Additional Chalcogen Bonded Directly To The Hetero Ring Patents (Class 540/354)
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Patent number: 8946409Abstract: Provided herein are polycyclic ?-lactam compounds, compositions thereof and methods for the treatment and prevention of diseases such as cancer, including pancreatic cancer and pancreatic cancers resistant to mainline chemotherapeutic agents.Type: GrantFiled: January 27, 2012Date of Patent: February 3, 2015Assignee: Board of Regents, The University of Texas SystemInventors: Frederick F. Becker, Bimal K. Banik
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Publication number: 20140066423Abstract: Provided herein are polycyclic ?-lactam compounds, compositions thereof and methods for the treatment and prevention of diseases such as cancer, including pancreatic cancer and pancreatic cancers resistant to mainline chemotherapeutic agents.Type: ApplicationFiled: January 27, 2012Publication date: March 6, 2014Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: Frederick F. Becker, Bimal K. Banik
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Publication number: 20110065912Abstract: A stereoselective synthesis of novel ?-lactam dimers as useful precursors for the preparation of paclitaxel, docetaxel, and analogues thereof. More particularly, the new ?-lactams are prepared from readily available and enantiomerically pure chiral auxiliaries. The ?-lactams are then reacted with a suitably protected taxane to produce diastereomerically enriched side chain-bearing taxanes. Finally, the chiral auxiliary is cleaved and protecting groups are removed to provide the desired taxane.Type: ApplicationFiled: November 4, 2010Publication date: March 17, 2011Applicant: ACCORD HEALTHCARE LTD.Inventors: Mettilda LOURDUSAMY, Gaétan Caron
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Patent number: 7906502Abstract: Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.Type: GrantFiled: June 21, 2006Date of Patent: March 15, 2011Assignee: AstraZeneca ABInventors: Susanne Alenfalk, Mikael Dahlstrom, Fana Hunegnaw, Staffan Karlsson, Ingemar Starke
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Publication number: 20090137796Abstract: The present invention relates to a stereoselective synthesis of novel ?-lactam dimers as useful precursors for the preparation of paclitaxel, docetaxel, and analogues thereof. More particularly, the new ?-lactams are prepared from readily available and enantiomerically pure chiral auxiliaries. The ?-lactams are then reacted with a suitably protected taxane to produce diastereomerically enriched side chain-bearing taxanes. Finally, the chiral auxiliary is cleaved and protecting groups are removed to provide the desired taxane.Type: ApplicationFiled: November 3, 2006Publication date: May 28, 2009Applicant: BIOXEL PHARMA INC.Inventors: Mettilda Lourdusamy, Gaétan Caron
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Patent number: 7501404Abstract: Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd? are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.Type: GrantFiled: April 4, 2006Date of Patent: March 10, 2009Assignee: DAIMEDInventors: Thomas Bannister, Cassandra Celatka, Nizal S. Chandrakumar, Hongfeng Deng, Zihong Guo, Lei Jin, Tsvetelina Lazarova, Jian Lin, Scott T. Moe, Pamela Nagafuji, Manuel Navia, Amy Ripka, Michael J. Rynkiewicz, Kerry L. Spear, James E. Stickler, Roger Xie
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Patent number: 6900312Abstract: The present discovery consists in new thiazole-substituted ?-lactams of general formula (I), as well as the method for their preparation. R1, R2, R3, R4, R5, R6, R7, and R8 are, independently from each other, a hydrogen atom, a halogen, a hydroxy, amino, nitro, or thiol group, an optionally substituted alkyl, heteroalkyl, aryl, aralkyl, cycloalkyl, cycloaralkyl, heterocycloalkyl, heteroaralkyl, or heteroaryl rest.Type: GrantFiled: July 16, 2002Date of Patent: May 31, 2005Assignee: Priaton GmbHInventors: Juergen Kolb, Alexander Doemling
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Patent number: 6890921Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the ?-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: March 15, 2000Date of Patent: May 10, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allen Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
