3-position Substituent Contains Ethylenic Or Acetylenic Unsaturation Or Nitrogen Patents (Class 548/231)
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Publication number: 20100184781Abstract: The present invention relates to novel oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof, and processes for preparing the same, and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof can be usefully employed as an anticoagulant for treating thromboembolism and tumors via inhibition of coagulation factor Xa.Type: ApplicationFiled: May 9, 2008Publication date: July 22, 2010Applicant: LEGOCHEM BIOSCIENCE LTD.Inventors: Young Lag Cho, Ho Young Song, Dae Yon Lee, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Publication number: 20100137274Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: June 30, 2009Publication date: June 3, 2010Applicant: Bayer Schering Pharma AGInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Publication number: 20100063043Abstract: The invention relates to the field of blood coagulation, more particularly, to novel compounds of general formula (I), to a method for producing said compounds and to their use as active ingredients in medicaments for the prevention and/or the treatment of diseases.Type: ApplicationFiled: August 31, 2009Publication date: March 11, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Röhrig, Karl-Heinz Schlemmer
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Publication number: 20100041646Abstract: The present application relates to novel 1,4-phenylene-bis-oxazolidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.Type: ApplicationFiled: October 20, 2006Publication date: February 18, 2010Applicant: BAYER HEALTHCARE AGInventors: Susanne Rohrig, Jens Pohlmann, Sabine Arndt, Mario Jeske, Metin Akbaba, Elisabeth Perzborn, Christoph Gerdes, Karl-Heinz Schlemmer
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Publication number: 20090312363Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.Type: ApplicationFiled: February 14, 2007Publication date: December 17, 2009Inventors: James Elliot Bradner, Ralph Mazitschek, Tang Weiping, Stuart S. Schreiber
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Publication number: 20090221655Abstract: The present invention provides a compound of Formula (I) Or a pharmaceutically acceptable salt thereof wherein: W is CH2NHC(?Z)R1, C(?Z)NHR2, or CH2het; X is H, C1-6alkyl, or C2-6alkenyl; Y is H, or F; Z is O, or S; R1 is C1-6alkyl, NHC1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, or OC1-4alkyl; R2 is H, C1-4alkyl, or —OC1-4alkyl; and het is a five-(5) or six-(6) membered heterocyclic ring having 1-4 heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen within the ring, wherein each carbon atom in het is optionally substituted with C1-4alkyl, C2-4alkenyl, C2-4alkynyl, halo, OR3, CN, NO2, NHR3R3, oxo, CF3, OCF3, C(?O)C1-4alkyl, OC(?O)C1-4alkyl, or C(?O)OR3; wherein R3 is H, or C1-4alkyl.Type: ApplicationFiled: January 22, 2007Publication date: September 3, 2009Applicant: Pitzer, Inc.Inventors: Vara Prasad Venkata Nagendra Josyula, Allison Laura Choy
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Patent number: 7576111Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: GrantFiled: October 31, 2007Date of Patent: August 18, 2009Assignee: Bayer Schering Pharma AGInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Publication number: 20090099355Abstract: The present invention relates to processes for the production of 4-(biphenylyl)azetidin-2-one phosphonic acid derivatives of formulaType: ApplicationFiled: May 25, 2006Publication date: April 16, 2009Applicant: MICROBIA, INC.Inventors: Stephen Antonelli, Timothy C. Barden, Peter Lee, Eduardo J. Martinez, Wayne C. Schairer, John J. Talley
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Publication number: 20090075979Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.Type: ApplicationFiled: December 29, 2006Publication date: March 19, 2009Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Cameron J. Smith, Adrian A. Dowst, Yi-Heng Chen
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Publication number: 20090048305Abstract: The present invention provides certain ortho-fluorophenyl oxazolidinones of the following formula I: or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: ApplicationFiled: August 6, 2008Publication date: February 19, 2009Inventor: Mikhail Fedorovich Gordeev
