Polycyclo Ring System Containing The Hetero Ring As One Of The Cyclos Patents (Class 540/203)
  • Publication number: 20150031662
    Abstract: A pharmaceutical composition, comprising a combination of an antibiotically active compound of the formula (I): with a ?-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another ?-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).
    Type: Application
    Filed: October 13, 2014
    Publication date: January 29, 2015
    Inventors: Eric Desarbre, Bérangère Gaucher, Malcom G.P. Page, Patrick Roussel
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • Patent number: 8753794
    Abstract: Disclosed are an N-acyl-?-lactam derivative represented by the following general formula, from which a photoresist composition capable of controlling an acid diffusion length to be short is obtained; a polymer obtained by polymerizing the N-acyl-?-lactam derivative represented by the following general formula as one of starting materials; and a photoresist composition containing the polymer.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: June 17, 2014
    Assignee: Kuraray Co., Ltd.
    Inventors: Takashi Fukumoto, Shuji Matsunaga, Miki Tsuruta
  • Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Publication number: 20130178456
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8450477
    Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C.
    Type: Grant
    Filed: September 15, 2008
    Date of Patent: May 28, 2013
    Assignee: Basilea Pharmaceutica A.G.
    Inventors: Marc Muller, Xiaoping Wu, Lin Xu
  • Publication number: 20120148954
    Abstract: Disclosed are an N-acyl-?-lactam derivative represented by the following general formula, from which a photoresist composition capable of controlling an acid diffusion length to be short is obtained; a polymer obtained by polymerizing the N-acyl-?-lactam derivative represented by the following general formula as one of starting materials; and a photoresist composition containing the polymer.
    Type: Application
    Filed: August 27, 2010
    Publication date: June 14, 2012
    Inventors: Takashi Fukumoto, Shuji Matsunaga, Miki Tsuruta
  • Patent number: 8188306
    Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 29, 2012
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Gang Shen
  • Publication number: 20110301133
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Application
    Filed: December 8, 2009
    Publication date: December 8, 2011
    Applicant: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20110251169
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: April 5, 2011
    Publication date: October 13, 2011
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20110224187
    Abstract: The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Application
    Filed: October 14, 2009
    Publication date: September 15, 2011
    Inventors: Anandan Palani, Michael Y. Berlin, Aslanian G. Robert, Vaccaro M. Henry, Chan Tin-Yau, Xiao Dong, Degrado Sylvia, Rao U. Ashwin, Chen Xiao, Lee Yoon Joo, Sofolarides J. Michael, Shao Ning, Huang R. Ying, Liu Zhidan, Wang Li Yuan, Pu Haiyan
  • Publication number: 20110178291
    Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C.
    Type: Application
    Filed: September 15, 2008
    Publication date: July 21, 2011
    Inventors: Marc Muller, Xiaoping Wu, Lin Xu
  • Publication number: 20110082129
    Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
    Type: Application
    Filed: June 25, 2009
    Publication date: April 7, 2011
    Inventors: Christopher Adams, Qi-Ying Hu, Leslie Wighton McQuire, Julien Papillon
  • Patent number: 7902157
    Abstract: Disclosed are compounds of the formula wherein Z1 is —CH2—or —C(O)—, R4 and R5 are carbon chains (and optionally, together can form a C2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R1 and R3 are as defined herein. Also disclosed are methods of treating pain, and methods of inhibiting the absorption of cholesterol using a compound of formula I.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: March 8, 2011
