Carbocyclic Ring Having Silicon As Part Of One Substituent And The -coo- As Part Of Another Substituent Patents (Class 556/441)
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Patent number: 5849750Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.Type: GrantFiled: March 5, 1997Date of Patent: December 15, 1998Assignee: California Institute of TechnologyInventor: Andrew Gordon Myers
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Patent number: 5723643Abstract: A method to make high-purity acryloxy- or methacryloxy-functional organosilicon compounds in high yields by inhibiting gelation of the reaction product during preparation. The method comprises (A) reacting an acrylate or methacrylate ester of an alcohol comprising an aliphatically unsaturated bond or a phenol comprising an aliphatically unsaturated bond with a (B) SiH-functional silicon compound in the presence of (C) a hydrosilylation reaction catalyst and (D) a polymerization inhibitor described by formula ##STR1## where n is 0 or 1; M is an atom selected from the group consisting of N, P, As, Sb, O, S, Se, Sn, and I; R is a monovalent hydrocarbon group or hydrogen atom; m is 1, 2, or 3; and X is a conjugate base of an organic acid or inorganic acid.The present method can further comprise distillation of the reaction mixture resulting from the reaction of component (A) and (B) in the presence of component (D).Type: GrantFiled: April 15, 1997Date of Patent: March 3, 1998Assignee: Dow Corning Toray Silicone Co., Ltd.Inventors: Ryuzo Mikami, Tadashi Okawa
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Patent number: 5705659Abstract: Intermediate compounds represented as formula (I) useful for the synthesis of 16-phenoxy-prostatrienoic acid derivatives and a preparing method thereof are disclosed. ##STR1## wherein R is tetrahydropyranyl, tetrahydrofuranyl, 2-ethoxyethyl, t-butyldimethylsilyl, triisopropylsilyl or triethylsilyl group; R.sup.1 and R.sup.2 are independently hydrogen or ester-forming group; P is hydrogen, trimethylsilyl or tri-n-butyltin; and wavy line means epi-stereoisomeric mixture.Type: GrantFiled: June 20, 1996Date of Patent: January 6, 1998Assignee: Korea Institute of Science and TechnologyInventors: Hokoon Park, Sun Ho Jung, Yong Sup Lee, Ki Hong Nam
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Patent number: 5693668Abstract: This invention relates to silylated aromatic fluoroketones possessing acetylcholinesterase-inhibiting properties and to their use in the treatment of Alzheimer disease and senile dementia.Type: GrantFiled: January 31, 1995Date of Patent: December 2, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Daniel Schirlin, Jean-Noel Collard, Jean-Marie Hornsperger, Prakash R. Keshary
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Patent number: 5608104Abstract: Described is a detection method of a pyrethroid compound which comprises providing a first antibody against the pyrethroid compound, said first antibody having been obtained by immunizing a responder with an immunogen which is a first conjugate between a first carrier and a first haptenic compound represented by the following formula (1) or (2): ##STR1## mixing the first antibody with the sample solution, causing any unreacted portion of the first antibody to be bound on a second conjugate as a coated antigen, said second conjugate being formed of a second carrier and a second haptenic compound and having been coated on a surface of a solid phase carrier, whereby an antigen-antibody conjugate is obtained; andreacting the antigen-antibody conjugate with a second antibody against the first antibody, said second antibody having a labelled enzyme linked therewith.Type: GrantFiled: September 27, 1994Date of Patent: March 4, 1997Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Hideo Ohkawa, Koji Kitajima, Kenji Kodaka, Yasunori Fumoto, Takako Kumeta
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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: 5498738Abstract: The present invention a process for the preparation of a compound of the formula (X) useful as precursor for the A-ring in taxanes ##STR1## wherein R' is an ##STR2## in which R" is a linear, branched or cyclic alkyl group of 1 to 10 carbon atoms. The invention further relates to the novel compound (X) and to novel intermediates in said process.Type: GrantFiled: June 28, 1994Date of Patent: March 12, 1996Inventors: Esko Karvinen, Ari Koskinen
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Patent number: 5495037Abstract: A side-chain liquid crystalline polysiloxane having the following formula is disclosed: ##STR1## wherein Me is methyl; m is an integer of 40 to 80; n is an integer of 1 to 12; Ar is phenylene, biphenylene or naphthalene; Ar' is phenylene or naphthalene; X is halogen or methyl; and R is C.sub.1 -C.sub.4 alkyl.Type: GrantFiled: September 9, 1994Date of Patent: February 27, 1996Assignee: National Science CouncilInventors: Chain-Shu Hsu, Yi-Jing Leu, Li-Jen Shih, Ging-Ho Hsiue
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Patent number: 5475125Abstract: The invention discloses novel polyester emulsifiers. Compounds of the invention are made by reacting (a) a dimethicone copolyol, (b) a diacid and (c) a fatty alcohol alkoxylate containing 4 to 20 carbon atoms. The compounds of the invention by virtue of (a) the silicone group, (b) the fatty alcohol terminal group and (c) the polyoxyalkylene present in the compound are extremely efficient emulsifiers for a variety of oils at heretofore unknown levels.Type: GrantFiled: January 23, 1995Date of Patent: December 12, 1995Assignee: Siltech Inc.Inventor: A. J. O'Lenick, Jr.