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Publication number: 20040167115Abstract: The subject invention concerns N-thiolated &bgr;-lactam compounds, their analogs and pharmaceutically acceptable salts, esters and amides thereof. The subject invention also concerns methods for inducing tumor cell death or inhibiting tumor cell proliferation, and methods for inducing DNA damage, inhibiting DNA replication, activating p38 MAP kinase, or activating caspase cascade activation, or releasing cytochrome C from mitochondria into the cytoplasm in a tumor cell. Methods for treating cancer using N-thiolated &bgr;-lactam compounds, as well as pharmaceutical compositions comprising the same are further disclosed.Type: ApplicationFiled: May 6, 2003Publication date: August 26, 2004Inventors: Q. Ping Dou, Edward Turos, David M. Smith
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Publication number: 20040132991Abstract: Disclosed are taxanes having utility as intermediates in the preparation of paclitaxel, taxotere and analogs thereof, and methods related to the preparation of the same.Type: ApplicationFiled: October 9, 2003Publication date: July 8, 2004Applicant: Phytogen Life Sciences Inc.Inventor: Ragina Naidu
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Publication number: 20040106790Abstract: The present invention relates to novel intermediates for the preparation of 3-methylenecephams. More specifically, the present invention relates to the intramolecular cyclization of penicillin sulfoxide derived monocyclic azetidinone as precursors to cephalosporin antibiotics.Type: ApplicationFiled: November 12, 2003Publication date: June 3, 2004Inventors: Robin D.G. Cooper, Anthony G.M. Barrett
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Patent number: 6730782Abstract: Taxane derivatives having an amino substituted C13 side chain.Type: GrantFiled: February 25, 2002Date of Patent: May 4, 2004Assignee: Florida State UniversityInventors: Robert A. Holton, Hossain Nadizadeh, Kasthuri Rengan, Chunlin Tao
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Publication number: 20040072309Abstract: A process for producing a compound represented by the following formula (II) which comprises treating a compound represented by the following formula (I) (wherein R1, R2 and R3 represent each a specific substituent) with an enzyme capable of asymmetrically hydrolyzing an ester and the novel compound (II). The process of the present invention makes it possible to easily obtain an optically active 2-azetidinone derivative in a large amount at a low cost.Type: ApplicationFiled: September 5, 2003Publication date: April 15, 2004Inventors: Kouji Sato, Tsutomu Yagi, Yutaka Kitagawa, Shigeru Ichikawa, Akihiro Imura
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Patent number: 6602864Abstract: 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: GrantFiled: June 3, 1998Date of Patent: August 5, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
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Patent number: 6544976Abstract: This invention provides compounds having the following general structure: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.Type: GrantFiled: June 12, 2000Date of Patent: April 8, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: James C. Lanter, Suying Zhang, Boyu Zhao
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Publication number: 20030004335Abstract: The present invention relates to a method for the preparation of a compound of the general formula (I) whereinType: ApplicationFiled: May 9, 2002Publication date: January 2, 2003Applicant: Tessenderio Chemie S.A.Inventors: Marcel Maurice Ghislain Ceresiat, Marc Belmans, Jacqueline Marchand-Brynaert, Mathieu Laurent
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Publication number: 20020137927Abstract: Novel &bgr;-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling &bgr;-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.Type: ApplicationFiled: December 5, 2001Publication date: September 26, 2002Inventors: John K. Thottathil, Ivan D. Trifunovich, David J. Kucera, Wen-Sen Li
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Patent number: 6403789Abstract: A halogenating agent of the formula (1) and a method of halogenating hydroxyl group wherein R1 and R2 are the same or different and are each ethyl, propyl, isopropyl, butyl, isobutyl or allyl; X is chlorine atom or bromine atom; and Y is chlorine ion, bromine ion, dichlorophosphate ion, dibromophosphate ion, chlorosulfonate ion, bromosulfonate ion, chlorooxalate ion or bromooxalate ion.Type: GrantFiled: September 26, 2000Date of Patent: June 11, 2002Assignee: Otsuka Kagaku Kabushiki KaishaInventors: Daisuke Suzuki, Ryo Kikuchi, Masaru Yasui
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Patent number: 6395895Abstract: Taxane derivatives having a 3′ butenyl substituted C13 side chain.Type: GrantFiled: October 27, 1999Date of Patent: May 28, 2002Assignee: Florida State UniversityInventors: Robert A. Holton, Ki-byung Chai, Hossain Nadizadeh