    Assignee: Schering Corporation
    Inventors: Duane A. Burnett, Brian A. McKittrick
  • Patent number: 7884080
    Abstract: The present invention relates to Azetidinone Derivatives of structural formula 1: and compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: February 8, 2011
    Assignee: Schering Plough Corporation
    Inventors: Robert G. Aslanian, Chad E. Bennett, Duane A. Burnett, Tin-Yau Chan, Eugenia Y. Kiselgof, Chad E. Knutson, Joel M. Harris, Brian A. McKittrick, Anandan Palani, Elizabeth M. Smith, Henry M. Vaccaro, Dong Xiao, Hyunjin M. Kim
  • Publication number: 20100305315
    Abstract: A process for the production of a compound of formula (I) wherein ALINKERB represents a linker moiety of formula (V): A[G1-G2*-G3]B; wherein A and B indicate the orientation of the group of formula (V) in formula (I); G1, G2 and G3 have specific meanings described herein and may be present or absent, with the proviso that at least one of G1 or G3 is present; which linker group may furthermore optionally contain one or more groups of formula (VI); and/or other substituents; and R1 represents hydrogen or a C1-C4-alkyl group; R2 represents hydrogen or a C1-C4-alkyl group; R3 independently at each occurrence, represents hydrogen or a C1-C4-alkyl group; x is 0 or 1; y is 0 or 1; z independently at each occurrence, is 0 or 1; and (—) represents a single bond between a primary, secondary or tertiary carbon atom of the moiety ALINKERB and the adjacent nitrogen atom; in which process (A) a compound of formula (II) is reacted with a compound of formula (III) wherein Pr represents an amino protecting group selected from
    Type: Application
    Filed: December 4, 2008
    Publication date: December 2, 2010
    Inventors: Eric Desarbe, Florian Richalet
  • Publication number: 20100009957
    Abstract: A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are ?-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds are suitable for use with ?-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.
    Type: Application
    Filed: September 24, 2007
    Publication date: January 14, 2010
    Inventors: Timothy A. Blizzard, Helen Y. Chen, Jane Yang Wu, Seongkon Kim, Sookhee Ha, Christopher J. Mortko, Narayan Variankaval, Anna Chiu
  • Patent number: 7605288
    Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: October 20, 2009
    Assignee: University of Kansas
    Inventors: Brian Blagg, Gang Shen, Randell C. Clevenger
  • Patent number: 7465720
    Abstract: Disclosed is a total synthesis of a biologically active ?-Lactam—Compound 3, which is related to Salinosporamide A and Omuralide, both structurally and by its activity as a proteasome inhibitor. Also disclosed are proteasome inhibiting compounds having the formula: wherein: R1 is a cyclolower alkyl group; or R1 is a lower alkyl group; and R2 is either hydrogen or a lower alkyl group; R3 is either hydrogen or a lower alkyl group; R4 a halo-lower alkyl group; and R5 is either hydrogen or a lower alkyl group.
    Type: Grant
    Filed: September 12, 2005
    Date of Patent: December 16, 2008
    Assignee: President and Fellows of Harvard College
    Inventors: Elias J. Corey, Philip C. Hogan
  • Publication number: 20080070890
    Abstract: The present invention relates to Spirocyclic Azetidinone Compounds, compositions comprising a Spirocyclic Azetidinone Compound and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of a Spirocyclic Azetidinone Compound.
    Type: Application
    Filed: September 13, 2007
    Publication date: March 20, 2008
    Inventors: Duane A. Burnett, Brian A. McKittrick
  • Patent number: 7297788
    Abstract: The present invention refers to highly functionalised spiro-fused azetidinones of formula I: having a cyclohexane moiety with the desired number of protected or unprotected hydroxyl groups which are introduced with high stereo and regioselectivity, as well as processes for their synthesis.
    Type: Grant
    Filed: May 25, 2004
    Date of Patent: November 20, 2007
    Assignee: Laboratorios Del Dr. Esteve. S.A.
