Patents Represented by Attorney Sidney B. Williams, Jr.
  • Patent number: 4225720
    Abstract: Process for the purification of L-(.alpha.S,5S)-.alpha.-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid (AT-125). Also provided are AT-125 analogs prepared in the process.
    Type: Grant
    Filed: January 2, 1979
    Date of Patent: September 30, 1980
    Assignee: The Upjohn Company
    Inventor: David G. Martin
  • Patent number: 4208409
    Abstract: Some new phosphinic acid derivatives of aminothio methylcarbamates have been synthesized and tested as pesticides. The new compounds are active against insects, mites, and nematodes. The N-[(phosphinyl)amino]thio- and N-[(phosphinothioyl)amino]thio- methylcarbamates are readily prepared by the general procedure of reacting a phosphinic acid amide with sulfur dichloride so as to obtain the corresponding N-(chlorothio)phosphinic acid amide which reactant will react with a methylcarbamate so as to produce the corresponding object compounds, the N-[(phosphinothioyl)amino]thio- methylcarbamates of this invention. Various formulations for pesticidal use are described along with appropriate rates of application.
    Type: Grant
    Filed: November 20, 1978
    Date of Patent: June 17, 1980
    Assignee: The Upjohn Company
    Inventor: Stephen J. Nelson
  • Patent number: 4207239
    Abstract: Isochromans, isothiochromans, 2-benzoxepins, and 2-benzothiepins are described. These compounds are useful for preparing corresponding amino derivatives that possess antihypertensive and CNS activity.
    Type: Grant
    Filed: January 2, 1979
    Date of Patent: June 10, 1980
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4206123
    Abstract: Isochromans, isothiochromans, 2-benzoxepins, and 2-benzothiepins are described. These compounds are useful for preparing corresponding amino derivatives that possess antihypertensive and CNS activity.
    Type: Grant
    Filed: January 2, 1979
    Date of Patent: June 3, 1980
    Inventor: John M. McCall
  • Patent number: 4206131
    Abstract: A process for preparing 1.alpha.-hydroxylated calciferols is described. Intermediates used in the process are also provided.
    Type: Grant
    Filed: June 19, 1978
    Date of Patent: June 3, 1980
    Assignee: The Upjohn Company
    Inventor: William G. Salmond
  • Patent number: 4201733
    Abstract: Some new phosphinic acid derivatives of aminothio methylcarbamates have been synthesized and tested as pesticides. The new compounds are active against insects, mites, and nematodes. The N-[(phosphinyl)amino]thio- and N-](phosphinothioyl)amino]thio-methylcarbamates are readily prepared by the general procedure of reacting a phosphinic acid amide with sulfur dichloride so as to obtain the corresponding N-(chlorothio)phosphinic acid amide which reactant will react with a methylcarbamate so as to produce the corresponding object compounds, the N-[(phosphinyl)amino]thio- and N-[(phosphinothioyl)-amino]thio-methylcarbamates of this invention. Various formulations for pesticidal use are described along with appropriate rates of application.
    Type: Grant
    Filed: February 3, 1978
    Date of Patent: May 6, 1980
    Assignee: The Upjohn Company
    Inventor: Stephen J. Nelson
  • Patent number: 4188324
    Abstract: Process for the purification of L-(.alpha.s,5s)-.alpha.-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid (AT-125). Also provided are AT-125 analogs prepared in the process.
    Type: Grant
    Filed: November 13, 1978
    Date of Patent: February 12, 1980
    Assignee: The Upjohn Company
    Inventor: David G. Martin
  • Patent number: 4181665
    Abstract: Isochromans, isothiochromans, 2-benzoxepins, and 2-benzothiepins are described. These compounds are useful for preparing corresponding amino derivatives that possess antihypertensive and CNS activity.
    Type: Grant
    Filed: January 2, 1979
    Date of Patent: January 1, 1980
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4179510
    Abstract: Isochromans, isothiochromans, 2-benzoxepins and 2-benzothiepins are described. The compounds possess hypotensive and antipsychotic properties; methods and compositions using them are described.
