Abstract: A pathological mechanism in FOP patients is further revealed, and development of a novel therapeutic drug, therapeutic method, diagnostic method, etc. utilizing an obtained finding is provided. The inventors have found a novel finding that in FOP, ectopic ossification, which occurs by an inflammation due to an injury, etc., is mediated by PAR1 to occur. From this finding, the inventors completed the present invention relating to a drug, etc. characterized by suppressing ectopic ossification in FOP by inhibiting PAR1.

Abstract: Disclosed are a pyrimidinyl group-containing tricyclic compound and applications thereof in preparing a cancer-treating medicament. Specifically disclosed are a compound as represented by formula (I), a pharmaceutically acceptable salt of same, or an isomer thereof.

Abstract: The present application relates generally to methods for treating prostate cancer with substituted tricyclic derivative is 2-[3-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-5-[(S)-(oxan-4-yl)(phenyl)methyl]-5H-pyrido[3,2-b]indol-7-yl]propan-2-ol as a bromodomain inhibitor, or the pharmaceutically acceptable salt thereof.

Abstract: Novel pyrido[3,4-b]indole-6-carboxylic acid compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[3,4-b]indole-6-carboxylic acid compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Pyrido[3,4-b]indole-3-carboxylic acid compounds are provided. The pyrido[3,4-b]indole-3-carboxylic acid compounds have the formula I: wherein Ring A, R1, R2, R3, and R4 are as described herein. The pyrido[3,4-b]indole-3-carboxylic acid compounds inhibit protein kinase CK2 activity and may be used as anticancer and/or antitumor agents, as well as agents for treating inflammation, pain, immunological disorders, diabetes, viral infections, and neurodegenerative diseases.

Abstract: Described herein are compounds having the following structure: formula (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof. Also disclosed are compositions containing the compounds, methods of inhibiting activity of DYRK1 A in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.

Abstract: The pyrrolo[2,3-b]quinoline compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.

Abstract: The present invention provides a compound or a method for treating an RNA viral infection in a human, particularly COVID-19. The compound is a certain tricyclic compound.

Abstract: In one example presented herein, is a pharmaceutical composition. The pharmaceutical composition can include halobetasol propionate, from 0 wt % to 3 wt % ethoxylated castor oil, a first compound, and a second compound. The first compound and the second compound can be selected from; N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate, and sodium lauryl sulfoacetate. The first compound and the second compound are not the same.

Abstract: The invention relates to a composition for induction of activity of a nuclear receptor PPAR? and inhibition of HDAC in a subject in need thereof, which comprises a synergistic combination of benzoate and phenylbutyrate and/or phenylacetate in association with a pharmaceutical carrier.

Abstract: A method of use for Cpd 1 as an inhibitor of dihydroorotate dehydrogenase (DHODH) function in treating or ameliorating a hematological cancer in a subject in need thereof comprising, administering an effective amount of Cpd 1 to the subject, having the structure: or a form or pharmaceutical composition thereof.

Abstract: The present invention provides compounds of Formula (I): (I) wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subject (e.g., a human).

Abstract: A method for treating or preventing cancer in a subject comprising administering a treatment effective amount of a chemotype 4 compound.

Abstract: Methods of treatment of addiction and/or dependence, methods of promoting cessation of various addictions, such as smoking and/or vaping, and methods of promoting a reduction in various addictions, such as smoking and/or vaping, uses of cytisine as an addiction cessation treatment, and dosage regimens for the foregoing are provided.

Abstract: Methods of treatment of addiction and/or dependence, methods of promoting cessation of various addictions, such as smoking and/or vaping, and methods of promoting a reduction in various addictions, such as smoking and/or vaping, uses of cytisine as an addiction cessation treatment, and dosage regimens for the foregoing are provided.

Abstract: Disclosed are methods and pharmaceutical compositions for treating a cancer in a subject in need thereof, the cancer characterized by proteolytic cleavage by taspase1 of the mixed-lineage leukemia 1 gene product (MLL1), the method comprising administering to the subject a therapeutic agent that inhibits cleavage by taspase1 of MLL1. Suitable therapeutic agents may include agents that inhibit the kinase activity of casein kinase II (CKII). Cancer treated by the disclosed methods and pharmaceutical compositions may include leukemia such as Acute Lymphoblastic Leukemia (ALL) and/or Acute Myeloid Leukemia (AML) and in particular, leukemia characterized by rearrangements in MLL1.

Abstract: Use of carrimycin in Mycobacterium tuberculosis infection resistance comprises the main steps: measuring the activity of carrimycin in Mycobacterium tuberculosis resistance by adopting an absolute concentration method through taking clinical first-line antituberculotics, i.e., isoniazid and rifampicin as controls. The result indicates that carrimycin has obvious superior activity to clinically-separated Mycobacterium tuberculosis including drug-resistant bacteria compared with those of the clinical first-line control drugs, i.e., the isoniazid and the rifampicin, and use of carrimycin in manufacturing drugs for treating tubercle Bacillus infected diseases are expected to be developed.

Abstract: In one aspect, the invention provides compounds of Formula I Formula Ia, Formula Ib, Formula Ic, and Formula Id and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula Ia, Formula Ib, Formula Ic, or Formula Id. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease, diabetes bone loss, and cancer, using a compound of Formula I, Formula Ia, Formula Ib, Formula Ic, or Formula Id.

Abstract: The invention provides compounds of Formula XXIII: wherein R1 is hydrogen, alkyl, acyl, or silyl, R2 is hydrogen, alkyl, benzyl, acyl, or ester, and R3 is hydrogen, alkyl, an aromatic group, azacyclic, carbocycle, aryl, cycloalkyl, heterocycloalkyl, heterocycle, heteroaryl, heteroalkyl, acyl, or ester, as well as derivatives and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The invention relates to an adhesive transdermal therapeutic system containing, as an active principle, an association of valentonin (VLT) and 6-methoxyharmalan (6-MH).

Abstract: The invention provides a combination comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline or a pharmaceutically acceptable derivative thereof, mupirocin or a pharmaceutically acceptable derivative thereof and neomycin or a pharmaceutically acceptable derivative thereof. This triple combination is particularly useful for the treatment and/or prevention of microbial infections.

Abstract: A composition comprising a tricyclic indole compound. The composition has a higher purity and better impurity profile than known compositions comprising said tricyclic indole compound and as a consequence has superior properties, particularly when said compound is destined for use in vivo as a therapeutic or diagnostic agent.

Abstract: The invention relates to a composition for induction of activity of a nuclear receptor PPAR? and inhibition of HDAC in a subject in need thereof, which comprises a synergistic combination of benzoate and phenylbutyrate and/or phenylacetate in association with a pharmaceutical carrier.

Abstract: The present invention relates to use of pyrroloquinoline quinone (PQQ), a derivative and/or a salt thereof of formula (I) in the preparation of a drug for treating and/or preventing primary Sjogren's syndrome, secondary Sjogren's syndrome as well as dry mouth, dry eye and multiple system damages accompanied by the involvement of other exocrine glands and other organs outside the glands caused by Sjogren's syndrome. In formula (I), R1, R2 and R3 being same or different, each independently representing lower alkyl, lower alkenyl, lower alkynyl, aralkyl, alkaryl, phenyl, a hydrogen atom, sodium atom or a potassium atom; and PQQ or pharmaceutical combinations of PQQ combined with active vitamin D, NAC, resveratrol, epigallocatechin gallate, curcumin, anthocyanin, vitamin E, vitamin C, or vitamin D and the like. The drug and the pharmaceutical combinations can treat Sjogren's syndrome and associated diseases which are derivative of Sjogren's syndrome.

Abstract: The present disclosure provides, among other things, compositions and methods useful for inhibiting bacteria, such as Mycobacterium tuberculosis. These compositions and methods find many uses in medicine and research, e.g., treating subjects afflicted with active or latent bacterial infections. The compositions described herein are also useful for decontaminating surfaces (e.g., surgical tools or implants).

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: Provided herein are tricyclic small molecule inhibitors of maternal embryonic leucine zipper kinase (MELK). The compounds are useful for treating cancer and other conditions or diseases associated with aberrant MELK expression. Also provided herein are pharmaceutical compositions comprising a tricyclic compound of the invention and a pharmaceutically acceptable carrier. The invention also provides methods of treating cancers associated with over-expression of MELK.

Abstract: Pharmaceutical compositions and methods of their use are provided for reducing inflammation in a subject, blocking leukocyte recruitment, inhibiting tumor metastasis, treating sepsis and preventing/reducing acute kidney injury.

Abstract: An SP-141 compound is a novel small molecule that can serve as a molecular-targeted chemotherapeutic agent. In one embodiment, the labeled compound can comprise SP-141, which comprises 6-methoxy-1-(naphthalen-1-yl)-9 H-pyrido[3,4-b]indote. The compound inhibits expression of oncogenes such as the Mouse Double Minute 2 protein. The compound can bind directly to Mouse Double Minute 2 to inhibit cancer growth including breast cancer growth.

Abstract: Provided are crystal forms I, II, III and IV of a pyrroloquinoline quinone sodium salt and a preparation method thereof. Also provided are a pharmaceutical composition, a cosmetic composition, a functional food or a nutritional agent containing the above-mentioned crystal forms. The crystal forms have excellent properties in terms of solubility, crystal stability, hygroscopicity and the like.

Abstract: The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The present application provides a hetero-cyclic compound which may significantly improve the service life, efficiency, electrochemical stability, and thermal stability of an organic light emitting device, and an organic light emitting device in which the hetero-cyclic compound is contained in an organic compound layer.

Abstract: The present disclosure provides substituted 9H-pyrimido [4,5-b] indoles and 5H-pyrido [4,3-b] indoles and related analogs represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, W, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.

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: The invention provides compounds of Formula XXIII: wherein R1 is hydrogen, alkyl, acyl, or silyl, R2 is hydrogen, alkyl, benzyl, acyl, or ester, and R3 is hydrogen, alkyl, an aromatic group, azacyclic, carbocycle, aryl, cycloalkyl, heterocycloalkyl, heterocycle, heteroaryl, heteroalkyl, acyl, or ester, as well as derivatives and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 to R5 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.

Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.

Abstract: In one embodiment, the present application discloses 2-aza-, 2-oxa- and 2-thia-2,3-dihydro-6-azaphenalene compounds and compositions, and methods for treating a neurological disease in a patient in need thereof using the compounds and compositions as disclosed herein.

Abstract: It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R1, R2, R3, Y, and Z are as defined in claim 1.

Abstract: The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and/or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.

Abstract: A composition of redox-reagent containing metal-containing complex and thionine or its derivative as electron transfer mediator for use in an electrochemical biosensor, and a biosensor containing the same are provided. With the increase in reaction rate between redox enzyme-thionine (or its derivative)-metal-containing complex in the composition of redox-reagent containing metal-containing complex and thionine or its derivative, glucose detection efficiency markedly increases, and the composition is hardly influenced from high humidity and interfering substances. Accordingly, the composition of redox-reagent is useful in fabricating an electrochemical biosensor for detecting glucose in blood.

Abstract: The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.

Abstract: Novel antiviral compounds of Formulae (I)-(III) are provided: (I) (II) (III) The inventive compounds, pharmaceutical compositions thereof, and kits including the inventive compounds are useful for the prevention and treatment of infectious diseases caused by viruses, for example, by Flaviviridae virus (e.g., Dengue virus (DENY)), Kunjin virus, Japanese encephalitis virus, vesicular stomatitis virus (VSV), herpes simplex virus 1 (HSV-1), human cytomegalovirus (HCMV), poliovirus, Junin virus, Ebola virus, Marburg virus (MARV), Lassa fever virus (LASV), Venezuelan equine encephalitis virus (VEEV), or Rift Valley Fever virus (RVFV).

Abstract: This invention relates to methods of treating and ameliorating congenital and neonatal hyperinsulinism and post-prandial hypoglycemia, comprising the step of administering an antagonist of the Glucagon-Like Peptide-1 (GLP-I) receptor, e.g. a GLP-I fragment or analogue thereof.

Abstract: A yellow reduced pyrroloquinoline quinone crystal having a solubility in water of 0.040 to 0.20 (mg/mL).

Abstract: Compounds as inhibitors of CSCPK and related kinases. The compounds are thiazole-substituted indolin-2-ones and are prepared from indolin-2-ones. They are included in pharmaceutical compositions and both the compounds and the pharmaceutical compositions are used in inhibiting cancer stem cells and in the treatment of a protean kinase related disorders.

Abstract: Disclosed are methods of treating Parkinson's disease by (i) providing a pharmaceutical composition in unit dosage form that is a film having a first portion including apomorphine particles containing an acid addition salt of apomorphine and a second portion containing a pH neutralizing agent, where the film contains the acid addition salt of apomorphine in an amount effective to treat Parkinson's disease, and (ii) administering the film by placing the film sublingually in the mouth of the subject and contacting sublingual mucosal tissue with the film.