Patents Represented by Attorney Henry C. Jeanette
  • Patent number: 5712280
    Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the Formula 1.0 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
    Type: Grant
    Filed: April 7, 1995
    Date of Patent: January 27, 1998
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Alan K. Mallams, Adriano Afonso, Dinanath F. Rane, Randall R. Rossman, F. George Njoroge
  • Patent number: 5703090
    Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a novel compound of the formula (Ia), (Ib) or (Ic) ##STR1## wherein: R and R.sup.1 are H, alkyl, halogeno, OH, alkoxy, NH.sub.2, alkylamino, dialkylamino, CF.sub.3, SO.sub.3 H, CO.sub.2 R.sup.3, NO.sub.2, SO.sub.2 NH.sub.2, or CONHR.sup.4 ;n is 0 or 1;R.sup.2 is a group of the formula R.sup.5 C(O)--, R.sup.5 CH.sub.2 C(O)--, R.sup.5 C(R.sup.6).sub.2 C(O)--, R.sup.5 SO.sub.2 --, R.sup.5 CH.sub.2 SO.sub.2 --, R.sup.5 SCH.sub.2 C(O)--, R.sup.5 OC(O)--, R.sup.5 NHC(O)--, R.sup.5 C(O)C(O)-- or R.sup.5 SC(O)--;R.sup.5 is alkyl, aryl, arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl or heterocycloalkyl; andR.sup.6 is alkyl or C(R.sup.6).sub.2 is a carbocyclic ring;or pharmaceutically aceptable salts thereof.
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: December 30, 1997
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Joseph M. Kelly, Ronald L. Wolin
  • Patent number: 5700806
    Abstract: Novel compounds of Formula (7.0a), (7.0b) or (7.0c): ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the formula (7.0a), (7.0b) or (7.0c) to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: December 23, 1997
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, F. George Njoroge
  • Patent number: 5696121
    Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sub.25)(R.sub.48), are disclosed.Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: December 9, 1997
    Assignee: Schering Corporation
    Inventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
  • Patent number: 5684013
    Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a novel compound of the formula (Ia), (Ib) or (Ic) ##STR1## wherein: R and R.sup.1 are H, alkyl, halogeno, OH, alkoxy, NH.sub.2, alkylamino, dialkylamino, CF.sub.3, SO.sub.3 H, CO.sub.2 R.sub.3, NO.sub.2, SO.sub.2 NH.sub.2, or CONHR.sub.4 ;n is 0 or 1;R.sup.2 is a group of the formula R.sup.5 C(O)--, R.sup.5 CH.sub.2 C(O)--, R.sup.5 C(R.sup.6).sub.2 C(O)--, R.sup.5 SO.sub.2 --, R.sup.5 CH.sub.2 SO.sub.2 --, R.sup.5 SCH.sub.2 C(O)--, R.sup.5 OC(O)--, R.sup.5 NHC(O)--, R.sup.5 C(O)C(O)-- or R.sup.5 SC(O)--;R.sup.5 is alkyl, aryl, arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl or heterocycloalkyl; andR.sup.6 is alkyl or C(R.sup.6).sub.2 is a carbocyclic ring;or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: November 4, 1997
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Joseph M. Kelly, Ronald L. Wolin
  • Patent number: 5684197
    Abstract: A process for producing a hydrazide of the formula: ##STR1## is disclosed. The process comprises reacting a hydrazone of the formula: ##STR2## wherein said hydrazone is in toluene, with a mixture of Grignard reagents, wherein said Grignard reagents are in a suitable organic solvent; wherein: (A) Z is a suitable carbonyl protecting group; (B) R is a suitable --OH protecting group; (C) R.sup.1 is selected from: H, a non-enolizable alkyl, a non-enolizable substituted alkyl, aryl, substituted aryl, --S-aryl, --S-(substituted aryl), --S-alkyl, --S-(substituted alkyl), alkoxy, substituted alkoxy, aryloxy, or substituted aryloxy; (D) said mixture of Grignard reagents comprises R.sup.2 MgX in admixture with R.sup.3 MgX; (E) R.sup.2 is a suitable alkyl, substituted alkyl, alkenyl, alkynyl, aryl, substituted aryl, or aralkyl group capable of adding to the --C.dbd.N group of the hydrazone to produce the hydrazide; (F) R.sup.
