Ring In Alcohol Moiety Patents (Class 560/31)
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Patent number: 8796459Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: GrantFiled: September 14, 2012Date of Patent: August 5, 2014Assignee: Gilead Sciences, Inc.Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
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Publication number: 20140206878Abstract: Methods of preparing a class of oxazolidinones useful to impede bacterial growth are disclosed.Type: ApplicationFiled: November 25, 2013Publication date: July 24, 2014Applicant: TRIUS THERAPEUTICS, INC.Inventors: Carrie A. Costello, Jacqueline A. Ware, Robert J. Duguid
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Patent number: 8598347Abstract: The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.Type: GrantFiled: March 30, 2010Date of Patent: December 3, 2013Assignee: Dong-A Pharmaceutical. Co., LtdInventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Hyun Joo Shim, Moohi Yoo
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Publication number: 20130296332Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
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Publication number: 20130281453Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.Type: ApplicationFiled: October 21, 2011Publication date: October 24, 2013Applicant: The Scripps Research InstituteInventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
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Publication number: 20130267729Abstract: Disclosed are methods for preparing compounds of Formula 1 and 1A. The first method utilizes a benzyl carbamate amine protecting group and an intermediate of Formula 4. The second method utilizes a tert-butyl carbamate amine protecting group and an intermediate of Formula 7. The third method utilizes a dibenzyl amine protecting group. Also disclosed is a compound, phenylmethyl N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]carbamate (a compound of Formula 4). Further disclosed is a method for preparing a compound of Formula 14 from a compound of Formula 15 and a compound of Formula 1 or 1A.Type: ApplicationFiled: September 23, 2011Publication date: October 10, 2013Applicant: E.I. du Pont de Nemours and CompanyInventor: Joerg Bruening
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Publication number: 20130137720Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.Type: ApplicationFiled: November 30, 2012Publication date: May 30, 2013Applicant: The Regents of the University of Colorado, a body corporatedInventors: Xiang Wang, Wenqing Xu
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Patent number: 8367868Abstract: The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: where: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:Type: GrantFiled: October 4, 2007Date of Patent: February 5, 2013Assignee: Archimica S.r.l.Inventors: Giorgio Bertolini, Barbara Verzola, Domenico Vergani
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Publication number: 20130005972Abstract: A method for generating a radiolabeled tracer. The method includes providing a phosphine molecule having at least one carbocyclic, aromatic, or pyrrolidinyl ring with an OH substitute. The OH of this phosphines molecule is then condensed with an acid to produce a phosphine ester. Staudinger ligation is then performed to generate the radiolabeled tracer by treating the phosphine ester with a radiolabeled azide having a PET radioisotope moiety.Type: ApplicationFiled: March 29, 2011Publication date: January 3, 2013Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Dhanalakshmi Kasi, Umesh Gangadharmath, Joseph Walsh, Hartmuth Kolb
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Patent number: 8153844Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.Type: GrantFiled: June 27, 2007Date of Patent: April 10, 2012Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard F. Davis, Rafael Shapiro, Eric G. Taylor
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Publication number: 20120016126Abstract: The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.Type: ApplicationFiled: March 30, 2010Publication date: January 19, 2012Applicant: DONG-A PHARMACEUTICAL. CO., LTDInventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Hyun Joo Shim, Moohi Yoo
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Publication number: 20120016125Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.Type: ApplicationFiled: March 30, 2010Publication date: January 19, 2012Applicant: DONG-A PHARMACEUTICAL. CO., LTDInventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Moohi Yoo, Geun Gho Lim, Sun Ki Chang