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Patent number: 5457108Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.Type: GrantFiled: September 17, 1993Date of Patent: October 10, 1995Assignee: Bayer AktiengesellschaftInventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
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Patent number: 5451696Abstract: A compound of the formula ##STR1##Type: GrantFiled: September 30, 1994Date of Patent: September 19, 1995Assignee: Roussel-UCLAFInventors: Marc Benoit, Sylvain Laugraud, Jean-Louis Brayer
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Patent number: 5449815Abstract: Object: To provide novel prostaglandin E.sub.1 analogues which have more excellent pharmaceutical effects, longer duration of the effects and less side-effects than the prior art prostaglandin E.sub.1 's.Constitution: A PGE.sub.1 analogue represented by the formula: ##STR1## (wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an allyl group, and R.sup.2 is an alkyl group having 3 to 6 carbon atoms, an alkenyl group having 3 to 6 carbon atoms), or a salt thereof.Type: GrantFiled: October 19, 1993Date of Patent: September 12, 1995Assignees: Taisho Pharmaceutical Co., Ltd., Fumie SatoInventors: Fumie Sato, Takehiro Amano, Kazuya Kameo, Tohru Tanami, Masaru Mutoh, Naoya Ono, Jun Goto
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Patent number: 5436359Abstract: There are disclosed novel hydroquinone derivatives of the formulas: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments, and the derivatives of the formula (II) are intermediates for the production thereof.Type: GrantFiled: March 12, 1993Date of Patent: July 25, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirotomo Masuya, Masayoshi Yamaoka
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Patent number: 5416211Abstract: Processes for preparing 5-substituted pyrrolo[2,3-d]pyrimidines which are useful as intermediates for the preparation of pyrrolo[2,3-d]pyrimidine antineoplastic agents or as antineoplastic agents themselves are provided.Type: GrantFiled: May 24, 1993Date of Patent: May 16, 1995Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Thomas M. Wilson
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Patent number: 5412134Abstract: The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, diphenylsilane in the presence of tris(triphenylphosphine) rhodium (I) chloride, or iridium tetrachloride to yield the corresponding diprotected cyclobutanol. This compound is useful as an intermediate in the preparation of antiviral agents.Type: GrantFiled: May 26, 1992Date of Patent: May 2, 1995Assignee: E. R. Squibb & Sons, Inc.Inventors: Janak Singh, Gregory S. Bisacchi, Richard H. Mueller
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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: 5403944Abstract: Novel organosiloxane compounds have at least one unit ##EQU1## any other units being present in this organosiloxane are ##EQU2## wherein R is a C.sub.1-8 alkyl or aryl, R.sup.1 is H or a C.sub.1-5 alkyl, R.sup.2 is H, C.sub.1-5 alkyl or OR.sup.1, R.sup.3 is a C.sub.1-5 alkyl, R" is H, a monovalent C.sub.1-8 hydrocarbon or halogenated hydrocarbon group, a is 0, 1 or 2, b 0, 1, 2 or 3 and n 1 to 6, provided the--C(R.sup.1).dbd.CH--(CR.sup.1.sub.2).sub.n --O--group and the two R.sup.2 groups are linked to the aromatic ting at the para- and meta-positions in relation to the group --CH.dbd.C[C(O)OR.sup.3 ].sub.2.The compounds are useful as UV sunscreens. Compositions containing them are also included.Type: GrantFiled: January 7, 1993Date of Patent: April 4, 1995Assignee: Givaudan-Roure CorporationInventors: Georg Frater, Rolf Schwarzenbach, Stephane F. M. Van Oycke
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Patent number: 5380883Abstract: A compound of the formula ##STR1##Type: GrantFiled: April 12, 1993Date of Patent: January 10, 1995Assignee: Roussel-UclafInventors: Marc Benoit, Sylvain Laugraud, Jean-Louis Brayer
