which have improved hygroscopicity and corrosion characteristics. The novel mepiquat plant growth regulator compositions of the invention can be readily prepared from technical mepiquat chlorid inter alia by electrochemical ion exchange processes or by quaternization of N-methylpiperidine with dimethylcarbonate as starting material.Type: GrantFiled: April 10, 1998Date of Patent: September 11, 2001Assignees: BASF Corporation, BASF AktiengesellschaftInventors: Reiner Kober, David G. Hobbs, Scott W. Gibson, Kenneth Eugene Fersch, Wilhelm Rademacher, Jörg Botzem, Markus Frede, Matthias Dernbach, Reimer Göttsche, Reinhard Dötzer
-
Patent number: 6271248Abstract: Compounds of the formula wherein X, Y, R1, R2, R3, R4 and R5 are as described herein, inhibit the activity of endothelin.Type: GrantFiled: January 20, 2000Date of Patent: August 7, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, Joel C. Barrish, John Lloyd
-
Patent number: 6265609Abstract: The present invention relate to thio-substituted pentanedioic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders and prostate diseases.Type: GrantFiled: January 12, 1999Date of Patent: July 24, 2001Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Eric Wang, Barbara S. Slusher, Rena Lapidus
-
Patent number: 6262087Abstract: The present invention relates to substituted indane or dihydroindole compounds of Formula (I) wherein A is an indole. These compounds have high affinity for D4 receptors.Type: GrantFiled: June 21, 1999Date of Patent: July 17, 2001Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, Benny Bang-Andersen, Henrik Pedersen, Ivan Mikkelsen, Robert Dancer
-
Patent number: 6258133Abstract: A poly(oxyalkylene)pyridyl or piperidyl ether having the formula: wherein A is a nitrogen-containing ring selected from the group consisting of 3-pyridyl, 4-pyridyl, 3-piperidyl and 4-piperidyl; R1 and R2 are independently hydrogen or lower alkyl and each R1 and R2 is independently selected in each —O—CHR1—CHR2— unit; R3 is hydrogen, alkyl having 1 to about 100 carbon atoms, phenyl, aralkyl having about 7 to about 100 carbon atoms or alkaryl having about 7 to about 100 carbon atoms; n is an integer from about 5 to about 100; and x is an integer from 0 to 4. The poly(oxyalkylene)pyridyl and piperidyl ethers of the present invention are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: June 2, 1999Date of Patent: July 10, 2001Assignee: Chevron Chemical Company LLCInventor: Richard E. Cherpeck
-
Patent number: 6255291Abstract: A composition containing alph-alanine, adenosine compound and a glucan. Methods for treating cancer and immunological disorders with said composition.Type: GrantFiled: February 27, 1998Date of Patent: July 3, 2001Assignee: Peregrine Pharmaceuticals, Inc.Inventor: Yveta Germano
-
Patent number: 6255120Abstract: A combinatorial chemical library comprising a plurality of members of the Formula [S]—C(O)—L′-Z containing hydroxyamides is disclosed, in which [S] represents a solid support and L′-Z is a linker/compound residue. In this library, Z is and Y is —NR3R4 or —OR9. R3 and R4 are independently selected from the group consisting of H, alkyl, aralkyl, heteroarylalkyl, heterocycloalkyl, —CH(R5)CH(R6)OH, —CH(R5)C(O)NHR6 and —CH(R5)C(O)NHCH(R6)C(O)NHR7. R3 and R4 together are wherein X=O or NR8 and R9 is aryl, aralkyl or R7CH═CH(CH2){overscore (n)}. The combinatorial library can be optionally encoded with identifiers T′-L, which are covalently attached to the solid support. The methods of synthesizing such a library are described. The use of such library in assays to discover biologically active compounds is also disclosed.Type: GrantFiled: May 15, 1998Date of Patent: July 3, 2001Assignee: Pharmacopeia, Inc.Inventors: Roland Ellwood Dolle, III, Cullen Lee Cavallaro, Timothee Felix Herpin
-