    Inventors: Pedro Noheda Marin, Manuel Bernabe Pajares, Sergio Maroto Quintana, Nuria Tabares Cantero
  • Patent number: 7291728
    Abstract: The present invention is directed to a compound of formula I: wherein R1 and R2 are independently selected from H, halogen, protected or unprotected hydroxy, alkylsilyloxy, substituted or unsubstituted alkyl or cycloalkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, nitro, amino, mercapto or alkylthio; R3 and R4 are independently selected from H, substituted alkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl; Z is —(CRaRb)n— wherein n is a number selected from 1, 2, 3 and Ra and Rb are each independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy, substituted or unsubstituted amino or halogen; Y is
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: November 6, 2007
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Pedro Noheda Marin, Manuel Bernabe Pajares, Sergio Maroto Quintana, Nuria Tabares Cantero
  • Patent number: 6821963
    Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: November 23, 2004
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
  • Patent number: 6602864
    Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: August 5, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
  • Patent number: 6566355
    Abstract: There are described compounds of the formula in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an &agr;- or &bgr;-amino acid or a residue of the general formula Q—X—Y—  (a) wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulfur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear “spacer” with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulfur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulfur, and Y represents one of the groups —CO—, —CS—, —CONH— and (where X contains neither sulfur nor carbonyl as a terminal component) —SO2—; and in which R1 and R2 together signify a group of the formula wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R3 represents
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: May 20, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christian Hubschwerlen, Robert Charnas, Ingrid Heinze, Klaus Gubernator
  • Publication number: 20030087888
    Abstract: The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.
    Type: Application
    Filed: May 14, 2002
    Publication date: May 8, 2003
    Inventors: Alicia Regueiro-Ren, Robert M. Borzilleri, Gregory D. Vite, Soong-Hoon Kim
  • Patent number: 6432396
    Abstract: The present invention provides a method of limiting the presence of a microorganism by contacting the microorganism with polymer-bound metal-containing compositions. The compositions include metal-containing compounds that may be prepared by reacting or polymerizing metal-containing monomers. The microorganism may be present in a liquid that is contacted with the polymer-bound metal-containing composition. Alternatively, the microorganism may be present in a solid that is contacted with the polymer-bound metal-containing composition.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: August 13, 2002
    Assignee: 3M Innovative Properties Company
    Inventors: Kevin D. Landgrebe, David J. Hastings, Terrance P. Smith, Gregory D. Cuny, Ashok Sengupta, Chandrika D. Mudalige, Frank A. Brandys
  • Publication number: 20020091115
    Abstract: The invention is directed to aza-bridged-bicyclic compounds having Formula (I): 1
    Type: Application
    Filed: June 26, 2001
    Publication date: July 11, 2002
    Inventors: Alexey B. Dyatkin, Bruce E. Maryanoff, William J. Hoekstra, Wei He, William A. Kinney
  • Publication number: 20010044532
    Abstract: The invention relates to a process for the preparation of N,N′-carbonylbislactams by reaction of phosgene with at least one lactam which is characterized in that the tertiary amine is chosen from the group consisting of non-nucleophilic aliphatic tertiary amines.
    Type: Application
    Filed: April 23, 2001
    Publication date: November 22, 2001
    Inventors: Hubert Bonnard, Laurence Ferruccio, Jean-Pierre Senet, Pierre-Yves Le Roy
  • Publication number: 20010021779
    Abstract: A method for separation of enantiomers of a lactam represented by formula (I): 1
    Type: Application
    Filed: December 22, 2000
    Publication date: September 13, 2001
    Applicant: Degussa-Huels Aktiengesellschaft