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Patent number: 8058468Abstract: The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds around the lead compound (3,4-dichloro-phenyl)-carbamic acid 2-isobutoxycarbonylamino-1-methyl-ethyl ester, which are especially useful for combating infections with gram-positive bacteria and especially MRSA.Type: GrantFiled: December 21, 2006Date of Patent: November 15, 2011Assignee: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNOInventors: Frank Henri Johan Schuren, Henricus Matheus Wilhelmus Maria Thijssen, Roy Christiaan Montijn
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Patent number: 7902401Abstract: Compounds of Formula I are useful in the treatment of epilepsy, neuropathic pain, acute and chronic inflammatory pain, migraine, tardive dyskinesia and other related CNS disorders. wherein: A and R1 to R8 are defined in the specification.Type: GrantFiled: December 14, 2006Date of Patent: March 8, 2011Assignee: NPS Pharmaceuticals, Inc.Inventors: Guy A. Higgins, Methvin Issac, Abdelmalik Slassi, Tao Xin
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Publication number: 20110039874Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.Type: ApplicationFiled: April 16, 2010Publication date: February 17, 2011Applicant: Northeastern UniversityInventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
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Publication number: 20110021571Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.Type: ApplicationFiled: September 16, 2010Publication date: January 27, 2011Applicant: XenoPort, Inc.Inventors: Mark A. Gallop, Fenmei Yao, Maria J. Ludwikow, Thu Phan, Ge Peng
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Publication number: 20100298538Abstract: The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D-mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.Type: ApplicationFiled: November 19, 2008Publication date: November 25, 2010Applicant: BCN PÉPTIDES, S.A.Inventors: Llorenç Rafecas Jane, Antonio Riera Escale, Rosario Ramon Albalate, Monica Alonso Xalma
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Publication number: 20100280108Abstract: A compound of general formula (I) wherein, R11, R12, R13, R14, R15, W, Y, R1, R2, R3, R4, R5, and R6 take various meanings for use in the treatment of cancer.Type: ApplicationFiled: December 19, 2008Publication date: November 4, 2010Applicant: Pharma Mar, S.A.Inventors: Alberto Rodriguez Vicente, Maria Garranzo García-Ibarrola, Carmen Murcia Pérez, Francisco Sánchez Sancho, Maria del Carmen Cuevas Marchante, Cristina Mateo Urbano, Isabel Digón Juárez
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Publication number: 20100105942Abstract: The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: where: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:Type: ApplicationFiled: October 4, 2007Publication date: April 29, 2010Inventors: Giorgio Bertolini, Barbara Verzola, Domenico Vergani
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Publication number: 20100099898Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.Type: ApplicationFiled: December 23, 2009Publication date: April 22, 2010Inventor: Michael R. Reeder
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Publication number: 20090306016Abstract: Disclosed are compounds of formula R—X—Y that may be used to inhibit the action of fatty acid amide hydrolase (FAAH). Inhibition of fatty acid amide hydrolase (FAAH) will slow the normal degradation and inactivation of endogenous cannabinoid ligands by FAAH hydrolysis and allow higher levels of those endogenous cannabinergic ligands to remain present. These higher levels of endocannabinoid ligands provide increased stimulation of the cannabinoid CB1i and CB2 receptors and produce physiological effects related to the activation of the cannabinoid receptors. They will also enhance the effects of other exogenous cannabinergic ligands and allow them to produce their effects at lower concentrations as compared to systems in which fatty acid amide hydrolase (FAAH) action is hot inhibited. Thus, a compound that inhibits the inactivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAAH) may increase the levels of endocannabinoids and, thus, enhance the activation of cannabinoid receptors.Type: ApplicationFiled: July 27, 2007Publication date: December 10, 2009Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
