6-position Substituent Contains Hetero Ring Patents (Class 514/196)
-
Patent number: 4898731Abstract: An antibacterial synergistic composition consisting essentially of a mixture of a penicillin or cephalosporin derivative of the formula ##STR1## and a penicillin of the formula ##STR2## preferably in association with a pharmaceutical carrier.Type: GrantFiled: June 24, 1985Date of Patent: February 6, 1990Assignees: Astra Lakemedel Aktiebolag, Astra Pharmaceutical Products, Inc.Inventors: Peter Bamberg, Bertil A. Ekstrom, Ulf E. Forsgren, Berndt O. H. Sjoberg
-
Patent number: 4861768Abstract: Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.Type: GrantFiled: February 18, 1987Date of Patent: August 29, 1989Assignee: Taiho Pharmaceutical Company, LimitedInventors: Sigeru Torii, Hideo Tanaka, Motoaki Tanaka, Shozo Yamada, Akira Nakai, Hisashi Ohbayashi
-
Patent number: 4836957Abstract: A preparation containing an active form of vitamin D.sub.3 which is stabilized by incorporation of an amino acid that is neither one containing a sulfur atom or an acid amino group in its structure, nor an acidic amino acid, nor a salt of a basic amino acid is disclosed. Examples of said amino acids that may be used as stabilizers of the active form of vitamin D.sub.3 include neutral amino acids such as alanine, valine, proline, phenylalanine, tryptophan, leucine, isoleucine, glycine and serine, and basic amino acids such as lysine, arginine and histidine.Type: GrantFiled: February 11, 1986Date of Patent: June 6, 1989Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kaoru Nemoto, Kazuo Igusa, Toshichika Ogasawara
-
Patent number: 4820701Abstract: Antibacterial agents have the formula (I) or are pharmaceutically acceptable salts or in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.3 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R.sup.4 is hydrogen or formamido, R.sup.5 is hydrogen, C.sub.1-6 alkyl, substituted alkyl, aryl or aralkyl, R.sup.6 and R.sup.7 are the same or different and represent hydrogen, C.sub.1-6 alkyl, substituted alkyl, halogen, amino, phenyl, substituted phenyl, hydroxyl or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 form the residue of an optionally substituted 5- or 6-membered carbocyclic ring or a 5- or 6- membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphr or nitrogen, and X represents ##STR2## or tautomers thereof wherein R.sup.8 and R.sup.9 are the same or different and each represents hydroxy, or protected hydroxy.Type: GrantFiled: October 21, 1987Date of Patent: April 11, 1989Assignee: Beecham Group p.l.c.Inventors: Robert Southgate, Colin H. Frydrych
-
Patent number: 4816452Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is hydrogen or an amino protecting group and R is substituted methyl; optionally substituted C.sub.2-12 alkyl, alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl. These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organisms.Type: GrantFiled: July 25, 1986Date of Patent: March 28, 1989Assignee: Beecham Group P.L.C.Inventors: Michael J. Pearson, Richard L. Elliott
-
Patent number: 4748163Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing >C.dbd.O or >C.dbd.N--R.sup.7,Z representing O, S, or NR.sup.10, andR.sup.2 represents hydrogen or a protective group.Type: GrantFiled: February 21, 1986Date of Patent: May 31, 1988Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
-
Patent number: 4734407Abstract: Antibacterially active and animal growth-regulating novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical of the formula ##STR2## Z represents oxygen, sulphur or --N--R.sup.Type: GrantFiled: March 10, 1986Date of Patent: March 29, 1988Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
-
Patent number: 4731360Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.Type: GrantFiled: August 16, 1985Date of Patent: March 15, 1988Assignee: Merck & Co., Inc.Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
-
Patent number: 4729989Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.Type: GrantFiled: June 28, 1985Date of Patent: March 8, 1988Assignee: Merck & Co., Inc.Inventors: Jose Alexander, Joseph A. Fix
-