    Inventors: Kurt Guenther, Stefan Merget, Karlheinz Drauz, Hans-Peter Krimmer
  • Patent number: 6281227
    Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: August 28, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
  • Patent number: 6268369
    Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: July 31, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Dhanapalan Nagarathnam, George Chiu, T. G. Murali Dhar, Wai C. Wong, Mohammad R. Marzabadi, Charles Gluchowski, Bharat Lagu, Shou Wu Miao
  • Patent number: 6248733
    Abstract: This invention relates to the use of compounds having the general structure: wherein: Z1 and Z2 each independently represent an arene nucleus, which has from 5 to 14 ring atoms; G1 and G2 each independently represent a metal ligating group; R represents a hydrogen atom, a halogen atom, an alkyl group, an acylamino group, an alkoxy group, a sulfonamido group, an aryl group, a thiol group, an alkylthio group, an arylthio group, an alkylamino group, an arylamino group, an amino group, an alkoxycarbonyl group, an acyloxy group, a nitro group, a cyano group, an alkylsulfonyl group, an arylsulfonyl group, an alkylsulfoxyl group, an arylsulfoxyl group, an aryloxyl group, a hydroxyl group, a thioamido group, a carbamoyl group, a suffamoyl group, a formyl group, an acyl group, a ureido group, an aryloxycarbonyl group, a silyl group, or a sulfoalkoxy group; L1 represents a nitrogen heterocycle; L2 represents a monodentate or polydentate (e.g.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: June 19, 2001
    Assignee: 3M Innovative Properties Company
    Inventors: Kevin D. Landgrebe, Charles E. Shelburne, Terrance P. Smith, Gregory D. Cuny
  • Patent number: 5750681
    Abstract: Bicyclic .beta.-lactams comprising a 5- or 6-membered lactone or lactam ring are obtained in a process comprising a base induced intramolecular cyclization of a 4-substututed .beta.-lactam having a leaving group in the 1-position. An intramolecular nucleophile transfer reaction is proposed as the operative mechanism and the bicyclic .beta.-lactams are obtained in the required stereochemical form for biological activity. The compounds provided are useful intermediates for the preparation of antibiotics and .beta.-lactamase inhibitors.
    Type: Grant
    Filed: June 19, 1995
    Date of Patent: May 12, 1998
    Assignee: University of Notre Dame Du Lac
    Inventors: Min Teng, Marvin J. Miller
  • Patent number: 5728827
    Abstract: This invention provides a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, particularly for azetidinones substituted in the C-3 and C-4 positions and optionally substituted at the ring nitrogen, comprising reacting a .beta.-(substituted-amino)amide, a .beta.-(substituted-amino)acid ester, or a .beta.-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent.
    Type: Grant
    Filed: January 4, 1996
    Date of Patent: March 17, 1998
    Assignee: Schering Corporation
    Inventors: Tiruvettipuram Kannapan Thiruvengadam, Timothy McAllister, Chou-Hong Tann
  • Patent number: 5700931
    Abstract: Disclosed is a novel .beta.-lactam compound, a 7-substituted-2-oxa-7-azabicyclo?3.2.0!heptan-6-one represented by the general formula ##STR1## in which R is an alkyl, cycloalkyl, aryl, halogen-substituted aryl or alkaryl group, having usefulness as an intermediate for the synthesis of various biologically active compounds. The compound can be prepared by the reaction of an isocyanate compound RNCO, R being the same as above, and 2,3-dihydrofuran, preferably, under pressurization up to 2000 atmospheres or higher.
    Type: Grant
    Filed: May 29, 1996
    Date of Patent: December 23, 1997
    Assignee: Japan as represented by Director General of Agency of Industrial Science and Technology
    Inventors: Yoichi Taguchi, Akihiro Oishi, Isao Shibuya, Tohru Tsuchiya
  • Patent number: 5698548
    Abstract: Novel compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is ##STR2## R.sub.2 and R.sub.3 are independently selected from --CH.sub.2 --, --CH(lower alkyl)--, --C(di-lower alkyl)--, --CH.dbd.CH-- and --C(lower alkyl).dbd.CH--; or R.sub.1 with R.sub.2, or R.sub.1 with R.sub.3, form --CH.dbd.CH-- or --CH.dbd.C(lower alkyl)--;u and v are independently 0-3, provided both are not zero;R.sub.4 is B--(CH.sub.2).sub.m C(O)--; m is 0-5;B--(CH.sub.2).sub.q --; q is 0-6;B--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r ; Z is --O--, --C(O)--, phenylene, --N(R.sub.8)-- or --S(O).sub.0-2 --, e and r is 0-5; the sum of e and r is 0-6;B--(C.sub.2 -C.sub.6 alkenylene)--; B'--(C.sub.4 -C.sub.6 alkadienylene)--;B--(CH.sub.2).sub.t --Z--(C.sub.2 -C.sub.6 alkenylene)--; t is 0-3; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6;B--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --; V is cycloalkylene, f is 1-5, g is 0-5; the sum of f and g is 1-6;B--(CH.sub.2).sub.t --V--(C.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: December 16, 1997
