Double Bond Between Ring Members Of The Five-membered Hetero Ring Patents (Class 540/353)
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Patent number: 8252782Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).Type: GrantFiled: December 18, 2009Date of Patent: August 28, 2012Assignee: Pfizer Inc.Inventors: Steven Joseph Brickner, Mark Edward Flanagan, Manjinder Singh Lall
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Publication number: 20020042408Abstract: The present invention relates to carbapenems and provides a compound of the formula (I): 1Type: ApplicationFiled: February 13, 2001Publication date: April 11, 2002Applicant: ZENECA LIMITEDInventors: Michael John Betts, Gareth Morse Davies, Michael Lingard Swain
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Patent number: 5994345Abstract: Carbapenems substituted with a naphthosultam at position 2 and linked through a CH.sub.2 group are disclosed. Pharmaceutical compositions and methods of treatment are also included. The naphthosultam is substituted with at least one cationic group --A--Q--L--B. ##STR1## A--Q--L--B represents a side chain wherein in part: A is a C.sub.1-6 alkylene group, straight or branched, and optionally interrupted or terminated by 1-2 of --O--, --S--, NR.sup.a --, --C(O)-- and CH.dbd.CH--Q is ##STR2## L represents a C.sub.1-8 alkylene group, straight or branched, and unsubstituted or substituted with 1-3 R.sup.c groups andB represents ##STR3## The carbapenems of the present invention are useful against gram positive microorganisms, especially methicillin resistant Staphylococci.Type: GrantFiled: October 8, 1998Date of Patent: November 30, 1999Assignee: Merck & Co., Inc.Inventors: Lovji D. Cama, Robert R. Wilkening, Ronald W. Ratcliffe, Kenneth J. Wildonger, Wanying Sun
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Patent number: 5770729Abstract: The present invention provides an ozonide reducing agent for use in the ozonolysis reaction of an organic compound, the ozonide reducing agent finding wide applications, and being safe and inexpensive from a commercial viewpoint and easy to treat for disposal.The ozonide reducing agent of the invention is a compound wherein sulfur has, at both ends of its molecule, a hydrocarbon residue substituted by a polar functional group.Type: GrantFiled: January 22, 1996Date of Patent: June 23, 1998Assignee: Otsuka Kagaku Kabushiki KaishaInventors: Michio Sasaoka, Daisuke Suzuki, Takashi Shiroi
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Patent number: 5721360Abstract: The present invention refers to process for the preparation of a tiazoline-azetidinone of formula I ##STR1## which comprises N-protecting in position 1 of (3S,4S)-3-phenylace tamido-4-acetoxy-azetidin-2-one, converting the product thus obtained into the corresponding thioamide and subsequently ciclyzing and deprotecting.Type: GrantFiled: June 6, 1996Date of Patent: February 24, 1998Assignee: Biochimica OPS SpaInventors: Gianfranco Cainelli, Achille Umani Ronchi, Michele Contento, Mauro Panunzio, Sergio Sandri, Marco Da Col, Leone Dall'Asta
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Patent number: 5288860Abstract: The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.Type: GrantFiled: January 11, 1993Date of Patent: February 22, 1994Assignee: Otsuka Kagaku Kasbushiki KaishaInventors: Sigeru Torii, Hideo Tanaka, Masatoshi Taniguchi, Michio Sasaoka, Takashi Shiroi, Yutaka Kameyama
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Patent number: 5206361Abstract: The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.Type: GrantFiled: March 7, 1991Date of Patent: April 27, 1993Assignee: Otsuka Kagaku Kabushiki KaishaInventors: Sigeru Torii, Hideo Tanaka, Masatoshi Taniguchi, Michio Sasaoka, Takashi Shiroi, Yutaka Kameyama
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Patent number: 4824849Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.Type: GrantFiled: August 28, 1987Date of Patent: April 25, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr.
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Patent number: 4810788Abstract: An azetidinone derivative represented by the formula (I) ##STR1## wherein R.sup.1 is substituted or unsubstituted phenyl or substituted or unsubstituted phenoxy, R.sup.2 is hydrogen, optionally substituted hydrocarbon residue or aminoprotecting group selected from acyl, silyl, sulfonyl and phosphonyl derived from organic or inorganic acid, ##STR2## (wherein R.sup.3 is hydrogen or lower alkyl), X.sup.1 and X.sup.2 are the same or different and are halogen, hydroxyl, alkoxy, acyloxy, SR.sup.4 (wherein R.sup.4 is straight chain or branched chain lower alkyl substituted or unsubstituted, substituted or unsubstituted phenyl or substituted or unsubstituted heterocyclic group), amino or hydrogen, one of X.sup.1 and X.sup.2 being hydrogen when the other is not, and R.sup.5 is substituted or unsubstituted phenyl or substituted or unsubstituted heterocyclic group, and a process for preparing the same.Type: GrantFiled: May 6, 1987Date of Patent: March 7, 1989Assignee: Otsuka Kagaku Yakuhin Kabushiki KaishaInventors: Sigeru Torii, Hideo Tanaka, Junzo Nokami, Michio Sasaoka, Norio Saito, Takashi Siroi
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Anti-depressant spiro hexahydro arylquinolizine derivatives, composition, and method of use therefor
Patent number: 4710504Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.Type: GrantFiled: April 4, 1986Date of Patent: December 1, 1987Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr. -
Patent number: 4656264Abstract: An azetidinone compound represented by the formula ##STR1## wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a carboxyl-protecting group, X represents a hydrogen atom or chlorine atom and Y represents --I, --ONO.sub.2, --OH, ##STR2## or --SR.sup.4 in which R.sup.3 is a lower alkyl group or --OR.sup.5 (wherein R.sup.5 is a halogen-containing lower alkyl group) and R.sup.4 is a substituted or unsubstituted, 5-membered aromatic heterocyclic residue containing sulphur and/or nitrogen atom or atoms.Type: GrantFiled: April 29, 1986Date of Patent: April 7, 1987Assignee: Otsuka Kagaku Kabushiki KaishaInventors: Shigeru Torii, Hideo Tanaka, Junzo Nogami, Michio Sasaoka, Norio Saito, Takashi Shiroi