Patent number: 6248893Abstract: Infrared radiation-sensitive compounds have been found that are represented by Structure DYE as follows: wherein R is a secondary or tertiary amine that contains no heterocyclic group, R1 and R2 are independently carbocyclic aromatic groups, and M+ is a monovalent cation. These compounds have a &lgr;max above 700 nm and are can be used in a number of photosensitive or heat-sensitive imaging materials.Type: GrantFiled: June 8, 2000Date of Patent: June 19, 2001Assignee: Eastman Kodak CompanyInventors: Kevin W. Williams, Shiying Zheng, Thap DoMinh
-
Patent number: 6245918Abstract: Process for the preparation of an ionic compound, Q+A− liquid at less than 150° C., wherein a trialkyloxonium of the anion is reacted with an amine in a hydrocarbon solvent. The aforesaid ionic compound can be used as a solvent in numerous catalytic reactions.Type: GrantFiled: June 1, 1999Date of Patent: June 12, 2001Assignee: Institut Francais du PetroleInventors: Hélène Olivier, Frédéric Favre
-
Patent number: 6224734Abstract: The invention provides novel mepiquat plant growth regulator compositions which have improved hygroscopicity and corrosion characteristics. The novel mepiquat plant growth regulator compositions of the invention can be readily prepared from technical mepiquat chlorid inter alia by electrochemical ion exchange processes or by quaternization of N-methylpiperidine with dimethylcarbonate as starting material.Type: GrantFiled: September 22, 1999Date of Patent: May 1, 2001Assignees: BASF Aktiengesellschaft, BASF CorporationInventors: Reiner Kober, David G. Hobbs, Scott W. Gibson, Kenneth Eugene Fersch, Wilhelm Rademacher, Jörg Botzem, Markus Frede, Matthias Dernbach, Reimer Göttsche, Reinhard Dötzer
-
Patent number: 6194599Abstract: The present invention provides a process for preparing biaryl compounds comprising reacting an arylzinc reagent with an arylchloride in the presence of a nickel catalyst or a palladium catalyst. The present invention specifically provides a process for the preparation of 2-(4′-methylphenyl)benzonitrile comprising reacting a 4-methylphenylzinc reagent with 2-chlorobenzonitrile in the presence of a nickel catalyst or a palladium catalyst.Type: GrantFiled: April 8, 1997Date of Patent: February 27, 2001Assignee: Catalytica, Inc.Inventors: Joseph A. Miller, Robert P. Farrell
-
Patent number: 6162810Abstract: A new family of inadone and tetralone tubulin-binding compounds (TBs) is disclosed. Unlike classical TBs, which inhibit mitosis among affected dividing cells, the TBs of the invention possess two unique properties: (1) they induce apoptosis among stationary phase (non-dividing) malignant cells, yet do not impair the viability of normal nonproliferating cells; and, (2) they affect cells which have acquired MDR more powerfully than they affect cells without MDR. Thus, the TBs of the invention provide means to target malignant cells for chemotherapy, even after previous therapies have failed, without affecting normal cells and tissues in the host.Type: GrantFiled: September 4, 1998Date of Patent: December 19, 2000Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Hsien C. Shih, Howard B. Cottam, Lorenzo Leoni
-
Patent number: 6162793Abstract: The compounds of formula (I): ##STR1## in which R is a hydrogen atom, an alkyl, optionally substituted by a halogen atom or a (CH.sub.2).sub.m Ar radical or a ##STR2## in which m represents an integer (1-8), n and p, identical or different, represent an integer (0-6), A and B, identical or different, represent a hydrogen or a halogen or an alkyl and Ar represents an aryl or heteroaryl, and Z represents a hydrogen or the remainder of a carboxylic acid, preparation process and use as medicaments.Type: GrantFiled: February 11, 1999Date of Patent: December 19, 2000Assignee: Hoechst Marion RousselInventors: Constantin Agouridas, Jean-Francois Chantot, Alexis Denis, Jean-Marie Pejac
-
