Patent classifications
A61K31/665
SUSTAINED RELEASE INJECTABLE FORMULATION CONTAINING A POLY L LACTIC ACID FILLER AND A HYALURONIC ACID FILLER CONJUGATE AND A METHOD FOR PREPARING THE SAME
Disclosed are a sustained-release injection formulation containing a biodegradable polymer double microcapsule that contains a conjugate of poly-L-lactic acid (hereinafter referred to as “PLLA”) filler and hyaluronic acid (hereinafter referred to as “HA”) and is capable of controlling the release rate of PLLA, and a method of preparing the same.
SUSTAINED RELEASE INJECTABLE FORMULATION CONTAINING A POLY L LACTIC ACID FILLER AND A HYALURONIC ACID FILLER CONJUGATE AND A METHOD FOR PREPARING THE SAME
Disclosed are a sustained-release injection formulation containing a biodegradable polymer double microcapsule that contains a conjugate of poly-L-lactic acid (hereinafter referred to as “PLLA”) filler and hyaluronic acid (hereinafter referred to as “HA”) and is capable of controlling the release rate of PLLA, and a method of preparing the same.
Compositions and methods for mitigating aflatoxin B1-induced liver injury
A method for providing a therapy to a subject that has been exposed to an Aflatoxin B1 can include administering a compound having a structure of Formula 1 to the subject after exposure to the Aflatoxin B1: ##STR00001## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and/or R.sup.6 are each individually a chemical moiety and n is 1, 2, 3, 4, or 5. The compound can be Amprenavir or a derivative thereof, prodrug thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combination thereof. The prodrug can be Amprenavir phosphate.
Use of thyroid beta-agonists
Methods useful for treating X-linked adrenoleukodystrophy are provided.
Methods for the preparation of ribosides
- Steven Donald Axt ,
- Pavel Robertovich Badalov ,
- Katrien Brak ,
- Silvio Campagna ,
- Andrei Chtchemelinine ,
- Edward Doerffler ,
- Morin Mae Frick ,
- Detian Gao ,
- Lars V. Heumann ,
- Brittanie Hoang ,
- Willard Lew ,
- Robert Ronald MILBURN ,
- Sean Timothy Neville ,
- Bruce Ross ,
- Erik Rueden ,
- Robert William Scott ,
- Dustin Siegel ,
- Andrew C. Stevens ,
- Clarissa Tadeus ,
- Tiago Vieira ,
- Andrew W. Waltman ,
- Xianghong Wang ,
- Mark Charles Whitcomb ,
- Lydia Wolfe ,
- Chia-Yun Yu
Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl.sub.3-2LiCl, LaCl.sub.3, CeCl.sub.3, NdCl.sub.3, or YCl.sub.3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
Methods for the preparation of ribosides
- Steven Donald Axt ,
- Pavel Robertovich Badalov ,
- Katrien Brak ,
- Silvio Campagna ,
- Andrei Chtchemelinine ,
- Edward Doerffler ,
- Morin Mae Frick ,
- Detian Gao ,
- Lars V. Heumann ,
- Brittanie Hoang ,
- Willard Lew ,
- Robert Ronald MILBURN ,
- Sean Timothy Neville ,
- Bruce Ross ,
- Erik Rueden ,
- Robert William Scott ,
- Dustin Siegel ,
- Andrew C. Stevens ,
- Clarissa Tadeus ,
- Tiago Vieira ,
- Andrew W. Waltman ,
- Xianghong Wang ,
- Mark Charles Whitcomb ,
- Lydia Wolfe ,
- Chia-Yun Yu
Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl.sub.3-2LiCl, LaCl.sub.3, CeCl.sub.3, NdCl.sub.3, or YCl.sub.3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
SELECTIVE PHOSPHATASE INHIBITORS BASED ON ILLUDALIC ACID
The present disclosure provides novel selective phosphatase inhibitor compounds based on illudalic acid. The present disclosure provides a streamlined method of synthesizing illudalic acid and a method for synthesizing phosphatase inhibitor compounds. The method of this invention provides convergent benzannulation of β-keto amides and esters, followed by a one-pot reduction/hydrolysis sequence. The concise synthetic approach provided by this invention enables rapid assembly of illudalog compounds of this invention that are potent protein tyrosine phosphatase receptor-type D (PTPRD) inhibitors.
Methods of Identifying Novel Dosing Regimens
Methods for identification of new dosing strategies which optimize positive treatment outcomes and patient safety. Specifically, new dosing strategies for fosfomycin and pharmaceutically acceptable salt thereof which have improved treatment outcomes in mammals. For example, a method of treating mammals having a bacterial infection with fosfomycin or a pharmaceutically acceptable salt thereof using improved dosing regimens.
Methods of Identifying Novel Dosing Regimens
Methods for identification of new dosing strategies which optimize positive treatment outcomes and patient safety. Specifically, new dosing strategies for fosfomycin and pharmaceutically acceptable salt thereof which have improved treatment outcomes in mammals. For example, a method of treating mammals having a bacterial infection with fosfomycin or a pharmaceutically acceptable salt thereof using improved dosing regimens.
COMBINATION COMPRISING ZIDOVUDINE AND AN ANTIMICROBIAL COMPOUND
The invention provides a combination comprising zidovudine or a pharmaceutically acceptable derivative thereof and an antimicrobial compound selected from nitrofurantoin, mecillinam, fosfomycin, cephalexin and faropenem, or a pharmaceutically acceptable derivative or prodrug thereof. These combinations are particularly useful for the treatment of microbial infections.