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Publication number: 20020049315Abstract: Crystalline forms of [2R-[2&agr;(R*),3&bgr;(R*)]]-3-(1-hydroxyethyl)-&ggr;-methyl-&bgr;,4-dioxo-2-azetidinebutanoic acid(4-nitrophenyl)methyl ester and crystalline form of (&ggr;R,2R,3S)-&agr;-diazo-3-[(1R)-1-hydroxyethyl]-&ggr;-methyl-&bgr;,4-dioxo-2-azetidinebutanoic acid (4-nitrophenyl)methyl ester are disclosed.Type: ApplicationFiled: August 2, 2001Publication date: April 25, 2002Inventor: John M. Williams
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Patent number: 6335324Abstract: Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.Type: GrantFiled: December 13, 1999Date of Patent: January 1, 2002Assignee: Bristol-Myers Squibb Co.Inventors: Gregory S. Bisacchi, William A. Slusarchyk, Uwe Treuner, James C. Sutton, Robert Zahler, Steven Seiler, David R. Kronenthal, Michael E. Randazzo, Mark D. Schwinden, Zhongmin Xu, Zhongping Shi
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Publication number: 20010037020Abstract: A &bgr;-lactam of the formula: 1Type: ApplicationFiled: March 13, 2001Publication date: November 1, 2001Inventor: Robert H. Holton
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Patent number: 6303594Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: March 15, 2000Date of Patent: October 16, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allan Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
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Patent number: 6281227Abstract: 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: GrantFiled: December 2, 1999Date of Patent: August 28, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
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Patent number: 6225463Abstract: The object of the present invention is the development of new chiral auxiliaries for improved &bgr;-lactam formation that control both the diastereoselectivity of &bgr;-lactam formation and which can be removed without destruction of the sensitive azetidinone ring, providing valuable intermediates for coupling to the C-13 hydroxyl group of anti-tumor taxanes, such as paclitaxel. Further, the object of the present invention is enantiomerically pure (S)-(−)-1-(p-methoxy-phenyl)propyl-1-amine.Type: GrantFiled: December 15, 1998Date of Patent: May 1, 2001Assignees: Pharmachemie B.V., Cancer Research Campaign Technology Ltd.Inventors: Dick de Vos, Stephen Brown, Allan M. Jordan, Nicholas J. Lawrence, Alan Th. McGown
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Patent number: 6221860Abstract: This invention relates to methods for treating diseases or disorders mediated by lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which method comprises administration to a mammal in need thereof of an effective Coenzyme A independent transacylase (CoA-IT) inhibiting amount of a triphenylmethylazetidinone. This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a triphenylmethylazetidinone.Type: GrantFiled: November 8, 1999Date of Patent: April 24, 2001Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, James David Winkler
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Patent number: 6214841Abstract: This application relates to a novel compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, processes and Intermediates for its preparation, pharmaceutical formulations comprising the novel compound of formula (I), and the use of the compound of formula (I) as an antithrombotic agent.Type: GrantFiled: November 8, 1999Date of Patent: April 10, 2001Assignee: Eli Lilly and CompanyInventors: Charles Van Jackson, Kenneth Dean Kurz, Robert Theodore Shuman
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Patent number: 6194567Abstract: A halogenating agent of the formula (1) and a method of halogenating hydroxyl group wherein R1 and R2 are the same or different and are each ethyl, propyl, isopropyl, butyl, isobutyl or allyl; X is chlorine atom or bromine atom; and Y is chlorine ion, bromine ion, dichlorophosphate ion, dibromophosphate ion, chlorosulfonate ion, bromosulfonate ion, chlorooxalate ion or bromooxalate ion.Type: GrantFiled: October 13, 1999Date of Patent: February 27, 2001Assignee: Otsuka Kagaku Kabushiki KaishaInventors: Daisuke Suzuki, Ryo Kikuchi, Masaru Yasui
