Abstract: Prodrugs of proton pump inhibitors of Formulas 1 through 4, where the symbols are as defined in the specification, and the R group includes at least one acidic group or its pharmaceutically acceptable salt, have improved aqueous solubility and bioavailability.
Type:
Grant
Filed:
July 15, 2003
Date of Patent:
May 24, 2005
Assignees:
Winston Pharmaceuticals, Inc., The United States of America as represented by the Department of Veteran Affairs, The Reagents of the University of California
Inventors:
Michael Garst, George Sachs, Jai M. Shin
Abstract: A clear aqueous formulation for topical application in the oral cavity of humans to treat leukoplakia contains water, ?-carotene, a water miscible polyol, an unsaturated fatty acid ester, and a surfactant, preferably polyethoxylated castor oil or POE(20) sorbitan monooleate. The formulation preferably also contains a pharmaceutically acceptable anti-oxidant, preferably d-alpha-tocopherol (vitamin E), and is in the form of an oral rinse or as a gel well suited for spreading on gums or other parts of the oral cavity. The formulation is applied in a gel form on a substantially regular daily basis to areas in the oral cavity where leukoplakia lesions are present. Persistent application of the gel results in substantial diminution or total elimination of the leukoplakia lesions.
Type:
Grant
Filed:
January 21, 2003
Date of Patent:
May 10, 2005
Assignee:
Micelle Products, Inc.
Inventors:
Wenjie Li, Edward Alosio, David a. Rutolo, Jr., Brincini Faith Dema-Ala
Abstract: Compounds of the formula where the variations have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of transiently increasing triglyceride levels and reducing serum thyroxine levels.
Type:
Grant
Filed:
October 29, 2003
Date of Patent:
May 3, 2005
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Tien T. Duong, Janet A. Takeuchi, Ling Li, Kwok Yin Tsang, Xiaoxia Liu, Jayasree Vasudevan, Liming Wang, Santosh C. Sinha, Haiqing Yuan, Roshantha A. Chandraratna
Abstract: Compounds of the formula where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effect of reducing serum thyroxine levels.
Type:
Grant
Filed:
April 3, 2003
Date of Patent:
April 26, 2005
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Haiqing Yuan, Roshantha A. Chandratratna
Abstract: 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.
Type:
Grant
Filed:
August 5, 2002
Date of Patent:
March 8, 2005
Assignee:
Allergan, Inc.
Inventors:
Kah-Hiing John Ling, Wu Yang, Jinsong Ni, Haiqing Yuan, Diane D. S. Tang-Liu
Abstract: A method of identifying a compound which is an inhibitor of the enzyme cytochrome P450RAI is performed by selecting a compound that has retinoid activity in an art recognized assay and includes a benzoic acid, benzoic acid ester, naphthoic acid ester or heteroaryl carboxylic acid or ester moiety, with a partial structure of —A(R2)—(CH2)n—COOR8 where n is 0 and the remaining variables are as described in the specification and claims. Thereafter, a compound having the cytochrome P450RAI inhibitory activity is identified and selected where the compound has the —A(R2)—(CH2)2—COOR8 partial structure wherein the variable n is 1 or 2.
Type:
Grant
Filed:
August 5, 2002
Date of Patent:
February 15, 2005
Assignee:
Allergan, Inc.
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
Type:
Grant
Filed:
October 11, 2002
Date of Patent:
February 15, 2005
Assignee:
Allergan, Inc.
Inventors:
Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
Abstract: Compounds of the formula
where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
Type:
Grant
Filed:
December 9, 2003
Date of Patent:
November 16, 2004
Assignee:
Allergan, Inc.
Inventors:
Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
Abstract: A clear aqueous formulation for topical application in the oral cavity of humans to treat leukoplakia contains water, &bgr;-carotene, a water miscible polyol, an unsaturated fatty acid ester, and a surfactant, preferably polyethoxylated castor oil. The formulation preferably also contains a pharmaceutically acceptable anti-oxidant, preferably d-alpha-tocopherol (vitamin E), and is in the form of an oral rinse or as a gel well suited for spreading on gums or other parts of the oral cavity. The formulation is applied in a gel form on a substantially regular daily basis to areas in the oral cavity where leukoplakia lesions are present. Persistent application of the gel results in substantial diminution or total elimination of the leukoplakia lesions.
