Chen Chen

US Patent:

6346534, Feb 12, 2002

Filed:

May 12, 2000

Appl. No.:

09/570239

Inventors:

Yun-Fei Zhu - San Diego CA
Keith M. Wilcoxen - San Diego CA
R. Scott Struthers - Encinitas CA
Chen Chen - San Diego CA
Yinghong Gao - San Diego CA
Fabio C. Tucci - San Diego CA

Assignee:

Neurocrine Biosciences, Inc. - San Diego CA

International Classification:

A01N 4354

US Classification:

514258, 544281, 544282

Abstract:

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein Ar, B, R , R , R , R , R , R , R and m are as defined herein.

US Patent:

6469166, Oct 22, 2002

Filed:

Jun 29, 2001

Appl. No.:

09/896250

Inventors:

Thomas R. Webb - Olivenhain CA
Chen Chen - San Diego CA
James R. McCarthy - Solana Beach CA
Terence J. Moran - San Diego CA

Assignee:

Neurocrine Biosciences, Inc. - San Diego CA
Janssen Pharmaceutica N.V. - Beerse

International Classification:

C07D49504

US Classification:

544278

Abstract:

This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO ; R is NR R or OR ; R is C alkyl, C alkyloxy or C alkylthio; R is hydrogen, C alkyl, C alkylsulfonyl, C alkylsulfoxy or C alkylthio; R is hydrogen, C alkyl, mono- or di(C cycloalkyl)methyl, C cycloalkyl, C alkenyl, hydroxyC alkyl, C alkylcarbonyloxyC alkyl or C alkyloxyC alkyl; R is C alkyl, mono- or di(C cycloalkyl)methyl, Ar CH , C alkyloxy-C alkyl, hydroxyC alkyl, C alkenyl, thienylmethyl, furanylmethyl, C alkylthioC alkyl, morpholinyl, mono- or di(C alkyl)aminoC alkyl, di(C alkyl)amino, C alkylcarbonylC alkyl, C alkyl substituted with imidazolyl; or a radical of formula -Alk-OâCO-Ar ; or R and R taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

US Patent:

6482836, Nov 19, 2002

Filed:

Oct 19, 1999

Appl. No.:

09/403393

Inventors:

Charles Huang - San Diego CA 92129
Keith M. Wilcoxen - San Diego CA 92103
Chen Chen - San Diego CA 92129
Mustapha Haddach - San Diego CA 92108
James R. McCarthy - San Diego CA 92075

International Classification:

A61K 314706

US Classification:

514313, 514314, 514311, 546159, 546152, 546176

Abstract:

This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R is C alkyl, NR R , OR or SR ; R is hydrogen, C alkyl, C alkyloxy or C alkylthio; R is Ar or Het ; R and R are each independently selected from hydrogen, halo, C alkyl, C alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C alkyl)amino; R is hydrogen, C alkyl, C alkylsulfonyl, C alkylsulfoxy or C alkylthio; R is hydrogen, C alkyl, mono- or di(C cycloalkyl)methyl, C cycloalkyl, C alkenyl, hydroxyC alkyl, C alkylcarbonyloxy-C alkyl or C alkyloxyC alkyl; R is C alkyl, mono- or di(C cycloalkyl)-methyl, Ar CH , C alkyloxyC alkyl, hydroxyC alkyl, C alkenyl, thienylmethyl, furanylmethyl, C alkylthioC alkyl, mono- or di(C alkyl)aminoC alkyl, di(C alkyl)amino, C alkylcarbonylC alkyl; or R and R taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C alkyl or C alkyloxyC alkyl; and Ar and Ar are each optionally substituted phenyl; and Het is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

US Patent:

6537998, Mar 25, 2003

Filed:

Oct 16, 2000

Appl. No.:

09/688774

Inventors:

Yun-Fei Zhu - San Diego CA
Timothy D. Gross - San Diego CA
Yinghong Gao - San Diego CA
Zhiqiang Guo - San Diego CA
Chen Chen - San Diego CA

Assignee:

Neurocrine Biosciences, Inc. - San Diego CA

International Classification:

C07D48704

US Classification:

5142595, 544263, 544281, 544282

Abstract:

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein Ar, A, B, Q, R , R , R , R , R , R and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

US Patent:

6608197, Aug 19, 2003

Filed:

Jan 25, 2001

Appl. No.:

09/771107

Inventors:

Yun-Fei Zhu - San Diego CA
Chen Chen - San Diego CA
Fabio C. Tucci - San Diego CA
Zhiqiang Guo - San Diego CA
Timothy D. Gross - San Diego CA
Martin Rowbottom - La Jolla CA
R. Scott Struthers - Encinitas CA

Assignee:

Neurocrine Biosciences, Inc. - San Diego CA

International Classification:

C07D23947

US Classification:

