Ortho Fused Patents (Class 560/119)
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Publication number: 20040082806Abstract: A process for producing a 2-oxobicyclo[3.1.Type: ApplicationFiled: September 11, 2003Publication date: April 29, 2004Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami
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Publication number: 20040077882Abstract: Bicyclic cyclopropane derivatives of the general Formula (I) 1Type: ApplicationFiled: September 9, 2003Publication date: April 22, 2004Inventors: Norbert Moszner, Armin de Meijere, Frank Zeuner, Urs Karl Fischer
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Patent number: 6689590Abstract: A composition comprising pravastatin sodium substantially free of pravastatin lactone is described.Type: GrantFiled: July 23, 2002Date of Patent: February 10, 2004Assignee: Biogal Gyogyszergyar Rt.Inventors: Vilmos Keri, Lajos Deak, Iiona Forgacs, Csaba Szabo, Edit Arvai Nagyne
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Publication number: 20030187287Abstract: The invention relates to a new synthesis intermediate product of formula I 1Type: ApplicationFiled: May 27, 2003Publication date: October 2, 2003Inventors: Andreas Steinmeyer, Werner Boidol, Ludwig Zorn
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Patent number: 6541515Abstract: Compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The culture Cytospora sp. MF 6608 (ATCC PTA-1691) is also disclosed, as well as processes for making a compound of the present invention employing the culture.Type: GrantFiled: August 9, 2001Date of Patent: April 1, 2003Assignee: Merck & Co., Inc.Inventors: Sheo Bux Singh, Hiranthi Jayasuriya, Ziqiang Guan, Keith C. Silverman, Russell B. Lingham, Anne W. Dombrowski, Daria J. Hazuda, Jon D. Polishook
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Patent number: 6506929Abstract: A process is disclosed for the preparation of simvastatin which enables highly regio selective C-methylation of the 2′-position group of lovastatin without requiring protection/deprotection of 13-OH of lovastatin and lactone ring opening/closure.Type: GrantFiled: April 24, 2001Date of Patent: January 14, 2003Assignee: Apotex Inc.Inventors: Khashayar Karimian, Tim Fat Tam, Yong Tao, Yiwei Li, Gary Doucette
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Patent number: 6444452Abstract: A novel process for recovering a compound from a fermentation broth that includes the stages of forming an enriched solution of the compound by extraction, obtaining a salt of the compound from the enriched solution, purifying a salt of the compound and trans-salifying the salt of the compound to a metal salt of the compound is disclosed.Type: GrantFiled: November 28, 2000Date of Patent: September 3, 2002Assignee: Biogal Gyogyszergyar Rt.Inventors: Vilmos Keri, Lajos Deak, Ilona Forgacs, Csaba Szabo, Edit Arvai Nagyne
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Patent number: 6392086Abstract: The present inventions relate to a (1S,5R,6S)- or (1SR, 5RS, 6SR)-3-fluoro-2-oxobicyclo[3.1.0]hex-3-ene-6-carboxylic acid derivative represented by Formula (1): [in the formula, R represents OR1 or NR1R2, wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a (C3-C6 cycloalkyl) (C1-C6 alkyl) group, an aryl group, an aryl (C1-C6 alkyl) group, a (C1-C6 alkoxy) (C1-C6 alkyl) group, a C1-C6 hydroxyalkyl group, a (C1-C6 alkylthio) (C1-C6 alkyl) group, or a C1-C6 mercaptoalkyl group], and a process for producing the same, and a process for efficiently producing a fluorine-containing amino acid compound acting on group 2 metabotropic glutamate receptors, which has treatment effects or prevention effects on psychiatric diseases or neurological diseases, characterized by hydrogenating the derivative, and subsequently, subjecting it to hydantoination or aminocyanidation, followed by hydrolysis.Type: GrantFiled: June 7, 2001Date of Patent: May 21, 2002Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa, Hisanako Ito, Takeo Taguchi
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Patent number: 6376700Abstract: An alicyclic compound of the formula (1) is disclosed: wherein R1 and R2 each independently is a hydroxyl group, a C1-8 hydroxyalkyl group, or a C3-8 hydroxycycloalkyl group; R3, R4 and R5 each independently is a hydrogen, a C1-8 hydroxyalkyl group, a C1-6 carboxylic acid or a C3-8 carboxylic acid ester; k is an integer of 0, 1, 2, 3, 4, 5 or 6. The compound of the formula (1) can be applied to dissolution inhibitors for preparing positive photoresist composition.Type: GrantFiled: June 30, 2000Date of Patent: April 23, 2002Assignee: Everlight USA, Inc.Inventors: Shang-Wern Chang, Yen-Cheng Li, Shang-Ho Lin, Wen-Chieh Wang
