Plural Rings In Substituent Q Patents (Class 564/171)
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Publication number: 20020040060Abstract: The invention relates to compounds of the formula 1Type: ApplicationFiled: June 21, 2001Publication date: April 4, 2002Inventors: Michael Bos, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
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Patent number: 6340691Abstract: Compounds of the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: January 27, 2000Date of Patent: January 22, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, Derek C. Cole, James M. Chen, Jamie M. Davis, George T. Grosu
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Publication number: 20020002200Abstract: Novel dephenylethylene compounds that are administered orally to decrease circulating concentrations of glucose are provided. The effect on insulin resistant rats is also shown. The effects on lipid and leptin concentrations are also shown. The compounds are orally effective anti-diabetic agents that may normalize glucose and lipid metabolism in subjects with diabetes.Type: ApplicationFiled: February 5, 2001Publication date: January 3, 2002Inventors: Bishwagit Nag, Debendranath Dey, Satyanarayana Medicherla, Partha Neogi
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Publication number: 20010053774Abstract: Novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.Type: ApplicationFiled: December 14, 2000Publication date: December 20, 2001Applicant: GLAXO WELLCOME INC..Inventor: Timothy Mark Willson
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Patent number: 6306903Abstract: The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain.Type: GrantFiled: August 29, 2000Date of Patent: October 23, 2001Assignee: Newron Pharmaceuticals S.p.A.Inventors: Paolo Pevarello, Mario Varasi, Patricia Salvati, Claes Post
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Patent number: 6291689Abstract: A method for the preparation of citalopram is described comprising reduction of the oxo group of a compound of formula (IV), wherein R1 is CN, C1-6 alkyloxycarbonyl or C1-6 alkylaminocarbonyl, ring closure of the resulting hydroxy compound thereby obtaining the corresponding 1-(4-fluorophenyl)-1,3-dihydroisobenzofuran, then if R1 is cyano using it directly in the next step and if R1 is C1-6 alkyloxycarbonyl or C1-6 alkylaminocarbonyl, conversion of the compound to the corresponding compound wherein R1 is a cyano; and alkylation of the resulting 5-cyano compound with 3-dimethyl-aminopropylhalogenide in basic conditions thereby obtaining citalopram.Type: GrantFiled: May 3, 2000Date of Patent: September 18, 2001Assignee: H. Lundbeck A/SInventors: Hans Petersen, Klaus Peter Bøgesø, Michael Bech Sommer
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Patent number: 6229026Abstract: A method for the preparation of citalopram comprising the steps of reacting a compound of Formula (IV) wherein R1 is C1-6 alkyl and X is O or NH, successively with a Grignard reagent of 4-halogen-fluorophenyl and a Grignard reagent of 3-halogen-N,N-dimethylpropylamine, respectively, effecting ring-closure of the resulting compound of Formula (V) wherein R1 and X are as defined above, and converting the resulting 1,3-dihydroisobenzofuran compound to the corresponding 5-cyano derivative, i.e. citalopram.Type: GrantFiled: January 7, 2000Date of Patent: May 8, 2001Assignee: H. Lundbeck, A/SInventor: Hans Petersen
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Publication number: 20010000513Abstract: Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells.Type: ApplicationFiled: December 14, 2000Publication date: April 26, 2001Inventors: Claude Forsey Purchase, Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6214877Abstract: This invention provides compounds of Formula I having the structure wherein: B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: April 10, 2001Inventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
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Patent number: 6207852Abstract: The present invention relates to smooth muscle spasmolytic agents, pharmaceutical compositions containing them and method of using said compounds and compositions for the treatment of urinary incontinence, gastric hyperactivity (ex. Irritable Bowel Syndrome) and other smooth muscle contractile conditions. More particularly, the present invention relates to certain substituted esters, amides and ketones having smooth muscle relaxing properties while avoiding, on administration to a mammal, adverse side effects such as prominent antimuscarinic, arrhythmogenic and cardiodepressive effects.Type: GrantFiled: December 23, 1998Date of Patent: March 27, 2001Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
