Patents Represented by Attorney Grant D. Green
  • Patent number: 7141562
    Abstract: Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R2 is aryl or heteroaryl, and R1, R3, R4, R5, R6, R7, R8, R9, Ra, Rb, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: November 28, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: Hans Maag, Meng Sui, Shu-Hai Zhao
  • Patent number: 7135470
    Abstract: The invention provides compounds of the formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein: A, Y, Z and R1 are as defined herein. Also provided are compositions comprising, methods of preparing, and methods for using the subject compounds.
    Type: Grant
    Filed: May 4, 2005
    Date of Patent: November 14, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
  • Patent number: 7135476
    Abstract: Compounds of the formula (I): and pharmaceutically acceptable salts or prodrugs thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Grant
    Filed: August 11, 2004
    Date of Patent: November 14, 2006
    Assignee: Roche Palo Alto LLC
    Inventor: Robin Douglas Clark
  • Patent number: 7105666
    Abstract: The present invention provides a method for producing 2-, 6-, 8- and 9-substituted purine compounds from 4,6-dihalo-5-nitro-2-alkyl-pyrimidine compounds in solution or by solid phase techniques. The present process provides for the sequential introduction of amine substituents at the 4- and 6-positions, displacement of an alkylsulfony group at the 2-position of the pyrimidine, reduction of the nitro group and formation of the imidazole portion of the purine compound. Furthermore, the methods of the present invention are ideally suited to the preparation of a library of purine compounds.
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: September 12, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: Lars G.J. Hammarström, Nancy Elisabth Krauss, Sharada Shenvi Labadie, David Bernard Smith, Francisco Xavier Talamas
  • Patent number: 7105525
    Abstract: The present invention provides compounds of the Formula I: wherein R1 is alkyl, cycloalkyl, cycloalkylalkyl, or —CH2-alkenyl, X1 is O, NH, N(alkyl), S or —C(?O), Z is N or CH; and R2 and R3are as defined herein, pharmaceutical compositions comprising same, and methods for their use.
    Type: Grant
    Filed: May 4, 2005
    Date of Patent: September 12, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: David Michael Goldstein, Julie Anne Lim
  • Patent number: 7091347
    Abstract: The present invention discloses compounds corresponding to formula wherein A, R, X, Y, R, R1 and R2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.
    Type: Grant
    Filed: March 6, 2003
    Date of Patent: August 15, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: Jian Jeffrey Chen, Nolan James Dewdney, Christoph Martin Stahl
  • Patent number: 7091200
    Abstract: This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X-Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: August 15, 2006
    Assignee: Syntex U.S.A. LLC
    Inventors: Cyrus Kephra Becker, Joan Marie Caroon, Chris Richard Melville, Fernando Padilla, Jürg Roland Pfister, Xiaoming Zhang
  • Patent number: 7081462
    Abstract: The present invention discloses compounds corresponding to formula I: wherein A, Z, Z1, Y, R1 and R2 are as defined in the specification, as well as pharmaceutical formulations, methods of making and uses thereof.
    Type: Grant
    Filed: May 4, 2005
    Date of Patent: July 25, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: David Michael Goldstein, Ronald Charles Hawley, Alfred Sui-Ting Lui, Eric Brian Sjogren
  • Patent number: 7081531
    Abstract: Compounds having the formula (I), Ar—(F)-(E)-(CR3R4)—(CHR5)m-(T)-(Q)-Ar1, are useful as CCR-3 receptor antagonists, wherein T is a bridged heterocyclyl group having one N atom and a bridge of one to two bridgehead carbon atoms; Ar and Ar1 are aryl or heteroaryl; F is alkylene, alkenylene, or a bond; E is —C(?O)N(R10)—, —SO2N(R10)—, —N(R11)C(?O)N(R10)—, —N(R11)SO2N(R10)—, —N(R11)C(?S)N(R10)—, —N(R11)C(?O)—, —N(R11)SO2—, —N(R12)C(?O)CH(R13)—, or CH(R13)C(?O)N(R12)—; Q is —C(?O)— or C1-2alkylene; and R3, R4, R5, R9, R10, R11, R12, and R13 are defined as set forth in the specification.
