Patents by Examiner Diana G. Rivers

Patent number: 5190947
Abstract: The invention relates to the codeine salt of [2-[(2,6-dichlorophenyl)-amino]-phenyl]-acetic acid of formula ##STR1## to processes for the preparation thereof, to pharmaceutical compositions comprising that salt, and to its use as an analgesic drug.Compositions comprising the salt of formula I are used especially in the case of severe painful conditions.
Type: Grant
Filed: August 16, 1991
Issued: March 2, 1993
Assignee: Ciba-Geigy Corporation
Inventors: Walter Riess, Alfred Sallmann
Patent number: 5180722
Abstract: A camptothecin analog having the structure shown below: ##STR1## where Z is H or C.sub.1-8 alkyl and R is NO.sub.2, NH.sub.2, N.sub.3, hydrogen, halogen, COOH, OH, O--C.sub.1-3 alkyl, SH, S--C.sub.1-3 alkyl, CN, CH.sub.2 NH.sub.2, NH--C.sub.1-3 alkyl, CH.sub.2 --NH--C.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH--, or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S-- CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH.sub.2).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, CHO, C.sub.1-3 alkyl or NHCOCHR.sup.1 NR.sup.2 R.sup.3, where R.sup.1 is the side-chain of an .alpha.-amino acid and R.sup.2 and R.sup.3, independently are hydrogen or a lower alkyl group or R.sup.
Type: Grant
Filed: September 13, 1990
Issued: January 19, 1993
Assignee: Research Triangle Institute
Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
Patent number: 5179084
Abstract: The present invention relates to phosphoric acid esters of oxetanocins having an antiviral activity which are represented by general formula (I): ##STR1## wherein R.sub.1 represents a phosphoric acid ester residue, X represents hydrogen, hydroxy or hydroxymethyl group, and B represents a purine base residue, and pharmacologically acceptable salts thereof.
Type: Grant
Filed: April 4, 1990
Issued: January 12, 1993
Assignee: Nippon Kayaku Kabushiki Kaisha
Inventors: Seiichi Saito, Shigeru Hasegawa, Masayuki Kitagawa, Nobuyoshi Shimada, Katsutoshi Takahashi, Jun-ichi Seki, Hiroo Hoshino, Yukihiro Nishiyama, Kenichi Matsubara, Takemitsu Nagahata
Patent number: 5175291
Abstract: A process for preparing 1,3-dipropyl-8-(3-oxocyclopentyl)-xanthine.
Type: Grant
Filed: April 25, 1991
Issued: December 29, 1992
Assignee: Boehringer Ingelheim KG
Inventor: Ulrike Kufner-Muhl
Patent number: 5175290
Abstract: 1,3-Substituted-8-(oxo-substituted cycloalkyl)xanthines and pharmaceutically acceptable salts of such compounds are disclosed. Preferred compounds include the cis and trans isomers of 1,3-dipropyl-8-(3-hydroxycyclopentyl)xanthine and the cis and trans isomers of 1,3-dipropyl-8-(4-hydroxycyclohexyl)xanthine. The compounds are potent and selective bronchodilators and/or cardiotonic agents.
Type: Grant
Filed: September 16, 1988
Issued: December 29, 1992
Assignee: Marion Merrell Dow Inc.
Inventors: Waclaw J. Rzeszotarski, Roger N. Hiner, Scott W. Feeney
Patent number: 5175288
Abstract: A process for preparing pharmaceutically active compounds of formula (A): ##STR1## wherein X is hydrogen, hydroxy, chloro, C.sub.1-6 alkoxy or phenyl C.sub.1-6 alkoxy; and R.sub.a and R.sub.b are hydrogen, or acyl or phosphate derivatives thereof, which process comprises the preparation of an intermediate of formula (I): ##STR2## wherein R.sub.1 is C.sub.1-6 alkyl, or phenyl C.sub.1-6 alkyl in which the phenyl group is optionally substituted; R.sub.2 is hydrogen, hydroxy, chlorine, C.sub.1-6 alkoxy, phenyl C.sub.1-6 alkoxy or amino; and R.sub.3 is halogen, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, azido, an amino group or a protected amino group, via the reaction of a compound of formula (II): ##STR3## wherein R.sub.2 and R.sub.3 are as defined for formula (I) with: (a) a compound of formula (III): ##STR4## wherein R.sub.4 and R.sub.5 are independently hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.4 and R.sub.5 together are C.sub.
Type: Grant
Filed: April 9, 1990
Issued: December 29, 1992
Assignee: Beecham Group p.l.c.
Inventors: Trevor J. Grinter, Graham R. Geen, Martin J. Parratt
Patent number: 5166198
Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is hydrogen or (when R.sub.3 =H and Z is a bond or CH.sub.2) hydroxy, acyloxy, hydroxymethyl or acyloxymethyl;Z is a bond, or a group CHR.sub.8 wherein R.sub.8 is hydrogen, or (when R.sub.3 =R.sub.4 =H), R.sub.8 is hydroxy, acyloxy, hydroxymethyl or acyloxymethyl;R.sub.5 is a group of formula: ##STR2## wherein R.sub.6 and R.sub.7 are independently selected from hydrogen,C.sub.1-6 alkyl and optionally substituted phenyl.
Type: Grant
Filed: March 28, 1990
Issued: November 24, 1992
Assignee: Beecham p.l.c.
Inventors: Michael R. Harnden, David M. Duckworth, Halina T. Serafinowska
Patent number: 5164390
Abstract: 6-substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.
Type: Grant
Filed: July 2, 1991
Issued: November 17, 1992
Assignee: Ortho Pharmaceutical Corporation
Inventors: Zoltan G. Hajos, Ramesh M. Kanojia, Jeffery B. Press
Patent number: 5155098
Abstract: This invention relates to a N-heteroaryl-purin-6-amine of the formula ##STR1## where R.sub.1 is hydrogen, lower alkyl, and arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl, or R.sub.4 and R.sub.5 taken together are aryl; R.sub.6 is hydrogen, lower alkyl, aryl, arylloweralkyl, ##STR2## where R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic and anitconvulsant agents.
Type: Grant
Filed: May 6, 1991
Issued: October 13, 1992
Assignee: Hoechst-Roussel Pharmaceuticals Inc.
Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olson
Patent number: 5151429
Abstract: 17.beta.-Acyl-4-aza-5.alpha.-androst-1-en-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents, aralkyl selected from benzyl and phenethyl and heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl;and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulation of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
Type: Grant
Filed: September 23, 1991
Issued: September 29, 1992
Assignee: Merck & Co., Inc.
Inventors: Gary H. Rasmusson, Glenn F. Reynolds
Patent number: 5151430
Abstract: Specific 17.beta.-thiobenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as antiandrogenic agents of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is phenyl substituted with one or more of: --SH, --SC.sub.1 --C.sub.4 alkyl, --SO--C.sub.1 --C.sub.4 alkyl, --SO.sub.2 --C.sub.1 --C.sub.4 alkyl, --SO.sub.2 N--(C.sub.1 -C.sub.4 alkyl).sub.2, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m SH, --S(CH.sub.2).sub.n OCOCH.sub.3, where m is 1-4, n is 1-3, and providing C.sub.1 -C.sub.4 alkyl is only present when one of the above sulfur-containing radicals is present, wherein the dotted line can represent a double bond, and pharmaceutically acceptable esters and salts thereof. Also included is a pharmaceutical formulation thereof. The above compounds are active as antiandrogenic agents and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
Type: Grant
Filed: August 16, 1991
Issued: September 29, 1992
Assignee: Merck & Co., Inc.
Inventors: Nathan G. Steinberg, Gary H. Rasmusson, Thomas N. Salzmann
Patent number: 5144034
Abstract: This invention relates to a new process for preparing certain optically active cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1'R-cis isomer of carbovir, (1'R-cis)-2-amino-1,9-dihydro-9[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-p urin-6-one, an antiviral agent.
Type: Grant
Filed: April 6, 1990
Issued: September 1, 1992
Assignee: Glaxo Inc.