544309, 544310, 544311, 544314, 514269

Abstract:

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R , R , R , R , R , R , R and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

US Patent:

6610678, Aug 26, 2003

Filed:

Oct 8, 2002

Appl. No.:

10/266662

Inventors:

Charles Huang - San Diego CA 92129
Keith M. Wilcoxen - San Diego CA 92103
Chen Chen - San Diego CA 92129
Mustapha Haddach - San Diego CA 92108
James R. McCarthy - San Diego CA 92075

International Classification:

A61K 3133

US Classification:

514183, 51421201, 5142312, 51426621, 51426623, 51426631, 5142664, 514315, 540484, 540596, 544106, 544283, 544293, 544298, 544319, 544326, 546184, 546205, 548400, 548518

Abstract:

This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R is C alkyl, NR R , OR or SR ; R is hydrogen, C alkyl, C alkyloxy or C alkylthio; R is Ar or Het ; R and R are each independently selected from hydrogen, halo, C alkyl, C alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C alkyl)amino; R is hydrogen, C alkyl, C alkylsulfonyl, C alkylsulfoxy or C alkylthio; R is hydrogen, C alkyl, mono- or di(C cyclo-alkyl)methyl, C cycloalkyl, C alkenyl, hydroxyC alkyl, C alkylcarbonyloxy-C alkyl or C alkyloxyC alkyl; R is C alkyl, mono- or di(C cycloalkyl)-methyl, Ar CH , C alkyloxyC alkyl, hydroxyC alkyl, C alkenyl, thienylmethyl, furanylmethyl, C alkylthioC alkyl, mono- or di(C alkyl)aminoC alkyl, di(C alkyl)amino, C alkylcarbonylC alkyl; or R and R taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C alkyl or C alkyloxyC alkyl; and Ar and Ar are each optionally substituted phenyl; and Het is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

US Patent:

6613777, Sep 2, 2003

Filed:

Feb 20, 2001

Appl. No.:

09/623634

Inventors:

Chen Chen - San Diego CA 92129
Keith M. Wilcoxen - San Diego CA 92103
Charles Q. Huang - San Diego CA 92129
James R. McCarthy - Solana Beach CA 92075

International Classification:

A61K 3144

US Classification:

514303, 546119

Abstract:

This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R is C alkyl, NR R , OR or SR ; R is C alkyl, C alkyloxy, or C alkylthio; R is Ar or Het ; R is hydrogen or C alkyl; R is hydrogen, C alkyl, mono- or di(C cycloalkyl)methyl, C cycloalkyl, C alkenyl, hydroxyC alkyl, C alkylcarbonyloxyC alkyl, mono- or di(C alkyl)amino-C alkyl or C alkyloxyC alkyl; R is C alkyl, mono- or di(C cycloalkyl)methyl, Ar C alkyl, Ar oxyC alkyl, C alkyloxyC alkyl, hydroxyC alkyl, C alkenyl, thienylmethyl, furanylmethyl, tetrahydrofuranylmethyl, C alkylthioC alkyl, mono- or di(C alkyl)aminoC alkyl, di(C alkyl)amino, or C alkylcarbonylC alkyl; or R and R taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl, morpholinyl, or thiomorpholinyl group, optionally substituted with 1 or 2 substituents each independently selected from C alkyl or C alkyloxyC alkyl; and and Ar and Ar are each optionally substituted phenyl; and Het is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

US Patent:

6664261, Dec 16, 2003

Filed:

Mar 2, 1999

Appl. No.:

09/117717

Inventors:

Chen Chen - San Diego CA
Thomas R. Webb - Olivenhain CA
James R. McCarthy - Solana Beach CA
Terence J. Moran - San Diego CA
Keith M. Wilcoxen - Groton Long Point CA
Charles Huang - San Diego CA

Assignee:

Neurocrine Biosciences, Inc. - San Diego CA

International Classification:

A61K 31505

US Classification:

514258, 544250, 544281

Abstract:

This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R is NR R or OR ; R is C alkyl, C alkyloxy or C alkylthio; R is hydrogen, C alkyl, C alkylsulfonyl, C alkylsulfoxy or C alkylthio; R is hydrogen, C alkyl, mono- or di(C cycloalkyl)methyl, C cycloalkyl, C alkenyl, hydroxyC alkyl, C alkylcarbonyloxyC alkyl or C alkyloxyC alkyl; R is C alkyl, mono- or di(C cycloalkyl)methyl, Ar CH , C alkyloxyC alkyl, hydroxyC alkyl, C alkenyl, thienylmethyl, furanylmethyl, C alkylthioC alkyl, morpholinyl, mono- or di(C alkyl)aminoC alkyl, di(C alkyl)amino, C alkylcarbonylC alkyl, C alkyl substituted with imidazolyl; or a radical of formula âAlkâOâCOâAr ; or R and R taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).