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Publication number: 20080300288Abstract: Non-nucleoside inhibitors of HIV-1 reverse transcriptase are described. Such inhibitors may be used as part of a combination therapy to treat HIV infection. Compounds described herein exhibit antiviral potency. In addition, compounds described herein exhibit metabolic stability. Also described herein are processes for preparing Non-nucleoside inhibitors of HIV-1 reverse transcriptase.Type: ApplicationFiled: June 29, 2006Publication date: December 4, 2008Applicant: PURDUE RESEARCH FOUNDATIONInventors: Mark S. Cushman, Bo-Liang Deng
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Publication number: 20080262056Abstract: The present invention relates to novel oxazolidinones derivatives of oxindoles of formula I or a pharmaceutically acceptable salt thereof wherein: Y1 is CH or CF; R1 is —C1-4alkyl, optionally substituted with a fluoro atom, or R1 is —C3-5cycloalkyl; and R2 is —C1-2alkyl. These compounds are useful as antibacterial agents.Type: ApplicationFiled: July 19, 2005Publication date: October 23, 2008Inventors: Gary Wayne Luehr, Rama Jain, Adam Robert Renslo, Mikhail Fedorovich Gordeev, Vara Prasad Venkata Nagendra Josyula
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Patent number: 7166618Abstract: The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or optionally, at least one therapeutic agent, such as, steroids, nonsteroidal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhiType: GrantFiled: June 18, 2003Date of Patent: January 23, 2007Assignee: NitroMed, Inc.Inventors: Ramani R. Bandarage, David S. Garvey, L. Gordon Letts, Joseph D. Schroeder, Sang William Tam
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Patent number: 7109223Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.Type: GrantFiled: August 25, 2003Date of Patent: September 19, 2006Assignee: Merck & Co. Inc.Inventors: Yongxin Han, John Colucci, Xavier Billot, Marie-Claire Wilson, Robert Young
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Patent number: 7087629Abstract: Compounds of formula (I) or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q3 and Q5; R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: March 6, 2003Date of Patent: August 8, 2006Assignee: AstraZeneca ABInventor: Michael Barry Gravestock
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Patent number: 7074785Abstract: Novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, A, R4 and m have the meanings given in the description, a number of processes for preparing these substances, and their use for controlling pests, and also novel intermediates and their preparation.Type: GrantFiled: September 4, 2002Date of Patent: July 11, 2006Assignee: Bayer Cropscience AGInventors: Thomas Seitz, Martin Füsslein, Johannes Rudolf Jansen, Udo Kraatz, Angelika Lubos-Erdelen, legal representative, Andreas Turberg, Olaf Hansen, Christoph Erdelen, deceased
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Patent number: 7002020Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.Type: GrantFiled: August 17, 2000Date of Patent: February 21, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel
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Patent number: 6969726Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: June 2, 2004Date of Patent: November 29, 2005Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 6897230Abstract: Oxazolidinones having a bicyclic[3.1.0]hexane containing moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof, and wherein the variables R1, R2, R3, R4, R4a, A, Ar, HAr, n, r, and s are as defined herein.Type: GrantFiled: April 17, 2002Date of Patent: May 24, 2005Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasumichi Fukuda, Milton L. Hammond
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Patent number: 6743811Abstract: Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.Type: GrantFiled: June 27, 2002Date of Patent: June 1, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Robert C. Gadwood
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Publication number: 20040077626Abstract: The present invention describes difluororthioacetamide oxazolidinones as novel antibacterial agents, and antimicrobial combination therapies for combating infective diseases caused by gram-positive and gram-negative bacteria.Type: ApplicationFiled: June 16, 2003Publication date: April 22, 2004Inventors: Jackson Boling Hester, Wade J. Adams, Jeffrey Charles Stevens, Mikhail Fedor Gordeev, Upinder Singh, Carole Scott
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Patent number: 6586452Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: July 9, 2001Date of Patent: July 1, 2003Assignee: Merck & Co., Inc.Inventors: Thomas Shih, Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Howard C. H. Kuo, Prasun K. Chakravarty, Matthew J. Wyvratt, Sriram Tyagarajan, Richard Berger