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Patent number: 5359101Abstract: Anionically polymerizable monomers containing at least one silicon or titanium atom form polymeric photoresists having good dry etch resistance for use in microlithography. The monomers are of the formula ##STR1## wherein A is --H or --CH.dbd.CH.sub.2 ; X is a strong electron withdrawing group;Y is a strong electron withdrawing group containing at least one silicon or titanium atom.Preferably Y is ##STR2## wherein n is 1-5 and R.sup.2, R.sup.3 and R.sup.4 are C.sub.1 -C.sub.10 alkyl. A particularly preferred monomer is 3-trimethylsilylpropyl 2-cyanoacrylate.Methods for applying a resist coating by vapor deposition of these monomers and exposure to radiation are described. A positive or negative tone image can be produced, depending upon the imaging method employed. The imaging layer may be applied over a planarizing layer to form a multilayer photoresist.Type: GrantFiled: October 1, 1991Date of Patent: October 25, 1994Assignee: Loctite Ireland, Ltd.Inventors: John Woods, Pauline Coakley
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Patent number: 5348684Abstract: The novel silylalkyl or silylalkenyl compounds correspond to the general formula (I) ##STR1## Here the symbols A.sup.1, A.sup.2, A.sup.3 denote aromatic or heteroaromatic molecular units such as 1,4-phenylene or pyrimidine-2,5-diyl which are combined via a single bond (for k, m=0) or via functional groups M.sup.1,M.sup.2 such as CO--O or CH.sub.2 --O; j, k, l, m, n are zero or 1 (j+l+n=2 or 3). The radicals R.sup.2, R.sup.3, R.sup.4, R.sup.5 are hydrogen or alkyl/alkenyl, cycloalkyl, and the radicals R.sup.6, R.sup.7, R.sup.8 have a comparable meaning (hydrogen); R.sup.1 is alkyl/alkenyl or one of the substituents known from LC chemistry such as an .alpha.-haloalkanoic radical. In some cases compounds have wide and polymorphous liquid crystalline phases.Type: GrantFiled: August 20, 1992Date of Patent: September 20, 1994Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Hemmerling, Hans-Rolf Dubal, Claus Escher, Gerhard Illian, Yoshio Inoguchi, Ingrid Muller, Mikio Murakami, Dieter Ohlendorf, Rainer Wingen
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Patent number: 5329035Abstract: A process for producing a 2,3-disubstituted-4-substituted cyclopentanone, an enantiomorph thereof, or a mixture of these in an arbitrary ratio.The process comprises (A) subjecting a 4-substituted-2-cyclopentenone, an enantiomorph thereof, or a mixture of these in an arbitrary ratio, and an organocopper compound to conjugate addition-reaction, and thereafter (B) reacting the resulting enolate intermediate with a halide in the presence of a phenyl organotin compound.Type: GrantFiled: March 29, 1993Date of Patent: July 12, 1994Assignee: Teijin LimitedInventors: Ryoji Noyori, Masaaki Suzuki, Toshio Tanaka, Seizi Kurozumi
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Patent number: 5326844Abstract: A primer composition has blended therein an organic silicon compound having in a molecule at least one group of the formula: ##STR1## wherein R.sup.1 is a monovalent hydrocarbon group or a group represented by QSi( R.sup.4 O).sub.a (R.sup.5).sub.3-a, Q is a divalent organic group, R.sup.4 and R.sup.5 each are a monovalent hydrocarbon group, a is an integer of 0 to 3, R.sup.2 and R.sup.3 each are a hydrogen atom or a monovalent hydrocarbon group, and n is 0, 1 or 2. The primer composition is a useful adhesive since it is effective for joining silicone elastomers and similar adherends to supports such as paint coated metals and resins.Type: GrantFiled: April 7, 1993Date of Patent: July 5, 1994Assignee: Shin-Etsu Chemical Company, LimitedInventors: Hironao Fujiki, Masanobu Miyakoshi, Takeo Yoshida, Yoshifumi Inoue, Masatoshi Arai
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Patent number: 5300668Abstract: 1-[4'-(2"-Ethyl-5",7"-dimethylimidazo[4,5-b]pyridin-3-yl)methylphenyl]cyclo pent-3-ene-1-carboxylic acid and its pharmaceutically acceptable salts inhibit angiotensin II in mammals and are useful in treating conditions such as hypertension, congestive heart failure and glaucoma and as the active ingredient in pharmaceutical compositions for treating such conditions.Type: GrantFiled: March 10, 1993Date of Patent: April 5, 1994Assignee: Pfizer Inc.Inventor: Paul A. Dasilva Jardine
