The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
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Patent number: 6316634Abstract: A method for preparation of a cycloheptimidazole compound having formula (5), wherein: R4 is a lower alkyl group, comprising reacting a compound of formula (1), with an alkylamidine hydrochloride.Type: GrantFiled: March 14, 2001Date of Patent: November 13, 2001Assignee: Kotobuki Pharmaceutical Co LtdInventors: Tsuyoshi Tomiyama, Akira Tomiyama, Naoto Ueyama, Akira Ohno
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Patent number: 6303620Abstract: Disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds of formula I wherein D, E, G, J, R1, a, b, c, and d are defined in the specification, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: May 6, 1999Date of Patent: October 16, 2001Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Michael Ankersen
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Patent number: 6297261Abstract: A compound having the formula (I) or a pharmaceutically acceptable salt thereof where the variables are defined in the specification are useful in the treatment of sickle-cell anemia.Type: GrantFiled: September 30, 1999Date of Patent: October 2, 2001Assignee: Neurosearch A/SInventors: Palle Christophersen, Ove Pedersen
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Patent number: 6291507Abstract: A pharmaceutical composition which comprises a compound of formula (I) or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1, and wherein A and B form an optionally substituted alkylene chain so as to form a ring with the carbon atoms to which they are attached; X is CH2 or SO2, R1 is an optionally substituted aryl or heteroaryl ring; R2 is a specified organic group such as carboxy, and R3 is hydrogen or a specified organic group; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and are claimed as such.Type: GrantFiled: July 26, 2000Date of Patent: September 18, 2001Assignee: Astrazeneca UK LimitedInventors: Alan W Faull, Andrew J Barker, Jason G Kettle
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Patent number: 6291530Abstract: Disclosed are compounds of formula (I) wherein W is CH or N; R is (mono- or di cabocyclic or heterocyclic aryl)-lower alkyl; R1 is hydrogen or lower alkyl; R2 and R3 are hydrogen, lower alkyl, lower alkoxy-lower alkyl or aryl-lower alkyl; or R2 and R3 joined together represent lower alkylene optionally interrupted by O, NH, N-lower alkyl or S so as to form a ring with the amide nitrogen; X is O, S, SO, S2 or a direct bond; X1 is O, S, SO, SO2 or a direct bond; Y is a direct bond, lower alkylene or lower alkylidene; and Z is carboxyl, 5-tetrazolyl,, hydroxymethyl or carboxyl derivatized in the form of a pharmaceutically acceptable ester, and pharmaceutically acceptable salts thereof; which arm useful as LTB-4 antagonists.Type: GrantFiled: March 23, 1999Date of Patent: September 18, 2001Assignee: Novartis AGInventors: Paul David Greenspan, Roger Aki Fujimoto
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Patent number: 6277998Abstract: There are disclosed an industrially favorable process for producing a tetrazole compound of general formula (1): characterized in that a nitrile of general formula (2): R1CN (2) is reacted with hydrazine or a salt thereof in the presence of a catalyst, followed by reaction with a nitrous acid compound of general formula (3): ANO2 (3) or a nitrile of general formula (2) is reacted with hydrogen sulfide, followed by reaction with an alkyl halide of general formula (4): R4J (4) with hydrazine or a salt thereof, and then with a nitrous acid compound of general formula (3); and an intermediate of general formula (5): R1C(═R5)R6 (5) which is useful for the production of the tetrazole compound (in which R1 to R6, A and J in the above formulas are as defined in the specification).Type: GrantFiled: September 14, 2000Date of Patent: August 21, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Hideki Ushio, Takayuki Higashii, Masayoshi Minai, Akihiko Nakamura
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Patent number: 6274604Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.Type: GrantFiled: May 5, 1999Date of Patent: August 14, 2001Assignee: Merck & Co., Inc.Inventor: Carl Mendel
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Patent number: 6271375Abstract: A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.Type: GrantFiled: April 27, 2000Date of Patent: August 7, 2001Assignee: Zambon Group S.p.A.Inventors: Marco Villa, Pietro Allegrini, Katiuscia Arrighi, Maurizio Paiocchi
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Patent number: 6271261Abstract: Novel IL-8 receptor antagonists and methods of using them are provided.Type: GrantFiled: December 17, 1998Date of Patent: August 7, 2001Assignee: SmithKline Beecham CorporationInventor: Katherine L Widdowson