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Publication number: 20090275771Abstract: Urethanes are prepared by oxidative carbonylation of at least one amino compound in the presence of carbon monoxide, oxygen and organic, at least one hydroxyl-group-carrying compound. The carbonylation is carried out in the absence of halogen-containing promoters. The carbonylation is also carried out in the presence of a metal complex catalyst which contains neutral bidentate N-chelate ligands of the (N˜N) type, two monoanionic N,O-chelate ligands of the general type (N˜O)? or tetradentate dianionic chelate ligands (O˜N˜N˜O)2?.Type: ApplicationFiled: January 28, 2009Publication date: November 5, 2009Inventors: Andreas Jacob, Stefan Wershofen, Stephan Klein, Jorg Sundermeyer, Fuming Mei
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Patent number: 6972292Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: August 5, 2002Date of Patent: December 6, 2005Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Patent number: 6486342Abstract: A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.Type: GrantFiled: August 23, 2000Date of Patent: November 26, 2002Assignee: Virginia Commonwealth UniversityInventors: Donald J. Abraham, Gajanan S. Joshi, Stephen J. Hoffman, Melissa Grella, Richmond Danso-Danquah, Amal Yousseff, Martin Safo, Sanjeev Kulkarni
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Patent number: 6414158Abstract: The invention relates to novel carbazate intermediates of formula (II), and to a process for their preparation, and their usefulness in the preparation of (1,3,4) oxadiazine derivatives useful as pesticides, in particular as anthelminthicides, insecticides, acaricides, and nematicides.Type: GrantFiled: July 6, 2000Date of Patent: July 2, 2002Assignee: Bayer AKtiengesellschaftInventors: Hubert Dyker, Andrew Plant, Jürgen Scherkenbeck, Christoph Erdelen, Achim Harder
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Patent number: 6172108Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description, and medicinal products containing the same which are useful as Neuropeptide Y receptorType: GrantFiled: December 16, 1999Date of Patent: January 9, 2001Assignee: Adir et CompagnieInventors: Antonio Monge Vega, Ignacio Aldana Moraza, Daniel-Henri Caignard, Jacques Duhault, Jean Boutin, Odile Dellazuana
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 5985919Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.Type: GrantFiled: October 30, 1997Date of Patent: November 16, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
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Patent number: 5977170Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sub.4 and R.sub.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thenyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.Type: GrantFiled: June 11, 1998Date of Patent: November 2, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Susan Christman
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Patent number: 5968975Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.Type: GrantFiled: June 11, 1998Date of Patent: October 19, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Susan Christman
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Patent number: 5955501Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.Type: GrantFiled: June 7, 1995Date of Patent: September 21, 1999Assignee: Procyon Pharmaceuticals, Inc.Inventors: Paul E. Driedger, James Quick
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Patent number: 5917037Abstract: The present invention relates to a process for the preparation of N-carboxyalkyl-3-fluoro-4-dialkylaminoanilines, which comprises reacting, in a first step, an orthonitrochlorobenzene of the formula (1) ##STR1## in which X is Cl or F, with a secondary amine of the formula (2) HNR.sup.1 R.sup.2, in which R.sub.1 and R.sup.2, independently of one another, are identical or different and are an alkyl radical having from 1 to 10 carbon atoms or, together with the N atom to which they are bonded, form a ring having from 3 to 7 members, in the presence of a base in the presence or absence of a solvent at from -10 to 120.degree. C., reacting, in a second step, the 2-chloro-4-dialkylamino-5-fluoronitrobenzene with hydrogen at from 30 to 150.degree. C.Type: GrantFiled: March 5, 1998Date of Patent: June 29, 1999Assignee: Clariant GmbHInventors: Thomas Schach, Theodor Papenfuhs
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Patent number: 5856354Abstract: The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.Type: GrantFiled: October 17, 1997Date of Patent: January 5, 1999Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