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Patent number: 5200530Abstract: The invention relates to a new process for the reduction of 15-keto carbacyclin intermediates in the presence of cerium(III) Salts.Type: GrantFiled: July 31, 1991Date of Patent: April 6, 1993Assignee: Schering AktiengesellschaftInventors: Helmut Dahl, Gabriela Buttner, Dieter Peschel
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Patent number: 5175338Abstract: An isocarbacyclin derivative represented by the following formula [VII'] ##STR1## wherein A represents, a hydrocarbylcarboxylate group, a carboxymethoxycarbonyl group, an amide group, an acyloxymethyl group or a hydroxymethyl group; R.sup.4 represents H, a methyl group or a vinyl group; R.sup.5 represents a (substituted)alkyl group, a phenyl group, a phenoxy group or a cycloalkyl group; R.sup.e22 and R.sup.e32 represent H or a hydroxyprotecting group; n is 0 or 1;and a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 14, 1990Date of Patent: December 29, 1992Assignee: Teijin LimitedInventors: Atsuo Hazato, Toshio Tanaka, Noriaki Okamura, Kiyoshi Bannai, Seizi Kurozumi, Masaaki Suzuki, Ryoji Noyori
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Patent number: 5169960Abstract: The invention relates to a process for the production of E/Z mixtures of 2-(bicyclo[3.3.0]octan-3-ylidene)-acetic acid derivatives of Formula I, ##STR1## in which either the E or the Z portion predominates.Type: GrantFiled: September 12, 1991Date of Patent: December 8, 1992Assignee: Schering AktiengesellschaftInventors: Hartmut Rehwinkel, Helmut Vorbruggen, Hans-Joachim Gais, Gerhard Schmiedl, Jorg Bund
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Patent number: 5149711Abstract: A 2-cyclopentenone derivative represented by the following formula ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 10 carbon atoms which may be substituted by a substituted or unsubstituted phenyl or phenoxy group, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and each represents a hydrogen atom or a lower alkanoyl group, and the wavy line shows that the bonded state of the double bond is E or Z.This compound is useful for treating, for instance, malignant tumors.Type: GrantFiled: March 7, 1989Date of Patent: September 22, 1992Assignee: Teijin LimitedInventors: Atsuo Hazato, Seizi Kurozumi
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Patent number: 5079259Abstract: A 9-chloroprostane of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha. or .beta.-position and R.sub.1, R.sub.4, R.sub.5, A, B, W, D and E are as described hereinafter which are useful as medical agents.Type: GrantFiled: September 8, 1987Date of Patent: January 7, 1992Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Walter Elger, Olaf Loge, Ekkehard Schillinger
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Patent number: 5077422Abstract: Organosilicon compounds having at least one unit of the general formula ##STR1## in which R represents alkyl, R' is a divalent alkylene, oxyalkylene, alkenylene or oxyalkenylene, Z represents an alkyl, alkoxy or hydroxyl group, a has a value of 0, 1, 2, or 3 and c is 0 or 1, wherein at least one of Z and R' is linked to the multivalent aryl group via an ether linkage, are useful for absorbing UV radiation. Especially if polymeric (with e.g. diorganosiloxane units) they can be incorporated in sunscreen preparations to improve their substantivity to the skin. A process for preparing the compounds is also disclosed.Type: GrantFiled: November 6, 1989Date of Patent: December 31, 1991Assignee: Dow Corning LimitedInventors: Andre R. L. Colas, Stephen E. Cray, Georg Frater