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Patent number: 6262103Abstract: A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.Type: GrantFiled: April 16, 1999Date of Patent: July 17, 2001Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, Mark Stewart Chambers, Sarah Christine Hobbs, Angus Murray MacLeod, Austin John Reeve
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Patent number: 6252084Abstract: A class of novel 1H-indole-3-acetamides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: October 31, 1997Date of Patent: June 26, 2001Assignee: Eli Lilly and CompanyInventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
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Patent number: 6248770Abstract: The present invention relates to new benzimidazoles of general formula wherein Ra to Rc, A, Ar and B are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof the prodrugs, the derivatives thereof which contain a group which is negatively charged under physiological conditions, instead of a carboxy group, and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein Rc denotes one of the amidino groups mentioned in claim 1 which have valuable pharmacological properties, particularly an antithrombotic activity.Type: GrantFiled: June 24, 1999Date of Patent: June 19, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Uwe Ries, Iris Kauffmann, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6239284Abstract: The invention concerns aromatic tetralcyclic compounds of the retinoid type of general formula (I). The invention also concerns the method for preparing them and the pharmaceutical compositions containing at least one of said compounds.Type: GrantFiled: July 15, 1999Date of Patent: May 29, 2001Assignee: Centre Europeen de Bioprospective-CEBInventors: Bertrand Leblond, Abdallah Deyine, Alain-René Schoofs, Pierre Germain, Bernard Pourrias
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Patent number: 6232334Abstract: Benzimidazole derivatives of the formula (I): wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; R2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes,Type: GrantFiled: August 18, 1999Date of Patent: May 15, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6225288Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.Type: GrantFiled: March 16, 2000Date of Patent: May 1, 2001Assignee: Merk Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Erich Grimm, Renee Aspiotis, Sebastien Francoeur, Robert Zamboni, Petpiboon Prasit, Christopher Bayly, Dan McKay, Cameron Black
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Patent number: 6174883Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: June 7, 1995Date of Patent: January 16, 2001Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 6156774Abstract: Mercapto amino acid derivatives of formula (I), wherein R is hydrogen, a salt-forming cation of a in vivo hydrolysable ester-forming group; R.sub.1 is selected from (a) and (b) in which A is a monocyclic aryl or heteroaryl ring and B is a monocyclic aryl, alicyclic or heterocyclic ring, C and D are independently --Z.sub.p --(CR.sub.8 CR.sub.9).sub.q -- or --(CR.sub.8 CR.sub.9).sub.q --Z.sub.p -- where p is 0 or 1, q is 0 to 3 provided that p+q in C is not 0, R.sub.8 and R.sub.9 are independently hydrogen or (C.sub.1-6)alkyl or together represent oxo and Z is O, NR.sub.10 or S(O).sub.x where R.sub.10 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl and x is 0-2, and wherein C and D are linked ortho to one another on each of the rings A and B in formula (b); R.sub.2 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl; R.sub.3 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms, (C.sub.3-7)cycloalkyl, fused aryl(C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.Type: GrantFiled: April 7, 1999Date of Patent: December 5, 2000Assignee: SmithKline Beecham P.L.C.Inventors: John Hargreaves Bateson, Desmond John Best, Brian Peter Clarke, Martin Leonard Gilpin, David Witty
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Patent number: 6143774Abstract: The invention relates to the new products of formula (I): ##STR1## in which: R.sub.1 represents alkyl, optionally substituted or cycloalkyl optionally interrupted by heteroatoms,R.sub.2 ; R.sub.3 both represent or carry an acid function or an acid isosteric function,and Y represents phenyl substituted in particular by a dioxol radical,these products being in all the isomeric forms and the salts, as medicaments.Type: GrantFiled: June 9, 1998Date of Patent: November 7, 2000Assignee: Hoechst Marion RousselInventors: Bertrand Heckmann, Simone Jouquey, Jean-Paul Vevert, Jidong Zhang
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Patent number: 6143776Abstract: Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.Type: GrantFiled: February 2, 2000Date of Patent: November 7, 2000Assignee: Sunesis Pharmaceuticals, Inc.Inventor: Daniel A. Erlanson
