Benzene Ring Containing Patents (Class 564/155)
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Publication number: 20010053863Abstract: Allylated amide compounds are formulated into curable compositions with a free radical curing agent, and optionally, one or more fillers, for use as adhesives in the manufacture of microelectronic devices.Type: ApplicationFiled: June 29, 2001Publication date: December 20, 2001Inventors: Rose Ann Schultz, Donald Herr, Chaodong Xiao
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Publication number: 20010051731Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: ApplicationFiled: May 1, 2001Publication date: December 13, 2001Inventors: Fred T. Bizzarro, Nancy-Ellen Haynes, Ramakanth Sarabu
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Publication number: 20010051719Abstract: Novel carboxamide derivatives having CNS activity, processes for their preparation and their use as medicamentsType: ApplicationFiled: May 4, 2001Publication date: December 13, 2001Applicant: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Francis David King, Paul Adrian Wyman
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Patent number: 6326398Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.Type: GrantFiled: February 28, 2000Date of Patent: December 4, 2001Assignee: Pfizer Inc.Inventors: Yuan-Ching Phoebe Chiang, Robert L. Dow
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Patent number: 6316669Abstract: Bis-amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of bis-amido polybiguanides is also disclosed. The bis-amido polybiguanides are useful in the preservation of pharmaceutical compositions, particularly ophthalmic and otic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting/cleaning contact lenses.Type: GrantFiled: September 19, 2000Date of Patent: November 13, 2001Assignee: Alcon Manufacturing, Ltd.Inventors: Joonsup Park, Nathaniel D. McQueen
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Patent number: 6313122Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: March 20, 2000Date of Patent: November 6, 2001Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6310244Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3. A substrate of solid phase synthesis of the formula III is also disclosed.Type: GrantFiled: July 23, 1998Date of Patent: October 30, 2001Assignee: Pharmacopeia, Inc.Inventors: Vinh D. Tran, Vu Van Ma, Ruiyan Liu
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Patent number: 6307044Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.Type: GrantFiled: June 10, 1999Date of Patent: October 23, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
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Patent number: 6297400Abstract: A new composition of matter for a diamidodiol and a method for preparing the diamidodiol. The exemplary diamidodiol has the formula C15H30N2O4 and is prepared by reacting a first quantity of 2-amino-2-methyl-1-propanol with a second quantity of a di-substituted malonyl dichloride (i.e., diethylmalonyl dichloride), preferably in ethyl acetate as solvent. A tetraamido macrocycle is prepared from the diamidodiol in two steps by oxidizing the diamidodiol to form a diacid followed by coupling using a known procedure of the diacid with an aryl diamine (e.g., 1,2-diaminobenzene)to yield the tetraamido macrocycle.Type: GrantFiled: July 2, 1999Date of Patent: October 2, 2001Assignee: The Clorox CompanyInventors: James E. Deline, Michael M. Ott
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Patent number: 6297283Abstract: The present invention relates to compounds represented by the following general formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyl, indenyl, pyridyl, indolyl, isoindolyl, quinolyl or isoquinolyl group which may be substituted; X is a lower alkylene group which may be substituted, or the like; Y is a single bond or an alkylene group; Z is a group of —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH— or —CH═CH—C≡C—, or the like; and R is a hydrogen atom, a lower alkyl group or the like, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.Type: GrantFiled: April 9, 1999Date of Patent: October 2, 2001Assignee: Kowa Co., Ltd.Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
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Patent number: 6291413Abstract: N,N diacyl O-substituted imide bleach activators and compositions employing them are provided. Bleach additive and bleaching compositions including the bleach activators and methods of cleaning fabrics are also provided.Type: GrantFiled: May 10, 2000Date of Patent: September 18, 2001Assignee: The Procter & Gamble CompanyInventors: Gregory Scot Miracle, Robert Richard Dykstra
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Patent number: 6262302Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: September 17, 1999Date of Patent: July 17, 2001Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
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Patent number: 6258966Abstract: A chiral ligand of the formula (II) or formula (II′), was synthesized. The chiral ligand (II) or formula (II′) can chelate to metals to form a catalytic complex to catalyze the addition of trimethylsilyl cyanide to aldehydes to give optically active cyanohydrin, individually.Type: GrantFiled: October 13, 1999Date of Patent: July 10, 2001Assignee: Everlight USA, Inc.Inventors: Biing-Jiun Uang, Chun-Tzu Yang
