Abstract: The invention relates to (.+-.) trans-2-[-4(1-hydroxyhexyl) phenyl]-5-oxocyclopentaneheptanoic acid, and ester and unsaturated derivatives thereof, prostaglandin derivatives. More particularly, the present invention concerns compounds of the formula I ##STR1## wherein the wavy bonds indicate that .alpha. or .beta. configuration, the dashed bond represents either a single or double bond, which double bond may be a cis or trans double bond and R is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.1 wherein m is 0-10, and R.sub.1 is an aliphatic ring having from about 3 to about 7 carbon atoms, or an aryl or heteroaryl ring having from about 4 to about 10 carbon atoms and wherein the heteroatom is selected from the group consisting of N, O and S. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
Abstract: Iridoid derivatives synthesized using genipin, which is an aglycon of geniposide, as the starting material are useful as an anti-hyperlipemia agent and as a cholagogue.
Type:
Grant
Filed:
June 23, 1994
Date of Patent:
October 17, 1995
Assignee:
Tsumura & Co.
Inventors:
Yuuichi Fujii, Ichiro Arai, Akira Hatta, Akemi Tatsugi, Hiroshi Mitsuhashi, deceased, by Mieko Mitsuhashi, legal representative, by Hiroyuki Mitsuhashi, legal representative, by Tomoaki Mitsuhashi, legal representative, Masaharu Kigawa
Abstract: A process for preparing the novel compound 2-bromo, 1', 2'-dichloroperfluoro diethyl ether of formula:BrCFhd 2--CF.sub.2 --O--CFCl--CF.sub.2 Clwhere BrCF.sub.2 --CF.sub.2 OF is reacted with the olefin CFCl.dbd.CFCl, with bromohypofluorite being introduced into the reaction mixture in the form of a solution in an inert solvent based on chlorofluorohydrocarbon.
Type:
Grant
Filed:
November 8, 1993
Date of Patent:
October 10, 1995
Assignee:
Ausimont S.r.l.
Inventors:
Pierangelo Calini, Guglielmo Gregorio, Giorgio Guglielmo
Abstract: There is disclosed a pharmaceutical composition for providing antiinflammatory, antipyretic, analgesic, antiallergic, immunosuppressing or immunomodulating activity which comprises a pyridine derivative of the formula (I): ##STR1## wherein R is an optionally substituted pyridine ring, X is a oxygen atom or --S(O).sub.n --, wherein n is 0, 1 or 2, A is a bivalent C.sub.1-15 hydrocarbon residue whose branched moiety may have a substituent, Y is an oxygen or sulfur atom, R.sub.3 is a hydrogen atom or an optionally substituted hydrocarbon residue, R.sub.4 is an optionally substituted hydrocarbon residue or an optionally substituted monocyclic or bicyclic heterocyclic group, R.sub.3 and R.sub.4 may be joined together with the carbamoyl group or the thiocarbamoyl group to which they are attached to form an optionally substituted heterocyclic group, or R.sub.3 or R.sub.
Abstract: A process for making t-butylthiol by reacting hydrogen sulfide and an olefin having a carbon number of 3 to 15 in the presence of a HZSM-5, HZSM-12, or MCM-22 zeolite catalyst. The reaction takes place under autogenous pressure conditions and a temperature of about 70.degree. C. to about 160.degree. C.
Abstract: A process for the production of alkyl tert alkyl ether, comprising the steps of providing a liquid hydrocarbon feedstock containing diolefin in an amount greater than or equal to about 2% wt, mixing said feedstock with an alcohol selected from the group consisting of methanol, ethanol, propanol and mixtures thereof and with hydrogen so as to provide a mixture of said feedstock, alcohol and hydrogen and contacting said mixture with an etherification catalyst under etherification process conditions including a pressure sufficient to maintain said hydrogen in a liquid phase, and a space velocity (LHSV) of less than or equal to about 1 h.sup.-1 so as to provide said alkyl tert alkyl ether without poisoning said catalyst.
Abstract: A process for preparing a compound of the formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen, R.sub.2 is e.g. C.sub.2 -C.sub.12 alkylene and R.sub.3 is e.g. C.sub.1 -C.sub.18 alkyl;which process comprises reacting, in water, in the absence of an organic solvent, a compound of the formula (II)Cl--COOR.sub.3 (II)wherein R.sub.3 is as defined above with a compound of the formula (III) ##STR2## where R.sub.1 is e.g. as defined above and R.sub.2 ' is e.g. as defined above for R.sub.2, at a temperature of from 0.degree. to 60.degree. C., 1 to 1.5 mol of the compound of the formula (II) being used per mol --NH-- group in the compound of the formula (III); and neutralizing the hydrochloric acid formed with an inorganic base.
Type:
Grant
Filed:
May 11, 1994
Date of Patent:
September 12, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Primo Carrozza, Giovanni Da Roit, Valerio Borzatta
Abstract: A process is disclosed for producing a fluorinated ether of the formula R.sub.2 CHOCF.sub.2 A, where A is Cl or F, and each R is H, (CF.sub.2).sub.n Cl, (CF.sub.2).sub.n F or (CF.sub.2).sub.n H (n is an integer from 1 to 10) by reacting a first reactant of the formula R.sub.2 CHOY where Y is H, COF, COCl or COOCHR.sub.2 (R is as defined above), a second reactant selected of the formula CZ.sub.2 Cl.sub.2 or COZ.sub.2 where each Z is independently Cl or F (provided that when A is Cl, the second reactant is CZ.sub.2 Cl.sub.2), and HF; and recovering the fluorinated ether from the reaction products. Also disclosed are bis-ethers of the formula (CF.sub.3 (CF.sub.2).sub.m).sub.2 CHOCF.sub.2 OCH (CF.sub.2).sub.m CF.sub.3).sub.2, where m is an integer of 0 to 3, which can also be produced by the process.
