C07C243/18

MARMELIN ANALOGS AND METHODS OF USE IN CANCER TREATMENT
20170144965 · 2017-05-25 ·

A pharmaceutical composition can include: a marmelin analog compound, and a pharmaceutically acceptable carrier having the compound. The compound can be present in a therapeutically effective amount to treat or inhibit a disease state. The disease state can be cancer. The cancer can be selected from brain cancers, head and neck cancers, thyroid cancers, gastrointestinal cancers, esophageal cancers, stomach cancers, pancreatic cancers, liver cancers, colo-rectal cancers, lung cancers, kidney cancers, prostate cancers, bladder cancers, testicular cancers, breast cancers, ovarian cancers, cervical cancers, and melanomas. The carrier includes a cyclodextrin, which may form a complex with the compound. The compounds and compositions can be used to treat or inhibit progression of cancers. Colorectal, bladder, and prostate cancers are examples of some of the cancers that can be treated with the marmelin analog compounds.

MARMELIN ANALOGS AND METHODS OF USE IN CANCER TREATMENT
20170144965 · 2017-05-25 ·

A pharmaceutical composition can include: a marmelin analog compound, and a pharmaceutically acceptable carrier having the compound. The compound can be present in a therapeutically effective amount to treat or inhibit a disease state. The disease state can be cancer. The cancer can be selected from brain cancers, head and neck cancers, thyroid cancers, gastrointestinal cancers, esophageal cancers, stomach cancers, pancreatic cancers, liver cancers, colo-rectal cancers, lung cancers, kidney cancers, prostate cancers, bladder cancers, testicular cancers, breast cancers, ovarian cancers, cervical cancers, and melanomas. The carrier includes a cyclodextrin, which may form a complex with the compound. The compounds and compositions can be used to treat or inhibit progression of cancers. Colorectal, bladder, and prostate cancers are examples of some of the cancers that can be treated with the marmelin analog compounds.

Compositions and methods for the treatment of neuromuscular disorders and neurodegenerative diseases
09642915 · 2017-05-09 · ·

The invention relates to the compound of ##STR00001##
or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing neuromuscular disorders and neurodegenerative diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, or parenteral-administration, or syrup, or injection. Such compositions may be used to treatment or management of neuromuscular disorders and neurodegenerative diseases such as Parkinson's disease, scleroderma, restless leg syndrome, hypertension and gestational hypertension.

Compositions and methods for the treatment of neuromuscular disorders and neurodegenerative diseases
09642915 · 2017-05-09 · ·

The invention relates to the compound of ##STR00001##
or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing neuromuscular disorders and neurodegenerative diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, or parenteral-administration, or syrup, or injection. Such compositions may be used to treatment or management of neuromuscular disorders and neurodegenerative diseases such as Parkinson's disease, scleroderma, restless leg syndrome, hypertension and gestational hypertension.

Polymerizable compound, polymerizable composition, polymer, optically anisotropic body, and method for producing polymerizable compound

A polymerizable compound has a practical low melting point, excellent solubility in a general-purpose solvent, and can produce an optical film at low cost, exhibits low reflected luminance, and achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article. A carbonyl compound is useful as a raw material for producing the polymerizable compound. (In the formula (I), Y.sup.1 to Y.sup.8 represent C(O)O, G.sup.1 and G.sup.2 represent a C.sub.1-20 divalent linear aliphatic group, Z.sup.1 and Z.sup.2 represent a C.sub.2-10 alkenyl group that is unsubstituted, or substituted with a halogen atom, A.sup.x represents a C.sub.2-30 organic group with at least one aromatic ring, A.sup.y represents a hydrogen atom or C.sub.1-20 alkyl group, A.sup.1 represents a trivalent aromatic group, A.sup.2 and A.sup.3 represent a C.sub.3-30 divalent alicyclic hydrocarbon group, A.sup.4 and A.sup.5 represent a C.sub.6-30 divalent aromatic group or the like, and Q.sup.1 represents a hydrogen atom.) ##STR00001##

SEMICARBAZIDE-SENSITIVE AMINE OXIDASE INHIBITORS FOR USE AS ANALGESICS IN TRAUMATIC NEUROPATHY AND NEUROGENIC INFLAMMATION

The invention relates to a compound having SSAO/VAP-1 inhibitor activity for use in the treatment of hyperalgesia and allodynia implicated in traumatic neuropathy or neurogenic inflammation. Accordingly, the invention relates to a compound having SSAO/VAP-1 inhibitor activity for use in the inhibition of pathological activation and dysfunctions of peptidergic sensory nerves caused by mechanical damage or chemical activation of peptidergic sensory nerves in neurogenic inflammation.

SEMICARBAZIDE-SENSITIVE AMINE OXIDASE INHIBITORS FOR USE AS ANALGESICS IN TRAUMATIC NEUROPATHY AND NEUROGENIC INFLAMMATION

The invention relates to a compound having SSAO/VAP-1 inhibitor activity for use in the treatment of hyperalgesia and allodynia implicated in traumatic neuropathy or neurogenic inflammation. Accordingly, the invention relates to a compound having SSAO/VAP-1 inhibitor activity for use in the inhibition of pathological activation and dysfunctions of peptidergic sensory nerves caused by mechanical damage or chemical activation of peptidergic sensory nerves in neurogenic inflammation.

INHIBITORS OF HISTONE LYSINE SPECIFIC DEMETHYLASE (LSD1) AND HISTONE DEACETYLASES (HDACS)

A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.

INHIBITORS OF HISTONE LYSINE SPECIFIC DEMETHYLASE (LSD1) AND HISTONE DEACETYLASES (HDACS)

A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.

Thyromimetics

Compounds are provided having the structure of Formula (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1, and Y.sup.2 are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation. ##STR00001##