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Publication number: 20020045658Abstract: Compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The culture Cytospora sp. MF 6608 (ATCC PTA-1691) is also disclosed, as well as processes for making a compound of the present invention employing the culture.Type: ApplicationFiled: August 9, 2001Publication date: April 18, 2002Inventors: Sheo Bux Singh, Hiranthi Jayasuriya, Ziqiang Guan, Keith C. Silverman, Russell B. Lingham, Anne W. Dombrowski, Daria J. Hazuda, Jon D. Polishook
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Patent number: 6369194Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.Type: GrantFiled: November 9, 1998Date of Patent: April 9, 2002Assignee: Yale UniversityInventor: Harry H. Wasserman
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Patent number: 6365382Abstract: The very effective conversion of ML-236B substances and derivatives thereof into 6′-hydroxylated products with the microorganisms of species Amycolatopsis orientalis, or with an extract or a hydroxylation-effective enzyme derived from said microorganism, is described. The products obtained are suitable as HMG-CoA reductase inhibitors or intermediates thereof. Thus, the products can be used, for example, as an antihypercholesterolemic in pharmacy.Type: GrantFiled: December 27, 2000Date of Patent: April 2, 2002Assignee: LEK Pharmaceuticals and Chemical Company D.D.Inventors: Sa{haeck over (s)}o Kranjc, Irena Ivanc, Manica Schauer
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Patent number: 6333428Abstract: The present invention provides fluorobicyclo[3.1.0]hexane derivatives represented by the formula [wherein R1 and R2 are the same or different and each represents a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a C3-8 cycloalkyl-C1-5 alkyl group: Y1 and Y2 are the same or different and each represents a hydrogen atom, a C1-10 alkylthio group, a C3-8 cycloalkylthio group, a C3-8 cycloalkyl-C1-5 alkylthio group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or one represents a hydrogen atom and the other represents a hydroxyl group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or Y1 and Y2 together represent an oxygen atom or —X(CH2)nX— (X represents an oxygen atom or a sulfur atom: N is 2 or 3)], pharmaceutically acceptable salts thereof, or hydrates thereof.Type: GrantFiled: February 22, 2001Date of Patent: December 25, 2001Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: 6316498Abstract: Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X1 represents hydrogen or fluorine; and R1 and R2 are the same or different and each represents hydrogen or lower C1-10 alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, bipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.Type: GrantFiled: July 27, 2000Date of Patent: November 13, 2001Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Patent number: 6306629Abstract: The present invention is related to a new microorganism Streptomyces exfoliatus YJ-118 and a method for producing pravastatin sodium by using this microorganism which shows a strong tolerance to ML-236B and a high hydroxylation activity of ML-236B to pravastatin.Type: GrantFiled: December 29, 1999Date of Patent: October 23, 2001Assignee: Yungjin Pharmaceutical Ind. Co., Ltd.Inventors: Joo-Kyung Lee, Joo-Woong Park, Dong-Jin Seo, Sang-Choon Lee, Ji-Yoon Kim
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Patent number: 6217793Abstract: Provided are novel acetylene compounds which are useful as a component for a liquid crystal composition used for a liquid crystal element, a liquid crystal composition containing said compounds and a liquid crystal element using said liquid crystal composition. The acetylene compound is represented by Formula (1): n-CmH2m+1—C≡C—A—Z1—B—Y1—R1 (1) wherein m represents an integer of 2 to 24; R1 represents a linear or branched alkyl group, a linear or branched alkoxyalkyl group, a linear or branched alkenyl group, or a linear or branched alkenyloxyalkyl group each of which may be substituted with a halogen atom; R1 may have an asymmetric carbon atom, and the asymmetric carbon atom may be optically active; A and B represents a cyclic group such as a phenylene group, a biphenylene group, a naphthylene group and the like each of which may be substituted with a halogen atom.Type: GrantFiled: May 17, 1999Date of Patent: April 17, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Yoshiyuki Totani, Hiroe Kayashima, Tsutomu Ishida, Masakatsu Nakatsuka