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Patent number: 6255285Abstract: The present invention has as its object providing phenethylamine derivatives that typically function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds represented by the general formula (1): (wherein A is typically an amino acid residue, R1 is typically R6—CO—, R2 is typically a hydrogen atom, R3 is typically —CO—R7, R4 is typically an alkyl group, R5 is typically a hydroxyl group, R6 is typically an alkyl group, and R7 is typically an amino group).Type: GrantFiled: February 15, 2000Date of Patent: July 3, 2001Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Ken-ichiro Kotake, Toshiro Kozono, Tsutomu Sato, Hisanori Takanashi
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Patent number: 6242609Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.Type: GrantFiled: April 7, 1999Date of Patent: June 5, 2001Assignee: Konica CorporationInventor: Fumio Ishii
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Patent number: 6235823Abstract: Disclosed are a crystalline polypropylene resin composition comprising a crystalline polyproplylene resin and a &bgr;-nucleating agent, and a method of increasing the proportion of &bgr;-form crystals in a crystalline polypropylene resin molding comprising molding the composition, the &bgr;-nucleating agent being a diamide compound.Type: GrantFiled: January 13, 1993Date of Patent: May 22, 2001Assignee: New Japan Chemical Co., Ltd.Inventors: Naoki Ikeda, Masafumi Yoshimura, Kazuaki Mizoguchi, Hiroshi Kitagawa, Yuji Kawashima, Kiyoshi Sadamitsu, Yasuyuki Kawahara
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Patent number: 6204391Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.Type: GrantFiled: September 21, 1998Date of Patent: March 20, 2001Assignee: The Regents of the University of CaliforniaInventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
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Patent number: 6197798Abstract: Compounds of the formula I wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, cycloalkyl or heterocyclyl; R2, R3, R4 and R5 are independently hydrogen, optionally substituted alkyl, halo, amino, substituted amino, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aralkoxycarbonyl, (alkyl, aryl or aralkyl)-thio, (alkyl, aryl or aralkyl)-oxy, acyloxy, (alkyl, aryl or aralkyl)-aminocarbonyloxy; or any two of R2, R3, R4 and R5 at adjacent positions are alkylenedioxy; R6 is hydrogen, optionally substituted alkyl, amino, substituted amino, acylamino, wherein Ra is hydrogen or optionally substituted alkyl, Rb and Rc are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; or Rb and Rc together represent lower alkylene or lower alkylene interrupted by O, S, or N—(H, alkyl or aralkyl); Rd is optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; and Re is opType: GrantFiled: July 20, 1999Date of Patent: March 6, 2001Assignee: Novartis AGInventors: Cynthia A. Fink, Gary M. Ksander, Paivi J. Kukkola, Eli M. Wallace, Mahavir Prashad
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Patent number: 6194437Abstract: The compounds of the instant invention are novel compounds of Formula I or a pharmaceutically acceptable salt thereof wherein Ar is phenyl or pyridyl unsubstituted or substituted. Ar1 can be independently selected from Ar and can also include pyridyl-N-oxide, indolyl, imidazole, and pyridyl; R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, imidazole, tetrazole, thiazole (a), (b), (c), or (d), wherein Ar2 is phenyl or pyridyl. The instant compounds antagonize the bombesin receptors in mammals and are therefore effective in treating and/or preventing depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders, inflammatory bowel disease, sleep disorders, and memory impairment.Type: GrantFiled: February 3, 1999Date of Patent: February 27, 2001Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, Martyn Clive Pritchard
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Patent number: 6194612Abstract: This invention features a template for synthesizing combinatorial libraries, methods of synthesizing combiatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.Type: GrantFiled: April 7, 1998Date of Patent: February 27, 2001Assignees: The Scripps Research Institute, CombiChem, Inc.Inventors: Dale L. Boger, Soan Cheng, Peter L. Myers
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Patent number: 6184249Abstract: Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in the therapy of indications associated with the androgen receptor, such as, hirsutism, acne and androgenetic alopecia, and in the therapy and diagnosis of cell hyperplasia dependent on androgens.Type: GrantFiled: December 18, 1998Date of Patent: February 6, 2001Assignee: Biophysica, Inc.Inventors: Milos Sovak, Allen L. Seligson, James Gordon Douglass, III, Brian Campion, Jason W. Brown
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Patent number: 6162807Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: January 11, 2000Date of Patent: December 19, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6153652Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: November 21, 1997Date of Patent: November 28, 2000Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
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Patent number: 6140369Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease or Alzheimer's which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.Type: GrantFiled: September 7, 1999Date of Patent: October 31, 2000Assignee: Centaur Pharmaceuticals, Inc.Inventors: William David Flitter, William A. Garland, Allan L. Wilcox, Richard E. Paylor
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Patent number: 6130315Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.Type: GrantFiled: August 24, 1998Date of Patent: October 10, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