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Patent number: 6136834Abstract: A tetrazole derivative of formula (I) ##STR1## wherein R is H, alkyl, alkoxy, carbocyclic ring, alkyl or alkoxy substituted by carbocyclic ring;AA.sup.1 and AA.sup.2 is a bond or ##STR2## and ##STR3## respectively, or AA.sup.1 and AA.sup.2, together, may have the formula (a); ##STR4## and Y is formula (b) ##STR5## wherein the Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO.sub.2, NR.sup.26, methylene in alkylene replaced by O, S, --SO--, --SO.sub.2 -- or --NR.sup.26 --; and E is H, alkyl, or COOR.sup.27.Type: GrantFiled: June 29, 1998Date of Patent: October 24, 2000Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Makoto Tanaka, Tohru Miyazaki, Hiroyuki Ohno
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Patent number: 6133302Abstract: 5-(3-phenyl-3-oxo-propyl)-1H-tetrazole derivatives of formula (I) wherein each of R and R.sub.1, being the same or different, is hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, phenyl, benzyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, SOR.sub.4 or SO.sub.2 R.sub.4 wherein R.sub.4 is C.sub.1 -C.sub.6 alkyl, --N(R.sub.5 R.sub.6) in which each of R.sub.5 and R.sub.6 is, independently, hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 acyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl; R.sub.3 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl or a group --N(R.sub.7 R.sub.8) in which each of R.sub.7 and R.sub.8 is, independently, hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, phenyl, or one of R.sub.7 and R.sub.8 is hydrogen and the other is COR.sub.9 wherein R.sub.9 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl or a group --N(R.sub.10 R.sub.11) in which R.sub.Type: GrantFiled: December 30, 1999Date of Patent: October 17, 2000Assignee: Pharmacia & Upjohn SpAInventors: Paolo Pevarello, Antonio Giordani, Manuela Villa, Carmela Speciale, Mario Varasi
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Patent number: 6077864Abstract: A compound of the formula ##STR1## wherein n, X, Y and Ar are as defined herein, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: June 17, 1999Date of Patent: June 20, 2000Assignee: Pfizer Inc.Inventors: Laurence Edward Burgess, James Patrick Rizzi
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Patent number: 6069257Abstract: A process for preparing certain substituted benzopyran compounds of formula (I) ##STR1## is disclosed.Type: GrantFiled: July 6, 1999Date of Patent: May 30, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Robert Gordon Giles, Norman John Lewis, Paul Oxley, John Kirby Quick
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Patent number: 6060492Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.Type: GrantFiled: June 25, 1997Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Anthony John Shuker, Mark Alan Winter
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 6048984Abstract: The invention relates to compounds of formula (I): and to their use as herbicides, and to intermediates useful in their preparation.Type: GrantFiled: August 19, 1999Date of Patent: April 11, 2000Assignee: Rhone-Poulenc Agriculture LimitedInventors: Kouichi Araki, Takako Brett, Kei Domom, Atsushi Go, Masahito Ito, Hideshi Mukaida, Yukiko Oe
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Patent number: 6048983Abstract: A process for preparing certain substituted benzopyran compounds is disclosed.Type: GrantFiled: February 8, 1999Date of Patent: April 11, 2000Assignee: SmithKline Beecham pl.cInventors: Robert Gordon Giles, Paul Oxley
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Patent number: 6046227Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta..sub.3 receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: December 4, 1998Date of Patent: April 4, 2000Assignee: Eli Lilly and CompanyInventors: Thomas Alan Crowell, Charles David Jones, Anthony John Shuker
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Patent number: 6040454Abstract: The invention is directed to a process for preparing a 5-substituted tetrazole, the process comprising the step of reacting a nitrile with an inorganic azide salt in an aromatic hydrocarbon solvent in the presence of an amine salt. According to the invention, a 5-substituted tetrazole can be produced in a high yield with ease and safety using inexpensive raw materials while the reaction is easily controlled to inhibit a side reaction.Type: GrantFiled: January 9, 1998Date of Patent: March 21, 2000Assignee: Toyo Kasei Kogyo Company LimitedInventors: Kiyoto Koguro, Toshikazu Oga, Norihito Tokunaga, Sunao Mitsui, Ryozo Orita