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Patent number: 6518427Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.Type: GrantFiled: June 28, 2001Date of Patent: February 11, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Bharat V. Kamdar
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Patent number: 6515135Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.Type: GrantFiled: June 28, 2001Date of Patent: February 4, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Bharat V. Kamdar
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Patent number: 6512112Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.Type: GrantFiled: June 28, 2001Date of Patent: January 28, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Bharat V. Kamdar
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Patent number: 6441005Abstract: Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.Type: GrantFiled: July 26, 2000Date of Patent: August 27, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Robert C. Gadwood
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Patent number: 6441188Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.Type: GrantFiled: June 28, 2001Date of Patent: August 27, 2002Assignee: Pharmacia & Upjohn companyInventors: Robert C. Gadwood, Bharat V. Kamdar
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Patent number: 6387896Abstract: The present invention provides compounds of formula I useful as antimicrobial agents wherein W, X, Y, R1, R2 and n are as defined in thereof.Type: GrantFiled: May 17, 2000Date of Patent: May 14, 2002Assignee: Pharmacia & Upjohn Co.Inventors: Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Jr., Paul D. Johnson
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Patent number: 6277985Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.Type: GrantFiled: September 9, 1996Date of Patent: August 21, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Bharat V. Kamdar
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Patent number: 6239152Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.Type: GrantFiled: January 22, 1999Date of Patent: May 29, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
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Patent number: 6194441Abstract: The invention concerns a compound of formula (I) wherein for example R1 is of the formula —NHC(═O)Ra wherein Ra is hydrogen, or (1-4C)alkyl; R2 and R3 are independently hydrogen or fluoro, R4 is hydrogen, (1-4C)alkyl, halo or trifluoromethyl; R5 and R6 are, for example, independently hydrogen, (1-4C)alkyl, an acetylene of the formula -≡-H or -≡-(1-4C)alkyl, or a group of formula (IA) wherein, for example, Z is hydrogen or (1-4C)alkyl; X and Y are (1-4C)alkyl, halo, cyano, phenyl or heteroaryl; provided that X, Y and Z do not define a (2-4C)alkenyl group and provided that at least one of R5 and R6 is a group of formula (IA) or an acetylene of the formula -≡-H or -≡-(1-4C)alkyl; and pharmaceutically acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.Type: GrantFiled: February 18, 2000Date of Patent: February 27, 2001Assignee: Zeneca Ltd.Inventors: David Anthony Roberts, Michael John Betts
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Patent number: 6143068Abstract: This invention relates to a process for preparing perylene pigment compositions by reaction of(a) a perylene tetracarboxylic compound;(b) about 0.01 to about 20% by weight, relative to the perylene tetracarboxylic compound, of a non-pigmentary cyclic anhydride or imide of formula (I) ##STR1## wherein W is O or NR' (where R.sup.1 is hydrogen, a metal, or optionally substituted alkyl, cycloalkyl, aralkyl, or aryl), R.sup.2, R.sup.3, and R.sup.4 are various combinations of substituents and/or fused-on rings, and the dotted line is an optional double bond representing R.sup.2 --C.dbd.C--R.sup.3 ;(c) ammonia or a primary alkyl, aralkyl, or aryl amine; optionally in the presence of(d) a solvent and/or(e) one or more dispersants.Type: GrantFiled: January 25, 2000Date of Patent: November 7, 2000Assignee: Bayer CorporationInventors: Gregory R. Schulz, Michael J. Greene
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Patent number: 6143772Abstract: Compounds derived from 3-(benzofuran-5-yl) oxazolidin-2-one, of general formula (I) ##STR1## in which: R.sub.1 represents a phenyl group, a phenylmethyl group, an alkyl group or a fluoroalkyl group, and R.sub.2 represents a hydrogen atom or a methyl group. Application in therapeutics.Type: GrantFiled: May 8, 1998Date of Patent: November 7, 2000Assignee: SynthelaboInventors: Samir Jegham, Frederic Puech, Philippe Burnier, Danielle Berthon