Inventors: M. Ross Johnson, Michael R. Peel, Daniel D. Sternbach
Patent number: 5138057
Abstract: A process for the preparation of a compound of formula (I) ##STR1## which process comprises reacting a compound of formula (II): ##STR2## wherein the amino group is optionally protected, with a side chain intermediate of formula (III): ##STR3## wherein Q is a leaving group, R.sub.x and R.sub.y are protected hydroxymethyl or acyloxymethyl, or group(s) convertible to hydroxymethyl or acyloxymethyl; and R.sub.z is hydrogen or a group convertible thereto; and thereafter converting the 6- and 8- chloro substituents to hydrogen by means of reduction; converting R.sub.x and R.sub.y when other than hydroxymethyl or acyloxymethyl, to hydroxymethyl or acyloxymethyl, optionally converting R.sub.x /R.sub.y hydroxymethyl to acyloxymethyl or vice versa, deprotecting the 2-amino group where necessary and converting R.sub.z, (when other than hydrogen) to hydrogen; and optionally forming a pharmaceutically acceptable salt thereof.
Type: Grant
Filed: September 19, 1989
Issued: August 11, 1992
Assignee: Beecham Group p.l.c.
Inventors: Graham R. Geen, John C. Hanson
Patent number: 5127934
Abstract: Organic stabilizers are used to stabilize various materials which are normally unstable neat or in solution. These compositions exhibit bactericidal, fungicidal and algaecidal properties.
Type: Grant
Filed: February 7, 1990
Issued: July 7, 1992
Assignee: Rohm and Haas Company
Inventor: John R. Mattox
Patent number: 5126452
Abstract: This invention relates to new process for preparing certain optically active purine substituted cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1R-cis isomer of carbovir, (1R-cis)-amino-1,9-dihydro-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-pur in-6-one, an antiviral agent, and certain intermediates.
Type: Grant
Filed: April 6, 1990
Issued: June 30, 1992
Assignee: Glaxo Inc.
Inventors: Robert Vince, Mark L. Peterson, John W. Lackey, Robert A. Mook, Jr., John J. Partridge
Patent number: 5122607
Abstract: New intermediate compounds are disclosed of the formula I, ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl having 1 to 4 carbon atoms,or acid-addition salts thereof of formula Ib, ##STR2## wherein X represents an acid residue, and a process for the preparation of the intermediate compounds.
Type: Grant
Filed: June 21, 1990
Issued: June 16, 1992
Assignee: Richter Gedeon Vegyesczeti Gyar RT.
Inventors: Janos Kreidl, Csaba Szantay, Lajos Szaho, Maria Farkas nee Kirjak, Gyorgy Kalaus, Katalin Nogradi, Andras Nemes, Judit Meszaros nee Brill, Zsuzsanna Aracs nee Tischler, Bela Stefko, Janos Sapi, Ida Deutsch nee Juhasz, Istvan Hegedus, Bela Benke, Kalman Graf, Kalmam Gaf, Katalin Horvath nee Berki
Patent number: 5122606
Abstract: The invention relates to a method of producing 20(S)-camptothecin, 20(R)-camptothecin and analogs thereof. The method involves the resolution of an mixture of enantiomers of an intermediate lactone.
Type: Grant
Filed: March 7, 1991
Issued: June 16, 1992
Assignee: Research Triangle Institute
Inventors: Mansukh C. Wani, Allan W. Nicholas, Monroe E. Wall
Patent number: 5122526
Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show anti-leukemic and anit-tumor activity.
Type: Grant
Filed: December 31, 1990
Issued: June 16, 1992
Assignee: Research Triangle Institute
Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
Patent number: 5110932
Abstract: The present invention relates to novel acridinium esters which are useful as luminescent labels in specific binding assays such as immunoassays or nucleic acid hybridization assays. More particularly, polysubstituted aryl acridinium esters are highly stable labels for use in a chemiluminescent immunoassay.
Type: Grant
Filed: March 1, 1990
Issued: May 5, 1992
Assignee: Ciba Corning Diagnostics Corp.
Inventors: Say-Jong Law, Steve C. S. Chang, Stephen A. Palmacci, Roger S. Cubicciotti
Patent number: RE34185
Abstract: Non-aqueous solutions of 3-isothiazolones are stabilized against chemical decomposition by using organic hydroxylic solvents. These compositions exhibit bactericidal, fungicidal and algaecidal properties.
Type: Grant
Filed: October 31, 1990
Issued: February 23, 1993
Assignee: Rohm and Haas Company
Inventor: David R. Amick