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Patent number: 5075478Abstract: A process for preparing prostaglandin derivatives by reacting a trans bis-tin ethylene with an organo metal compound then with a compound selected from an epoxide, aldehyde, or ketone, then, without isolation and in the same reaction vessel, reacting with an organo lithium compound, a cuprate complex and a cyclopentenone to produce a prostaglandin intermediate having an unprotected hydroxyl group on the omega side chain.Type: GrantFiled: January 17, 1991Date of Patent: December 24, 1991Assignee: G. D. Searle & Co.Inventors: James R. Behling, John R. Medich
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Patent number: 5055604Abstract: A process for preparing a prostaglandin derivative by reacting an alkyne with zirconocene chloride hydride to produce a zirconium intermediate which is reacted with an alkyllithium and a first copper reagent selected from R.sup.2 Cu(CN)Li or the mixture CuCN and R.sup.2 Li to produce a higher order cuprate complex intermediate and reacting the higher order cuprate complex intermediate with a cyclopentenone to produce the prostaglandin derivative.Type: GrantFiled: April 17, 1990Date of Patent: October 8, 1991Assignee: G. D. Searle & Co.Inventors: Kevin A. Babiak, James R. Behling, John H. Dygos, John S. Ng
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Patent number: 5053290Abstract: Novel diorganopolysiloxanes containing benzalmalonate functional groups, well adapted as coatings for optical fibers, as well as lubricants for plastic substrates, e.g., PVC substrates, have one of the following formulae: ##STR1## in which A and/or B is a benzalmalonate radical.Type: GrantFiled: September 11, 1989Date of Patent: October 1, 1991Assignee: Rhone-Poulenc ChimieInventors: Edith Canivenc, Serge Forestier, Michel Gay, Gerard Lang, Herve Richard
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Patent number: 5001255Abstract: Compounds of the formula ##STR1## the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.Type: GrantFiled: July 1, 1988Date of Patent: March 19, 1991Assignee: Sandoz Pharm. Corp.Inventors: Faizulla G. Kathawala, Sompong Wattanasin
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Patent number: 4992261Abstract: Organosilicon compounds having at least one unit of the general formula ##STR1## in which R represents alkyl, R' is a divalent alkylene, oxyalkylene, alkenylene or oxyalkenylene, Z represents an alkyl, alkoxy or hydroxyl group, a has a value of 0, 1, 2 or 3 and c is 0 or 1, wherein at least one of Z and R' is linked to the multivalent aryl group via an ether linkage, are useful for absorbing UV radiation. Especially if polymeric (with e.g. diorganosiloxane units) they can be incorporated in sunscreen preparations to improve their substantivity to the skin. A process for preparing the compounds is also disclosed.Type: GrantFiled: November 6, 1989Date of Patent: February 12, 1991Assignee: Dow Corning LimitedInventors: Andre R. L. Colas, Stephen E. Cray, Georg Frater
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Patent number: 4939172Abstract: Novel cyclopropane carboxylic acid esters of all possible stereoisomeric forms and mixtures thereof of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, fluorine, chlorine and bromine, R is selected from the group consisting of optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, optionally unsaturated cycloalkyl of 3 to 8 carbon atoms optionally substituted, optionally substituted aryl of 6 to 14 carbon atoms and optionally substituted heterocycle, Z is selected from the group consisting of hydrogen, --CH.sub.3, --CN and --C.tbd.CH and Y is selected from the group consisting of hydrogen, --OH, optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, --CN, --(CH.sub.2).sub.m --OAlk, --(CH.sub.2).sub.m --S--Alk, ##STR2## m is 0,1,2,3 or 4, Alk is alkyl of 1 to 12 carbon atoms, --Si(Alk').sub.3, Alk' is optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, --O--Ar and --(CH.sub.2).sub.Type: GrantFiled: February 8, 1988Date of Patent: July 3, 1990Assignee: Roussel UclafInventors: Joseph Cadiergue, Jacques Demassey, Jean-Pierre Demoute, Jean Tessier