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Patent number: 6037367Abstract: Compounds of formula (I) wherein: R.sub.1 is --(CR.sub.4 R.sub.5).sub.n C(O)O(CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n C(O)NR.sub.4 (CR.sub.4 R.sub.5).sub.m R.sub.6, (CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6, or --(CR.sub.4 R.sub.5).sub.r R.sub.6 : W is alkynyl or 2 carbon atoms; R.sub.3 is H or R.sub.7 ; Z is C(O)R.sub.13, (CH.sub.2).sub.0-1 C(O)OR.sub.13, (CH.sub.2).sub.0-1 C(O)NR.sub.10 R.sub.13, (CH.sub.2).sub.0-1 C(R.sub.8 R.sub.8)OR.sub.8, --NHC(O)R.sub.7, (CH.sub.2).sub.0-1 NR.sub.10 R.sub.13, NH[C(O)C(O)OR.sub.8 ], CH.sub.2 NH[C(O)CNR.sub.10 R.sub.13 ], CH.sub.2 S(O).sub.q R.sub.7, CH[S(O).sub.q R.sub.7 ].sub.2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R.sub.7 is --(CR.sub.4 R.sub.5).sub.q R.sub.11 or C.sub.1-6 alkyl wherein the R.sub.11 or C.sub.Type: GrantFiled: September 14, 1998Date of Patent: March 14, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, James S. Frazee
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Patent number: 6034248Abstract: The present invention provides an azole compound represented by the formula (I): ##STR1## wherein Ar is an optionally substituted phenyl group; R.sup.1 and R.sup.2, the same or different, are a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; R.sup.3 is a hydrogen atom or an acyl group; X is a nitrogen atom or a methine group; A is Y.dbd.Z (Y and Z, the same or different, are a nitrogen atom or a methine group optionally substituted with a lower alkyl group) or an ethylene group optionally substituted with a lower alkyl group; n is an integer from 0 to 2; and Az is an optionally substituted azolyl group, or its salt, which is useful for a prevention and therapy of a fungal infection of a mammal as a antifungal agent.Type: GrantFiled: October 17, 1996Date of Patent: March 7, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Kenji Okonogi, Akihiro Tasaka
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Patent number: 6034105Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.Type: GrantFiled: December 18, 1998Date of Patent: March 7, 2000Assignee: Merck & Co., Inc.Inventor: Carl M. Mendel
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Patent number: 6034249Abstract: This invention relates to an organomercapto Au(I) complex having the formula ##STR1## wherein M is a cationic counterion;SOL is a solubilizing group;A is a substituted or unsubstituted divalent organic linking group;and n is 1 to 4 and wherein the compound is symmetrical.It further relates to a method of manufacturing an organomercapto Au(I) complex comprising reacting an Au(I) complex with an organomercapto ligand and isolating the resulting organomercapto Au(I) complex from the reaction mixture.Type: GrantFiled: November 6, 1997Date of Patent: March 7, 2000Assignee: Eastman Kodak CompanyInventors: Roger Lok, Weimar W. White, Brian P. Cleary
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Patent number: 6028092Abstract: This invention relates to novel formulations of salts of certain benzopyran compounds, to compositions containing them and their use in the treatment of certain disorders.Type: GrantFiled: June 17, 1998Date of Patent: February 22, 2000Assignee: SmithKline Beecham p.l.cInventors: Christopher John Banton, Phillip Christopher Buxton
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Patent number: 6025380Abstract: The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of macular degeneration.Type: GrantFiled: June 2, 1999Date of Patent: February 15, 2000Assignee: SmithKline Beecham plcInventor: James Hill
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Patent number: 6020357Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: December 22, 1997Date of Patent: February 1, 2000Assignee: DuPont Pharmaceuticals CompanyInventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
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Patent number: 6008368Abstract: Pharmaceutical compositions comprising a compound selected from a class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II antagonist compounds of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.Type: GrantFiled: November 24, 1997Date of Patent: December 28, 1999Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
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Patent number: 6004989Abstract: Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.Type: GrantFiled: March 29, 1999Date of Patent: December 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6001823Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.Type: GrantFiled: June 5, 1995Date of Patent: December 14, 1999Inventors: Scott Hultgren, Meta Kuehn, Zheng Xu, Derek Ogg, Mark Harris, Matti Lepisto, Jan Kihlberg, Charles Hal Jones
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Patent number: 5990142Abstract: The present invention relates to novel 4-oxo-4H-1-benzopyran compounds containing benzyloxymethyl, 3-phenylpropyl, or other araliphatic substituents in their 8-position. These compounds show a leukotriene-antagonistic activity. The compounds are characterized by good oral adsorption. The compounds of the present invention may be used as anti-inflammatory and antiallergic medicaments, and in the treatment of cardiovascular diseases.Type: GrantFiled: October 15, 1998Date of Patent: November 23, 1999Assignee: Laboratorios Menarini S.A.Inventors: Germano Carganico, David Mauleon Casellas, Jaime Pascual Avellana, M. Luisa Garcia Perez, Albert Palomer Benet