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Patent number: 6147255Abstract: The invention relates to novel bicyclic aromatic compounds which have the general formula (I): ##STR1## as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.Type: GrantFiled: January 26, 1998Date of Patent: November 14, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6121255Abstract: A phloroglucide derivative having the following formula: ##STR1## wherein Q is halogen; X is CH.sub.2 or C.dbd.O; Y is cephalosporin having a formula of ##STR2## wherein Ph is phenyl, Ac is acetoxy, or pharmaceutically acceptable salts thereof, and an antibacterial pharmaceutical composition derived thereof.Type: GrantFiled: May 4, 1998Date of Patent: September 19, 2000Assignee: National Science CouncilInventors: Jih Ru Hwu, Shwu-Chen Tsay, Gholam H. Hakimelahi, Chun Chieh Lin, Wen Nan Tseng, Ali A. Moshfegh, Abdolmajid Azaripour, Hasan Mottaghian
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Patent number: 6083987Abstract: A phenylenediamine derivative or a salt thereof in accordance with the present invention is expressed by the following formula 1: ##STR1## wherein A represents a group expressed by --CO--, --CH.sub.2 CO--, --CS--, or --SO.sub.2 --; Y represents a carbon atom or nitrogen atom; R.sub.1 represents a lower alkyl group; R.sub.2 represents a hydrogen, lower alkyl, alkenyl, benzyl, or benzoyl group; and each of R.sub.3 and R.sub.4 represents an alkyl group having 1-10 carbon atoms. The phenylenediamine derivative above mentioned, as a radical scavenger, has antioxidant effect and lipid peroxidation inhibitory activity so as to be available for inhibiting brain infarction or brain edema.Type: GrantFiled: June 2, 1998Date of Patent: July 4, 2000Assignee: Shiseido Co., Ltd.Inventors: Chikao Nishino, Kazuyuki Miyazawa, Hideo Kanno
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Patent number: 6057345Abstract: Compounds of the formula, ##STR1## and pharmaceutically-acceptable salts thereof, which are useful as antagonists of the pain-enhancing effects of E-type prostaglandins, processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for treating pain comprising the administration of such compounds.Type: GrantFiled: October 30, 1998Date of Patent: May 2, 2000Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6013827Abstract: This invention relates to componds of formula I ##STR1## which are useful as PDE IV inhibitors and for treating diseases related thereto.Type: GrantFiled: July 11, 1996Date of Patent: January 11, 2000Assignee: SmithKline Beecham CorporationInventors: Joseph Bordas-Nagy, Peter Gorycki, Kevin Scott Webb
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Patent number: 5965579Abstract: The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.Type: GrantFiled: November 21, 1997Date of Patent: October 12, 1999Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 5948819Abstract: An .alpha.-substituted phenylacetic acid derivative useful as an agricultural fungicide, represented by general formula (I), or a salt thereof, a process for producing the same, an intermediate for the production thereof, and an agricultural fungicide containing the same as the active ingredient, wherein R.sup.1 represents halogen, alkyl, OH, alkylthio, alkylsulfinyl, alkylsulfonyl, amino or nitro; Q represents aryl, heterocycle, mono- or disubstituted methyleneamino, (substituted amino-)methyl, alkyl, alkenyl, alkynyl, substituted carbonyl or substituted sulfonyl; X represents hydrogen, halogen, alkyl or OH; Y represents OH, alkylthio or amino; Z represents oxygen or sulfur; M represents oxygen, S(O)i (i being 0, 1 or 2), NR.sup.2 (R.sup.2 being hydrogen, alkyl or acyl) or a single bond; and n represents 0, 1 or 2.Type: GrantFiled: October 7, 1996Date of Patent: September 7, 1999Assignee: Shionogi & Co., LtdInventors: Toshikazu Ohtsuka, Takami Murashi, Shinji Suzuki, Michio Masuko, Hideyuki Takenaka
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Patent number: 5948418Abstract: Novel sulfhydryl group-containing amides and disulfide group-containing bis-amides useful for treating or preventing an abnormal biological condition or a disease, and/or improving the texture or appearance of the skin, as well as compositions containing amides and bis-amides and methods for their use are described. Such types of abnormal biological conditions or diseases include skin atrophy, i.e., the thinning and/or general degradation of the dermis often characterized by a decrease in collagen and/or elastin as well as decreased number, size and doubling potential of fibroblast cells, and other maladies including, but are not limited to dry skin, severe dry skin, dandruff, acne, keratoses, psoriasis, eczema, skin flakiness, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, hyperkeratotic skin, inflammatory dermatoses, age-related skin changes and skin in need of cleansers.Type: GrantFiled: July 30, 1997Date of Patent: September 7, 1999Assignee: Estee Lauder, Inc.Inventors: Daniel H. Maes, Jules Zecchino, Althea Knight