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Patent number: 6204292Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.Type: GrantFiled: July 17, 1998Date of Patent: March 20, 2001Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
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Patent number: 6177586Abstract: The starting materials for a production process of a vitamin D3 derivative are disclosed, e.g., a cyclopentene derivative represented by the formula (1-2): wherein R11 is a hydrogen atom, tri(C1 to C7 hydrocarbon) silyl group, C2 to C7 acyl group, group forming an acetal bond together with an oxygen atom of a hydroxyl group, and X1 is a bromine or iodine atom; and a heptanoic acid derivative represented by the formula (2-4): wherein X2 is a bromine atom or iodine atom.Type: GrantFiled: June 8, 1999Date of Patent: January 23, 2001Assignee: Teijin LimitedInventors: Masayasu Tabe, Atsuo Hazato, Kenji Manabe, Qinqzhi Gao, Hiroko Tanaka
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Patent number: 6160009Abstract: Compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.Type: GrantFiled: May 28, 1999Date of Patent: December 12, 2000Assignee: Eli Lilly and CompanyInventors: Steven Marc Massey, James Allen Monn, Matthew John Valli
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Patent number: 6143783Abstract: The present invention relates to compounds of the formula ##STR1## in which R.sup.1 is defined in the specification, and non-toxic metabolically labile esters and amides thereof are useful as modulators of metabotropic glutamate receptor function.Type: GrantFiled: November 11, 1999Date of Patent: November 7, 2000Assignee: Eli Lilly and CompanyInventors: James Allen Monn, Matthew John Valli
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Patent number: 6118019Abstract: A 3-alkoxypropionic ester derivative, an olefin polymerization solid catalyst component using the same, an olefin polymerization catalyst using the same, and a process for the preparation of a polyolefin using the same. The 3-alkoxypropionic ester derivative is represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrocarbon group having from 1 to 10 carbon atoms; R.sup.2 represents a hydrocarbon group having from 1 to 20 carbon atoms; R.sup.3 represents a hydrocarbon group having from 1 to 20 carbon atoms; and R.sup.4 represents a branched hydrocarbon group having 3 or more carbon atoms.Type: GrantFiled: December 29, 1998Date of Patent: September 12, 2000Assignee: Showa Denko K.K.Inventors: Masaki Fushimi, Shintaro Inazawa
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Patent number: 5958960Abstract: Compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.Type: GrantFiled: May 13, 1998Date of Patent: September 28, 1999Assignee: Eli Lilly and CompanyInventors: Steven Marc Massey, James Allen Monn, Matthew John Valli
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Patent number: 5925782Abstract: The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.Type: GrantFiled: May 5, 1997Date of Patent: July 20, 1999Assignee: Eli Lilly and CompanyInventor: James A. Monn
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Patent number: 5916920Abstract: Compounds of the formula ##STR1## in which X represents a bond, S, O or NR.sup.a ; and R is as defined in the specification are useful as modulators of metabotropic glutamate receptor function.Type: GrantFiled: November 14, 1996Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Carmen Dominguez Fernandez, David Reed Helton, Steven Marc Massey, James Allen Monn
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Patent number: 5834404Abstract: The present invention is directed to substituted bicycloheptanedion e derivatives represented by a general formula ?I!; ##STR1## wherein R represents C.sub.1 -C.sub.4 alkyl, R.sup.1 represents hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aralkyl, C.sub.2 -C.sub.4 haloalkynyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.4 haloalkenyl, etc. and R.sup.2 represents optionally substituted phenyl or optionally substituted pyridyl, the salts thereof and herbicides comprising the same as the active ingredient.Type: GrantFiled: July 15, 1997Date of Patent: November 10, 1998Assignee: Nippon Soda Co., ltd.Inventors: Takahiro Sagae, Masao Yamaguchi, Hiroyuki Adachi, Kazuyuki Tomida, Akihiro Takahashi, Takashi Kawana