    Type: Grant
    Filed: December 12, 1996
    Date of Patent: November 4, 1997
    Assignee: Schering Corporation
    Inventors: William Leong, Lyman Smith
  • Patent number: 5679692
    Abstract: Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: AR.sup.1 represents ##STR2## AR.sup.2 represents ##STR3## or a five-membered heterocyclic aromatic group selected from the group consisting of Formulas I to XII, wherein the substitutable carbon atoms of the five-membered heterocyclic group can optionally be substituted with a group R.sup.1.Also disclosed are pharmaceutical compositions containing compounds of Formula 1.0.Further disclosed is a method for treating asthma, allergy and inflammation by administering an anti-asthmatic, anti-allergic or anti-inflammatory, respectively, effective amount of a compound of Formula 1.0.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: October 21, 1997
    Assignee: Schering Corporation
    Inventors: Richard Friary, John J. Piwinski, Jesse K. Wong
  • Patent number: 5672611
    Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the Formula 1.0 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: September 30, 1997
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Alan K. Mallams, Adriano Afonso, Dinanath F. Rane, Randall R. Rossman, F. George Njoroge
  • Patent number: 5670676
    Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethylformamide; at a temperature within the range of about -78.degree. to about 0.degree. C.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: September 23, 1997
    Assignee: Schering Corporation
    Inventors: Richard W. Draper, Eugene J. Vater
  • Patent number: 5665735
    Abstract: Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: AR.sup.1 represents ##STR2## AR.sup.2 represents ##STR3## or a five-membered heterocyclic aromatic group selected from the group consisting of Formulas I to XII, wherein the substitutable carbon atoms of the five-membered heterocyclic group can optionally be substituted with a group R.sup.1.Also disclosed are pharmaceutical compositions containing compounds of Formula 1.0.Further disclosed is a method for treating asthma, allergy and inflammation by administering an anti-asthmatic, anti-allergic or anti-inflammatory, respectively, effective amount of a compound of Formula 1.0.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: September 9, 1997
    Assignee: Schering Corporation
    Inventors: Richard Friary, John J. Piwinski, Jesse K. Wong
  • Patent number: 5665726
    Abstract: Derivatives of benzo[5,6]cyclohepta pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.
    Type: Grant
    Filed: May 3, 1995
    Date of Patent: September 9, 1997
    Assignee: Schering Corporation
    Inventors: John J. Piwinski, Ashit K. Ganguly, Michael J. Green, Jesse Wong
  • Patent number: 5661152
    Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound containing a tricyclic ring system to a biological system. In particular, the method inhibits cellular growth in a mammal such as a human being.Novel compounds of the formula: ##STR1## are disclosed. Also disclosed are processes for making 3-substituted compounds of Formula 4.0.Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formula 4.0.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: August 26, 1997
    Assignee: Schering Corporation
    Inventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski
  • Patent number: 5648484
    Abstract: A process for producing a compound of the formula ##STR1## comprises the following sequence of steps: ##STR2## wherein the various radicals are as defined in the specification.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: July 15, 1997
    Assignee: Schering Corporation
    Inventor: Guang-Zhong Wu
  • Patent number: 5648360
    Abstract: Disclosed are novel compounds having structural formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is hydrogen, halo, --CF.sub.3 or lower alkyl; Y is --(CH.sub.2).sub.n --, wherein n is 0, 1, 2 or 3, --C(O)--, --CH.sub.2 C(O)--, --CH.sub.2 CH.sub.2 C(O)-- or --CH(OH)--; A is --N(R)-- and B is --CH.sub.2 --, or A is --CH.sub.2 -- and B is --N(R)--; R is hydrogen, lower alkyl, lower alkanoyl, --CO.sub.2 R.sup.1, (a) or (b); R.sup.1 is hydrogen, lower alkyl or --CH.sub.2 CCl.sub.3 ; and - - - - represents an optional double bond, with the proviso that the ring containing Y has only one optional double bond. Also disclosed are pharmaceutical compositions comprising these compounds and their use in treating allergy and inflammation.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: July 15, 1997
    Assignee: Schering Corporation
    Inventors: James J. Kaminski, Shing-Chun C. Wong, Nicholas I. Carruthers
  • Patent number: 5633250
    Abstract: Disclosed us a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula 1.0.Further disclosed is a method of treating allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimers, Schizophrenia, and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: May 27, 1997
    Assignee: Schering Corporation
    Inventor: Neng-Yang Shih
  • Patent number: 5602248
    Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethyl formamide; at a temperature within the range of about -78.degree. to about 0.degree. C., under anhydrous conditions under an inert atmosphere.
    Type: Grant
    Filed: March 16, 1995
    Date of Patent: February 11, 1997
    Assignee: Schering Corporation
    Inventors: Richard W. Draper, Eugene J. Vater
  • Patent number: 5563292
    Abstract: Novel compounds of Formula 1 ##STR1## or a pharmaceutically acceptable salt or solvate thereof are disclosed. Also disclosed are pharmaceutical compositions containing compounds of Formula 1. Methods of treating allergy, inflammation and hyperproliferative skin diseases with compounds of Formula 1 are also disclosed.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: October 8, 1996
    Assignee: Schering Corporation
    Inventors: Neng-Yang Shih, Pietro Mangiaracina
  • Patent number: 5561117
    Abstract: The invention is drawn to bridged bis-aryl carbinol compounds of formula (I): ##STR1## wherein, a, b, c, d, Q, Z, L and R.sup.1 -R.sup.9 are as defined in the specification, their pharmaceutical composition and method of using them in treating asthma, allergy and inflammation.
    Type: Grant
    Filed: September 23, 1994
    Date of Patent: October 1, 1996
    Assignee: Schering Corporation
    Inventors: Jesse K. Wong, John J. Piwinski
  • Patent number: 5514687
    Abstract: Benzopyrido piperidylidene compounds of the formula ##STR1## wherein R is H, Cl, Br, F or I, which are useful in treating asthma, allergy and/or inflammation.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: May 7, 1996
    Assignee: Schering Corporation
    Inventors: Jesse K. Wong, John J. Piwinski, Michael J. Green
  • Patent number: 5464840
    Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: November 7, 1995
    Assignee: Schering Corporation
    Inventors: Pauline C. Ting, Daniel M. Solomon, Wing C. Tom