Patent classifications
C07C205/57
Indole derivatives and their use as protein kinase inhibitors
The present invention relates inter alia to a compound of formula (I) wherein R.sub.1, R.sub.2 and R.sub.3, are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.
PHARMACEUTICAL COMPOSITIONS COMPRISING MONOTERPENES
The present invention provides a process for purifying a monoterpene or sesquiterpene having a purity greater than about 98.5% (w/w). The process comprises the steps of derivatizing the monoterpene (or sesquiterpene) to produce a monoterpene (or sesquiterpene) derivative, separating the monoterpene (or sesquiterpene) derivative, and releasing the monoterpene (or sesquiterpene) from the derivative. Also encompassed by the scope of the present invention is a pharmaceutical composition comprising a monoterpene (or sesquiterpene) having a purity greater than about 98.5% (w/w). The purified monoterpene can be used to treat a disease such as cancer. The present monoterpene (or sesquiterpene) may be administered alone, or may be co-administered with radiation or other therapeutic agents, such as chemotherapeutic agents.
PHARMACEUTICAL COMPOSITIONS COMPRISING MONOTERPENES
The present invention provides a process for purifying a monoterpene or sesquiterpene having a purity greater than about 98.5% (w/w). The process comprises the steps of derivatizing the monoterpene (or sesquiterpene) to produce a monoterpene (or sesquiterpene) derivative, separating the monoterpene (or sesquiterpene) derivative, and releasing the monoterpene (or sesquiterpene) from the derivative. Also encompassed by the scope of the present invention is a pharmaceutical composition comprising a monoterpene (or sesquiterpene) having a purity greater than about 98.5% (w/w). The purified monoterpene can be used to treat a disease such as cancer. The present monoterpene (or sesquiterpene) may be administered alone, or may be co-administered with radiation or other therapeutic agents, such as chemotherapeutic agents.
Multiple-component solid phases containing at least one active pharmaceutical ingredient
The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to binary phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.
Multiple-component solid phases containing at least one active pharmaceutical ingredient
The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to binary phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.
METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG
The present invention provides processes for preparing a prostacyclin analogue of Formula I
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.10 is a linear or branched C.sub.1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG
The present invention provides processes for preparing a prostacyclin analogue of Formula I
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.10 is a linear or branched C.sub.1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
Onium Salt, Resist Composition, And Patterning Process
Provided is a novel onium salt used for a resist composition that has high sensitivity and excellent resolution, improved LWR and CDU, and that can inhibit collapse of a resist pattern for both of positive-type and negative-type resists in lithography: an onium salt represented by the following general formula (1),
##STR00001## wherein R.sup.ALU represents any one of a tertiary ether, tertiary carbonate, or acetal formed together with the adjacent oxygen atom and having a cyclic structure; R.sup.F represents any one of a fluorine atom, a fluorine-containing alkyl group having 1 to 6 carbon atoms, and a nitro group; R.sup.a represents a hydrocarbyl group having 1 to 20 carbon atoms; n1 represents an integer of 0 or 1; n2 and n3 represent an integer of 1 or 2; one of R.sup.F and one of OR.sup.ALU are bonded to carbon atoms adjacent to each other; n4 represents an integer of 0 to 3; and Z.sup.+ represents an onium cation.
Onium Salt, Resist Composition, And Patterning Process
Provided is a novel onium salt used for a resist composition that has high sensitivity and excellent resolution, improved LWR and CDU, and that can inhibit collapse of a resist pattern for both of positive-type and negative-type resists in lithography: an onium salt represented by the following general formula (1),
##STR00001## wherein R.sup.ALU represents any one of a tertiary ether, tertiary carbonate, or acetal formed together with the adjacent oxygen atom and having a cyclic structure; R.sup.F represents any one of a fluorine atom, a fluorine-containing alkyl group having 1 to 6 carbon atoms, and a nitro group; R.sup.a represents a hydrocarbyl group having 1 to 20 carbon atoms; n1 represents an integer of 0 or 1; n2 and n3 represent an integer of 1 or 2; one of R.sup.F and one of OR.sup.ALU are bonded to carbon atoms adjacent to each other; n4 represents an integer of 0 to 3; and Z.sup.+ represents an onium cation.
Process for the synthesis of non-racemic cyclohexenes
This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation M.sup.m+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R.sup.10a, R.sup.10b, R.sup.10c, R.sup.10d, R.sup.10a, R.sup.10b, R.sup.10c, R.sup.10d, Z and Z have the meanings as defined in the description.