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Patent number: 4924020Abstract: There is disclosed a novel phthalic acid ester-modified organopolysiloxane having the general formula ##STR1## where in R.sup.1 is a monovalent hydrocarbon group, R.sup.2 is a group R.sup.1 or a group with the formula ##STR2## with the proviso that at least one of the groups R.sup.2 in each molecule is the group with the formula ##STR3## in which R.sup.3 is an alkyl group, R.sup.4 is an alkylene group, and m is a positive integer.The organosiloxane is useful as a co-reactant in the preparation of organic resins such as polyesters, polyamides and polyimides.Type: GrantFiled: November 10, 1988Date of Patent: May 8, 1990Assignee: Toray Silicon Company, Ltd.Inventors: Tadashi Okawa, Toshio Suzuki
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Patent number: 4916238Abstract: This invention relates to a novel process for making an allenic prostanoic acid derivative in the form of a single stereoisomer, or a mixture of stereosiomers, represented by the formula (I): ##STR1## wherein R is lower alkyl, R.sup.1 is a protecting group which can be selectively removed in the presence of R.sup.2, R.sup.2 is an acid-labile, base-stable protecting group, X is --(CH.sub.2).sub.2 --, trans --CH.dbd.CH-- or --C.tbd.C--, Y is --C(R.sup.3)(OR.sup.2)CH.sub.2 --, in which --OR.sup.2 is in the .alpha. or .beta. configuration and R.sup.3 is hydrogen or methyl, Z is alkyl, or phenyl, benzyl or phenoxy each optionally substituted on the phenyl ring, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..Type: GrantFiled: December 13, 1988Date of Patent: April 10, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Gary F. Cooper, Colin C. Beard, David Y. Jackson, Douglas L. Wren
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Patent number: 4912241Abstract: Organosilicon compounds having at least one unit of the general formula ##STR1## in which R represents alkyl, R' is a divalent alkylene, oxyalkylene, alkenylene or oxyalkenylene, Z represents an alkyl, alkoxy or hydroxyl group, a has a value of 0, 1, 2 or 3 and c is 0 to 1, wherein at least one of Z and R' is linked to the multivalent aryl group via an ether linkage, are useful for absorbing UV radiation. Especially if polymeric (with e.g. diorganosiloxane units) they can be incorporated in sunscreen preparations to improve their substantivity to the skin. A process for preparing the compounds is also disclosed.Type: GrantFiled: July 29, 1988Date of Patent: March 27, 1990Assignee: Dow Corning LimitedInventors: Andre R. L. Colas, Stephen E. Cray, Georg Frater
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Patent number: 4876399Abstract: The present invention is directed to novel taxols useful as a chemotherapeutic agent. Moreover, the present invention is directed to the process of preparing taxols and various intermediates in said process. A key intermediate is this process is 2,5-dihydroxy-2-patchoulenes. Therefore the present invention is also related to said intermediate and the process for its preparation.Type: GrantFiled: November 2, 1987Date of Patent: October 24, 1989Assignee: Research Corporation Technologies, Inc.Inventors: Robert A. Holton, Rouh-Rong Juo, Richard Lowenthal
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Patent number: 4849535Abstract: Cyclopentenylheptanoic acid derivatives having the formula: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.4 alkyl and --(A)-- is: ##STR2## wherein M is hydrogen or triorganosilyl group, are prepared by reacting a compound having the formula: ##STR3## ps wherein X is halogen, with a compound having the formula: The derivatives belong to the pharmacologically-active class of compounds called "prostaglandins".Type: GrantFiled: February 24, 1986Date of Patent: July 18, 1989Assignees: Ajinomoto Co., Inc., Mochida Pharmaceutical Co., Ltd.Inventors: Hirokazu Naora, Takashi Onuki, Asao Nakamura