    Assignee: Schering Corporation
    Inventors: Sundeep Dugar, John W. Clader, Duane A. Burnett
  • Patent number: 5656624
    Abstract: 4-[(Heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: A is optionally substituted heterocycloalkyl, heteroaryl, benzofused heterocycloalkyl, or benzofused heteroaryl;Ar.sup.1 and Ar.sup.2 are optionally substituted aryl;Q is a bond or, with the 3-position ring carbon of the azetidinone, forms a spiro group; andR.sup.1 is alkylene; alkylene wherein a carbon in the chain is replaced by --O--, --C(O)--, phenylene, --NR.sup.8 --, --S(O).sub.0-2 -- or cycloalkylene; or alkenylene; or, when Q is a bond, R.sup.1 can be alkylene substituted by one or two hydroxy groups or hydroxy derivatives, wherein the alkylene chain can optionally be joined to Ar.sup.1 through --O-- or --S(O).sub.0-2 -- or joined to the azetidinone ring through a --S(O).sub.
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: August 12, 1997
    Assignee: Schering Corporation
    Inventors: Wayne D. Vaccaro, Duane A. Burnett, John W. Clader
  • Patent number: 5648484
    Abstract: A process for producing a compound of the formula ##STR1## comprises the following sequence of steps: ##STR2## wherein the various radicals are as defined in the specification.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: July 15, 1997
    Assignee: Schering Corporation
    Inventor: Guang-Zhong Wu
  • Patent number: 5585487
    Abstract: Disclosed is a method for the preparation of a .beta.-thiolactam compound, i.e. a 7-substituted-2-oxa-7-azabicyclo [3.2.0]-heptan-6-thione, represented by the general formula ##STR1## in which R is an alkyl or aryl group, having usefulness as an intermediate for the synthesis of various biologically active compounds. The compound can be prepared by the reaction of an isothiocyanate compound R--NCS, R being the same as above, and 2,3-dihydrofuran, preferably, under pressurization up to 2000 atmospheres or higher at an elevated temperature.
    Type: Grant
    Filed: March 8, 1996
    Date of Patent: December 17, 1996
    Assignee: Japan as represented by Director General of Agency of Industrial Science and Technology
    Inventors: Akihiro Oishi, Yoichi Taguchi, Isao Shibuya, Tohru Tsuchiya
  • Patent number: 5550230
    Abstract: Disclosed is a novel .beta.-lactam compound, a 7-substituted-2-oxa-7-azabicyclo[3.2.0]heptan-6-one represented by the general formula ##STR1## in which R is an alkyl, cycloalkyl, aryl, halogen-substituted aryl or alkaryl group, having usefulness as an intermediate for the synthesis of various biologically active compounds. The compound can be prepared by the reaction of an isocyanate compound RNCO, R being the same as above, and 2,3-dihydrofuran, preferably, under pressurization up to 2000 atmospheres or higher.
    Type: Grant
    Filed: March 1, 1995
    Date of Patent: August 27, 1996
    Assignee: Japan as represented by Director General of Agency of Industrial Science and Technology
    Inventors: Yoichi Taguchi, Akihiro Oishi, Isao Shibuya, Tohru Tsuchiya
  • Patent number: 5510343
    Abstract: There are described compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxycarbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --;and in which R.sup.1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula --S--Het, wherein Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R.sup.2 represents the sulpho group --SO.sub.3 H or R.sup.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 23, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Charnas, Klaus Gubernator, Ingrid Heinze, Christian Hubschwerlen
  • Patent number: 5453502
    Abstract: The invention provides 1,3,4 substituted and bicyclic derivatives of 2-azetidinones and processes therefor. These compounds are valuable intermediates useful in the preparation of 1-carba(dethia)cephalosporin antibiotics.