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Patent number: 5854283Abstract: The optically pure forms of monoocarbamates of halogenated 2-phenyl-1,2-ethanediol and dicarbamates of 2-phenly-1,2-ethaniediol have been found to be effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.Type: GrantFiled: January 9, 1997Date of Patent: December 29, 1998Assignee: Yukong LimitedInventors: Yong Moon Choi, Min Woo Kim, Jeonghan Park
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Patent number: 5837873Abstract: A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.Type: GrantFiled: March 24, 1995Date of Patent: November 17, 1998Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Lynn M. Codacovi, Steven J. Wittenberger
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Patent number: 5831114Abstract: Substituted N-phenyl- and N-heteroarylalkylcarbamates of formula (I), in which Q is a group (1), (2) or (3); R is halogen, trifluoromethyl, cyano, nitro or C.sub.1 -C.sub.3 haloalkoxy; Z is hydrogen or halogen; or Z and R together in the 2- and 3-position of the phenyl ring form a group --OCF.sub.2 O--; R.sub.1 is C.sub.1 -C.sub.5 alkyl; R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, methyl or ethyl; X is oxygen, sulfur, --SO-- or --SO.sub.2 --, Y is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or cyano; n is 0, 1 or 2; n.sub.1 is 0 or 1; and m is 0 or 1, with the proviso that m is 1 if Q is group (1) or (2); and the diastereomers and enantiomers thereof, exhibit pre- and post-emergence herbicidal properties. The preparation of these compounds and their use as herbicidally active ingredients are described.Type: GrantFiled: May 28, 1997Date of Patent: November 3, 1998Assignee: Novartis Finance CorporationInventors: Hermann Rempfler, Fredrik Cederbaum, Felix Spindler, Willy Urs Lottenbach
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Patent number: 5817863Abstract: The present invention relates to a novel process for preparing triazolinones of the general formula (I) ##STR1## in which R.sup.1 represents halogenoalkyl, andR.sup.2 represents hydrogen, hydroxyl or amino, or represents alkyl, alkenyl, alkinyl, alkoxy, alkylamino, dialkylamino, cycloalkyl, cycloalkylalkyl, phenyl or phenylalkyl which are in each case optionally substituted,and also to novel intermediates for preparing these triazolinones and to processes for preparing the intermediates themselves.Type: GrantFiled: July 23, 1997Date of Patent: October 6, 1998Assignee: Bayer AktiengesellschaftInventor: Heinz-Jurgen Wroblowsky
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Patent number: 5801271Abstract: Disclosed is a 7-(N-substituted amino)-3-oxo-2-phenylheptanoate derivative, 7-(N-substituted amino)-3-hydroxy-2-phenylheptanoate derivative, and 7-(N-substituted amino)-3-benzenesulfonyloxy-2-phenylheptanoate derivative, which are quite important major intermediates for an antidepressant. The 7-(N-substituted amino)-3-oxo-2-phenylheptanoate derivative can be manufactured by condensing an enolate of phenylacetates with a 5-(N-substituted amino) pentanoate derivative.Type: GrantFiled: July 16, 1997Date of Patent: September 1, 1998Assignee: Takasago International CorporationInventors: Nobuo Seido, Takenobu Nishikawa, Tsukasa Sotoguchi, Yoshifumi Yuasa, Takashi Miura, Hidenori Kumobayashi
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Patent number: 5733935Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.Type: GrantFiled: June 17, 1996Date of Patent: March 31, 1998Assignee: Nihon Nohyaku Co., Ltd.Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
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Patent number: 5723647Abstract: N-(4-Bromo-2-fluorobenzyl)carbamates and a process for their preparationThe invention relates to N-(4-bromo-2-fluorobenzyl)carbamates of the formula (I), ##STR1## where R is (C.sub.1 -C.sub.12)alkyl, benzyl or phenyl, where the benzyl and phenyl radicals can also be substituted by (C.sub.1 -C.sub.3)alkyl or (C.sub.1 -C.sub.3)alkoxy, and to a process for preparing these compounds.Type: GrantFiled: September 20, 1996Date of Patent: March 3, 1998Assignee: Hoechst AktiengesellschaftInventors: Norbert Beye, Karl-Ernst Mack
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Patent number: 5705521Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in radiation oncology applications. The compounds are capable of acting on hemoglobin in whole blood.Type: GrantFiled: June 7, 1995Date of Patent: January 6, 1998Assignee: The Center for Innovative TechnologyInventor: Donald J. Abraham