Patent number: 4707474Abstract: Compositions comprising a cloxacillin salt and liquid paraffin, arachis oil or fractionated coconut oil are useful in treating infectious keratoconjunctivitis in cattle and domestic animals.Type: GrantFiled: May 6, 1983Date of Patent: November 17, 1987Assignee: Beecham Group p.l.c.Inventor: Robert J. Bywater
-
Patent number: 4692441Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.Type: GrantFiled: August 16, 1985Date of Patent: September 8, 1987Assignee: Merck & Co., Inc.Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
-
Patent number: 4684664Abstract: Disclosed herein are derivatives of .beta.-(4-isocyano-1,2,3,4-diepoxycyclopentyl)acrylic acid, the derivatives showing an antibacterial activity, an antifungal activity and an antimycoplasmal activity.Type: GrantFiled: January 16, 1985Date of Patent: August 4, 1987Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Katsuhisa Osugi, Isao Ichinose, Eisaku Takahashi, Masato Arahira
-
Patent number: 4647457Abstract: .beta.-lactams of the formula ##STR1## wherein R.sup.1 signifies hydrogen or a group readily cleavable by hydrolysis, A signifies the group R.sup.2 --N.dbd.C(CH.sub.3)--CH.dbd.C< or O.dbd.C(CH.sub.3)--CH.sub.2 --C(R.sup.3)<, R.sup.2 signifies hydroxy, lower alkoxy or arylamino and R.sup.3 signifies arylthio, lower alkanoylthio, lower alkoxycarbonylhydrazino or a N-containing saturated heterocycle attached via a N-atom, and pharmaceutically acceptable salts thereof, are disclosed. The compounds and their salts exhibit .beta.-lactamase inhibiting activities against .beta.-lactamases from bacteria.Type: GrantFiled: March 2, 1984Date of Patent: March 3, 1987Assignee: Hoffmann-La Roche Inc.Inventor: Solange Adam-Molina
-
Patent number: 4629726Abstract: A 2-substituted or unsubstituted-6-(2-oxo-1, 3-dioxolan-4-yl)-2-penem-3-carboxylic acid derivative represented by the following formula (Ia) and: ##STR1## wherein R is hydrogen, a light metal or a carboxy-protecting group, R.sup.1 is an alkyl group, R.sup.2 is hydrogen, methyl or a substituted methyl group. The compounds have antibacterial activity.Type: GrantFiled: July 20, 1984Date of Patent: December 16, 1986Assignee: Shionogi & Co., Ltd.Inventor: Shoichiro Uyeo
-
Patent number: 4623644Abstract: This invention relates to the hybridization of streptolydigin, tirandamycin and sorbic acid to penicillin and cephalosporin nuclei.Type: GrantFiled: August 7, 1985Date of Patent: November 18, 1986Assignee: The Upjohn CompanyInventors: Fritz Reusser, Kenneth L. Rinehart, Jr.
-
Patent number: 4623643Abstract: Penem derivatives are disclosed characterized by a substituted pyridiniomethyl group in the 2-position of the penem nucleus. The compounds of the present application exhibit better antibacterial activity than other known penem derivatives.Type: GrantFiled: June 10, 1985Date of Patent: November 18, 1986Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Franceschi, Ettore Perrone
-
Patent number: 4598074Abstract: Alpha-carboxy-3-thienylmethyl penicillin having either the R- or the S- configuration at C-10 is obtained in cyrstalline form. The isomers show improved stability and higher biological activity as compared to the amorphous RS material.Type: GrantFiled: May 2, 1983Date of Patent: July 1, 1986Assignee: Beecham Group P.L.C.Inventors: George Andreescu, Dennis E. Clark, William J. Kerr
-
Patent number: 4591459Abstract: beta-Lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.Type: GrantFiled: December 3, 1984Date of Patent: May 27, 1986Assignee: Pfizer Inc.Inventor: Wayne E. Barth
-
Patent number: 4540688Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof have antibacterial activity: ##STR1## wherein R is hydrogen, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyl; R.sup.1 is hydrogen or hydrocarbon; R.sup.2 is hydrogen, or optionally substituted hydrocarbon or optionally substituted heterocyclyl or CXR.sup.d, where X is O or S and R.sup.d is hydrogen or optionally substituted hydrocarbon or optionally substituted heterocyclyl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached, form an optionally substituted heterocyclyl group. A process for the preparation of such compounds and compositions comprising them, are also described.Type: GrantFiled: April 27, 1983Date of Patent: September 10, 1985Assignee: Beecham Group p.l.c.Inventor: Michael J. Driver
-