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Patent number: 4845282Abstract: The present invention provides an industrially very advantageous process for producing prostaglandins E.sub.1 with fewer steps and in higher yield. The process comprises reacting a 7-hydroxyprostaglandin E with a reactive derivative of an organic sulfonic acid in the presence of a basic compound to form the corresponding 7-organic sulfonyloxyprostaglandin E, treating the resulting 7-organic sulfonyloxyprostaglandin E, after or without isolation, in the presence of a basic compound to form a .DELTA..sup.7 -prostaglandin E, thereafter selectively reducing the carbon-carbon unsaturated bond existing on the .alpha.-chain. Some of the 7-hydroxyprostaglandins E and .DELTA..sup.7 -prostaglandins E used in the process are novel compounds.Type: GrantFiled: January 21, 1988Date of Patent: July 4, 1989Assignee: Teijin LimitedInventors: Ryoji Noyori, Masaaki Suzuki, Toshio Kawagishi, Seizi Kurozumi
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Patent number: 4837342Abstract: A prostacyclin analogue having the formula: ##STR1## wherein R.sup.1 is --CO.sub.2 R.sup.5 (wherein R.sup.5 is a hydrogen atom, a straight chain or branched alkyl group having from 1 to 12 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted phenyl group, or one equivalent of a cation), or --CONR.sup.6 R.sup.7 (wherein each of R.sup.6 and R.sup.7 is a hydrogen atom or an alkyl group having from 1 to 10 carbon atoms, or R.sup.6 and R.sup.7 together with the adjacent nitrogen atom, form a 5- or 6-membered substituted or unsubstituted hetero ring which may contain a hetero atom other than said nitrogen atom); A is --CH.sub.2 CH.sub.2 CH.sub.2 --, CH.sub.2 --O--CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 --O--CH.sub.2 -- or --CH.dbd.CHCH.sub.2 CH.sub. 2 --; B is trans --CH.dbd.CH-- or --C.Type: GrantFiled: February 13, 1987Date of Patent: June 6, 1989Assignees: Sagami Chemical Research Center, Toa Eiyo Ltd.Inventors: Masakatsu Shibasaki, Atsuo Takahashi, Tuyoshi Aoki, Kentaro Kogi, Yozo Nishimiya, Takeshi Nara, Takashi Yamaguchi
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Patent number: 4822909Abstract: 7-Fluoroprostaglandins represented by the following formula (I): ##STR1## In the formula (I), R.sup.1 is a hydrogen atom or an alkyl group having from 1 to 10 carbon atoms, R.sup.2, R.sup.3 and R.sup.4 are hydrogen atoms or the same or different protective groups, respectively, and R.sup.5 is a straight chained, branched or cyclic alkyl group having from 3 to 7 carbon atoms.Type: GrantFiled: June 9, 1987Date of Patent: April 18, 1989Assignee: Asashi Glass Company Ltd.Inventors: Yasuda Arata, Kato Masao, Yamabe Masaaki, Uchida Keiichi
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Patent number: 4810805Abstract: There are disclosed a (2-chloro-3-oxo-1-alkenyl)-bicyclo[3.3.0 octene derivative represented by the formula: ##STR1## wherein R.sup.1 represents --CH.sub.2 CH.sub.2 CH.sub.2 COOR.sup.5, --CH.sub.2 CH.sub.2 --O--CH.sub.2 COOR.sup.5, --CH.dbd.CHCH.sub.2 COOR.sup.5 or --CH.sub.2 CH.sub.2 C.tbd.C--COOR.sup.5 group where R.sup.5 in the groups represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, an acyl group having 1 to 7 carbon atoms, a tri(1 to 7 carbon atoms)-hydrocarbylsilyl group or a group forming an acetal bonding with an oxygen atom of a hydroxy group; R.sup.Type: GrantFiled: December 19, 1986Date of Patent: March 7, 1989Assignee: Mitsubishi Chemical Industries LimitedInventors: Masakatsu Shibasaki, Katsuhiko Iseki, Masaki Shinoda, Chiyoko Aoki, Yoshio Hayashi
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Patent number: 4797506Abstract: 6-substituted prostaglandins E.sub.1 which are compounds represented by the following formula [I] or their enantiomers or mixtures whereof in any ratio: ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.16 alkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenyl C.sub.3 -C.sub.10 cycloalkyl group, a substituted or unsubstituted phenyl (C.sub.1 -C.sub.2) alkyl group, or one equivalent cation; R.sup.2 and R.sup.3, which may be the same or different, represent a hydrogen atom, a tri (C.sub.1 -C.sub.7) hydrocarbon silyl group, or a group forming an acetal linkage together with an oxygen atom of a hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents a linear or branched C.sub.3 -C.sub.8 alkyl group, a linear or branched C.sub.3 -C.sub.8 alkenyl group, a linear or branched C.sub.3 -C.sub.8 alkynyl group, a phenyl group which may be substituted, a phenoxy group which may be substituted, a C.sub.3 -C.sub.Type: GrantFiled: October 18, 1985Date of Patent: January 10, 1989Assignee: Teijin LimitedInventors: Toshio Tanaka, Atsuo Hazato, Seizi Kurozumi