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Patent number: 5698731Abstract: A process is described for the preparation of aromatic carbamates in which an organic carbonate in a stoichiometric quantity or in a quantity higher than the stoichiometric value is reacted with an aromatic amine operating in the presence of a carbamation catalyst, wherein this catalyst is selected from N,N-substituted carbamate complexes of zinc or copper.The process gives high yields and selectivity in the useful reaction product.Type: GrantFiled: June 27, 1996Date of Patent: December 16, 1997Assignee: Ministero dell `Universita` e della Ricerca Scientifica e TecnologicaInventors: Aldo Bosetti, Pietro Cesti, Fausto Calderazzo
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Patent number: 5693617Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain proteasome inhibitors. The structure of the inhibitors are also disclosed.Type: GrantFiled: January 15, 1995Date of Patent: December 2, 1997Assignee: ProScript, Inc.Inventors: Ross L. Stein, Yu-Ting Ma, Stephen Brand
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Patent number: 5688817Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: November 18, 1997Assignee: Centre Int'l. De Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, William Robert Pilgrim
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Patent number: 5686621Abstract: Substituted hydrindanes and their use in controlling angiogenesis-dependent diseases in warm blooded animals are disclosed.Type: GrantFiled: June 6, 1995Date of Patent: November 11, 1997Assignee: Alcon Laboratories, Inc.Inventors: Abbot F. Clark, Raymond E. Conrow
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Method for lowering oxygen affinity of hemoglobin in redcell suspensions, in whole blood and in vivo
Patent number: 5661182Abstract: Drug compounds are used as allosteric modifiers of hemoglobin present in red blood cells. The compounds bind to only a single pair of symmetry related sites in the central water cavity of hemoglobin at the Lys 99.alpha., Arg 141.alpha., and Asn 108 .beta. residues. When one of the drug compounds is bound to hemoglobin, it will join three separate sub-units of the hemoglobin molecule and stabilize the hemoglobin in a lower oxygen affinity state. Because the compounds used in this method are either not bound by serum albumin or only interact to small degrees with serum albumin, the compounds are active in whole blood and in vivo. The process of allosterically modifying hemoglobin towards a low oxygen affinity state in whole blood and in vivo could be used in a wide variety of applications including in treatments for ischemia, heart disease, wound healing, Alzheimer's, depression, schizophrenia, adult respiratory distress syndrome (ARDS), etc.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Virginia Commonwealth UniversityInventors: Donald J. Abraham, Claude Poyart -
Patent number: 5648375Abstract: Allosteric hemoglobin modifier compound activity on p50 is potentiated by using the compound in combination with a hydrophobic compound such as an anesthetic.Type: GrantFiled: June 7, 1995Date of Patent: July 15, 1997Assignee: Virginia Commonwealth UniversityInventor: Donald J. Abraham
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Patent number: 5616711Abstract: A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-1) or an aminobutene derivative of formula (I-2): ##STR1## The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H.sub.2 receptor.Type: GrantFiled: August 6, 1993Date of Patent: April 1, 1997Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Hajime Matsumoto, Masakatsu Matsumoto, Yasuo Sekine, Masato Nishimura, Akihiko Hosoda
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Patent number: 5585512Abstract: There is disclosed an ester compound that is resistant to decomposition in blood, but is quickly hydrolyzed in cancer cells, and functions as an anticancer agent. The ester compound has a structure represented by formula (I) or formula (II): ##STR1## wherein R.sub.1 represents a methyl group, a methoxy group, or a trifluoroacetamido group; R.sub.2 represents a phenyl group or a phenylmethyl group; and the absolute configuration of the asymmetric center marked with an asterisk is R.Type: GrantFiled: February 27, 1995Date of Patent: December 17, 1996Assignee: Director-General of Agency of Industrial Science and TechnologyInventors: Yoshimitsu Yamazaki, Yoshikatsu Ogawa, Hiroaki Okuno