    Type: Grant
    Filed: October 31, 1977
    Date of Patent: December 18, 1979
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4172889
    Abstract: A process of treatment for the management of the condition known as rheumatoid arthritis. The process manages rheumatoid arthritis by controlling the inflammatory process in a rheumatoid joint by the intra-articular administration to said joint of an effective amount for controlling the inflammatory process of certain N.sup.4 -acyl-ara-cytidines, 5'-O-acyl-ara-cytidines and pharmaceutically acceptable acid addition salts thereof, and pharmaceutically acceptable acid addition salts of 5'-O-acyl-2,2'-anhydro-ara-cytidines.
    Type: Grant
    Filed: April 12, 1978
    Date of Patent: October 30, 1979
    Assignee: The Upjohn Company
    Inventors: William J. Wechter, Carter D. Brooks
  • Patent number: 4166062
    Abstract: 1-Alkoxyethanol-isochromas, -isothiochromas, -2-benzoxepins, and -2-benzothiepins are described. These compounds are useful for preparing the corresponding aminoalkoxyalkyl derivatives that possess antihypertensive and CNS activity.
    Type: Grant
    Filed: July 21, 1978
    Date of Patent: August 28, 1979
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Ruth E. TenBrink
  • Patent number: 4160840
    Abstract: Compounds of the formula: ##STR1## AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF WHEREIN R, R.sub.1, R.sub.2, R.sub.3, are selected from the group consisting of hydrogen, halogen and lower-alkyl of from one to four carbon atoms, inclusive; with the proviso that taken together they constitute the following substituents on the tetracyclic ring, 10-halo, 8,10-dihalo, 8,9-di-lower-alkyl, and 7,9-dilower-alkyl; R', R'.sub.1, R'.sub.2, and R'.sub.3 are selected from the group consisting of hydrogen, halogen and lower alkyl of from one to four carbon atoms, inclusive, with the proviso that when taken together they constitute the following substituents, 1-halo, 2-halo, 3-halo, 4-halo, 1-lower-alkyl, 2-lower-alkyl, 3-lower-alkyl, 4-lower-alkyl, 1,3-dihalo, 2,3-dihalo, 2,4-dihalo, 3,4-dihalo, 1,3-di-lower-alkyl, 2,3-di-lower-alkyl, 1,4-di-lower-alkyl; R.sub.4, R.sub.5, R.sub.6, and R.sub.
    Type: Grant
    Filed: December 5, 1977
    Date of Patent: July 10, 1979
    Inventor: Parimal K. Adhikary
  • Patent number: 4160037
    Abstract: 3-Benzoyl-1-phenyl-2-thioureas are disclosed as insecticides, miticides and nematicides.
    Type: Grant
    Filed: September 30, 1977
    Date of Patent: July 3, 1979
    Assignee: The Upjohn Company
    Inventor: Girts Kaugars
  • Patent number: 4153612
    Abstract: Isochromans, isothiochromans, 2-benzoxepins, and 2-benzothiepins are described. These compounds are useful for preparing corresponding amino derivatives that possess antihypertensive and CNS activity.
    Type: Grant
    Filed: December 7, 1977
    Date of Patent: May 8, 1979
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4143142
    Abstract: Compounds of the formula: ##STR1## AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF WHEREIN R, R.sub.1, R.sub.2, R.sub.3, are selected from the group consisting of hydrogen, halogen and lower-alkyl of from one to four carbon atoms, inclusive; with the proviso that taken together they constitute the following substituents on the tetracyclic ring, 10-halo, 8,10-dihalo, 8,9-di-lower-alkyl, and 7,9-dilower-alkyl; R', R'.sub.1, R'.sub.2, and R'.sub.3 are selected from the group consisting of hydrogen, halogen and lower alkyl of from one to four carbon atoms, inclusive, with the proviso that when taken together they constitute the following substituents, 1-halo, 2-halo, 3-halo, 4-halo, 1-lower-alkyl, 2-lower-alkyl, 3-lower-alkyl, 4-lower-alkyl, 1,3-dihalo, 2,3-dihalo, 2,4-dihalo, 3,4-dihalo, 1,3-di-lower-alkyl, 2,3-di-lower-alkyl, 1,4-di-lower-alkyl; R.sub.4, R.sub.5, R.sub.6, and R.sub.
