The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

This disclosure concerns compounds and a method for modulating the activity of calcium ion channels, including Ca.sup.2+-induced (or Ca.sup.2+-activated) calcium release channels and conformationally coupled calcium release channels such as ryanodine receptors. Some of the compounds have a structure according to formula I, or a stereoisomer, tautomer, hydrate, solvate, prodrug, or pharmaceutically acceptable salt thereof. ##STR00001##

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, ##STR00001##
wherein A is a radical selected from the group consisting of A-1 through A-11, L is —C(R.sup.12a)R.sup.12b—C(R.sup.13a)R.sup.13b—; or 1,2-phenylene G is a radical selected from the group consisting of ##STR00002##
and R.sup.1, R.sup.2, R.sup.12a, R.sup.12b, R.sup.13a, R.sup.13b and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, ##STR00001##
wherein A is a radical selected from the group consisting of A-1 through A-11, L is —C(R.sup.12a)R.sup.12b—C(R.sup.13a)R.sup.13b—; or 1,2-phenylene G is a radical selected from the group consisting of ##STR00002##
and R.sup.1, R.sup.2, R.sup.12a, R.sup.12b, R.sup.13a, R.sup.13b and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Compounds of formula (I) or (II) can modulate the activity of S1P receptors.

Compounds of formula (I) or (II) can modulate the activity of S1P receptors.

The present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidin-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolin-2-yl]benzonitrile of formula (1); a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases. ##STR00001##

The present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidin-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolin-2-yl]benzonitrile of formula (1); a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases. ##STR00001##

The present invention also relates to process for the preparation of N-(4-(6,7-dimethoxy quinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (S)-malate compound of formula-1a and its polymorphs thereof, represented by the following structural:

##STR00001##