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Patent number: 5827855Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 represents a group of formula (II) or (III): ##STR2## R.sup.2 is alkyl, alkenyl or alkynyl; R.sup.3 and R.sup.4 are each hydrogen, alkyl, alkenyl or alkynyl; R.sup.5 is hydrogen or a carboxy-protecting group; R.sup.a is a group of formula --OR.sup.6 ; R.sup.6 is hydrogen; R.sup.6a and R.sup.6b are each hydrogen, a hydroxy-protecting group, alkyl, alkanesulfonyl, halogenated alkanesulfonyl or arysulfonyl, and their salts and esters. Such compounds inhibit the synthesis of cholesterol, and can be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.Type: GrantFiled: December 28, 1995Date of Patent: October 27, 1998Assignee: Sankyo Company, LimitedInventors: Hiroshi Kogen, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Nobufusa Serizawa, Kiyoshi Hamano
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Patent number: 5750566Abstract: The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.Type: GrantFiled: June 29, 1995Date of Patent: May 12, 1998Assignee: Eli Lilly and CompanyInventors: James A. Monn, Darryle D. Schoepp
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Patent number: 5741925Abstract: Vinyl naphthenate monomer mixtures are prepared by transvinylation of naphthenic acid in the presence of a catalyst of a palladium carboxylate complexed with one or more aryl N-containing ligands and distilling the resulting vinyl naphthenate monomers in the presence of the catalyst at pot temperatures exceeding 80.degree. C. The catalyst is stable and can be re-used over several transvinylation reaction runs.Type: GrantFiled: January 13, 1997Date of Patent: April 21, 1998Assignee: Air Products and Chemicals, Inc.Inventors: Chung-Ling Mao, Francis Joseph Waller, Kenneth Merle Kem
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Patent number: 5700833Abstract: The present invention provides novel isocarbacyclin derivatives useful for search and study of prostacyclin receptor and as a therapeutic drug for central nervous system diseases, which derivatives are expressed by the following formula ?I!: ##STR1## ?where, R.sup.1 represents a hydrogen atom, an alkyl group, or cation of an appropriate amount, and R.sup.2 an alkylene group.Type: GrantFiled: January 31, 1996Date of Patent: December 23, 1997Assignees: Research Developement Corporation of Japan, Atsuo HazatoInventors: Yasuyoshi Watanabe, Masaaki Suzuki, Atsuo Hazato, Bengt Langstrom
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Patent number: 5532408Abstract: Provided are .alpha.-chain-modified isocarbacyclins of which the .alpha.-chain is modified with a phenylene group, a cycloalkylene group or a thiophendiyl group, and these .alpha.-chain-modified isocarbacyclins show the activity for inhibiting the DNA synthesis of human smooth muscle cell and are expected to be capable of inhibiting the hypertrophy of a blood vessel.Type: GrantFiled: April 5, 1995Date of Patent: July 2, 1996Assignee: Teijin LimitedInventors: Masahiro Koga, Toshio Tanaka, Takao Fujii, Tsukio Masegi
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Patent number: 5489613Abstract: Compounds of formula (I): ##STR1## have valuable platelet-aggregation inhibitory activities and may be used for the prophylaxis and treatment of such diseases as thrombosis.Type: GrantFiled: January 21, 1992Date of Patent: February 6, 1996Assignee: Sankyo Company, LimitedInventors: Kazuo Koyama, Shigeo Amemiya, Koichi Kojima, Shinsaku Kobayashi
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Patent number: 5468905Abstract: Compounds represented by general formulas (I) and (II), useful as the intermediates for agricultural chemicals, particularly herbicidal compounds, wherein R.sup.1 and R.sup.2 represent each hydrogen, alkyl or COOR.sup.3 :R.sup.3 represents alkyl: and R.sup.4 represents alkyl.Type: GrantFiled: May 25, 1994Date of Patent: November 21, 1995Assignee: Nippon Soda Co., Ltd.Inventors: Junji Suzuki, Masami Hatano, Shinichi Imaizumi
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Patent number: 5449684Abstract: Compounds isolated from a marine sponge, and derivatives thereof, have the formulae: ##STR1## in which R.sup.1 is H or lower alkyl; R.sup.2 is OH or CH.sub.3 ; R.sup.3 is OH or CH.sup.3, and R.sup.4 H or MPTA. The compounds have antitumor and antiviral activity. The invention also provides pharmaceutical compositions containing the compounds and methods of treatment employing them.Type: GrantFiled: February 3, 1994Date of Patent: September 12, 1995Assignee: PharmaMar, S.A.Inventors: Jun-Ichi Tanaka, Tatsuo Higa, Khanit Suwanoborirux, C. W. Jefford, G. Bernardinelli, Dolores G. Gravalos
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Patent number: 5405870Abstract: Compounds of formula (Ic): ##STR1## having valuable platelet-aggregation inhibitory activities useful for the prophylaxis and treatment of such diseases as thrombosis and pharmaceutical compositions containing said compounds.Type: GrantFiled: November 4, 1993Date of Patent: April 11, 1995Assignee: Sankyo Company, LimitedInventors: Kazuo Koyama, Shigeo Amemiya, Koichi Kojima, Shinsaku Kobayashi