    Type: Grant
    Filed: November 4, 1977
    Date of Patent: March 6, 1979
    Inventor: Parimal K. Adhikary
  • Patent number: 4134913
    Abstract: Novel pesticidal compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl of from 1 to 4 carbon atoms; R.sub.2 is hydrogen, halogen or lower alkyl of from 1 to 4 carbon atoms; R.sub.3 and R.sub.4 are the same or different and are hydrogen, alkyl of 1 to 8 carbon atoms, inclusive; haloalkyl, arylalkyl and ##STR2## WHEREIN ALKYL IS FROM 1 TO 4 CARBON ATOMS, CYCLOALKYL OF FROM 3 TO 6 CARBON ATOMS, ARYL AND R.sub.3 and R.sub.4 taken together are a member selected from the group piperidine, morpholine, pyrazole, tribromopyrazole, N-methylpiperazine, pyrrole, pyrrolidine, pyrrolidone.The compounds are combined with carriers to prepare compositions and are useful in controlling insect pests either as an insecticide or behavioral modifier and are particularly effective as miticides.
    Type: Grant
    Filed: April 28, 1977
    Date of Patent: January 16, 1979
    Assignee: The Upjohn Company
    Inventor: Victor L. Rizzo
  • Patent number: 4118484
    Abstract: A process of treatment for the management of the condition known as rheumatoid arthritis. The process manages rheumatoid arthritis by controlling the inflammatory process in a rheumatoid joint by the intra-articular administration to said joint of an effective amount for controlling the inflammatory process of certain N.sup.4 -acyl-ara-cytidines, 5'-O-acyl-ara-cytidines and pharmaceutically acceptable acid addition salts thereof, and pharmaceutically acceptable acid addition salts of 5'-O-acyl-2,2'-anhydro-ara-cytidines.
    Type: Grant
    Filed: March 29, 1976
    Date of Patent: October 3, 1978
    Assignee: The Upjohn Company
    Inventors: William J. Wechter, Carter D. Brooks
  • Patent number: 4096324
    Abstract: 5'-Esters of ara-cytidine (1-.beta.-D-arabinofuranosylcytosine) are prepared by reacting ara-cytidine with .beta.,.beta.,.beta.-trihaloethoxycarbonyl halide or other protective agency to form a protective amido group on the primary amino nitrogen of ara-cytidine and then reacting the thus-protected compound with a reagent reactive with the 5'-O-hydroxyl group, e.g., an acylating agent, to form the 5'-O-derivative. The .beta.,.beta.,.beta.-trihaloethoxycarbonyl or other protective group is then removed. Alternately, the primary amino group of ara-cytidine can be protected from acylation by protonation. The 5'-O-derivatives in their free base of salt form are characterized in that they display the property of sustained release of the compound, ara-cytidine, when administered intramuscularly or subcutaneously.
    Type: Grant
    Filed: January 30, 1976
    Date of Patent: June 20, 1978
    Assignee: The Upjohn Company
    Inventors: Robert C. Kelly, William J. Wechter
  • Patent number: 4094906
    Abstract: Certain alkanoyl chloride phenylhydrazones have been found to be active against insects and mites, and also active as herbicides. The phenylhydrazone ring can be substituted. Suitable substituent groups are halogen atoms, the nitro group, the trifluoromethyl group, and alkyl groups of from 1 to 6 carbon atoms, inclusive. The compounds are prepared by reacting an alkanoic acid phenylhy-drazide with phosphorus pentachloride to obtain an alkanoyl chloride (dichlorophosphinyl)phenylhydrazone intermediate that is reacted with phenol to produce the desired alkanoyl chloride phenylhydrazone. Certain compounds can be prepared by direct chlorination of an alkanaldehyde phenylhydrazone. Some of the compounds are novel. Methods of use and compositions are described.
    Type: Grant
    Filed: September 16, 1974
    Date of Patent: June 13, 1978
    Assignee: The Upjohn Company
    Inventor: Girts Kaugars
  • Patent number: PP4539
    Abstract: A new and distinct variety of a hybrid tomato plant substantially as herein shown and described, characterized as to novelty when compared to Walter, the most similar variety to it, by uniform crop characteristics, low grading loss, high yield, early maturity, low percentage of fruit with stems, low percentage of fruit ripening defects, multiple disease resistance and tolerance.
    Type: Grant
    Filed: December 11, 1978
    Date of Patent: May 27, 1980
    Assignee: The Upjohn Company
    Inventor: Carroll G. Briggs