Patent classifications
A61K31/4465
Substituted 1-arylalkyl-4-acylaminopiperidine compounds and methods of producing and using the same
The present invention provides using a substituted 1-arylalkyl-4-acylaminopiperidine compound of Formula I: ##STR00001##
to treat various clinical conditions including, but not limited to, hemorrhagic shock, nicotine withdrawal symptoms, gastrointestinal side effects of opioids, cancer therapy, epithelial wounds, herpes zoster infection, or opioid-induced pruritus. In compound of Formula I, R.sup.1 is C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; R.sup.2 is C.sub.1-6 alkylene; Y is optionally substituted aryl, optionally substituted heteroaryl, or a moiety of the formula —C(═O)—X.sup.1, wherein X.sup.1 is —OR.sup.3 or —NR.sup.4R.sup.5, where each of R.sup.3, R.sup.4 and R.sup.5 is H or C.sub.1-10 alkyl.
Targeted drugs associated with trimethylamine and/or trimeihylamine-n-oxide
Embodiments of a method and/or system can include administering, to a patient with one or more conditions associated with at least one of TMA, TMAO, and/or derivatives thereof, a therapeutically effective amount of a compound for affecting inhibiting one or more CutC enzymes and/or CntA enzymes associated with microorganisms from at least one taxon from a set of microorganism taxa.
Targeted drugs associated with trimethylamine and/or trimeihylamine-n-oxide
Embodiments of a method and/or system can include administering, to a patient with one or more conditions associated with at least one of TMA, TMAO, and/or derivatives thereof, a therapeutically effective amount of a compound for affecting inhibiting one or more CutC enzymes and/or CntA enzymes associated with microorganisms from at least one taxon from a set of microorganism taxa.
4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUNDS
The invention relates to compounds of formula I:
##STR00001## where a, R.sup.1, and R.sup.3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUNDS
The invention relates to compounds of formula I:
##STR00001## where a, R.sup.1, and R.sup.3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
CUBIC CYCLODEXTRIN FRAMEWORK-RGD COMPOSITION AND PREPARATION METHOD THEREFOR
A cubic cyclodextrin framework-RGD composition (RGD-COF) and a preparation method therefor. Specifically, the cyclodextrin framework-RGD composition contains a cyclodextrin framework (COF) having a cubic structure and RGD, and can escape from phagocytosis and clearance of macrophages, enhance migration and adhesiveness to damaged blood vessels, and efficiently target and aggregate activated platelets at damaged blood vessel sites, having application prospects on targeted diagnosis and treatment of diseases associated with uncontrolled hemorrhage, atherosclerosis and cerebral apoplexy. By utilizing the advantage that a cyclodextrin-metal organic framework (CD-MOF) has controllable dimensions, a cubic cyclodextrin framework-RGD composition for nanoscale intravenous injection or microscale topically external use is provided.
ALLOSTERIC INHIBITOR OF WEE1 KINASE
Disclosed is a method for selecting a cancer therapeutic for a patient that involves assaying a tumor biopsy sample from the subject to detect PAXIP1 expression, and selecting a WEE1 inhibitor as the cancer therapeutic if PAXIP1 is detected in the tumor biopsy sample.
CRYSTALLINE FORM OF A 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUND
The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
CRYSTALLINE FORM OF A 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUND
The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
GABA AGONISTS IN THE TREATMENT OF DISORDERS ASSOCIATED WITH METABOLIC SYNDROME AND GABA COMBINATIONS IN TREATMENT OR PROPHYLAXIS OF TYPE I DIABETES
In certain embodiments methods are provided for the therapeutic or prophylactic amelioration of one or more symptoms or disorders associated with metabolic syndrome. In various embodiments the methods involve administering to a subject in need thereof, a GABA receptor agonist, in an amount sufficient to ameliorate said one or more symptoms. In certain embodiments methods are provided for the prophylaxis or treatment of type I diabetes and related pathologies that involve the use of GABA or GABA agonists in combination with certain other compounds (e.g., one more antigens (e.g., GAD) that have a therapeutic effect in type I diabetes and/or an anti-CD3 antibody, an anti-CD20 antibody, exendin-4, and/or or a pro-insulin therapeutic).