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Patent number: 6127341Abstract: Compounds of the general formula I ##STR1## compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are described.Type: GrantFiled: June 1, 1998Date of Patent: October 3, 2000Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Jesper Lau, Bernd Peschke, Michael Ankersen, Kjeld Madsen, Nils Langeland Johansen
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Patent number: 6121326Abstract: Compounds which are useful as a tachykinin antagonist are substituted alkyltetraamine derivatives which are represented by the following formula (I) or a pharmaceutically acceptable salt, a complex compound or a solvate thereof. ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each is a phenyl group which may be substituted with one or more hydroxyl, lower alkoxy and/or acyloxy group(s). The compounds are useful as an anti-inflammatory agent, anti-allergic agent, analgesic, antiemetic, agent for irritable colon syndrome, agent for dermal disease, agent for vasospastic disease, agent for cerebral ischemic disease, antidepressant, antianxiety agent, agent for autoimmune disease, antispasmodic, and as a muscle relaxant, etc.Type: GrantFiled: January 5, 2000Date of Patent: September 19, 2000Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Atsushi Yamamoto, Ko Nakamura, Masanori Otsuka
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Patent number: 6110925Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.Type: GrantFiled: August 6, 1998Date of Patent: August 29, 2000Assignee: Research Corporation Technologies, Inc.Inventors: Robert M. Williams, Chenguang Yuan
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Patent number: 6096098Abstract: The present invention discloses asymmetrical bleach activators for use in both solid and liquid additive, bleaching and detergent compositions. The asymmetrical bleach activators display the unique ability to form both hydrophilic and hydrophobic bleaching agents in aqueous liquors such as bleaching solutions. Thus, fabrics, hard surfaces or dishes having hydrophobic stains such as dingy and or hydrophilic stains such as beverages can be effectively cleaned or bleached using the bleach activators of the present invention.Type: GrantFiled: April 15, 1999Date of Patent: August 1, 2000Assignee: The Procter & Gamble CompanyInventors: Gregory Scot Miracle, Robert Richard Dykstra, Kevin Lee Kott, Stefano Scialla
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Patent number: 6084065Abstract: The present invention relates to oligopeptidic compounds having the general formula (I):K--[--A--].sub.z --[--B--].sub.w --L (I)The compounds having general formula (I) are antifungals for agricultural purposes.Type: GrantFiled: October 4, 1994Date of Patent: July 4, 2000Assignee: Isagro SpaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Ernesto Signorini
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Patent number: 6071957Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.Type: GrantFiled: November 25, 1997Date of Patent: June 6, 2000Assignee: The University of Tennessee Research CorporationInventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
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Patent number: 6066765Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.Type: GrantFiled: March 30, 1998Date of Patent: May 23, 2000Assignee: Centaur Pharmaceuticals, Inc.Inventors: William Flitter, William Garland, Richard Paylor, Allan Wilcox
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Patent number: 6063819Abstract: Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short "spacer chains" bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains.Type: GrantFiled: February 18, 1998Date of Patent: May 16, 2000Assignee: Cypros Pharmaceutical Corp.Inventors: Paul J. Marangos, Brian W. Sullivan, Torsten Wiemann, Anne M. Danks, Marina Sragovicz, Lewis R. Makings
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Patent number: 6043284Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.Type: GrantFiled: February 5, 1998Date of Patent: March 28, 2000Assignee: Glaxo Wellcome Inc.Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
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Patent number: 6040339Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.Type: GrantFiled: May 28, 1998Date of Patent: March 21, 2000Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 6028192Abstract: The present invention relates to a process for the preparation of compounds of the formula 1 ##STR1## by reacting a secondary acid amide of the formula 2 ##STR2## with an acid chloride of the formula 3 ##STR3## in the presence of N,N-diisopropyl-N-ethylamine. R.sup.1, R.sup.2 and R.sup.3 are alkyl or alkenyl radicals, if required also aryl radicals. The compounds of the formula 1 are suitable for use as insecticides or bleach activators.Type: GrantFiled: January 27, 1998Date of Patent: February 22, 2000Assignee: Clariant GmbHInventors: Johannes Becherer, Klaus Delpy, Karl-Heinz Keil, Bernhard Mees
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Patent number: 6025328Abstract: The present invention provides illudin analogs of the general formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.Type: GrantFiled: February 20, 1998Date of Patent: February 15, 2000Assignee: The Regents of the University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Patent number: 6013837Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2)a-(X.sub.1).sub.b -Q.sub.1 -Q.sub.2 -C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radical or one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 -R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2, their preparation process and their use as pesticides.Type: GrantFiled: July 30, 1997Date of Patent: January 11, 2000Assignee: Hoechst Marion RousselInventors: Jacques Demassey, Michel Gohar, Christian Wehrey