    Type: Grant
    Filed: March 16, 1994
    Date of Patent: September 26, 1995
    Assignee: Eli Lilly and Company
    Inventors: James A. Aikins, Larry C. Blaszczak, Kevin P. Lund, John R. Rizzo
  • Patent number: 5252698
    Abstract: The present invention relates to porphyrin and metal ion-containing monomers and polymers. The monomers ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from H, alkyl having 1 to 6 carbon atoms, phenyl or phenyl substituted with 1 to 3 alkyl groups each having 1 to 6 carbons or with 1 to 3 halogen atoms and A is a metal atom, are used with a diamine or a dialdehyde respectively to produce a porphyrin polymer or a metal ion containing porphyrin polymer. These polymers are useful as electrical conductors and as liquid crystal polymers.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: October 12, 1993
    Assignee: SRI International
    Inventors: Tilak R. Bhardwaj, Susanna C. Ventura, Subhash C. Narang
  • Patent number: 5130425
    Abstract: This invention relates to spiro-lactams and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: July 12, 1991
    Date of Patent: July 14, 1992
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Patent number: 5096918
    Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.
    Type: Grant
    Filed: February 5, 1990
    Date of Patent: March 17, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventor: Keith B. Mallion
  • Patent number: 5055463
    Abstract: Provided are new antibacterial spirocyclic 6-amido carbapenems of the formula: ##STR1## wherein: R.sup.1 is hydrogen, C.sub.1-8 substituted or unsubstituted alkyl or C.sub.6-10 substituted or unsubstituted aryl;R.sup.2 is hydrogen, C.sub.1-8 substituted or unsubstituted alkyl or C.sub.2-8 substituted or unsubstituted acyl;R.sup.3 is hydrogen, C.sub.1-8 substituted or unsubstituted thioalkyl or C.sub.6-10 substituted or unsubstituted thioaryl, or 5 or 6 membered substituted or unsubstituted thioheteroaryl; andR.sup.4 is hydrogen, pharmaceutically acceptable alkali metal salt or biolabile ester,and a process for their synthesis through novel intermediates.
    Type: Grant
    Filed: August 30, 1990
    Date of Patent: October 8, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Thomas N. Salzmann
  • Patent number: 5039672
    Abstract: Certain spirocyclic heterocyclic compounds, and their pharmaceutically-acceptable salts, are inhibitors of the aldose reductase enzyme, and so are useful for the control of diabetic complications. Exemplary compounds include compounds of the formula ##STR1## wherein Y is ##STR2## X is --O-- or ##STR3## R.sub.1 and R.sub.2 are each independently H, alkyl C.sub.1 -C.sub.6,aryl or arylalkyl (C.sub.1 -C.sub.6);W.sub.1 and W.sub.2 are each independently hydrogen, halogen or nitro; andthe pharmaceutically acceptable base addition salts thereof.
    Type: Grant
    Filed: April 5, 1990
    Date of Patent: August 13, 1991
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Eric R. Larson
  • Patent number: 5017708
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, hydroxy, oxo, halogen, azido, amino, C.sub.1 -C.sub.3 alkylamino, or aminomethyl, in which said amino, C.sub.1 -C.sub.3 alkylamino and aminomethyl each is optionally substituted by one or two members selected from the group consisting of C.sub.1 -C.sub.3 alkyl and amino-protecting group; n is an integer of 1 to 3; p and q each is an integer of 0 to 3 with proviso that p+q=1 to 4 or acid-addition salts thereof, being useful materials for preparing side chains of antibacterial quinolonecarboxylic acids, cephalosporines, or other antibiotics.
    Type: Grant
    Filed: September 8, 1989
    Date of Patent: May 21, 1991
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masaru Ogata, Hiroshi Matsumoto, Sumio Shimizu, Shiro Kida