    Type: Grant
    Filed: February 26, 2004
    Date of Patent: July 25, 2006
    Assignee: Roche Palo Alto LLC
    Inventor: Leyi Gong
  • Patent number: 7074763
    Abstract: Aqueous formulations of nerve growth factor suitable for lyophilization and subsequent reconstitution in which nerve growth factor is admixed with sugars and buffer are provided.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: July 11, 2006
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Victoria M. Knepp
  • Patent number: 7074939
    Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —O—, —S—, or —S(O)—; and the other substituents are as defined in the specification; or individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: July 11, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Jeffrey Allen Campbell
  • Patent number: 7071177
    Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: July 4, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Nancy Elisabeth Krauss, Taraneh Mirzadegan, David Bernard Smith, Keith Adrian Walker
  • Patent number: 7049325
    Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a CH2, CH(OH), C(O), C?NOR4, NR5, O, S, S(O), or S(O)2, and the other substituents are as defined in the specification; or prodrugs, individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 7, 2001
    Date of Patent: May 23, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Chris Allen Broka, Woongki Kim, David Bernard Smith, Kevin L. McLaren
  • Patent number: 7049317
    Abstract: The invention provides compounds of Formula (I): wherein R1–R4 have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: May 23, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventor: Daisy Joe Du Bois
  • Patent number: 7019007
    Abstract: The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: March 28, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Daisy Joe Du Bois, Beihan Wang
  • Patent number: 6984643
    Abstract: Compounds of Formula (I): wherein Ar1 is aryl; Ar2 is hydrogen, cycloalkyl, aryl or heteroaryl; Z is —C(?O) or a single bond; R1, R2, R3, R4 and R5 are independently hydrogen or alkyl optionally substituted with hydroxy; alk is an alkylene chain of one to six carbon atoms; X is —O—, —NRh (where Rh is hydrogen or alkyl), (CR6R7)m(where R6 and R7 are independently in each occurrence hydrogen or alkyl and m is an integer from 0 to 3), or —S(O)n (wherein n is an integer from 0 to 2); or prodrugs thereof, and pharmaceutically acceptable salts thereof, are inhibitors of CCR3 useful for treating eosinophil induced diseases such as asthma.
    Type: Grant
    Filed: July 1, 2003
    Date of Patent: January 10, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: Daisy Joe Du Bois, Long Mao, Daniel Harry Rogers, John Patrick Williams
  • Patent number: 6977265
    Abstract: The invention provides compounds of Formula (I): wherein: R1-R5, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.
    Type: Grant
    Filed: November 29, 2002
    Date of Patent: December 20, 2005
    Assignee: Roche Palo Alto LLC
    Inventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
  • Patent number: 6965030
    Abstract: The present invention provides compounds of the Formula I: wherein R1 is alkyl, cycloalkyl, cycloalkylalkyl, or —CH2-alkenyl, X1 is O, NH, N(alkyl), S or —C(?O), Z is N or CH; and R2 and R3 are as defined herein, pharmaceutical compositions comprising same, and methods for their use.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: November 15, 2005
    Assignee: Roche Palo Alto LLC
    Inventors: David Michael Goldstein, Julie Anne Lim
  • Patent number: 6951918
    Abstract: This invention relates to compounds of Formula (I) wherein R1-R7, A, Z and n are as described in the Summary of the Invention that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for their preparation.
    Type: Grant
    Filed: February 7, 2002
    Date of Patent: October 4, 2005
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Sharon Marie Dankwardt, Harold Edgar Van Wart, Keith Adrian Murray Walker
  • Patent number: 6949560
    Abstract: The present invention discloses compounds corresponding to formula I: wherein A, Z, Z1, Y, R1 and R2 are as defined in the specification, as well as pharmaceutical formulations, methods of making and uses thereof.
    Type: Grant
    Filed: April 3, 2003
    Date of Patent: September 27, 2005
    Assignee: Roche Palo Alto LLC
    Inventors: David Michael Goldstein, Ronald Charles Hawley, Alfred Sui-Ting Lui, Eric Brian Sjogren