Abstract: Pyrimido[4,5-b]indole 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 pyrimido[4,5-b]indole 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: Provided herein are inhibitors of PARG, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the PARG inhibitory compounds for the treatment of disease.

Abstract: The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof.

Abstract: A compound represented by formula (I), an optical isomer thereof and a pharmaceutically acceptable salt thereof, as well as an application of said compound as an FXIa inhibitor.

Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use as Nrf2 activators and for their production.

Abstract: The present application provides tricyclic amine compounds, which are inhibitors of cyclin-dependent kinase 2 (CDK2), of Formula (I): as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

Abstract: The present invention relates to a selective A2A receptor antagonist, and in particular to a selective A2A receptor antagonist of Formula (I), a pharmaceutical composition comprising the antagonist, use of the antagonist in manufacturing a medicament and in treatment of a disease: wherein the groups in Formula (I) are defined as in the specification.

Abstract: The present disclosure relates to a series of tricyclic compounds, their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The disclosure also relates to process of preparation of these tricyclic compounds of Formula I. These compounds are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor. The disclosure also relates to the process of preparation of the tricyclic compounds, and to pharmaceutical compositions containing them. Formula (I) wherein D represents a tricyclic ring system selected from: Formula (II) or Formula (III).

Abstract: The present application provides pyrrolo[2,3-d]pyrimidinone inhibitors of cyclin-dependent kinase 2 (CDK2) of Formula (I): as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

Abstract: A 1H-pyrazolo[4,3-H]quinazoline compound represented by formula (I) can be used for treating cell proliferation dysfunction, and is an broad-spectrum and strongly-active inhibitor for a cell cyclin-dependent kinase (CDK).

Abstract: The present invention provides, inter alia, compounds of general formula (I) capable of inhibiting NF-?B. Pharmaceutical compositions containing and methods of using the compounds are also provided herein.

Abstract: The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

Abstract: A compound of formula I or a pharmaceutically acceptable salt or ester thereof is provided for the treatment of cancer wherein (i) the cancer is one that has the characteristic of being a type prone to being or becoming refractory or resistant to platinum drug based therapy and (ii) the treatment is with a dose of between 1 mg/m2 and 30 mg/m2 of compound per patient body surface area per administration. Method of treatment and novel dosage forms are also provided. Particularly treated arc ovarian cancers, particularly those expressing a-folate receptors, including epithelial ovarian, fallopian tube or peritoneal cancer.

Abstract: The present invention discloses a compound of the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.

Abstract: Disclosed herein are pyrido[3?,2?:4,5]thieno[3,2-d]pyrimidine and pyrimido[4?,5?:4,5]thieno[2,3-c]pyridazine compounds, which may be useful as positive allostenc modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

Abstract: The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof.

Abstract: An inductor includes a body having a first magnetic portion above and below a coil, and a second magnetic portion above and below the first magnetic portion. The magnetic flux density of the magnetic substance in the first magnetic portion is higher than that of the magnetic substance in the second magnetic portion.

Abstract: There is provided a material comprising a n-doped electrically conductive polymer comprising at least one electron-deficient aromatic moiety, each electron-deficient aromatic moiety having a gas-phase electron affinity (EA) of 1-3 eV; and at least one counter-cation covalently bonded to the polymer or to a further polymer comprised in the material, the polymer being n-doped to a charge density of 0.1-1 electron per electron-deficient aromatic moiety, the polymer being capable of forming a layer having a vacuum workfunction (WF) of 2.5-4.5 eV, and wherein all the counter-cations comprised in the material are immobilised such that any electron in the polymer cannot significantly diffuse or migrate out of the polymer. There is also provided a method of preparing the material.

Abstract: A novel imidazopyridine derivative compound and uses thereof are disclosed.

Abstract: A therapeutic method and composition which includes a cannabinoid chemically linked to a chemotherapy agent. The therapeutic composition is capable of crossing the blood-brain barrier, and delivery of the composition across the blood-brain barrier provides both chemotherapy for the treatment of brain cancer and alleviation of side effects caused by the chemotherapy agent. Once across the blood-brain barrier, the chemotherapy agent will be released to attack cancer cells, and the cannabinoid will be free to bind to cannabinoid receptors in the brain to alleviate side effects of chemotherapy such as nausea/vomiting, pain and decreased appetite.

Abstract: A method of treating a patient having cancer is provided comprising administering a therapeutically effective amount of a tricyclic compound or a pharmaceutically acceptable salt of the tricyclic compound to a patient. A method of inhibiting the mitosis of a cancerous cell is also provided.

Abstract: Provided is a dihydropyrazole azepine compound serving as an Akt inhibitor; specifically disclosed is a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to novel compounds of the formula (I) in which Q, Aa, Ab, Ac, Ad, R1 and n have the definitions given above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.

Abstract: The present invention relates to substituted pyrazolopyridinamine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and/or angiogenesis disorder, inflammatory disease and disease associated with inflammatory pain, as a sole agent or in combination with other active ingredients.

