Patent classifications
C07C271/06
Chemical derivatives and methods for synthesizing and compounding chemical derivatives related to capsaicin palmitate and capsaicin prodrugs
Capsaicin compositions and methods for enhancing hydrophobicity of a molecule useful for pharmaceutical applications, including: (1) a prodrug using a linker such as a carbamate between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (2) a prodrug using a linker such as an unsaturated carboxylic ester between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (3) esters of long-chain fatty acids and capsaicin where hydroxyl groups provide handles for attachment of additional capsaicin molecules; and (4) the use of carboxylic acid diesters to increase overall hydrophobicity of two or more covalently-linked capsaicin molecules. Formulations of palmitated esters of capsaicin are also described, which are designed to enhance hydrophobicity of a molecule useful for pharmaceutical applications, for example to provide compounded mixtures designed to optimize analgesic efficacy.
PROCESSES FOR THE PREPARATION OF FURAZANOBENZIMIDAZOLES AND CRYSTALLINE FORMS THEREOF
The present invention provides processes for preparing a compound of formula (I) and pharmaceutically acceptable salts thereof, comprising deprotecting a compound of formula (II), wherein each R.sup.3 independently represents a tertiary alkyl group, preferably wherein each R.sup.3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula (I) and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula (I) and their use in the treatment of proliferative disorders.
##STR00001##
PROCESSES FOR THE PREPARATION OF FURAZANOBENZIMIDAZOLES AND CRYSTALLINE FORMS THEREOF
The present invention provides processes for preparing a compound of formula (I) and pharmaceutically acceptable salts thereof, comprising deprotecting a compound of formula (II), wherein each R.sup.3 independently represents a tertiary alkyl group, preferably wherein each R.sup.3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula (I) and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula (I) and their use in the treatment of proliferative disorders.
##STR00001##
CHEMICAL DERIVATIVES AND METHODS FOR SYNTHESIZING AND COMPOUNDING CHEMICAL DERIVATIVES RELATED TO CAPSAICIN PALMITATE AND CAPSAICIN PRODRUGS
Capsaicin compositions and methods for enhancing hydrophobicity of a molecule useful for pharmaceutical applications, including: (1) a prodrug using a linker such as a carbamate between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (2) a prodrug using a linker such as an unsaturated carboxylic ester between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (3) esters of long-chain fatty acids and capsaicin where hydroxyl groups provide handles for attachment of additional capsaicin molecules; and (4) the use of carboxylic acid diesters to increase overall hydrophobicity of two or more covalently-linked capsaicin molecules. Formulations of palmitated esters of capsaicin are also described, which are designed to enhance hydrophobicity of a molecule useful for pharmaceutical applications, for example to provide compounded mixtures designed to optimize analgesic efficacy.
CHEMICAL DERIVATIVES AND METHODS FOR SYNTHESIZING AND COMPOUNDING CHEMICAL DERIVATIVES RELATED TO CAPSAICIN PALMITATE AND CAPSAICIN PRODRUGS
Capsaicin compositions and methods for enhancing hydrophobicity of a molecule useful for pharmaceutical applications, including: (1) a prodrug using a linker such as a carbamate between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (2) a prodrug using a linker such as an unsaturated carboxylic ester between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (3) esters of long-chain fatty acids and capsaicin where hydroxyl groups provide handles for attachment of additional capsaicin molecules; and (4) the use of carboxylic acid diesters to increase overall hydrophobicity of two or more covalently-linked capsaicin molecules. Formulations of palmitated esters of capsaicin are also described, which are designed to enhance hydrophobicity of a molecule useful for pharmaceutical applications, for example to provide compounded mixtures designed to optimize analgesic efficacy.
Amino acid carbamate complexes
Disclosed herein are amino acid carbamate complexes, methods of synthesis thereof, oral care compositions comprising the same, and methods of making and using thereof.
Amino acid carbamate complexes
Disclosed herein are amino acid carbamate complexes, methods of synthesis thereof, oral care compositions comprising the same, and methods of making and using thereof.
Amino acid carbamate complexes
Disclosed herein are amino acid carbamate complexes, methods of synthesis thereof, oral care compositions comprising the same, and methods of making and using thereof.
THIOL-ENE PRINTABLE RESINS FOR INKJET 3D PRINTING
A composition suitable for 3-D printing comprises, in one embodiment, a photopolymer including one or more thiol monomer, one or more alkene monomer, and a polymerization initiator. In another embodiment, the thiol monomer is selected from the group consisting of: glycol di(3-mercaptopropionate) [GDMP]; trimethylolpropane tris(3-mercaptopropionate) [TMPMP]; pentaerythritol tetrakis(3-mercaptopropionate) [PETMP] and 3,6-dioxa-1,8-octanedithiol [DODT]. In yet another embodiment, the alkene monomer comprises: an allyl-functional urethane/urea monomer synthesized from: an isocyanate moiety and a hydroxyl or amine functional allyl moiety. In still another embodiment, the hydroxyl or amine functional allyl moiety comprises 2-allyloxyethanol, allyl alcohol, and allylamine. In still yet another embodiment, the isocyanate moiety is selected from the group consisting of: isophorone diisocyanate (IDI), hexamethylene diisocyanate (HDI), trimethylhexamethylene diisocyanate (TMHDI), 1,3-bis(isocyanatomethyl)cyclohexane, and dicyclohexylmethane 4,4-Diisocyanate (HMDI).
Carbamate ester compound and acrylic rubber composition containing the same
A carbamate ester compound represented by the general formula:
ZOCONH(CH.sub.2).sub.nNHCOOZ[I]
wherein Z is [i], [ii], or [iii] below, and n is an integer of 2 to 10, ##STR00001## (wherein R.sup.1 and R.sup.2 are each independently a lower alkyl group having 1 to 5 carbon atoms, R.sup.3 is a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms, and a is 1 or 2). The carbamate ester compound is used as a vulcanizing agent for carboxyl group-containing acrylic rubber and improves the delay of the vulcanization rate by scorch suppression.