Abstract: A compound having selective modulating activity at the alpha 2B and or alpha 2C adrenergic receptor subtypes is represented by the general Formula (1): wherein R1-R6 is independently selected from the group consisting of H, C1-6 alkyl, halogen, CH2OH, CH2N(R7)2) CH2CN, C(O)R8, CF3, and aryl; wherein R7 is H or C1-6 alkyl; and R8 is H, C1-6 alkyl or aryl. The compounds of Formula (1) can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.
Type:
Grant
Filed:
January 13, 2009
Date of Patent:
July 24, 2012
Assignee:
Allergan, Inc.
Inventors:
Santosh C. Sinha, Todd M. Heidelbaugh, Smita S. Bhat, Ken Chow
Abstract: The present invention provides compounds which are N-(1-phenyl-2-arylethyl)-4,5-dihydro-2H-pyrrol-5-amine compounds and are subtype selective modulators of alpha 2B or alpha 2B and alpha 2C adrenoreceptors and are selected from the group of compounds represented by the formula
Type:
Grant
Filed:
December 7, 2009
Date of Patent:
May 22, 2012
Assignee:
Allergan, Inc.
Inventors:
Ken Chow, Janet A. Takeuchi, Ling Li, Todd M. Heidelbaugh, Phong X. Nguyen, Evelyn G. Corpuz, Wenkui K Fang, Santosh C. Sinha, Michael E. Garst
Abstract: Described herein are compounds useful as antagonists of sphingosine-1-phosphate receptors. Further described herein is the use of these compounds and related pharmaceutical compositions to treat disorders associated with sphingosine-1-phosphate-3 (S1P3) receptor modulation.
Type:
Grant
Filed:
August 9, 2010
Date of Patent:
May 1, 2012
Assignee:
Allergan, Inc.
Inventors:
Phong X. Nguyen, Todd M. Heidelbaugh, Ken Chow, Michael E. Garst
Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
January 3, 2011
Date of Patent:
March 27, 2012
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Haiqing Yuan, John E. Donello
Abstract: Disclosed herein is a compound of the formula (I): (I). Therapeutic methods, compositions and medicaments related thereto are also disclosed.
Type:
Grant
Filed:
January 4, 2008
Date of Patent:
February 21, 2012
Assignee:
Allergan, Inc.
Inventors:
Todd M. Heidelbaugh, Phong X. Nguyen, Ken Chow, Michael E. Garst
Abstract: The present invention provides novel compounds having the following general formula I wherein: A, B, X, Y, R1, R2, R3, R4, n, o and p are as defined in the specification. Such compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions or diseases and wound healing.
Type:
Grant
Filed:
March 23, 2007
Date of Patent:
January 17, 2012
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, John E. Donello, Haiqing Yuan, Vidyasagar Vuligonda, Tien T. Duong
Abstract: Described herein are compounds that can be useful as bioactive agents. More specifically, the compounds described herein can be useful as both ?2B and ?2C adrenergic agonists. Methods of synthesis and administration of the compounds are also disclosed.
Type:
Grant
Filed:
May 1, 2009
Date of Patent:
December 20, 2011
Assignee:
Allergan, Inc.
Inventors:
Janet A. Takeuchi, Ken Chow, Ling Li, Liming Wang
Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.
Type:
Grant
Filed:
June 5, 2009
Date of Patent:
December 6, 2011
Assignee:
Allergan, Inc.
Inventors:
Wenkui K. Fang, Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Michael E. Garst, Santosh C. Sinha, Daniel W. Gil, John E. Donello
Abstract: The present invention provides an ?-2A/?-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof. The present invention further provides a pharmaceutical composition that contains a pharmaceutical carrier and a therapeutically effective amount of an ?-2A/?-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof.
Type:
Grant
Filed:
September 9, 2010
Date of Patent:
September 20, 2011
Assignee:
Allergan, Inc.
Inventors:
Ken Chow, Todd M. Heidelbaugh, John E. Donello, Daniel W. Gill
Abstract: The present invention provides compounds are disclosed herein having the formula: Wherein n is 1 or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl; R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, —O—(C1-6 alkyl), —NH—(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O—(C1-6 alkyl), aryl, heteroaryl, —C(?O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X?O, NH, —C(?O)— or —N?CH—; and Each L is independently alkylene and carbonyl. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
Abstract: The present invention provides R, R1, R2, R3, X, c, d, e, f, g, x, y, a, b, z and n are defined in the specification. These compounds are useful in lowering IOP and/or treating glaucoma or providing neuroprotection to the eye of a human patient.
Abstract: A compound having selective modulating activity at the alpha 2B and/or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1: wherein n=1-4; X is C or N; R1-R6 can be the same or different and are independently selected from the group consisting of H, C1-6 alkyl, OCH3, OH, F, Cl, Br, CH2OH, CH2N(R7)2, C(O)R8, CH2CN, CF3; wherein R7 is H or C1-6 alkyl; and R8 is C1-6 alkyl or aryl. The compounds of Formula 1 can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.
Type:
Grant
Filed:
January 9, 2008
Date of Patent:
March 8, 2011
Assignee:
Allergan, Inc.
Inventors:
Santosh C. Sinha, Todd M. Heidelbaugh, Smita S. Bhat, Ken Chow, Michael E. Garst
Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
September 18, 2008
Date of Patent:
February 15, 2011
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Haiqing Yuan, John E. Donello
Abstract: Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
Type:
Grant
Filed:
March 28, 2008
Date of Patent:
February 8, 2011
Assignee:
Allergan, Inc.
Inventors:
Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
Abstract: A compound comprising or a pharmaceutically acceptable salt thereof, or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.