Abstract: Present invention relates to a low dose pharmaceutical composition, preferably oral composition comprising therapeutically effective amount of [(2-hydroxy-4-oxo-6,7,8,9-tetrahydro-4H,5H-10-thia-1,4a-diaza-benzo[a]azulene-3-carbonyl)-amino]-acetic acid (compound A) in the range of 2.5 mg to 60 mg. Present invention also relates to a method of treating inflammatory bowel disease in a mammal by administrating said low dose pharmaceutical composition. Further, present invention relates to a use of the compound A for the preparation of low dose pharmaceutical composition for the treatment of inflammatory bowel disease in a mammal.

Abstract: The present invention encompasses compounds of formula (I) wherein the groups A, R and q are defined in claim 1, their use as inhibitors of IGF-1R, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

Abstract: In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid prodrug (e.g., galangin prodrug).

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, A, 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. Compounds of the present disclosure are especially useful for treating cancer.

Abstract: The present invention provides, inter alia, compounds capable of inhibiting NF-?B. Pharmaceutical compositions containing and methods of using the compounds are also provided herein.

Abstract: A compound of formula I, (I) or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer.

Abstract: This disclosure reveals that cyclic corticotrophin releasing factor (CRF) antagonist peptides (such as astressin B, its functional fragments, and their derivatives) induce hair growth and prevent hair loss in vivo. This important discovery enables, for instance, methods of promoting hair growth, and methods of treating hair loss (such as the hair loss that occurs normally in some individuals or that is the result of a health disorder or therapeutic treatment). Exemplary cyclic CRF antagonist peptides useful in the disclosed methods are provided throughout the disclosure.

Abstract: The present disclosure describes the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogs/derivatives as well as their acceptable salts, for treating neuropathic pain resulting from chemotherapy. Methods, compositions, dose units and dose forms of tetrodotoxin related to the use are described.

Abstract: The present invention is directed to formulations comprising PVP polymer, a dispersion of a compound of Formula I (API), and citric acid, which formulations mitigate the effects of coadministering the compound of Formula I with a proton pump inhibitor compound.

Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), according to Formula I, below, wherein R1, R2, R3 and R4 are as defined herein, useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.

Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.

Abstract: The present invention provides, among other things, therapeutic compositions and methods that can effectively treat, slow or prevent a neurological disease (e.g., a neurodegenerative disease, e.g., mild cognitive impairment (MCI) or Alzheimer's disease (AD)), in particular, based on therapeutically effective amount of nifedipine, oxidized or nitroso nifedipine derivatives, lactam (e.g., a compound of formula (Ic) or (Ic-i), e.g., NFD-L1), thyroxine (T4), triiodothyronine (T3) and combinations thereof.

Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.

Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.

Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.

Abstract: Methods to restore and/or improve the libido, the sex drive, in males and females, without introducing any external unnatural drugs. The process utilizes a TENS/EMS (Transcutaneous Electrical Nerve Stimulation/Electronic Muscle Stimulation) machine to naturally generate the increased production by the human body's nerve fiber's neurotransmitters.

Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4 and n are defined herein, are useful as inhibitors of RSV.

Abstract: The invention provides compounds of formula I: and salts thereof wherein R1-R4 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts, and methods for their use in therapy. The compounds have useful antiviral properties.

Abstract: The present disclosure relates to pharmaceutical compositions useful for (and to a method of) treating autoimmune, respiratory and/or inflammatory diseases and conditions. The method involves administering to a subject in need thereof roflumilast N-oxide by inhalation. The present disclosure particularly relates to the treatment of asthma and chronic obstructive pulmonary disease (COPD) by administering roflumilast N-oxide by inhalation.

Abstract: The invention provides a method for treating prostate cancer in a subject comprising administering to the subject an effective amount of a selective inhibitor of one or more of CDK8 and CDK19. In some embodiments the inhibitor inhibits CDK19. In some embodiments, the inhibitor inhibits CDK8 at a Kd of lower than 200 nM and/or inhibits CDK19 at a Kd of lower than 100 nM. In some embodiments, the prostate cancer is androgen independent. In some embodiments, the prostate cancer is androgen independent due to one or more of androgen receptor gene amplification, androgen receptor gene mutation, ligand-independent transactivation of androgen receptor and activation of intracellular androgen synthesis. In some embodiments, the inhibitor inhibits increased activity of NF-?B. In some embodiments, the inhibitor does not inhibit increased basal levels of NF-?B. In some embodiments, inhibition of one or more genes by AR is not inhibited.

Abstract: A compound of formula (I), or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1.

Abstract: [Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D2 receptors. [Solution] The present invention provides a compound represented by the general formula (I): in which R1 is C1-6 alkyl or the like; R2 is hydrogen or the like; R3 and R4 are each hydrogen, C1-6 alkyl, R10R11N—C1-6 alkyl, aralkyl, or the like; R5 and R6 are hydrogen or the like; and R7 is hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine D2 receptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.

Abstract: This disclosure relates to novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities. A tricyclic heterocyclic compound represented by the formula (Ib), wherein the rings Ab and Bb, Xb, Yb, R1b, R2b, R3b, L1b, L2b, L3b and nb are as defined in the specification.

Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).

Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.

Abstract: In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid prodrug (e.g., galangin prodrug).