Provided is a method for producing an optically active substance, the method including an asymmetric induction, wherein an asymmetry inducer is allowed to act on a chiral molecule having a half-life of enantiomeric excess of shorter than 10 hours, thereby increasing abundance of one enantiomer of the chiral molecule. According to this method, one enantiomer of a chiral molecule that is susceptible to racemization can be selectively and efficiently obtained.

The present invention generally relates to targeted nanoparticle delivery to E-selectin- or P-selectin-positive cells or tissues. In particular, this invention discloses a method for preparing quinic acid-modified nanoparticles for targeted drug delivery to cancerous cells or tissues via E-selectin- or P-selectin-mediated transcytosis. The invention described herein also pertains to pharmaceutical compositions and methods for treating cancers.

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound KIN or composition described herein. (Formula (I))

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(III) or Compounds (1)-(65) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(III) or Compounds (1)-(65) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.

Compounds of structural Formula I were developed for the treatment of infections by filoviruses including Ebolavirus and Marburgvirus, wherein, R.sup.1, R.sup.2, R.sup.3, X and Y are defined in the specification.

##STR00001##

Compositions capable of promoting mitofusin activation may include a mitofusin activator having a structure represented by

##STR00001##

any stereoisomer thereof, or any pharmaceutically acceptable salt thereof. G is N or CH, and A is an optionally substituted 5- or 6-membered cycloalkyl or heterocycloalkyl ring. X is (CH.sub.2).sub.3,OCH.sub.2CH.sub.2, CH.sub.2OCH.sub.2, CH.sub.2CH.sub.2O, Cyc, CH.sub.2Cyc, NR.sup.1 (CH.sub.2).sub.3,NR.sup.1OCH.sub.2CH.sub.2, NR.sup.1CH.sub.2OCH.sub.2, NR.sup.1CH.sub.2CH.sub.2O, or NR.sup.1Y, R.sup.1 is H or C.sub.1-C.sub.6 alkyl, and Cyc is 1,2-cyclopropyl, 1,2-cyclobutyl, 1,3-cyclobutyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 1,2-cyclohexyl, 1,3-cyclohexyl, or 1,4-cyclohexyl. Z is (CH.sub.2).sub.n or (CH.sub.2).sub.n.sub.1 O(CH.sub.2).sub.n.sub.2. R.sup.2 is an optionally substituted aryl or heteroaryl group. Variable n is an integer ranging from 1 to 5, variable n.sub.1 is an integer ranging from 0 to 4, variable n.sub.2 is an integer ranging from 0 to 4, and n.sub.1+n.sub.2=n1.

Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: (I) wherein Ring A, Ring B, Ring C, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, L, m, n, and p are as defined herein. The compounds are modulators of G-protein coupled receptor 88 (GPR88). Also disclosed are pharmaceutical compositions comprising the compounds; and the compounds for use in the treatment of diseases mediated by GPR88, including Tourette's Syndrome, Huntington's Disease (HD), Addiction, Parkinson's Disease (PD), Schizophrenia, Alzheimer's disease, and Attention Deficit Hyperactivity Disorder (ADHD).

##STR00001##

Compounds of formula (1):

##STR00001##

wherein R.sub.1 represents a C(R.sub.2)(R.sub.3)[C(R.sub.4)(R.sub.5)].sub.m-L-R.sub.6 group or R.sub.7; and the preparation and the therapeutic uses of the compounds of formula (1) as agonists of TRPM8 receptors, useful especially in the treatment of oropharyngeal dysphagia.

Compounds of formula (1):

##STR00001##

wherein R.sub.1 represents a C(R.sub.2)(R.sub.3)[C(R.sub.4)(R.sub.5)].sub.m-L-R.sub.6 group or R.sub.7; and the preparation and the therapeutic uses of the compounds of formula (1) as agonists of TRPM8 receptors, useful especially in the treatment of oropharyngeal dysphagia.