Type:
Grant
Filed:
February 1, 2002
Date of Patent:
July 6, 2004
Assignee:
Micelle Products, Inc.
Inventors:
Wenjie Li, Edward Alosio, David A. Rutolo, Jr., Bricini Faith (Bim) Dema-Ala
Abstract: Compounds of the formula
where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effect of reducing serum thyroxine levels.
Type:
Grant
Filed:
February 4, 2003
Date of Patent:
July 6, 2004
Assignee:
Allergan, Inc.
Inventors:
Jayasree Vasudevan, Richard L. Beard, Haiqing Yuan, Roshantha A. Chandratratna
Abstract: Compounds of the formula
where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effect of reducing serum thyroxine levels.
Type:
Grant
Filed:
January 14, 2003
Date of Patent:
July 6, 2004
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Haiqing Yuan, Yang-Dar Yuan, Roshantha A. Chandraratna
Abstract: Novel food, dietary supplement and nutraceutical products containing phenol/protein complexes derived from vegetable sources have high antioxidant activity and very high levels of protein. The products provide novel means for administering high levels of plant antioxidants to human and mammals in the form of a protein concentrate. Due to their high antioxidant capacity these novel products are useful as aids in the prevention and treatment of many diseases.
Abstract: Compounds of Formula 1:
wherein the variables are defined in the specification have cytochrome P450RAI-1 and P450RAI-2 inhibitory activity, and are suitable for treatment of mammals with conditions which are treatable with retinoids, or which are controlled by or responsive to the organism's native retinoic acid. Formulations containing the compounds of the invention can also be co-administered with retinoids and/or Vitamin A to enhance or prolong the effects of medications containing retinoids, Vitamin A, or of the organism's native retinoic acid.
Abstract: Compounds of the formula
where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.
Type:
Grant
Filed:
June 3, 2003
Date of Patent:
May 11, 2004
Assignee:
Allergan, Inc.
Inventors:
Tien Duong, Richard L. Beard, Roshantha A. Chandraratna
Abstract: Compounds of the formula
where the variables have the meaning defined in the specification, are specific or selective agonists of RXR retinoid receptors.
Type:
Grant
Filed:
April 30, 2002
Date of Patent:
April 13, 2004
Assignee:
Allergan, Inc.
Inventors:
Jayasree Vasudevan, Dehua Huang, Vidyasagar Vuligonda, Roshanta S. Chandraratna
Abstract: Compounds of the formula
where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
Type:
Grant
Filed:
December 9, 2002
Date of Patent:
April 13, 2004
Assignee:
Allergan, Inc.
Inventors:
Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
Type:
Grant
Filed:
February 11, 2003
Date of Patent:
March 30, 2004
Assignee:
Allergan, Inc.
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
Abstract: Compounds of the formula
Y3(R4)—X—Y1(R1R2)—Z—Y2(R2)—A—B
where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.
Type:
Grant
Filed:
August 5, 2002
Date of Patent:
December 9, 2003
Assignee:
Allergan, Inc.
Inventors:
Tae K. Song, Min Teng, Roshantha A. Chandraratna
Abstract: A miniature or subminiature incandescent lamp designed to operate with an energy source of 20 volts or less includes a filament enclosed in a first glass envelope and supported by a pair of metal contact pins. A first glass bead seals the envelope and has a pair of openings through which the metal contact pins penetrate and wherein they are hermetically sealed. A second glass bead of low melting solder glass is larger than the first bead and is sealed below the first bead and extends circumferentially beyond the perimeter of the first bead. A third bead of high melting glass is disposed below the second bead also in sealing relationship with the second bead. The outside perimeter of the third bead is substantially co-extensive with that of the second bead. A second glass envelope is sealed to the outside perimeter of the second bead and is also in abutting relationship with the third bead. The interior of the first envelope is evacuated or contains an inert gas of the type normally used in incandescent lamps.
Type:
Grant
Filed:
May 5, 2000
Date of Patent:
December 9, 2003
Assignee:
Illumination Technology, Inc.
Inventors:
John B. Hartley, Muralidhar Theegala, Alexandrina Anghelus