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Patent number: 5374654Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 is a hydrogen atom, their salts with physiologically compatible bases, their cyclodextrin clathrates, and their use as medicinal agents.Type: GrantFiled: April 21, 1993Date of Patent: December 20, 1994Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Ulrich Klar, Bob Nieuweboer, Claus-Steffen Sturzebecher
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Patent number: 5369123Abstract: Novel nitrogen-substituted mevinic acid derivatives which inhibit the activity of HMG-CoA reductase. Pharmaceutical compositions, and methods of use for the treatment or prevention of hypercholesterolemia, atherosclerosis, hyperlipoproteinaemia and hyperlipidemia are provided, as are novel methods for preparation and intermediate compounds.Type: GrantFiled: October 9, 1992Date of Patent: November 29, 1994Assignee: E. R. Squibb & Sons, Inc.Inventors: Dinos P. Santafianos, Kathleen M. Poss, Eric M. Gordon, Peggy J. McCann
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Patent number: 5356561Abstract: In accordance with the present invention, there are provided carboxylate compounds represented by the following formula [A] and liquid crystal material comprising said compounds ##STR1## wherein R is a group selected from the group consisting of alkyl, alkoxy and halogenated alkyl group of 3-20 carbon atoms, X and Y represent each a group selected from the group consisting of --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --S--S--, ##STR2## or a single bond, A and B represent each a group selected from the group consisting of specific divalent aromatic and alicyclic group such as phenylene, cyclohexylene and tetrahydronaphthalene and R* is an optically active group of 4-20 carbon atoms containing at least one asymmetric carbon atom (hydrogen atoms attached to the carbon atoms of said optically active group may be substituted with halogen atoms), and m and n are each an integer of 0-2, with the proviso that both m and n do not become 0 at the same time.Type: GrantFiled: December 24, 1991Date of Patent: October 18, 1994Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Toyoji Shimizu, Shinichi Nishiyama, Nobuyuki Doi, Shoichi Miyakoshi, Tooru Yamanaka, Katsuo Taniguchi, Hideo Hama
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5292928Abstract: In a process for reacting a low molecular weight hydroxy compound with a carboxylic acid halide, a small amount of the acid halide is introduced into the reaction vessel and the remainder of the acid halide and the hydroxy compound are added gradually in an approximately stoichiometric ratio. The hydrogen halide formed is thus prevented from dissolving in the reaction medium. The heat of reaction to be dissipated is negligible.Type: GrantFiled: July 31, 1992Date of Patent: March 8, 1994Assignee: Hoechst AktiengesellschaftInventor: Karlheinz Miltenberger
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Patent number: 5288742Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different, is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: March 18, 1992Date of Patent: February 22, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, David Waterson
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Patent number: 5286746Abstract: Antihypercholesterolemic activity is exhibited by compounds of the formula ##STR1## wherein: X is hydrogen, alkali metal or ammonium;Y is hydrogen, alkyl, cycloalkyl, aryl, or aralkyl; ##STR2## R is hydrogen, alkyl, ammonium, alkylammonium, or alkali metal (such as Na, Li, or K); andn is 1 or 2.Type: GrantFiled: December 20, 1991Date of Patent: February 15, 1994Assignee: E. R. Squibb & Sons, Inc.Inventor: Kathleen M. Poss
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Patent number: 5272174Abstract: Derivatives of ML-236B carboxylic acid, its salts and esters and corresponding lactone have a hydroxy group at the 3"-position and optionally also at the 6'-position. These derivatives may be prepared by the enzymatic hydroxylation of a corresponding ML-236B compound employing an enzyme produced by a microorganism of the genus Streptomyces or Amycolata, especially Streptomyces sp. SANK 62285, Streptomyces sp. SANK 62385, Streptomyces sp. SANK 62485, Streptomyces sp. SANK 62585, Amycolata autotrophica SANK 62781. Amycolata autotrophica subsp. canberrica SANK 62882 or Amycolata autotrophica subsp. amethystina SANK 62981. These derivatives have the ability to inhibit cholesterol biosynthesis.Type: GrantFiled: July 23, 1992Date of Patent: December 21, 1993Assignee: Sankyo Company, LimitedInventors: Kouhei Furuya, Takao Okazaki, Yoshio Tsujita, Seigo Iwado, Kiyoshi Hamano, Masao Kuroda, Jun Yoshikawa, Toshiaki Iwai, Kunio Nakano