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Patent number: 5945454Abstract: Novel 2(4-substituted)-benzylamino-2-methyl-propanamides compounds, having CNS activity, of general formula (I) wherein: n is zero, 1, 2 or 3; X is --O--, --S--, --CH.sub.2 -- or --NH--; each of R and R.sub.1 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl; each of R.sub.2, R.sub.3 and R.sub.4 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl; and the pharmacetically acceptable salts thereof, are disclosed.Type: GrantFiled: January 8, 1998Date of Patent: August 31, 1999Assignee: Pharmacia & Upjohn, S.P.A.Inventors: Paolo Pevarello, Raffaella Amici, Mario Varasi, Alberto Bonsignori, Patricia Salvati
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Patent number: 5945557Abstract: Compounds with fungicidal and insecticidal properties having formula ##STR1## wherein A is N or CH; V is O or NH; m and n are the integers 0 and 1, provided that m+n is 0 or 1;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, and (C.sub.1 -C.sub.4)alkoxy;R is independently selected from hydrogen, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.12)alkenyl, (C.sub.2 -C.sub.12)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, halo(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.12)alkenyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.12)alkynyl, (C.sub.1 -C.sub.12)alkyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.12)alkenyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.12)alkynyl(C.sub.3 -C.Type: GrantFiled: June 23, 1998Date of Patent: August 31, 1999Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Ted Tsutomu Fujimoto, Steven Howard Shaber
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Patent number: 5939449Abstract: The invention relates to compounds of the formula: ##STR1## The compounds have great affinity for the neurotensin receptors.Type: GrantFiled: November 24, 1997Date of Patent: August 17, 1999Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 5935978Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: July 28, 1993Date of Patent: August 10, 1999Assignee: Rhone-Poulenc Rorer LimitedInventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Michael John Ashton, David Charles Cook, Susan Jacqueline Hills, Ian Michael McFarlane, Nigel Vicker
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Patent number: 5925646Abstract: The heterocyclic aryl-, alkyl- and cycloalkylacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.Type: GrantFiled: January 16, 1998Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
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Patent number: 5922771Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.Type: GrantFiled: August 19, 1996Date of Patent: July 13, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 5916922Abstract: A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: November 24, 1997Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Theodore Goodson, Jr., Richard Waltz Harper, David Kent Herron
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Patent number: 5900432Abstract: Compounds of formula I: ##STR1## wherein, ring C, A--B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: October 12, 1995Date of Patent: May 4, 1999Assignee: Zeneca LimitedInventors: James Roy Empfield, Cyrus John Ohnmacht, Keith Russell, Diane Amy Trainor, Paul James Warwick, Jr.
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Patent number: 5883106Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.Type: GrantFiled: February 6, 1998Date of Patent: March 16, 1999Assignee: Pfizer Inc.Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 5880156Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4) are as defined in the specification, and pharmaceutically tolerated salts thereof.Type: GrantFiled: January 30, 1996Date of Patent: March 9, 1999Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Heinz-Werner Kleemann, Wolfgang Scholz, Udo Albus
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Patent number: 5827891Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
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Patent number: 5783602Abstract: The invention relates to leukotriene-B.sub.4 derivatives of general formula I, ##STR1## in which R.sub.1 represents CH.sub.2 OH, CH.sub.3, CF.sub.3 COOR.sub.4 CONR.sub.5 R.sub.6, andR.sub.3 symbolizes H; C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl optionally substituted singly or multiply; C.sub.6 -C.sub.10 aryl radicals, independently of one another, optionally substituted singly or multiply by halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom,X and Y mean a direct bond, whereby the resulting olefin can be E- or Z-configured or X represents a fluorine atom in .alpha.- or .beta.-position, and Y means a hydrogen atom in .beta.-position.Type: GrantFiled: December 4, 1996Date of Patent: July 21, 1998Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
