Patents Assigned to Merrell Pharmaceuticals Inc.
  • Publication number: 20060014793
    Abstract: A process and diastereomeric salts useful for the optical resolution of racemic ?-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1 -piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1 -piperidinyl]-1-hydroxybutyl]-?,?-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-?,?-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(?)-di-paratoluoyltartaric acid or (?)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.
    Type: Application
    Filed: September 15, 2005
    Publication date: January 19, 2006
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: Mitsuo Nakamura, Masatoshi Shiga
  • Publication number: 20050032738
    Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of a 2?-halomethylidene derivative in conjunctive therapy with an effective antineoplastic amount of a S phase or M-phase specific agent.
    Type: Application
    Filed: September 17, 2004
    Publication date: February 10, 2005
    Applicant: Merrell Pharmaceuticals Inc.
    Inventor: Sai Sunkara
  • Publication number: 20040186137
    Abstract: A process and diastereomeric salts useful for the optical resolution of racemic &agr;-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(−)-di-paratoluoyltartaric acid or (−)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.
    Type: Application
    Filed: January 29, 2004
    Publication date: September 23, 2004
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: Mitsuo Nakamura, Masatoshi Shiga
  • Patent number: 6777555
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, n is an integer 0.
    Type: Grant
    Filed: February 12, 2003
    Date of Patent: August 17, 2004
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Publication number: 20040063659
    Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
    Type: Application
    Filed: September 18, 2003
    Publication date: April 1, 2004
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
  • Publication number: 20030220496
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1
    Type: Application
    Filed: February 12, 2003
    Publication date: November 27, 2003
    Applicant: Merrell Pharmaceuticals, Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Publication number: 20030130315
    Abstract: The present invention relates to a method of providing an antihistaminic effect in a hepatically impaired patient in need thereof comprising administering to said patient an effective antihistaminic amount of a compound of the formula 1
    Type: Application
    Filed: February 25, 2003
    Publication date: July 10, 2003
    Applicant: Merrell Pharmaceuticals, Inc.
    Inventors: James K. Woodward, Richard A. Okerholm, Mark G. Eller, Bruce E. McNutt
  • Patent number: 6566526
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 to 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: May 20, 2003
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6559312
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer of 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
    Type: Grant
    Filed: December 8, 2000
    Date of Patent: May 6, 2003
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6555689
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: April 29, 2003
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6552200
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1represented hydroxy, n is an integer 0.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: April 22, 2003
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6548675
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken to form a second bond between the carbon atoms R1 and R2 or where R1 represented hydroxy integer 0.
    Type: Grant
    Filed: December 5, 2000
    Date of Patent: April 15, 2003
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Publication number: 20020198407
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1
    Type: Application
    Filed: December 1, 2000
    Publication date: December 26, 2002
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6479663
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy m is an integer 0.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: November 12, 2002
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6441179
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
    Type: Grant
    Filed: March 28, 2001
    Date of Patent: August 27, 2002
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6420373
    Abstract: The present invention relates to novel 9-N-bicyclic nucleoside agents which are useful as selective inhibitors of proinflammatory cytokines.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: July 16, 2002
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: David R. Borcherding, Carl K. Edwards, III, H. Randall Munson
  • Patent number: 6399632
    Abstract: The present invention relates to a method of providing an antihistaminic effect in a hepatically impaired patient in need thereof comprising administering to said patient an effective antihistaminic amount of a compound of the formula wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A and B is hydrogen or hydroxy with the proviso that at least one of A or B is hydrogen; or a pharmaceutically acceptable salt and individual isomers thereof.
    Type: Grant
    Filed: September 15, 2000
    Date of Patent: June 4, 2002
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: James K. Woodward, Richard A. Okerholm, Mark G. Eller, Bruce E. McNutt
  • Patent number: 6348597
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
    Type: Grant
    Filed: April 4, 2001
    Date of Patent: February 19, 2002
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6340761
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: January 22, 2002
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Publication number: 20020007085
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1
    Type: Application
    Filed: December 5, 2000
    Publication date: January 17, 2002
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone