Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

Abstract: The present invention discloses a polypeptide compound, a pharmaceutical composition, and a preparation method and use thereof. The structural formula of the polypeptide compound is shown in general formula (I): Such polypeptide compounds as ?-opioid receptor agonists have the advantages of better activity and the potential to become clinical candidate compounds.

Abstract: The present invention relates to synthetic receptors for ionophoric compounds, such as ionophoric toxins. Hence, the invention provides synthetic molecules capable of binding different ionophoric compounds, thereby being suitable for use in the detection, isolation and detoxification of such ionophoric compounds. The present invention further provides the use of such synthetic receptors in human and veterinary medicine, such as in the diagnosis, prevention and/or treatment of disorders caused by such ionophoric compounds. Finally, the invention provides methods of preparing such synthetic receptors for ionophoric compounds.

Abstract: The invention relates in part to a method of maintaining heavy metal homeostasis in healthy humans, comprising chronically administering to healthy humans a pharmaceutical composition consisting of from about 1 mg to less than about 200 mg of Posiphen or a pharmaceutically acceptable salt thereof together with one or more pharmaceutically acceptable excipients, on a once a day basis. By virtue of this method, prophylactic treatment of a potential disease state such as a neurodegenerative disease, cardiovascular homeostasis, cancer, vital organ homeostasis, and the like. The invention also relates in part to a method of restoring heavy metal homeostasis in sick patients, comprising chronically administering to a sick patient a pharmaceutical composition consisting of from about 1 mg to less than about 200 mg of Posiphen or a pharmaceutically acceptable salt thereof together with one or more pharmaceutically acceptable excipients, on a once a day basis.

Abstract: The present invention relates to a pharmaceutical composition for treatment of a disease or condition characterized by or associated with stimulation of both DPr2 and TPr signaling, said composition comprising an effective amount of a dual receptor antagonist of DPr2 for prostaglandin D2 and TPr for thromboxane A2 and a pharmaceutically acceptable carrier.

Abstract: The present invention concerns a PTGDR-1 antagonist, a PTGDR-2 antagonist, a dual PTGDR-1/PTGDR-1 antagonist, or a combination of PTGDR-1 antagonist and PTGDR-2 antagonist, and pharmaceutical compositions containing them, for use for preventing and/or treating SLE.

Abstract: Provided are a tricyclic compound as shown in formula (I) as a CRTH2 inhibitor, or a pharmaceutically acceptable salt, a tautomer, a stereoisomer or a solvate thereof, and the use thereof in treating diseases related to CRTH2 receptors.

Abstract: Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.

Abstract: 1-(3,4-Dihydro-1H-pyrido[4, 3-b]indol-2(5H)-yl)-2-hydroxyethanones are disclosed. The compounds are inhibitors of human cGAS in interferon-producing cell types. They are thus useful as therapeutic agents for treating cGAS-related autoimmune diseases in humans.

Abstract: The present invention provides substituted 1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles and methods of using the compounds for treating brain disorders.

Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.

Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.

Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.

Abstract: The present invention relates to a method for the synthesis of compounds useful in the preparation of antibody drug conjugates (ADC), namely, monoprotected dimeric bifunctional prodrugs based on duocarmycin analogs. In a further aspect, compounds obtained by the method according to the present invention are provided. The monoprotected bifunctional prodrug is used for preparing antibody drug conjugates composed of an antibody moiety and the monoprotected bifunctional prodrug. The antibody compound conjugates thus obtained are provided. Further, a method of preparing an antibody drug conjugate composed of two identical or two different antibody moieties is provided as well as the antibody compound conjugate containing two different antibody moieties accordingly. These conjugates can be used in pharmaceutical compositions, in particular, for use in treatment of tumors, e.g. for use in ADC therapy.

Abstract: The combination of a repellent agent or an attractant agent with a wavelength-specific visual cue agent has been found to produce an unexpected and synergistic effect of increased repellency or attraction in dichromatic animals who are not maximally sensitive to the wavelength of the repellent or attractant agent. The method of the invention may be used to repel dichromatic-animal pests; or to prevent or minimize monetary damage, particularly to agricultural products, natural resources or private property. The method of the invention may also be used to attract dichromatic animals for the purpose of agricultural production, recreational opportunities (e.g., wild-rodent feeders), or the effective administration of target-animal pharmaceuticals or mitigation techniques.

Abstract: The invention relates to pharmaceutical compositions comprising a statin and a cannabinoid, and their use for the treatment of hypercholesterolemia and atherosclerosis. It has been found that compositions combining a statin and a cannabinoid are improved over existing statin formulations. The compositions of the invention for example allow for a lower effective dose of statin and a reduction of the adverse effects seen with statins taken alone. Dosing ranges and formulations suitable for oral, buccal, and sublingual administration are disclosed. Various specific cannabinoids such as cannabidiol and synthetic cannabidiols selected for their anti-inflammatory, antioxidant, and anti-atherosclerotic effect are shown to be particularly advantageous.

Abstract: It is described an industrially viable and advantageous process for the preparation of (S)-beta-aminosulfone (1) starting from the corresponding racemic compound, said (S)-beta-aminosulfone being a useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.

Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

Abstract: The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.

Abstract: Described herein are methods and uses of Nampt activators for treatment of cardiovascular diseases and disorders, and/or diabetes, symptoms thereof, and complications associated with diabetes.

Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

Abstract: An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, Y and R2 are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The invention relates to pharmaceutical compositions comprising a statin and a cannabinoid, and their use for the treatment of hypercholesterolemia and atherosclerosis. It has been found that compositions combining a statin and a cannabinoid are improved over existing statin formulations. The compositions of the invention for example allow for a lower effective dose of statin and a reduction of the adverse effects seen with statins taken alone. Dosing ranges and formulations suitable for oral, buccal, and sublingual administration are disclosed. Various specific cannabinoids such as cannabidiol and synthetic cannabidiols selected for their anti-inflammatory, antioxidant, and anti-atherosclerotic effect are shown to be particularly advantageous.

Abstract: The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I: or a pharmaceutically acceptable salt thereof.

Abstract: The present invention includes a low dose and sustained release formulation of 2,4-dinitrophenol (DNP). The compositions of the invention are useful for preventing or treating a disease or disorder, such as non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, insulin resistance and/or diabetes, in a subject in need thereof.

Abstract: The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

Abstract: The present invention relates to a method for detecting renal disease and for assessing the efficacy of dialysis treatment using imaging agents having desirable in vivo properties.

Abstract: The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.

Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.

Abstract: Compounds that inhibit digestion in blood-ingesting pests are described herein. In one embodiment, the compounds described herein block entry of blood into the midgut and thereby inhibit digestion and nutrient processing. In another embodiment, the compounds described herein prevent pathogens contained in the blood meal from entering the midgut where they could cross the epithelial cell layer and infect the mosquito. The compounds can be administered to a population of blood-ingesting pests, such as mosquitos, directly or indirectly in an effective amount to prevent mosquitoes from transmitting diseases such as malaria, dengue fever, West Nile virus and lymphatic filariasis. Preferably, the compounds are lethal to blood-ingesting pests. The compounds can be combined with one or more excipients to prepare compositions.

Abstract: A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided.

Abstract: The present invention relates to the compound ((2R,2?R)-bis(((tetrahydro-2H-pyran-4-carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.

Abstract: The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

Abstract: The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.

Abstract: The present invention provides one or more compounds of formula (I) for conjugation to small molecules, polymers, peptides, proteins, antibodies, antibody fragments etc.

Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

Abstract: Pharmaceutical compositions comprising an ester anesthetic and a cholinesterase inhibitor have been found to exhibit surprising and beneficial results in achieving a long-acting nerve block for example when administered to an interfascial plane or a peri-neural location in a subject. Such pharmaceutical compositions may also contain an amide anesthetic. Pharmaceutical compositions and methods of using such compositions as described herein provide a surprising and unexpected duration of pain control and a reduced need for the use of narcotics.

Abstract: The present invention relates to a composition for transfecting a cell with a genetic material comprising a first agent capable of directing the genetic material away from the acidic compartments in the cell and a second agent capable of stabilizing the microtubule or a network thereof. The invention also relates to the use of the composition in the manufacture of a medicament for treating a disease, a method for delivering a genetic material into a cell and a kit.

Abstract: The invention relates to a method of inducing emesis in animals, particularly companion animals such as dogs and cats, in situations where vomiting is desired. The method comprises administering an eye drop composition comprising a selective D2 family dopamine agonist as an active ingredient to the eye of the animal to induce emesis. The method and the composition are useful in situations involving ingestion of a potentially toxic substance or foreign body by the animal.

Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

Abstract: The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, D, E, G, J, L, M, Q, a, and b are accordingly described. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.

Abstract: The T cells specific to human collagen type II, one of the possible autoantigens, have a crucial role in the development of rheumatoid arthritis in the context of HLA-DR4. The protein-protein interactions between the T cell receptor (TCR) and the type II collagen linked to the allele MHC of class II HLA-DR4 may thus represent the target for the development of new drugs against rheumatoid arthritis. Using computational virtual screening techniques, families of pharmacologically active molecules have been identified that interfere with the TCR/collagen II-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.

Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: A compound having a group represented by the formula (Ia): wherein R1 represents a C1 to C8 fluorinated alkyl group, R2 represents a group having an optionally substituted C5 to C18 alicyclic hydrocarbon group, and * represents a binding site.

Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.

Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C?, D, E, F, G, H?, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.