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Patent number: 5763610Abstract: A composition comprising a nitrogen-containing olefinic compound and a process for using the nitrogen-containing olefinic compound to produce a water-soluble polymer which has applications in a subterranean formation are provided. The nitrogen-containing olefinic compound can be made from an amine and an alkylating agent. The polymer produced can be used in drilling fluids, workover fluids, completion fluids, permeability corrections, water or gas coning prevention, fluid loss prevention, matrix acidizing, fracture acidizing, and combinations of any two or more thereof.Type: GrantFiled: February 21, 1997Date of Patent: June 9, 1998Assignee: Phillips Petroleum CompanyInventors: Iqbal Ahmed, Ahmad Moradi-Araghi, Odd Ivar Eriksen
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Patent number: 5753715Abstract: The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.Type: GrantFiled: June 2, 1995Date of Patent: May 19, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Robert H. Chen, Maud Urbanski, Min Xiang, John Francis Barrett
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Patent number: 5750784Abstract: The present invention provides a method of effecting vasodilation, comprising:administering to a warm blooded animal in need of such treatment, an effective amount of a (1,5-inter) aryl prostaglandin derivative represented by the Formula I ##STR1## wherein n is 0 or an integer of from 1 to 6, R is selected from the group of radicals represented by the formulae:CO.sub.2 R', CONR'.sub.2, CH.sub.2 OR' and SO.sub.2 NR'.sub.2 'wherein R' is hydrogen or a lower alkyl radical having from one to six carbon atoms; R" is hydrogen or an acyl radical having the formula (CO)R'" wherein R'" is a saturated or unsaturated acyclic hydrocarbon radical having from 1 to about 10 carbon atoms, or --(CH.sub.2).sub.m R"" wherein m is 0 or an integer of from 1 to 6 and R"" is an aliphatic ring having from 3 to 7 carbon atoms or an aryl group, e.g. phenyl, or a heteroaryl group, e.g.Type: GrantFiled: February 18, 1997Date of Patent: May 12, 1998Assignee: AllerganInventors: June Chen, Robert M. Burk, David F. Woodward
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Patent number: 5747539Abstract: Fluorine-containing benzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meanings indicated, and their physiologically acceptable salts, have antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter, for example.Type: GrantFiled: May 15, 1996Date of Patent: May 5, 1998Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Dieter Dorsch, Manfred Baumgarth, Rolf Gericke, Klaus-Otto Minck, Norbert Beier
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5733935Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.Type: GrantFiled: June 17, 1996Date of Patent: March 31, 1998Assignee: Nihon Nohyaku Co., Ltd.Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
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Patent number: 5728737Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.Type: GrantFiled: January 23, 1997Date of Patent: March 17, 1998Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
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Patent number: 5721276Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, B, X and R.sub.1 are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: May 30, 1996Date of Patent: February 24, 1998Assignee: Adir et CompagnieInventors: Isabelle Lesieur, Patrick Depreux, Veronique Leclerc, Philippe Delagrange, Pierre Renard, Beatrice Guardiola Lemaitre
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Patent number: 5693611Abstract: Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I ##STR1## wherein: R', R", R'", R.sup.x1, R.sup.x2, R.sup.y1, R.sup.y2, R.sup.y3, R.sup.y4, and R.sup.0 are as defined herein below;R.sup.2 is a novel acyl side chain. Also provided are novel formulations and methods of inhibiting fungal and parasitic activity.Type: GrantFiled: January 17, 1997Date of Patent: December 2, 1997Assignee: Eli Lilly and CompanyInventors: Stacy Kay Henle, William Wilson Turner
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Patent number: 5677303Abstract: Enolethers and thioenolethers of formula I ##STR1## are disclosed. The compounds are useful for combatting phytopathogenic fungi.Type: GrantFiled: June 20, 1996Date of Patent: October 14, 1997Assignee: American Cyanamid CompanyInventors: Juergen Curtze, Guido Albert
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Patent number: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Leukotriene-B.sub.4 antagonists, process for their production and their use as pharmaceutical agents