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Patent number: 6187916Abstract: A process for the preparation of a taxane derivative of the formula in which R2 represents an RO—, RS— or RR′N— in which R represents an unsubstituted or substituted straight chain or branched alkyl, alkenyl or alkynyl, or cycloalkyl, saturated heterocyclic, cycloalkenyl, unsaturated heterocyclic, aryl or heterocyclic aromatic; R′ is a hydrogen or R defined above; R and R′ can be connected to form together with the nitrogen a cyclic structure; Y is oxygen or sulfur; R3 represents an unsubstituted or substituted straight chain or branched alkyl, alkenyl or alkynyl radical, an unsubstituted or substituted cycloalkyl, cycloalkenyl or an unsubstituted or substituted aryl; which comprises reacting a &bgr;-lactam of the formula in which R311 represents a radical R3 defined above or a protected R3 whenever R3 includes one or more active hydrogens; with a baccatin III derivative of the formula: in which M is an alkali metalType: GrantFiled: June 7, 1995Date of Patent: February 13, 2001Assignee: Research Foundation of State University of New YorkInventor: Iwao Ojima
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Patent number: 6174879Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: March 17, 1999Date of Patent: January 16, 2001Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 6071915Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I ##STR1## pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the .alpha.-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: May 8, 1998Date of Patent: June 6, 2000Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allen Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
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Patent number: 6054579Abstract: The invention relates to an efficient and facile method for the preparation of substituted lactams, as described herein. The method comprises reacting a difunctional component containing an activated carbon, an amine capable of forming an imine with the activated carbon of the difunctional component, and an isocyanide in a nucleophilic polar protic solvent and at a concentration of reactants which facilitates the formation of the substituted lactams. The invention also relates to novel substituted lactams, libraries comprising such lactams, and a method of generating libraries substituted lactams, using the method of the invention.Type: GrantFiled: June 19, 1998Date of Patent: April 25, 2000Assignee: LeukoSite, Inc.Inventor: Geraldine C. B. Harriman
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Patent number: 6051678Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.Type: GrantFiled: March 13, 1997Date of Patent: April 18, 2000Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
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Patent number: 6013791Abstract: A process for the preparation of a compound of formula (IVA) which process comprises subjecting a compound of formula (V), where R is an ester-forming group or carboxy-protecting group, and X and Y are hydrogen or halogen provided that at least one of X or Y is halogen, to reductive formylation.Type: GrantFiled: March 5, 1998Date of Patent: January 11, 2000Assignee: SmithKline Beecham p.l.c.Inventor: Richard Keith Anderson
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Patent number: 5892036Abstract: The invention relates to novel 2-bromo- and 2-nitroxy derivatives of 3-,bromo- and 3-dibromo-4-oxo-azetidines, to processes for the preparation thereof and to the use thereof.According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines are prepared by reacting derivatives of protected penicillanic lanic acid 1,1-dioxides with DBN reactant (1,5-diazabicyclo/3.4.Type: GrantFiled: September 10, 1997Date of Patent: April 6, 1999Assignee: PLIVA farmaceutskaInventor: Irena Lukic
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Patent number: 5866691Abstract: Novel .beta.-lactam monomers bearing various functional groups are prepared. The novel .beta.-lactam monomers can be joined into oligomeric compounds such as via preferred phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen bonding. The oligomeric compounds are useful as diagnostic and research reagents.Type: GrantFiled: July 19, 1996Date of Patent: February 2, 1999Assignee: ISIS Pharmaceuticals, Inc.Inventors: Vasulinga Ravikumar, Venkatraman Mohan
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Patent number: 5843939Abstract: 3-Bromo- and 3,3-dibromo-4-oxo-1-azetidines of the formula I ##STR1## wherein R.sub.1 is hydrogen or bromo,R.sub.2 is hydrogen or bromo,R.sub.3 is hydrogen, ##STR2## wherein R.sub.4 is hydrogen, methyl, benzyl or some other protective group,R.sub.5 is hydrogen, alkyl, alkylaryl, a heterocyclic ring,Y is a halo atom,X is a halo atom, alkoxy group, nitroxy group are provided along with processes for the preparation thereof and the use thereof.Type: GrantFiled: February 6, 1997Date of Patent: December 1, 1998Assignee: PLIVA, farmaceutska, kemijska, prehrambena i kozmeticka industrija, dionicko drustvoInventor: Irena Lukic