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Patent number: 5256811Abstract: compounds of formula I ##STR1## wherein R.sup.1 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.3-8 cycloalkyl(C.sub.1-8)alkyl, C.sub.1-8 hydroxyalkyl, C.sub.1-8 alkylthio, phenyl or substituted phenyl;R.sup.3 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, CO2(C.sub.1-8)alkyl, CO.sub.2 (C.sub.2-8) alkenyl, C.sub.1-8 alkylthio, (C.sub.1-2)alkyl CO.sub.2 (C.sub.1-8) alkyl or C.sub.1-8 aldehydroalkyl where the aldehyde function is protected by a suitable protecting group (for example, an acetal such as a dimethyl acetal);R.sup.4 represents a hydrogen atom, C.sub.1-8 alkyl or C.sub.2-8 alkenyl;Z represents a group (CH.sub.2).sub.n or a branched alkyl chain;n is 1 to 8;and each of a, b and c is independently a single or a double bond;can be prepared relatively easily and in good xxx at room temperature by reacting a compound of general formula II ##STR2## wherein R.sup.2, R.sup.3, R.sup.Type: GrantFiled: December 6, 1991Date of Patent: October 26, 1993Assignee: British Bio-Technology LimitedInventors: Richard S. Todd, Maxwell Reeve
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Patent number: 5247123Abstract: The invention is directed to deuterated vitamin D analogs, and processes and intermediates for their preparation. The end products, that is the deuterated vitamin D analogs, are useful for the treatment osteoporosis and cutaneous inflammations such as psoriasis, and contact dermatitis.Type: GrantFiled: July 2, 1992Date of Patent: September 21, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Bernard M. Hennessy, Milan R. Uskokovic
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Patent number: 5241104Abstract: Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.Type: GrantFiled: June 23, 1992Date of Patent: August 31, 1993Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Takaharu Matsuura
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Patent number: 5228898Abstract: This invention relates to substituted bicycloheptadione derivatives with high herbicidal activity which are represented by general formula (I) ##STR1## (where R.sup.1 is a lower alkyl group, a phenyl group which may be substituted, an aralkyl group which may be substituted, or a heterocyclic group which may be substituted;R.sup.2 is, same or different, a halogen, an alkoxy group, an alkylthio group, an alkylsulfonyl group, an alkyl group, an alkoxyalkyl group, or an alkoxylcarbonyl group, and n is 0 to 4;R.sup.3 and R.sup.4 are, same or different, hydrogen or a lower alkyl group).Type: GrantFiled: February 3, 1992Date of Patent: July 20, 1993Assignee: Nippon Soda Co., Ltd.Inventors: Akiyoshi Ueda, Shigemi Suga, Hiroyuki Adachi, Toshio Aihara, Kazuyuki Tomida, Hideki Yamagishi, Hideo Hosaka
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Patent number: 5210228Abstract: Compounds of either of general formulae I and II: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6, a, b, c, and d are variables.These compounds are useful in the treatment of hypercholesterolaemia in general and arteriosclerosis, familial hypercholesterolaemia or hyperlipidaemia in particular.Type: GrantFiled: September 16, 1991Date of Patent: May 11, 1993Assignee: British Bio-Technology LimitedInventors: Richard S. Todd, Christopher N. Lewis, Alan H. Davidson, Alan H. Drummond
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Patent number: 5206416Abstract: An isocarbacyclin derivative represented by the following formula: ##STR1## wherein R.sup.1 represents H or a linear or branched C.sub.1 -C.sub.10 alkyl group, R.sup.2 represents H, a methyl group or a vinyl group, and R.sup.3 represents an unsubstituted linear or branched C.sub.3 -C.sub.8 alkyl group or a C.sub.5 -C.sub.6 cycloalkyl group. and a pharmaceutaically acceptable salt thereof.Type: GrantFiled: September 24, 1991Date of Patent: April 27, 1993Assignee: Teijin LimitedInventor: Seizi Kurozumi
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Patent number: RE36520Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formula (II): ##STR1##Type: GrantFiled: November 4, 1998Date of Patent: January 18, 2000Assignee: Merck & Co., Inc.Inventors: Robert L. Smith, Wasyl Halczenko, George D. Hartman, Gerald E. Stokker, Edward S. Inamine, Otto D. Hensens, David R. Houck, Ta Jyh Lee