Patent number: 5559134Abstract: The invention relates to leukotriene-B.sub.4 antagonists of formula I ##STR1## in which n represents a whole number from 2 to 5,X represents a direct bond, 1 to 6 methylene units, an ortho-, meta- or para-substituted phenyl ring or a meta- or para-substituted pyridine ring,Y represents a bond to a hydrogen atom and simultaneously to a hydroxy group, a double-bound oxygen atom or --O--CH.sub.2 --CH.sub.2 --O--,R.sub.1 and R.sub.2 represent the radical OH, --O--(C.sub.1 -C.sub.4)--alkyl, O--(C.sub.3 -C.sub.6)--cycloalkyl, --O--(C.sub.6 -C.sub.10)--aryl, --O--(C.sub.7 -C.sub.12)--aralkyl, O--(CH.sub.2)--CO-- (C.sub.6 -C.sub.10)--aryl or the radical NHR.sub.3 with R.sub.3 meaning hydrogen, (C.sub.1 -C.sub.4)--alkyl, (C.sub.3 -C.sub.6)--cycloalkyl or (C.sub.7 -C.sub.12)--aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates.Type: GrantFiled: March 23, 1995Date of Patent: September 24, 1996Assignee: Schering AktiengesellschaftInventors: Bernd Buchmann, Werner Skuballa, Josef Heindl, Wolfgang Fr ohlich, Roland Ekerdt, Claudia Giesen -
Patent number: 5527945Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: August 31, 1994Date of Patent: June 18, 1996Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5514719Abstract: The invention provides agriculturally useful fungicidal phenylbenzamides of the formula ##STR1## wherein R.sub.1 and R.sub.2, which are identical or different, are each a hydrogen or halogen atom or an optionally halogenated alkyl radical having from 1 to 6 carbon atoms; and R.sub.3 and R.sub.4, which are identical or different, are each an alkyl radical having from 1 to 4 carbon atoms, or R.sub.3 and R.sub.4, taken together with the nitrogen atom to which they are attached, form a morpholino radical.Type: GrantFiled: June 17, 1994Date of Patent: May 7, 1996Assignee: Rhone-Poulenc AgrochimieInventors: Marie-Pascale LaTorse, Christian Schmitz
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Patent number: 5498792Abstract: There is disclosed a process of producing an N-alkylacetamide of the general formula (III): ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 are the same or different and are independently hydrogen, lower alkyl, lower alkoxy, lower alkenyl, halogen or trifluoromethyl; R.sup.1 and R.sup.2 are the same or different and are independently lower alkyl; and represents a chemical bond of E- or Z-configuration, or a mixture of these configurations, which includes the steps of:(a) reacting an acetonitrile of the general formula (I): ##STR2## wherein X.sup.1, X.sup.2, X.sup.3, R.sup.1 and are each as defined above, with an alkylamine of the general formula (IV):R.sup.2 --NH.sub.2 (IV)wherein R.sup.2 is as defined above, to give an N-alkylacetamidine of the general formula (II): ##STR3## wherein X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2 and are each as defined above; and(b) reacting the N-alkylacetamidine (II) with a nitrite derivative in the presence of an acid.Type: GrantFiled: September 16, 1994Date of Patent: March 12, 1996Assignees: Shionogi & Co., Ltd., Sumitomo Chemical Co., Ltd.Inventors: Katuhisa Masumoto, Akihiko Nakamura, Yujiro Kiyoshima, Mikio Sasaki, Asako Tanahashi
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Patent number: 5495019Abstract: The invention provides a process for the preparation of 3,3-diaryl acrylic acid amides of the general formula ##STR1## in which A, B and Q are as defined in the specification, by condensing a compound of formula ##STR2## with a compound of formulaCH.sub.3 --CO--Q (III)in which Q has the meaning given above, in a solvent in the presence of an alkali metal hydroxide, characterised in that the solvent is selected from alkanes, cycloalkanes or mixtures thereof.Type: GrantFiled: March 16, 1995Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Jurgen Curtze, Bodo Haertel
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Patent number: 5482969Abstract: Compounds of formula I: ##STR1## wherein, ring C, A-B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: March 11, 1994Date of Patent: January 9, 1996Assignee: Zeneca LimitedInventors: James R. Empfield, Cyrus J. Ohnmacht, Keith Russell, Diane A. Trainor, Paul J. Warwick, Jr.
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Patent number: 5476860Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.Type: GrantFiled: December 8, 1993Date of Patent: December 19, 1995Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)Inventor: Jean-Michel Bernardon
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Patent number: 5459262Abstract: A new process for the preparation of a phenylbenzamide derivative of the formula ##STR1## wherein R is C.sub.1 -C.sub.2 alkyl, substituted with 2 to 5 F, and each of R.sub.1 and R.sub.2, which can be identical or different, is methyl or ethyl, or --NR.sub.1 R.sub.2 is morpholino, comprising condensing a haloenone (I) with an acetoamide (II), according to scheme ##STR2## in the presence of an organic solvent and 1 to 2 equivalents of base, followed by converting the resulting product in two steps, one of which is a reduction, to the corresponding compound of formula (A). Phenylbenzamides of formula (A) are agricultural fungicides. The new process is suited to large-scale production of these compounds.Type: GrantFiled: February 8, 1994Date of Patent: October 17, 1995Assignee: Rhone-Poulenc AgrochimieInventor: Christian Schmitz