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Patent number: 5981580Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.Type: GrantFiled: October 20, 1998Date of Patent: November 9, 1999Assignee: G. D. Searle & Co.Inventors: Sean T. Nugent, Richard A. Mueller
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Patent number: 5977124Abstract: .beta.-adrenergic agonists for the treatment of diseases/conditions such as obesity and diabetes. The compounds have formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, W, X, Y and Z are as defined in the specification.Type: GrantFiled: November 4, 1997Date of Patent: November 2, 1999Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 5977117Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (I): ##STR1## where X and Y are selected from groups that include O, S, and NH; and Ar.sup.1, Ar.sup.2 and Ar.sup.3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteraryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.Type: GrantFiled: January 23, 1996Date of Patent: November 2, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
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Patent number: 5977376Abstract: The invention relates to compounds of formula (I): ##STR1## and to their use as herbicides.Type: GrantFiled: July 17, 1998Date of Patent: November 2, 1999Assignee: Rhone-Poulenc Agriculture LimitedInventors: Kouichi Araki, Takako Brett, Kei Domom, Atsushi Go, Masahito Ito, Hideshi Mukaida, Yukiko Oe
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Patent number: 5965565Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds 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 treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
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Patent number: 5965592Abstract: Compounds of the formula ##STR1## and their salts, in which R.sub.1, is a C.sub.1 -C.sub.7 aliphatic hydrocarbon radical; X.sub.1 is --CO; X.sub.2 is a divalent aliphatic hydrocarbon radical which comprises an ethyl group and an alkylene of 2 to 6 carbon atoms; R.sub.2 is hydroxy, carboxy or alkoxycarbonyl in which alkoxy is from 1 to 7 carbon atoms; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl or 5-tetrazolyl; and the rings A and B independently of one another are otherwise unsubstituted; can be prepared in a known manner and may be used as active ingredients for medicaments.Type: GrantFiled: July 29, 1998Date of Patent: October 12, 1999Assignee: Novartis CorporationInventors: Peter Buhlmayer, Franz Ostermayer, Tibur Schmidlin
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Patent number: 5962491Abstract: Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.Type: GrantFiled: September 8, 1997Date of Patent: October 5, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa
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Patent number: 5959120Abstract: The present invention provides an acetate ester compound of formula (III), ##STR1## a process for synthesizing compound (III), and a process for using that compound to prepare a pyrazolone compound, where the substituent definitions are as defined in the Summary of the Invention.Type: GrantFiled: June 12, 1997Date of Patent: September 28, 1999Assignee: Eastman Kodak CompanyInventors: Jared B. Mooberry, Thomas E. Gompf, Brian H. Johnston
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Patent number: 5955487Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## R.sub.1 is C.sub.1 -C.sub.7 alkyl that is unsubstituted or substituted by halogen or by hydroxy, or is C.sub.2 -C.sub.7 -alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkoxy, C.sub.1 -C.sub.7 alkoxy or C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.7 alkoxy;R.sub.2 is 1H-tetrazol-5-yl, carboxy, C.sub.1 -C.sub.7 alkoxycarbonyl, SO.sub.3 H, PO.sub.2 H.sub.2, PO.sub.3 H.sub.2 or halo-C.sub.1 -C.sub.7 alkanesulfonylamino;R.sub.3 is 1H-tetrazol-5-yl, hydroxymethyl, C.sub.1 -C.sub.7 alkoxymethyl, formyl, carboxy, C.sub.1 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.7 alkoxy-C.sub.1 -C.sub.7 alkoxycarbonyl, phenyl-C.sub.1 -C.sub.4 alkoxycarbonyl or carbamoyl, the amino group of which is unsubstituted or mono-substituted by C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 alkenyl or by phenyl-C.sub.1 -C.sub.7 alkyl or di-substituted by C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 alkenyl or by phenyl-C.sub.1 -C.sub.Type: GrantFiled: August 13, 1992Date of Patent: September 21, 1999Assignee: Ciba-Geigy CorporationInventors: Tibur Schmidlin, Paul Zbinden, Peter Buhlmayer
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Patent number: 5952377Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.Type: GrantFiled: October 20, 1998Date of Patent: September 14, 1999Assignee: G. D. Searle & Co.Inventors: Sean T. Nugent, Richard A. Mueller