Type:
Grant
Filed:
September 2, 1994
Date of Patent:
September 12, 1995
Assignee:
E. I. Du Pont de Nemours and Company
Inventors:
Carl G. Krespan, V. N. Mallikarjuna Rao
Abstract: Disclosed is an improved process for preparing ethyl t-butyl ether in one step which comprises reacting tertiary butanol and ethanol in the presence of a catalyst selected from zeolite beta and zeolite beta modified with multimetals selected from the group consisting of Groups IB, VB, VIB, VIIB or VIII of the Periodic Table at a temperature of about 20.degree. C. to 250.degree. C. and atmospheric pressure to about 1000 psig, wherein when the temperature is in the operating range above about 140.degree. C., the product comprises a two-phase mix of an ETBE-isobutylene and, optionally, diisobutylene product-rich phase and a heavier aqueous ethanol-rich phase.
Abstract: A process for the production of an ether alcohol is disclosed, which comprises subjecting a cyclic ketal to hydrogenolysis in the presence of a catalyst containing palladium in an amount of from 50 to 100% by weight, based on the total active catalytic component present. According to the inventive process, ether alcohols which are useful as perfumes or raw materials for perfumes can be produced easily with low cost and high yield.
Abstract: This invention refers to heterocyclic compounds of general formula ##STR1## and their pharmacologically accepted salts. The derivatives described in this invention are active in the gastro-intestinal apparatus; in particular, they have prokinetic effects, in other words they create specific stimulation on gastro-intestinal motility, facilitating the passage of the contents of the alimentary tract, and possess anti-emetic qualities, without side effects involving the central nervous system.
Type:
Grant
Filed:
April 6, 1994
Date of Patent:
August 29, 1995
Assignee:
Alfa Wassermann S.p.A.
Inventors:
Claudia Baldazzi, Silvano Piani, Maria Barbanti, Egidio Marchi
Abstract: A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
Abstract: Described are preferred processes for hydrolyzing activated esters using, as catalysts, siloxanes having 4-dialkylaminopyridyl groups incorporated into their polymer backbones. The preferred siloxane catalyst materials demonstrate unexpected catalytic efficacy in the hydrolysis as well as enzyme-like selectivity for ester substrates.
Type:
Grant
Filed:
April 15, 1994
Date of Patent:
August 15, 1995
Assignee:
Indiana University Foundation
Inventors:
Martel Zeldin, Wilmer K. Fife, Slawomir Rubinsztajn
Abstract: Compounds having the formula ##STR1## wherein --OR.sup.1 comprises alkanoyl or the C-13 side-chain of taxol; R.sup.2, R.sup.3, and R.sup.6 can be oxygenated or hydrogen in various combinations; and R.sup.4 and R.sup.5 are acyl groups,as well as a process for the preparation thereof, pharmaceutical compositions containing the above compounds, and a method for their use in inhibiting tumor growth.
Type:
Grant
Filed:
March 9, 1994
Date of Patent:
August 8, 1995
Assignee:
Abbott Laboratories
Inventors:
Larry L. Klein, Clinton M. Yeung, Leping Li
Abstract: Novel chemical compounds that can be used to synthesize halichondrin B and norhalichondrin B, and related derivatives. The total synthesis of halichondrin B and norhalichondrin B is also disclosed.
Type:
Grant
Filed:
March 12, 1993
Date of Patent:
July 25, 1995
Assignee:
President and Fellows of Harvard College
Inventors:
Yoshito Kishi, Francis G. Fang, Craig J. Forsyth, Paul M. Scola, Suk K. Yoon
Abstract: 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.
Abstract: The present invention is directed to a new class of 2-optionally substituted-4-piperazine-benzothiophene derivatives of the formula ##STR1## in which Y is represented by hydrogen or C.sub.1-3 alkyl; R is represented by a substituent selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, --CF.sub.3, --OCF.sub.3, and --OH; R.sub.1 is represented by hydrogen, cycloalkyl, C.sub.1-6 alkyl, phenyl optionally substituted, phenylalkyl, or phenylamidoalkyl; X is represented by hydrogen, --(CH.sub.2).sub.n X.sub.1, CH=CHX.sub.1 or CHX.sub.2 --(CH.sub.2).sub.q --CH.sub.3 ; n is an integer from 0-2; q is either the integer 0 or 1; X.sub.1 is represented by --OH--,--OR.sub.2, --NR.sub.2 R.sub.3, --CO.sub.2 R.sub.2, --CONR.sub.2 R.sub.3, --CN, or --COR.sub.2 ; R.sub.2 and R.sub.3 are each independently represented by hydrogen, C.sub.1-4 alkyl, phenyl optionally substituted, phenylalkyl, or R.sub.2 and R.sub.3 together form a (CH.sub.2).sub.m cycloalkyl, where m=2- 6; X.sub.2 is --OR.
Type:
Grant
Filed:
September 15, 1993
Date of Patent:
July 25, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Ronald C. Bernotas, Jeffrey S. Sprouse, Hsien C. Cheng