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Patent number: 6043266Abstract: A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is S(O).sub.g or O; R.sub.2 is H, methyl, or OH; R.sub.3 and R.sub.4 are independently H or halo; R.sub.5 is H, C.sub.1-12 alkyl, optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy; and g is 0, 1, or 2. The compounds are useful antimicrobial agents.Type: GrantFiled: May 17, 1999Date of Patent: March 28, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Michael Dalton Ennis, David John Anderson
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Patent number: 6019957Abstract: The present invention relates to a radiolabeled non-steroidal compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3, are the same or different and are a radioactive or nonradioactive halogen, a nitro, a cyano, a carbamoyl, a hydrogen, a perfluoroalkyl, a haloalkylamido, an isothiocyanate, an azide, a diazocarbonyl, a substituted oxirane, or a .beta.-chloroethylamine;R.sub.4 is a hydrogen, an alkyl, or is joined to R.sub.5 ;R.sub.5 is a radioactive or nonradioactive halogen, a hydrogen, a hydroxy, an alkyl, a haloalkyl, an alkoxy, an acyloxy, an amino, an alkylamino, a thio, a thioalkyl, or is joined to R.sub.4 ;R.sub.6 is a hydrogen, an alkyl, a halogen, or a haloalkyl;A.sub.1 and A.sub.2 are the same or different, and each is a direct link or an alkylene;X.sub.1 is a radioactive or nonradioactive halogen, an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or alkylene;R.sub.Type: GrantFiled: June 4, 1998Date of Patent: February 1, 2000Assignee: The University of Tennessee Research CorporationInventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
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Patent number: 5968958Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: June 19, 1997Date of Patent: October 19, 1999Assignee: Merck Frosst Canada, Inc.Inventors: Daniel Guay, Chun-Sing Li, Nathalie Ouimet
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Patent number: 5968962Abstract: A compound of the formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1, S(O).sub.g, or O; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -- aryl, --COR.sub.1--1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1--1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h --aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h --aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.Type: GrantFiled: August 13, 1996Date of Patent: October 19, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn
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Patent number: 5962683Abstract: A description is given of compounds of the formula I ##STR1## where r is 0 or 1 and y is a number from the range 1-3; X is a direct bond or --NR.sub.8 --, --CO--, --CONH-- or --COO-- or a divalent aliphatic or mixed aromatic-aliphatic C.sub.1 -C.sub.18 hydrocarbon radical;Z is an aromatic, aliphatic or mixed aromatic-aliphatic C.sub.3 -C.sub.18 hydrocarbon radical which is interrupted in the aliphatic moiety by one or more divalent functional groups, in each case in a carbon-carbon single bond, and/or in the aromatic or aliphatic moiety by one or more divalent functional groups, in each case in a carbon-hydrogen bond, possible functional groups being --O--, --NR.sub.8 --, --S--, --SO--, --SO.sub.Type: GrantFiled: June 17, 1997Date of Patent: October 5, 1999Assignee: Ciba Specialty Chemicals Corp.Inventors: Alfred Steinmann, Rolf Mulhaupt
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Patent number: 5929248Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.Type: GrantFiled: April 23, 1997Date of Patent: July 27, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5910504Abstract: A hetero-aromatic (Q) substituted phenyloxazolidinone antimicrobial of Formula (I) wherein Q is a 5-member hetero-aromatic having from one to four nitrogen atoms or alternatively a benzoannulated 5-member hetero-aromatic having from one to four nitrogen atoms where R.sup.1 is independently H, OCH.sub.3, F, or Cl; R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl (optionally substituted with one or more of F, Cl, hydroxy, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 acyloxy), C.sub.3 -C.sub.6 cycloalkyl, amino, C.sub.1 -C.sub.8 alkylamino, C.sub.1 -C.sub.8 dialkylamino, C.sub.1 -C.sub.8 alkoxy; and each Q is optionally substituted with one or more of H, F, Cl, Br, OR.sup.4, SR.sup.4, S(O).sub.n R.sup.4 (n=1 or 2), CN, O.sub.2 CR.sup.4, NHCOR.sup.4, NHCO.sub.2 R.sup.4, NHSO.sub.2 R.sup.4, CO.sub.2 R.sup.4, CON(R.sup.4).sub.2, COR.sup.4, C.sub.1 -C.sub.8 straight or branched chain alkyl or C.sub.3 -C.sub.Type: GrantFiled: August 4, 1997Date of Patent: June 8, 1999Assignee: Pharmacia & UpjohnInventor: Douglas K. Hutchinson
