Double Bond Between Ring Members Of The Five-membered Hetero Ring Patents (Class 540/353)
  • Patent number: 8252782
    Abstract: 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: Grant
    Filed: December 18, 2009
    Date of Patent: August 28, 2012
    Assignee: Pfizer Inc.
    Inventors: Steven Joseph Brickner, Mark Edward Flanagan, Manjinder Singh Lall
  • Publication number: 20020042408
    Abstract: The present invention relates to carbapenems and provides a compound of the formula (I): 1
    Type: Application
    Filed: February 13, 2001
    Publication date: April 11, 2002
    Applicant: ZENECA LIMITED
    Inventors: Michael John Betts, Gareth Morse Davies, Michael Lingard Swain
  • Patent number: 5994345
    Abstract: 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: Grant
    Filed: October 8, 1998
    Date of Patent: November 30, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Lovji D. Cama, Robert R. Wilkening, Ronald W. Ratcliffe, Kenneth J. Wildonger, Wanying Sun
  • Patent number: 5770729
    Abstract: 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: Grant
    Filed: January 22, 1996
    Date of Patent: June 23, 1998
    Assignee: Otsuka Kagaku Kabushiki Kaisha
    Inventors: Michio Sasaoka, Daisuke Suzuki, Takashi Shiroi
  • Patent number: 5721360
    Abstract: 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: Grant
    Filed: June 6, 1996
    Date of Patent: February 24, 1998
    Assignee: Biochimica OPS Spa
    Inventors: Gianfranco Cainelli, Achille Umani Ronchi, Michele Contento, Mauro Panunzio, Sergio Sandri, Marco Da Col, Leone Dall'Asta
  • Patent number: 5288860
    Abstract: 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: Grant
    Filed: January 11, 1993
    Date of Patent: February 22, 1994
    Assignee: Otsuka Kagaku Kasbushiki Kaisha
    Inventors: Sigeru Torii, Hideo Tanaka, Masatoshi Taniguchi, Michio Sasaoka, Takashi Shiroi, Yutaka Kameyama
  • Patent number: 5206361
    Abstract: 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: Grant
    Filed: March 7, 1991
    Date of Patent: April 27, 1993
    Assignee: Otsuka Kagaku Kabushiki Kaisha
    Inventors: Sigeru Torii, Hideo Tanaka, Masatoshi Taniguchi, Michio Sasaoka, Takashi Shiroi, Yutaka Kameyama
  • Patent number: 4824849
    Abstract: 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: Grant
    Filed: August 28, 1987
    Date of Patent: April 25, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr.
  • Patent number: 4810788
    Abstract: 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: Grant
    Filed: May 6, 1987
    Date of Patent: March 7, 1989
    Assignee: Otsuka Kagaku Yakuhin Kabushiki Kaisha
    Inventors: Sigeru Torii, Hideo Tanaka, Junzo Nokami, Michio Sasaoka, Norio Saito, Takashi Siroi
  • Patent number: 4710504
    Abstract: 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: Grant
    Filed: April 4, 1986
    Date of Patent: December 1, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr.
  • Patent number: 4656264
    Abstract: 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: Grant
    Filed: April 29, 1986
    Date of Patent: April 7, 1987
    Assignee: Otsuka Kagaku Kabushiki Kaisha
    Inventors: Shigeru Torii, Hideo Tanaka, Junzo Nogami, Michio Sasaoka, Norio Saito, Takashi Shiroi