Samuel John Gillett

US Patent:

6355806, Mar 12, 2002

Filed:

Sep 16, 1999

Appl. No.:

09/398613

Inventors:

Alan T. Johnson - Rancho Santa Margarita CA
Min Teng - Aliso Viejo CA
Vidyasagar Vuligonda - Irvine CA
Richard L. Beard - Newport Beach CA
Samuel J. Gillett - Albany CA
Tien T. Duong - Irvine CA
Roshantha A. Chandraratna - Mission Viejo CA

Assignee:

Allergen Sales, Inc. - Irvine CA

International Classification:

C07D21170

US Classification:

546348, 548202, 548215, 5483335, 549 80, 549506, 544239, 544335, 544406

Abstract:

Compounds of the formula wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.

US Patent:

6469028, Oct 22, 2002

Filed:

Mar 28, 2001

Appl. No.:

09/821673

Inventors:

Elliott S. Klein - Marina del Rey CA
Alan T. Johnson - Rancho Santa Margarita CA
Andrew M. Standeven - Corona del Mar CA
Richard L. Beard - Newport Beach CA
Samuel J. Gillett - Albany CA
Tien T. Duong - Irvine CA
Sunil Nagpal - Lake Forest CA
Vidyasagar Vuligonda - Irvine CA
Min Teng - Aliso Viejo CA
Roshantha A. Chandraratna - Mission Viejo CA

Assignee:

Allergan, Inc. - Irvine CA

International Classification:

C07D21514

US Classification:

514311, 514314, 514432, 514456, 546167, 546168, 549 23, 549362

Abstract:

Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

US Patent:

6521624, Feb 18, 2003

Filed:

Mar 23, 2000

Appl. No.:

09/535042

Inventors:

Elliott S. Klein - Marina del Ray CA
Alan T. Johnson - Rancho Santa Margarita CA
Andrew M. Standeven - Corona del Mar CA
Richard L. Beard - Newport Beach CA
Samuel J. Gillett - Albany CA
Tien T. Duong - Irvine CA
Sunil Nagpal - Lake Forest CA
Vidyasagar Vuligonda - Irvine CA
Min Teng - Aliso Viejo CA
Roshantha A. Chandraratna - Mission Viejo CA

Assignee:

Allergan, Inc. - Irvine CA

International Classification:

A61K 31495

US Classification:

514253, 514311, 514432, 514453

Abstract:

Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

US Patent:

56590423, Aug 19, 1997

Filed:

Oct 25, 1994

Appl. No.:

8/329023

Inventors:

Samuel J. Gillett - Albany CA
Michael E. Garst - Newport Beach CA
Alan T. Johnson - Rancho Santa Margarita CA

Assignee:

Allergan - Waco TX

International Classification:

C07D21330

US Classification:

546318

Abstract:

The present invention provides a method of preparation of ethyl 6-halonicotinate, wherein said halo is chloro or iodo, which comprises reacting the 6-halonicotinic acid with triethyl orthoacetate, to yield the ethyl-6-halonicotinate.

US Patent:

60082046, Dec 28, 1999

Filed:

Dec 30, 1998

Appl. No.:

9/222983

Inventors:

Elliott S. Klein - Marina del Rey CA
Alan T. Johnson - Rancho Santa Margarita CA
Andrew M. Standeven - Corona del Mar CA
Richard L. Beard - Newport Beach CA
Samuel J. Gillett - Albany CA
Tien T. Duong - Irvine CA
Sunil Nagpal - Lake Forest CA
Vidyasagar Vuligonda - Irvine CA
Min Teng - Aliso Viejo CA
Roshantha A. Chandraratna - Mission Viejo CA

Assignee:

Allergan Sales, Inc. - Irvine CA

International Classification:

C07C 6306
C07C 6538
C07F 704
A61K 3119

US Classification:

514 63

Abstract:

Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

US Patent:

59984716, Dec 7, 1999

Filed:

Aug 11, 1998

Appl. No.:

9/132435

Inventors:

Alan T. Johnson - Rancho Santa Margarita CA
Min Teng - Aliso Viejo CA
Vidyasagar Vuligonda - Irvine CA
Richard L. Beard - Newport Beach CA
Samuel J. Gillett - Albany CA
Tien T. Duong - Irvine CA
Roshantha A. Chandraratna - Mission Viejo CA

Assignee:

Allergan Sales, Inc. - Irvine CA

International Classification:

A61K 3121

US Classification:

514510

Abstract:

Compounds of the formula ##STR1## the symbols have the meaning described in the specification.

US Patent:

58772073, Mar 2, 1999

Filed:

Jun 24, 1997

Appl. No.:

8/880823

Inventors:

Elliott S. Klein - Marina del Rey CA
Alan T. Johnson - Rancho Santa Margarita CA
Andrew M. Standeven - Corona del Mar CA
Richard L. Beard - Newport Beach CA
Samuel J. Gillett - Oakland CA
Tien T. Duong - Irvine CA
Sunil Nagpal - Irvine CA
Vidyasagar Vuligonda - Irvine CA
Min Teng - Aliso Viejo CA
Roshantha A. Chandraratna - Mission Viejo CA

Assignee:

Allergan Sales, Inc. - Irvine CA

International Classification:

A61K 3135
C07D31104

US Classification:

514456

Abstract:

Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

US Patent:

59589540, Sep 28, 1999

Filed:

Dec 24, 1997

Appl. No.:

8/998319

Inventors:

Elliott S. Klein - Marina del Rey CA
Alan T. Johnson - Rancho Santa Margarita CA
Andrew M. Standeven - Ventura CA
Richard L. Beard - Newport Beach CA
Samuel J. Gillett - Albany CA
Tien T. Duong - Irvine CA
Sunil Nagpal - Lake Forest CA
Vidyasagar Vuligonda - Irvine CA
Min Teng - San Diego CA
Roshantha A. Chandraratna - Mission Viejo CA

Assignee:

Allergan Sales, Inc. - Irvine CA

International Classification:

C07D31158
C07D33506
C07D40506
A61K 3135

US Classification:

514333

Abstract:

2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula ##STR1## where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.