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Patent number: 5843975Abstract: The present invention relates to isoindole derivatives, and more particularly to 5-(hydroxymethyl)oxazolidine-2-one derivatives which are substituted at the 3 position by an indazole, benzisoxazole or benzisothiazole ring system, to a process for their preparation and to their application in therapy.Type: GrantFiled: December 2, 1997Date of Patent: December 1, 1998Assignee: SynthelaboInventors: Samir Jegham, Frederic Puech, Philippe Burnier
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Patent number: 5817826Abstract: The present invention relates to a compound represented by the formula: ##STR1## wherein a and b are each a carbon atom; a bond:- - - - -between a and b indicates that it is a single bond or a double bond;X is a hydrogen atom, an optionally substituted aryl group, an optionally substitued heteroaryl group, or an optionally substituted aralkyl group;Y is a hydrogen atom, an optionally substituted aryl group, an optionally substituted aralkyl group, or a carboxyl group or related functional groups thereof; andZ is a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted aralkyl, an optionally substituted arylalkenyl group, an optionally substituted heteroarylalkyl group, an optionally substituted heteroarylalkenyl group, an optionally substituted aryloxyalkyl group, an optionally substituted aralkyloxyalkyl group, an optionally substituted arylcarbonylalkyl group, an optionally substituted arylsulfonylalkyType: GrantFiled: August 5, 1997Date of Patent: October 6, 1998Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Toshiyuki Kato
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Patent number: 5747501Abstract: Compounds of the formula ##STR1## where W is ##STR2## n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is --O--, --S--, --NH, or --CH.sub.2 ; R.sub.1 is hydrogen, C.sub.1 to C.sub.8 alkyl, substituted C.sub.1 to C.sub.8 alkyl substituted with one hydroxy, C.sub.3 to C.sub.8 alkenyl, C.sub.3 to C.sub.8 alkynyl, aryl, C.sub.1 to C.sub.3 alkylaryl, C.sub.1 to C.sub.3 alkylheteroaryl, or --Q--R.sub.4 ; R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkylaryl, or C.sub.1 to C.sub.3 alkylheteroaryl; R.sub.4 is cyano, trifluoromethyl, --COR.sub.9, --CO.sub.2 R.sub.9, --CONR.sub.9 R.sub.10, --OR.sub.9, --SO.sub.2 NR.sub.9 R.sub.10, or --S(O).sub.q R.sub.9 ; R.sub.9 and R.sub.10 are each independently hydrogen, C.sub.1 to C.sub.8 alkyl, C.sub.1 to C.sub.3 alkylaryl, aryl, or R.sub.9 and R.sub.Type: GrantFiled: September 16, 1994Date of Patent: May 5, 1998Assignee: Pfizer, Inc.Inventors: John Eugene Macor, Martin James Wythes
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Patent number: 5748233Abstract: A CPU (11) checks a photographic storing mode for a still image or animate object which is determined when photography takes place and a compression rate mode (a compression rate depends on normal, economy, and the like). When the checked mode coincides with a photographic storing mode or compression rate mode stored in an EEPROM (12) when photographs were taken, a scale factor is read which is stored in the EEPROM (12) in correspondence with the respective modes and which has been used for compressing and coding. After that, the scale factor is set in a data compression/extension section (7) and is used as a scale factor for the compression/coding in the present photography. Accordingly, the time required to determine a scale factor is shortened, and an error generated when an image signal is stored is prevented. Accordingly, a good photographic result can be obtained.Type: GrantFiled: April 18, 1996Date of Patent: May 5, 1998Assignee: Ricoh Company, Ltd.Inventors: Tatsutoshi Kitajima, Yasushi Yamamoto
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Patent number: 5723480Abstract: Novel oxazolidinone derivatives of the formula I ##STR1## in which R.sup.1 is a phenyl radical which is unsubstituted or is monosubstituted by CN, H.sub.2 N--CH.sub.2 --, A.sub.2 N--CH.sub.2 --, H.sub.2 N--C(.dbd.NH)--, H.sub.2 N--C(.dbd.NH)--NH--, H.sub.2 N--C(.dbd.NH)--NH--CH.sub.2 --, HO--NH--C(.dbd.NH)-- or HO--NH--C(.dbd.NH)--NH--,X is O, S, SO, SO.sub.2, --NH-- or --NA--,B is ##STR2## A is alkyl having from 1 to 6 C atoms, R.sup.2 is H, A, Li, Na, K, NH.sub.4 or benzyl,R.sup.3 is H or (CH.sub.2).sub.n --COOR.sup.2,E is, in each case independently of each other, CH or N,Q is O, S or NH,m is 1, 2 or 3, andn is 0, 1, 2 or 3,and physiologically compatible salts thereof are provided, which inhibit the binding of fibrinogen to the corresponding receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and also tumors.Type: GrantFiled: May 29, 1996Date of Patent: March 3, 1998Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Guido Melzer, Sabine Bernotat-Danielowski