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Patent number: 6013673Abstract: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2., therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.Type: GrantFiled: January 23, 1998Date of Patent: January 11, 2000Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yuuki Nagao, Kazuhiko Torisu, Takayuki Maruyama
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Patent number: 6005010Abstract: Compounds of the formula ##STR1## where T is ##STR2## and R(A), R(B), R(C), R(D), R(E), R(F), x and y have the meanings indicated in the claims, and their pharmaceutically acceptable salts are effective inhibitors of the cellular sodium-proton antiporter (Na.sup.+ /H.sup.+ exchanger). These compounds are therefore outstandingly suitable for treatment of all illnesses which are to be attributed to increased Na.sup.+ /H.sup.+ exchange.Type: GrantFiled: August 20, 1997Date of Patent: December 21, 1999Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Hans-Willi Jansen, Wolfgang Scholz
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Patent number: 5977178Abstract: Compounds of peptide mimetic nature having the general formula I ##STR1## wherein a and b are independently 1 or 2, R.sup.1 and R.sup.2 are independently H or C.sub.1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.Type: GrantFiled: December 18, 1996Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
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Patent number: 5969184Abstract: The present invention is directed to the novel intermediate compounds of the formula: ##STR1## wherein, interalia, R.sub.4 is a substituted phenyl or an optionally substituted napthyl derivative.Type: GrantFiled: May 9, 1997Date of Patent: October 19, 1999Assignee: SmithKline Beecham CorporationInventors: Jerry Leroy Adams, Peter William Sheldrake, Timothy Francis Gallagher, Ravi Shanker Garigipati, Paul Elliot Bender, Jeffrey Charles Boehm, Joseph Sisko, Zhi-Qiang Peng, John C. Lee
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Patent number: 5962736Abstract: A logically ordered array of 10,240 different compounds, each compound prepared from the reaction product of an oxazolone, aldehyde and amine.Type: GrantFiled: January 26, 1998Date of Patent: October 5, 1999Assignee: Arqule, Inc.Inventors: Robert Zambias, David A. Bolten, Joseph C. Hogan, Paul Furth, David Casebier, Cheng Tu
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Patent number: 5962530Abstract: The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.Type: GrantFiled: May 29, 1998Date of Patent: October 5, 1999Assignee: Dr. Karl Thomae GmbHInventors: Wolfhard Engel, Wolfgang Eberlein, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim
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Patent number: 5955506Abstract: A group of benzamide compounds are disclosed. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The pharmaceutical compositions can arrest or slow the progressive loss of function.Type: GrantFiled: February 2, 1998Date of Patent: September 21, 1999Assignee: Centaur Pharmaceuticals, Inc.Inventors: William David Flitter, William A. Garland, Allan L. Wilcox, Richard E. Paylor
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Covalent lipid-phosphono-carboxylic acid conjugates and application thereof as antiviral medicaments
Patent number: 5955452Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.Type: GrantFiled: August 26, 1998Date of Patent: September 21, 1999Assignee: Roche Diagnostics GmbHInventors: Harald Zilch, Dieter Herrmann, Hans-George Opitz, Gerd Zimmermann, Edgar Voss -
Patent number: 5935585Abstract: Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: February 23, 1996Date of Patent: August 10, 1999Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Laurence Vigne
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Patent number: 5935979Abstract: The invention relates to novel substituted amino acid amides, to a process for their preparation and to their use as pesticides.Type: GrantFiled: July 16, 1997Date of Patent: August 10, 1999Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Gerd Hanssler, Klaus Stenzel
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Patent number: 5929118Abstract: The present invention relates to novel fluorobutenic acid hydrazides of the formula (I) ##STR1## in which Y represents C.dbd.O, C.dbd.S or SO.sub.2,R.sup.1 represents hydrogen or halogen andR.sup.2 represents alkyl, halogenoalkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkenyloxy, alkoxy, cycloalkyloxy, alkylthio or respectively optionally substituted aryl, aralkyl, aralkyloxy or hetaryl,to processes for their preparation and to their use for controlling animal pests.Type: GrantFiled: February 9, 1998Date of Patent: July 27, 1999Assignee: Bayer AktiengesellschaftInventors: Udo Kraatz, Wolfgang Kramer, Wolfram Andersch, Andreas Turberg, Norbert Mencke
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Patent number: 5888481Abstract: The invention relates to novel cinnamamides, a process for their manufacture and their use as UV absorbers. The cinnamamides of the invention may be used as UV absorbers in a variety of engineered resins such as polyamides (especially nylon 6 and 6,6), polycarbonates, polyacetals, polysulfones, polyimides, polyaryletherketones, and polyesters, (especially PET and PBT), as well as, other polymers such as polyvinylchloride and polyolefins (polyethylenes and polypropylenes).Type: GrantFiled: September 29, 1995Date of Patent: March 30, 1999Assignee: AlliedSignal Inc.Inventors: Keith A. Horn, Richard B. Heath, David B. Schwind