Patent number: 4540689Abstract: A penicillin derivative having an antibacterial activity similar to a penicillin antibiotic in a living body without affecting the intestinal bacterial colonies, a process for preparing the derivative and a pharmaceutical composition in a dosage unit form containing the derivative as an active ingredient are disclosed.Type: GrantFiled: September 16, 1982Date of Patent: September 10, 1985Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Shigeaki Muto, Kouichi Niimura, Takao Ando, Akihiko Kanno, Takao Furusho, Chikao Yoshikumi
-
Patent number: 4537886Abstract: A compound of formula (1) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is phenyl, substituted phenyl or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;X represents; ##STR2## wherein R.sup.Y is methyl or acetyl; R.sup.2 and R.sup.3 may be the same or different and each is hydrogen, an aryl group, a heterocyclyl group or a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group; and R.sup.4 is hydrogen, a C.sub.1-6 alkylcarbonyl group, an aryl group, a heterocyclyl group, a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group;R.sup.5 represents, hydrogen, methoxy or --NHCHO; and Y is: ##STR3## wherein Y.sup.1 is oxygen, sulphur or --CH.sub.2 -- and Z represents hydrogen, halogen or an organic group such as C.sub.1-4 alkoxy, --CH.sub.2 Q or --CH.dbd.Type: GrantFiled: March 29, 1983Date of Patent: August 27, 1985Assignee: Beecham Group p.l.c.Inventors: Andrew W. Taylor, Richard T. Cook
-
Patent number: 4534977Abstract: This invention is concerned with a low bulk density lyophilized pharmaceutical parenteral dosage unit of Sodium Piperacillin and method of making same.Type: GrantFiled: July 11, 1984Date of Patent: August 13, 1985Assignee: American Cyanamid CompanyInventor: Bruce E. Haeger
-
Patent number: 4521533Abstract: Salts of readily hydrolyzable esters of 6-alpha-(aminomethyl)penicillanic acid 1,1-dioxide and (a) prodrug forms of ampicillin and amoxicillin or (b) ampicillin and amoxicillin and a dibasic acid are readily absorbed following oral adminstration, and are useful in treating bacterial infections.Type: GrantFiled: July 12, 1984Date of Patent: June 4, 1985Assignee: Pfizer Inc.Inventors: Ernest S. Hamanaka, John G. Stam
-
Patent number: 4515789Abstract: A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbo nylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.Type: GrantFiled: April 7, 1983Date of Patent: May 7, 1985Assignee: Bayer AktiengesellschaftInventors: Karl G. Metzger, Wilfried Schrock, Dieter Habich, Paul Naab, Hans-Joachim Zeiler
-
Patent number: 4508723Abstract: 6-Amino-penam compounds, having an antimicrobial action, of the formula ##STR1## in which R.sub.1 is an azaoligocycloalkyl radical which is bonded via the ring nitrogen atom and contains at least one endo-bridge atom and a total of 7 to 12 ring atoms and can contain a double bond and/or, if desired, as a further ring hetero-atom, an oxygen atom, or a nitrogen atom which can link the radical X.sub.1, where X.sub.1 is hydrogen or lower alkyl, and/or, if desired, free, esterified or etherified hydroxyl which is bonded to a ring carbon atom, and in which R.sub.Type: GrantFiled: June 4, 1982Date of Patent: April 2, 1985Assignee: Ciba Geigy CorporationInventors: Karl Schaffner, Riccardo Scartazzini
-
Patent number: 4505915Abstract: This invention relates to a new class of penicillins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## attached to the 6-amino nitrogen moiety of the penicillin (or ring analogue thereof) nucleus represents a mono- or polycyclic N-containing heterocyclic group;X is S, SO, CH.sub.2, or O; m is 0, 1 or 2;R is, inter alia, hydrogen, substituted and unsubstituted: alkyl, aryl, alkenyl, heterocyclylalkyl, heterocyclylalkenyl, aralkenyl, aralkyl, --NR.sub.2, COOR, CONR.sub.2, --OR, or CN;R.sup.2 is H, or lower alkoxyl.Type: GrantFiled: March 16, 1981Date of Patent: March 19, 1985Assignee: Merck & Co., Inc.Inventor: John Hannah
-
Patent number: 4496587Abstract: The present invention provides a method for inhibiting the synthesis and release of toxins from bacteria which comprises contacting the bacteria with an antitoxic prostaglandin.Type: GrantFiled: April 29, 1983Date of Patent: January 29, 1985Assignee: The Upjohn CompanyInventors: Harold E. Renis, Mary J. Ruwart