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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: 5760219Abstract: Pyridyl substituted .beta.-lactam compounds used in preparing taxane derivatives having a 3' pyridyl substituted C13 side chain.Type: GrantFiled: September 20, 1996Date of Patent: June 2, 1998Assignee: Florida State UniversityInventors: Robert A. Holton, Kasthuri Rengan
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Patent number: 5750680Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.Type: GrantFiled: September 12, 1996Date of Patent: May 12, 1998Assignees: Hyundai Electronics Industries Co., Ltd., Korea Advanced Institute of Science & TechnologyInventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
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Patent number: 5691356Abstract: Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.Type: GrantFiled: September 4, 1996Date of Patent: November 25, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Spencer D. Kimball, Wan Fang Lau
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Patent number: 5670638Abstract: The azetidines of the present invention have the formula I ##STR1## wherein R.sup.1 is hydrogen or bromine,R.sup.2 is hydrogen or bromine, wherein at least one of R.sup.1 or R.sup.2 is bromine,R.sup.3 is hydrogen; Me.sub.2 --C.dbd.C--COOR.sup.4 wherein R.sup.4 is hydrogen, methyl, benzyl or some other carboxy-protective group, andX is bromine or nitroxy group (--ONO.sub.2).According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines are prepared by reacting derivatives of protected penicillanic acid 1,1-dioxides with DBN reactant (1,5-diazabicyclo/3.4.Type: GrantFiled: July 8, 1994Date of Patent: September 23, 1997Assignee: PLIVA farmaceutskaInventor: Irena Lukic
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Patent number: 5583146Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.Type: GrantFiled: January 17, 1995Date of Patent: December 10, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan F. Lau, Steven E. Hall, Wen-Ching Han
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Patent number: 5574156Abstract: A .beta.-lactam of the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, alkyl, acyl, acetal, ethoxyethyl, or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; and the enantiomers and diastereomers thereof.Type: GrantFiled: June 6, 1994Date of Patent: November 12, 1996Assignee: Florida State UniversityInventor: Robert A. Holton
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Patent number: 5561146Abstract: Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.Type: GrantFiled: October 14, 1994Date of Patent: October 1, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Kyoung S. Kim, Spencer D. Kimball, Jagabandhu Das, Edwin J. Iwanowicz, Wen-Ching Han
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Patent number: 5554746Abstract: Novel .beta.-lactam monomers bearing various functional groups are prepared. The novel .beta.-lactam monomers can be joined into oligomeric compounds such as via preferred phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen bonding. The oligomeric compounds are useful as diagnostic and research reagents.Type: GrantFiled: May 16, 1994Date of Patent: September 10, 1996Assignee: ISIS Pharmaceuticals, Inc.Inventors: Vasulinga Ravikumar, Venkatraman Mohan
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Patent number: 5539103Abstract: .beta.-lactam compounds which are reacted with a metal alkoxide for preparing N-acyl, N-sulfonyl and phosphoryl substituted isoserine esters.Type: GrantFiled: December 7, 1994Date of Patent: July 23, 1996Assignee: Florida State UniversityInventor: Robert A. Holton
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Patent number: 5453502Abstract: 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: GrantFiled: March 16, 1994Date of Patent: September 26, 1995Assignee: Eli Lilly and CompanyInventors: James A. Aikins, Larry C. Blaszczak, Kevin P. Lund, John R. Rizzo
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Patent number: 5423998Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.Type: GrantFiled: April 13, 1993Date of Patent: June 13, 1995Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 5300638Abstract: The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide with an imine derived from L-threonine; and to compounds of formula (III) which are produced in said process: ##STR1## wherein Ar is phenyl; R.sup.1 is hydrogen, an acyl radical of a carboxylic acid, or a carbonic acid ester radical; R.sup.2 is hydrogen or a carboxy protecting group; and R.sup.3 is hydrogen or a hydroxy protecting group.Type: GrantFiled: July 16, 1992Date of Patent: April 5, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Vittorio Farina, Sheila I. Hauck