Patent number: 6147082Abstract: The invention relates to a novel class of compounds that have structures related to certain naturally occurring or synthetic chalcones. The invention also relates to pharmaceutical compositions comprising the compounds and methods for treating certain disorders using the pharmaceutical compositions. The invention further relates to process for synthesizing the novel class of compounds.Type: GrantFiled: December 8, 1999Date of Patent: November 14, 2000Inventors: Ezio Bombardelli, Piero Valenti
-
Patent number: 6130226Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: March 18, 1999Date of Patent: October 10, 2000Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
-
Patent number: 6114380Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.Type: GrantFiled: September 8, 1997Date of Patent: September 5, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus
-
Patent number: 6087507Abstract: The present invention relates to a method of continuously separating pyridine or pyridine derivatives from aqueous solutions by extraction, wherein supercritical fluid is employed to extract the pyridine material from liquid media. The method of the invention, in particular, extracts pyridine or pyridine derivatives from aqueous solutions with pressurized carbon dioxide, which is used under pressure, or in the liquid state, or in the near critical state or in the supercritical state. The operating system is a continuously operating extraction system, so that a part, or all, of the pyridine and/or pyridine derivatives are transferred from the aqueous phase to the carbon dioxide phase, and thereafter the aqueous phase and carbon dioxide phase are separated from each other; and the pyridine and/or pyridine derivatives are separated from carbon dioxide; and the extract containing pyridine and/or pyridine derivatives is thereby obtained.Type: GrantFiled: April 26, 1999Date of Patent: July 11, 2000Assignee: Valtion Teknillinen TutkimuskeskusInventors: Antero Laitinen, Marko Maukonen
-
Patent number: 6066763Abstract: A process for preparing .alpha.-hydroxy acids by heating ammonium salts of .alpha.-hydroxy acids of general formula (I), removing the formed ammonia and water, adding water to the residue, and heating the obtained mixture, wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, alkyl(C.sub.1 -C.sub.6)thioalkyl (C.sub.1 -C.sub.6), phenyl or the like. This process is freed from the problem of disposal of by-products such as ammonium bisulfate and makes it possible to prepare a free .alpha.-hydroxy acid from an ammonium salt thereof economically and in a high yield.Type: GrantFiled: August 25, 1998Date of Patent: May 23, 2000Assignee: Nippon Soda Co., Ltd.Inventor: Koichi Hayakawa
-
Patent number: 6054583Abstract: This invention relates to a process for preparing 2-substituted pyridines via metal halogen exchange with sec-butyllithium on optionally substituted 2-bromo or 2-iodopyridines. The resulting lithopyridine intermediate is reacted with an electrophile to provide the desired 2-substituted pyridine. The substitution of sec-butyllithium for n-butyllithium in such a process results in an enhanced yield and purity of the desired 2-substituted pyridine.Type: GrantFiled: May 5, 1999Date of Patent: April 25, 2000Assignee: Rohm and Haas CompanyInventors: Martha Jean Kelly, Damian Gerard Weaver
-
Patent number: 6051714Abstract: Described are preferred processes for dechlorinating chlorinated pyridine compounds in the presence of zinc, an alkaline reagent and a phase transfer catalyst. Particularly preferred processes provide advantageous synthetic routes to 2,3,5-trichloropyridine starting with 2,3,5,6-tetrachloropyridine.Type: GrantFiled: March 12, 1999Date of Patent: April 18, 2000Assignee: Reilly Industries, Inc.Inventors: Phillip B. Lawin, Z. Jason Yang, Gregory F. Hillstrom, Michael P. Cruskie, Jr.