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Patent number: 5708167Abstract: Proposed is a novel and very efficient method for the preparation of an N-vinyl compound such as N-vinyl-2-pyrrolidone and N-vinyl-N-ethyl acetamide by the thermal decomposition of an N-(.alpha.-acyloxyethyl) compound which is a novel compound obtained by the addition reaction between an NH group-containing compound such as 2-pyrrolidone and N-ethyl acetamide and a vinyl carboxylate, e.g., vinyl acetate, in the presence of an alkali, e.g. alkali metal hydroxide. The reaction mixture after completion of this addition reaction as such, i.e. without isolating the N-(.alpha.-acyloxyethyl) compound, such as N-(.alpha.-acetoxyethyl)-2-pyrrolidone and N-(.alpha.-acetoxyethyl)-N-ethyl acetamide, is heated to effect in situ formation of the desired N-vinyl compound which can then be isolated by distillation under reduced pressure in a very high overall yield.Type: GrantFiled: August 23, 1995Date of Patent: January 13, 1998Assignee: Shin-Etsu Vinyl Acetate Co., Ltd.Inventors: Yoshihiro Honma, Shozo Tanaka, Mitsuyoshi Oshima, Soji Tanioka, Fumiaki Kawamoto
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Patent number: 5700946Abstract: The present invention provides a process for producing an N-vinyl compound, which comprises subjecting an N-(-alkoxyalkyl) compound to gas phase intramolecular alcohol elimination to convert said compound to an N-vinyl compound directly in one step, wherein a solid oxide containing phosphorus and an alkali metal and/or an alkaline earth metal is used as a catalyst. This process need not use any solvent or any auxiliary raw material and consequently can produce an N-vinyl compound simply and safely without generating any waste material derived from the auxiliary raw material.Type: GrantFiled: April 17, 1996Date of Patent: December 23, 1997Assignee: Nippon Shokubai Co., Ltd.Inventors: Yuuji Shimasaki, Hideyuki Kanbe, Akira Kurusu
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Patent number: 5684023Abstract: The present invention relates to benzofuranyl- and benzothienyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.Type: GrantFiled: July 17, 1995Date of Patent: November 4, 1997Assignee: Bayer AktiengesellschaftInventors: Bernd Riedl, Dieter Habich, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus Dieter Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
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Patent number: 5639890Abstract: N-Alkenylcarbamic esters of the general formula I ##STR1## where at least one of the R.sup.1 radicals is hydrogen and the second R.sup.1 radical is hydrogen or C.sub.1 -C.sub.4 --alkyl, the R.sup.2 radical is an aliphatic, cycloaliphatic, araliphatic or aromatic radical which can be linked to the R.sup.3 radical to form a 2- to 10-membered bridge, and the R.sup.3 radical is an aliphatic, cycloaliphatic or aromatic radical, from an alkenyl carboxylate of the general formula II ##STR2## where R.sup.1 has the abovementioned meaning, and R.sup.4 is hydrogen, an aliphatic, cycloaliphatic or aromatic radical, and a carbamic ester of the general formula III ##STR3## where the R.sup.2 and R.sup.3 radicals have the abovementioned meanings, are prepared by reacting the starting compounds in the presence of a base.Type: GrantFiled: August 29, 1996Date of Patent: June 17, 1997Assignee: BASF AktiengesellschaftInventors: Jochem Henkelmann, Marc Heider, Thomas Ruhl
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Patent number: 5412100Abstract: Fungicidal substituted acrylic esters of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl, aralkenyl, aryl or heteroaryl,R.sup.2 represents halogen, cyano, nitro, formyl, halogenoalkyl, alkoxyalkyl or alkylthioalkyl, or represents hydroximinoalkyl, alkoximinoalkyl, N-alkyliminoalkyl, N-aryliminoalkyl or N,N-dialkylhydrazonoalkyl, or represents alkoxy, alkylthio, halogenoalkoxy or halogenoalkylthio, or represents aryloxy or arylthio, or represents alkanoyl, alkoxycarbonyl, N,N-dialkylcarbamoyl or heterocyclylcarbonyl,R.sup.3 represents alkyl, or represents optionally substituted aralkyl,R.sup.4 represents dialkylamino or represents a radical --Z--R.sup.5,X represents oxygen or sulphur andY represents oxygen or sulphur or represents a radical ##STR2## where R.sup.5 represents alkyl or represents optionally substituted aralkyl,R.sup.Type: GrantFiled: July 1, 1993Date of Patent: May 2, 1995Assignee: Bayer AktiengesellschaftInventors: Alexander Klausener, Gerd Kleefeld, Wilhelm Brandes, Stefan Dutzmann, Gerd Hanssler