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Patent number: 4777184Abstract: Prostaglandin derivatives, and specifically derivatives of isocarbacyclin, have an optionally substituted methylene group as a substituent on the .alpha.-carbon atom of the .alpha.-side chain. They have a variety of physiological effects, notably a strong ability to inhibit blood platelet aggregation and a strong anti-ulcer activity.Type: GrantFiled: April 29, 1986Date of Patent: October 11, 1988Assignee: Sankyo Company LimitedInventors: Koichi Kojima, Shigeo Amemiya, Kazuo Koyama, Nobuyoshi Iwata, Takeshi Oshima
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Patent number: 4774028Abstract: Non-crosslinked, branched liquid crystalline organosilicon compounds exhibit the general formula(R.sub.3 SiO.sub.1/2).sub.w (R.sub.2 SiO).sub.x (RSiO.sub.3/2).sub.y (SiO.sub.4/2).sub.zwhere at least one R represents a mesogenic (liquid crystal forming) group, the remaning R represent monovalent hydrocarbon or halohydrocarbon radicals, w represents an integer having a value of at least 1, x, y, and z individually represent an integer including zero, the sum of x and y is at least 1 and the sum of w, x, y, and z is from 4 to 50, inclusive.Type: GrantFiled: May 23, 1985Date of Patent: September 27, 1988Assignee: Toray Silicone Co., Ltd.Inventors: Takeshi Imai, Naoyuki Koide
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Patent number: 4762935Abstract: This disclosure describes novel compounds which are useful as precursors in the synthesis of 9-oxo-11.alpha.,16-dihydroxy-16-vinyl-5-cis-13-trans-prostadienoate esters which possess activity as hypotensive agents and/or as vasodilators.Type: GrantFiled: October 6, 1986Date of Patent: August 9, 1988Assignee: American Cyanamid CompanyInventors: Allan Wissner, Kenneth E. Green, Philip R. Hamann, Jeremy Levin
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Patent number: 4736058Abstract: A novel prostacyclins expressed by the following formula (1) ##STR1## wherein a symbol between the 2-position and 3-position indicates single bond or double bond; G indicates --CO.sub.2 R.sup.5 or --CONR.sup.6 R.sup.7 in which R.sup.5 is a hydrogen atom, C.sub.1 -C.sub.10 alkyl group, substituted or unsubstituted alicyclic group, substituted or unsubstituted phenyl (C.sub.1 -C.sub.2) alkyl group, tri (C.sub.1 -C.sub.7) hydrocarbon-silyl group, or one equivalent cation, R.sup.6 and R.sup.7 are identical or different and each representing a hydrogen atom, or C.sub.1 -C.sub.10 alkyl group, or R.sup.6 and R.sup.7 are substituted or unsubstituted five to six-membered ring which may join together with a nitrogen atom to which they are linked and further contain a hetero atom; R.sup.1 indicates a hydrogen atom, or methyl group; R.sup.2 indicates an unsubstituted C.sub.3 -C.sub.8 alkyl group substituted or unsubstituted alicyclic group, or substituted C.sub.1 -C.sub.Type: GrantFiled: September 27, 1984Date of Patent: April 5, 1988Assignee: Teijin LimitedInventors: Shiro Ikegami, Seizi Kurozumi
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Patent number: 4734512Abstract: There are disclosed intermediates which can be converted into podophyllotoxin and related compounds, which are known antineoplastic agents. There are also disclosed processes for the preparation of such intermediates, and processes for the conversion of the intermediates into known intermediates which are readily converted into podophyllotoxin and related compounds.Type: GrantFiled: December 5, 1985Date of Patent: March 29, 1988Assignee: Bristol-Myers CompanyInventors: Takushi Kaneko, Henry S. L. Wong