-
Patent number: 6030803Abstract: Dibenzodihydropyridinecarboxylic esters are provided which comply with formula (1) or (2), wherein: R.sub.1 is substituted alkyl or cyano; R.sub.2 and R.sub.3 are independently hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R.sub.4 is hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R.sub.5 and R.sub.6 are independently alkyl, alkoxy or another substituent which is relatively resistant to oxidation; m and n are integers from 0 to 4; wherein, if m or n is at least 2, two groups R.sub.5 or R.sub.6 may be linked together; and Z is oxygen or sulphur. The new compounds are used in a method as chemiluminogenic reagents for detecting the presence of peroxidase activity at extremely low levels (10.sub.-20 moles). A kit containing the dibenzodihydropyridine-carboxylic esters for use in assaying peroxidase activity has also been described.Type: GrantFiled: January 7, 1999Date of Patent: February 29, 2000Assignee: De Staat der Nederlanden, vertegenwoordigd door de Minister van Welzijn, Volksgeszonheid en CultuurInventors: Marjorie Jacquemijns, Gijsbert Zomer
-
Patent number: 5965740Abstract: A compound represented by the formula (I): ##STR1## wherein R.sup.1 is an optionally substituted heterocyclic group; R.sup.2 is optionally substituted aryl or heterocyclic group; R.sup.3 is hydrogen, alkyl, alkenyl, or alkynyl; R.sup.4 is hydrogen, alkyl, alkoxy, halogen, nitro, cyano, or halogenated alkyl; M is oxygen, S(O).sub.i wherein i is 0, 1, or 2, NR.sup.5 wherein R.sup.5 is hydrogen, alkyl, or acyl, --Q--N.dbd.C(R.sup.6)--, --B--C(R.sup.8).dbd.N--, --CH.dbd.N--N.dbd.C(R.sup.9)--, or --CH.dbd.N--A--(CR.sup.10 R.sup.11)m--; and n is 0, 1, or 2, an intermediate for producing the same and an agrochemical composition containing the same as an active ingredient.Type: GrantFiled: February 20, 1998Date of Patent: October 12, 1999Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Akira Takase, Toshikazu Ohtsuka
-
Patent number: 5952258Abstract: Disclosed is a process for the preparation of pyridine bases by a reaction of an aliphatic aldehyde and/or ketone with ammonia under gaseous phase using a specified catalyst in which a specified metal or combined metals are carried in or onto specified zeolites, for example, such as zeolites having a specified specific density range.Type: GrantFiled: April 29, 1996Date of Patent: September 14, 1999Assignee: Daicel Chemical Industries, Ltd.Inventors: Morihito Saitoh, Yasutaka Tanaka
-
Patent number: 5929117Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: August 11, 1997Date of Patent: July 27, 1999Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
-
Patent number: 5925645Abstract: The 2-aryl-substituted pyridines are prepared by reacting pyridylaldehydes with organometallic compounds and then selectively reducing the products. The 2-aryl-substituted pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosis.Type: GrantFiled: March 13, 1997Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Rolf Angerbauer, Arndt Brandes, Michael Logers, Matthias Muller-Gliemann, Hilmar Bischoff, Delf Schmidt, Stefan Wohlfeil
-
Patent number: 5919944Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group, Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--, --C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: July 20, 1998Date of Patent: July 6, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Sameer Eldin
-
Patent number: 5900489Abstract: Processes for preparing substituted 3-aryl-5-haloalkyl-pyrazoles and, specifically, for preparing C.sub.1-5 alkyl esters of 5-?1-(C.sub.1-5 alkyl)-4-halo-5-(C.sub.1-3 haloalkyl)-1H-pyrazole-3-yl!-2,4-dihalo-benzoic acids such as isopropyl 5-?4-bromo-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-yl!-2-chloro-4-fluor obenzoate, are presented. The described processes include novel approaches for forming phenyl-diketones, forming and alkylating pyrazoles, brominating heterocyclic compounds, oxidizing alkyl-substituted benzene compounds, and esterifying carboxylic acids. These processes may be combined to prepare 3-aryl-5-haloalkyl pyrazoles, or alternatively, used in subcombinations or individually to prepare intermediates or other useful compounds.Type: GrantFiled: October 3, 1997Date of Patent: May 4, 1999Assignee: Monsanto CompanyInventors: Bruce C. Hamper, Michael K. Mao, Wendell Gary Phillips
-
Patent number: 5892038Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.Type: GrantFiled: December 8, 1997Date of Patent: April 6, 1999Assignee: Pharmacopeia, Inc.Inventors: Roland Ellwood Dolle, III, Hitesh K. Patel
-
