Patents by Inventor Robert S. Wilhelm

Robert S. Wilhelm has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5716954
    Abstract: Benzo or pyridopyridazinones and pyridazinthiones of the formula ##STR1## wherein: X and Y are nitrogen or carbon, provided that at least one is carbon, and Z is oxygen or sulfur;R.sup.1 is hydrogen, lower alkyl, aryl, aralkyl, heterocyclo, heterocyclo lower-alkyl, heteroaryl, or heteroaralkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from hydrogen, lower alkyl, halo, carboxy, alkoxycarbonyl, carbamoyl, lower-alkyl carbonyl, halocarbonyl, thiomethyl, trifluoromethyl, cyano or nitro;or a pharmaceutically acceptable ester, ether or salt thereof, have been found to be useful as an anti-inflammatory, antasthmatic, immunosuppressive, anti-allograft rejection, anti-graft-vs-host rejection, autoimmune disease or analgetic agent(s).
    Type: Grant
    Filed: January 5, 1995
    Date of Patent: February 10, 1998
    Assignee: Syntex U.S.A. Inc.
    Inventors: Robert S. Wilhelm, Bradley E. Loe, Bruce H. Devens, Robert Alvarez, Michael G. Martin
  • Patent number: 5530005
    Abstract: The use of 8-phenylcyclopentenoquinolines and 8-phenylcyclohexenoquinolines for treating atopic dermatitis, allograft rejection, graft-vs-host disease, and anti-autoimmune disease, and inducing immunosuppression, is disclosed.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: June 25, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert S. Wilhelm, Sabine Axt
  • Patent number: 5475003
    Abstract: The disclosed derivatives of 8-phenylcyclopentenoquinolines and 8-phenylcyclohexenoquinolines are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft, rejection agents, anti-graft-vs-host disease agents, anti-allergic agents, bronchodilation agents, anti-autoimmune agents, and analgetic agents.
    Type: Grant
    Filed: March 3, 1994
    Date of Patent: December 12, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert S. Wilhelm, Sabine Axt
  • Patent number: 5466697
    Abstract: The disclosed 8-aryl-1,6-naphthyridin-5-ones, compounds of Formula I, ##STR1## wherein: R.sub.1 is hydrogen, alkyl, lower alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkyl lower alkyl, heterocycloalkyl lower alkyl, aralkyl or heteroaralkyl; andR.sub.2 is aryl; or a pharmaceutically acceptable salt or N-oxide thereof are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft rejection agents, anti-graft-vs-host disease agents, anti-allergic agents (e.g., asthma, rhinitis and atopic dermatitis), bronchodilation agents, anti-autoimmune agents or analgetic agents.
    Type: Grant
    Filed: July 13, 1994
    Date of Patent: November 14, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert S. Wilhelm, Bradley E. Loe
  • Patent number: 5455252
    Abstract: A compound of the formula ##STR1## wherein: R.sup.1 is independently selected from hydrogen, lower-alkyl, cycloalkyl, cycloalkyl lower-alkyl, lower-alkoxy, formyl, (lower-alkyl)-hydroxylmethyl, aryl, benzyl, arylmethyl, pyridylmethyl,where aryl, benzyl, arylmethyl and pyridylmethyl are unsubstituted or independently mono, di or tri substituted with hydrogen, hydroxy, thiol, amino, halo, nitro, lower-alkylthio, lower-alkoxy, mono-lower-alkylamino, di-lower-alkylamino, hydroxycarbonyl, lower-alkoxycarbonyl, hydroxysulfonyl, lower-alkoxysulfonyl, lower-alkylsulfonyl, lower-alkylsulfinyl, trifluoromethyl, cyano, tetrazoyl, carbamoyl, lower-alkylcarbamoyl, and di-lower-alkylcarbamoyl; andR.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth in the specification.
    Type: Grant
    Filed: March 31, 1993
    Date of Patent: October 3, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert S. Wilhelm, Paul R. Fatheree, Ronnie L. Chin
  • Patent number: 5264437
    Abstract: The present invention relates to optionally substituted pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones or optionally substituted pyrido[2,3-d]pyrimidine-2(1H,3H)-ones, i.e., compounds of Formula I: ##STR1## wherein: Y is --CH.sub.2 -- or --C(O)--;R.sup.1 is hydrogen or --(CH.sub.2).sub.n --R.sup.7, wherein:R.sup.7 is aryl or heteroaryl, andn is 1 or 2,provided that when Y is --C(O)--, R.sup.7 is heteroaryl; andR.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are hydrogen, or one is selected from lower alkyl, halo, carboxy, methoxycarbonyl, carbamoyl, methylcarbamoyl, di-methylcarbamoyl, methylcarbonyl, methylthio, methylsulfinyl, methylsulfonyl, hydroxymethyl, amino, trifluoromethyl, cyano or nitro; orR.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently selected from hydrogen, lower alkyl, nitro, chloro, fluoro, methoxycarbonyl or methylcarbonyl, provided at least one is hydrogen, and R.sup.6 is hydrogen;or a pharmaceutically acceptable ester, ether or salt thereof.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: November 23, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert S. Wilhelm, Ronnie L. Chin, Bruce H. Devens, Robert Alvarez