Patent number: 5889058Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.Type: GrantFiled: November 3, 1994Date of Patent: March 30, 1999Assignee: Celltech LimitedInventors: John Robert Porter, Thomas Andrew Millican, John Richard Morphy, Nigel Robert Arnold Beeley
-
Patent number: 5869678Abstract: A process for preparing an N-oxide of pyridine or a halopyridine, said process comprising reacting a reaction mixture of said pyridine, or said halopyridine, and hydrogen peroxide in a reaction conducted at an elevated temperature in the presence of a catalytically effective amount of a heterogeneous catalyst, said heterogeneous catalyst being insoluble in said reactants, to form said 2-halopyridine-N-oxide or pyridine-N-oxide.Type: GrantFiled: February 3, 1997Date of Patent: February 9, 1999Assignee: Olin CorporationInventors: Henry W. Schiessl, Steven A. Manke
-
Patent number: 5861419Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: July 11, 1997Date of Patent: January 19, 1999Assignee: Merck Frosst Canad, Inc.Inventors: Daniel Dube, Richard Friesen, Rejean Fortin, Zhaoyin Wang, Jacques Yves Gauthier
-
Patent number: 5856498Abstract: This invention is concerned with a novel process for the preparation of a compound of structural formula I ##STR1## wherein R.sup.1 and R.sup.2 independently are aryl, C.sub.2-15 alkenyl or C.sub.1-15 alkyl, either unsubstituted or substituted with one or three substituents, which can be the same or different, selected from the group consisting of R.sup.a, wherein R.sup.a belongs to a group consisting of C.sub.1-6 alkyl, aryl, halo, --N(R.sup.3).sub.2, --NO.sub.2, --CN, --OR.sup.3, --C.sub.3-6 cycloalkoxy, --CO(R.sup.3), --COOR.sup.3, SO.sub.2 R.sup.3 and --SR.sup.3 ; wherein R3 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl and aryl, said alkyl, alkenyl or aryl optionally substituted with 1 to 3 groups of R.sup.a, which is an important antiasthmatic agent.Type: GrantFiled: September 16, 1997Date of Patent: January 5, 1999Assignee: Merck & Co., Inc.Inventors: Ilias K. Dorziotis, Ioannis N. Houpis, Jaemoon Lee, Ralph P. Volante
-
Patent number: 5852189Abstract: Relatively pure tertiaryaminoalkyllithium initiators suitable for anionic polymerization reactions are prepared at low temperatures in an organic ether by reacting an equivalent excess of lithium metal with a tertiaryaminoalkylhalide. The lithium initiators are very stable at moderate temperatures when the ether is replaced by an aliphatic, a cycloaliphatic, or an aromatic solvent. Yields of the initiator in excess of 98% are readily achieved.Type: GrantFiled: December 31, 1996Date of Patent: December 22, 1998Assignee: Bridgestone CorporationInventors: William L. Hergenrother, Michael L. Kerns, David F. Lawson
-
Patent number: 5808083Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.Type: GrantFiled: May 12, 1997Date of Patent: September 15, 1998Assignee: AllerganInventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
-
Patent number: 5808124Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: June 21, 1996Date of Patent: September 15, 1998Assignee: AllerganInventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
-
Patent number: 5750709Abstract: Method and apparatus are described for isolating natural therapeutic compositions from source materials. The method and apparatus isolate natural therapeutic compositions from waxes, fats, oils and other constituents of the source material with the use of supercritical, critical or near critical fluids.Type: GrantFiled: January 31, 1995Date of Patent: May 12, 1998Assignee: Aphios CorporationInventor: Trevor P. Castor
-
Patent number: 5747601Abstract: Vulcanization accelerators constituted by compounds belonging to the class of dihydropyridines having the general formula (I): ##STR1## and their use in natural or synthetic rubbers.Type: GrantFiled: February 20, 1997Date of Patent: May 5, 1998Assignee: Great Lakes Chemical Italia S.r.l.Inventors: Fabio Broussard, Mauro Adovasio, Jose Roncalli
-
Patent number: 5726319Abstract: There are disclosed certain compounds identified as substituted dipeptide analogs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such substituted dipeptide analogs as the active ingredient thereof are also disclosed.Type: GrantFiled: August 1, 1995Date of Patent: March 10, 1998Assignee: Merck & Co., Inc.Inventors: Peter Lin, William R. Schoen, Judith M. Pisano, Matthew J. Wyvratt
-
Patent number: 5717093Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.Type: GrantFiled: December 18, 1995Date of Patent: February 10, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus