Abstract: A use of a compound or a medicinal derivative thereof in inhibiting calcium/calmodulin-dependent protein kinase type II gamma (CaMK2?) protein activity is provided, and belongs to the technical field of protein inhibitors. Compared with traditional broad-spectrum immunomodulators, the compound has a strong targeting effect, and is more accurate, rapid, effective, safe, and stable. Moreover, the compound has a strong binding force with human-derived CaMK2? protein and mouse-derived CaMK2? protein, and binding constants are KD=2.54×10?5M and KD=6.84×10?5M respectively. Compared with traditional biological inhibitors, the compound has advantages of easy storage, stable activity, small molecular weight, lower production cost and easy absorption.

Abstract: The present disclosure relates to novel negative-type photoresist composition and methods of their use. The disclosure further relates to multiple trigger photoresist processes which allow for the improvement in contrast, resolution, and/or line edges roughness in some systems without giving up sensitivity. The photoresist compositions and the methods of the current disclosure are ideal for fine patent processing using, for example, ultraviolet radiation, extreme ultraviolet radiation, beyond extreme ultraviolet radiation, X-rays and changed particle. The disclosure further relates to sensitivity enhancing materials useful in the disclosed compositions and methods.

Abstract: A composition for treating substance use disorders of an effective amount of 18-Methoxycoronaridine salt (18-MC) in a pharmaceutical carrier. A method of treating substance use disorders, by administering an effective amount of 18-Methoxycoronaridine salt (18-MC) in a pharmaceutical carrier to an individual and preventing substance abuse in the individual. A method of preventing addictive behavior in an individual. A method of preventing craving in an individual. A composition of a metabolite of 18-MC salt. A method of treating substance use disorders by administering an effective amount of a metabolite of 18-MC salt in a pharmaceutical carrier to an individual and preventing substance abuse in the individual. A composition having various pharmacokinetic profiles as shown in the Figures.

Abstract: The present invention relates to a compound of formula (I) wherein Ar is (II) or (II); R is CH3 or OCH3; or a pharmaceutically acceptable acid addition salt or a corresponding enantiomer thereof. The compounds are modulators of ?-secretase (A ?42) and may be useful for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

Abstract: Provided are a series of novel pyridine or pyrimidine derivatives which inhibit CDK9 and may be useful for the treatment of hyperproliferative diseases. In particular the compounds are of use in the treatment of proliferative disease such as cancer including hematological malignancies such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, diffuse large B cell lymphoma, Burkitt's lymphoma, follicular lymphoma and solid tumors such as breast cancer, lung cancer, neuroblastoma and colon cancer.

Abstract: Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

Abstract: This invention provides a method for treating anxiety-related disorder or impulse control disorder, regulating food intake, attenuating food cravings, or treating anger and/or violence and disorders associated therewith in a patient, comprising administering to the patient in need thereof a therapeutically effective amount of ibogaine, ibogaine derivative, or a pharmaceutically acceptable salt and/or solvate thereof.

Abstract: The present invention relates to a compound of formula I, 1-1 or 1-2 wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, or lower alkoxy substituted by halogen; R1 may be different if n=2 or 3 n is 1, 2 or 3 Ar is a six membered heteroaryl group, selected from wherein R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R3 is hydrogen or halogen; or to a pharmaceutically active acid addition salt thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

Abstract: Compounds of the Formula (I), (II) and (III) wherein Ar is for example phenylene, biphenyleneor naphthylene, all of which are unsubstituted or substituted by C1-C4-alkyl, C2-C4-alkenyl, CN, OR11, SR11, CH 2OR11, COOR12, CONR12R13 or halogen; R1, R2, R7 and R8 independently of one another other are hydrogen or C1-C6-alkyl; R3 and R5 together and R4 and R6 together form a C2-C6-alkylene bridge which is unsubstituted or substituted by one ore more C1-C4-alkyl; R11 is hydrogen or C1-C6-alkyl; R12 and R13 independently of one another for example are hydrogen, phenyl, C1-C18-alkyl, C1-C18-alkyl which is interrupted by one or more O; n is 1-10; X is O, S or NR10; A and A1 are suitable linking groups; are suitable as photolatent bases.

Abstract: The present invention relates to a vasopressin receptor 1B (V1B) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in patients showing an elevated arginine vasopressin (AVP) level and/or an elevated copeptin level. The present invention further relates to a method for predicting the treatment response to a V1B antagonist in patients with depressive symptoms and/or anxiety symptoms.

Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Provided are: a charge-transporting varnish that contains a charge-transporting substance comprising an oligoaniline derivative represented by formula (1), a charge transporting substance that does not contain fluorine atoms, and an organic solvent; and an organic electroluminescent element including a thin film obtained from the varnish. (In the formula: R1 represents a hydrogen atom or an alkyl group that may be substituted; R2 to R10 each independently represent a hydrogen atom, a halogen atom, a nitro group, a cyano group, or an alkyl group, alkenyl group, alkynyl group, aryl group or heteroaryl group that may be substituted; A represents a prescribed fluorine atom-containing substituent; and k represents an integer from 1 to 20.

Abstract: Disclosed is a angiogenesis inhibition determining method using MALDI mass spectrometry, and more particularly, relate to a method for detecting whether small molecules are bound with a target protein and for measuring a binding distribution between the small molecules and the target protein by comparing a result of MALDI mass spectrometry with a result of immunofluorescence of the small molecules, which are used as drugs, for the target protein, and for determining as angiogenesis is inhibited in a portion overlapping with a portion where the drug small molecules are present after the MALDI mass spectrometry in the cell or in the biosample including organelles and a portion where the target protein is present after immunofluorescence, as well as for detecting presence or absence and a distribution state of small molecules used as drugs in a sample by using MALDI mass spectrometry.

Abstract: Provided are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance with Compound A. Also provided are methods of treating at least one phase of substance dependence on at least one substance in patients and certain methods of treating at least one phase of cocaine dependence in patients.

Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X6, X8, Q1, Q2, Q3, Q4, Q5, Q6, Ring A, Ring B, W, W?, R2, R3, R, R?, m, n and q are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.

Abstract: The present invention relates to Phosphate Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Phosphate Substituted Quinolizine Derivative, and methods of using the Phosphate Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.

Abstract: Described herein is a method of administering mirtazapine via the parenteral route to treat the decrease or loss of appetite and/or other disorders induced by undernutrition in cats.

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.

Abstract: Provided are compounds having formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as disclosed herein, or a pharmaceutically salt thereof. Pharmaceutical compositions comprising the compounds and methods of their use, for instance in treating senility, senile confusion, psychoses, psychoneuroses when anxiety and nervous tension were present, cerebral arteriosclerosis, nausea, depression, fatigue, debilitation, mild behavioral disorders, irritability, emotional instability, antisocial attitudes, anxiety, vertigo or incontinence, or symptom thereof, or in improving cognitive function in individuals, for instance, in individuals with Down syndrome and other conditions, are also provided.

Abstract: The present invention relates to methods for the treatment or prevention of symptoms associated with post-traumatic stress disorder, and related pharmaceutical compositions. Of particular interest are pharmaceutical compositions comprising a very low dose of cyclobenzaprine, alone, or in combination with an alpha-1-adrenergic receptor antagonist, a beta-adrenergic antagonist, an anticonvulsant, a selective serotonin reuptake inhibitor or a serotonin-norepinephrine reuptake inhibitor.

Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.

Abstract: A method for producing a pyrrolopyrimidine ring-containing tricyclic compound represented by Formula (1) or a salt thereof. The method comprising the steps of: (I) reacting an organoborane reagent with a compound represented by Formula (2) or a salt thereof, and (II) performing an intramolecular cyclization reaction of the reaction product of step (I) in the presence of a zerovalent palladium catalyst and an alkali metal hydroxide.

Abstract: Provided herein are methods, drug formulations, and dosing regimens for improving cognitive function in a normal or cognitively impaired subject. For instance, methods provided herein comprise administering a GABAA receptor antagonist so that peak concentration of the GABAA receptor antagonist occurs when the subject is asleep.

Abstract: This invention relates noribogaine derivatives, compositions and methods of use thereof.

Abstract: [Problem] Provided is a pharmaceutical, in particular, a pharmaceutical composition which is useful for the treatment of pain. [Means for Solution] The present inventors have made extensive studies using model animals with pain for the purpose of providing a therapeutic agent for pain. As a result, they have found that 11?-hydroxydehydrogenase type 1 (11?-HSD1) inhibitor, in particular, a triazole compound having a cyclic group at the 3-position (or 5-position) of a triazole ring has a good effect of ameliorating chronic pain. That is, according to the present invention, a pharmaceutical composition comprising an 11?-HSD1 inhibitor, in particular, the triazole compound of the present invention, as an active ingredient, is useful for the treatment of pain (particularly, neuropathic pain or fibromyalgia).

Abstract: An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects. The present invention provides a compound represented by Formula (I) below, or a salt thereof.

Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

Abstract: The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R1, R2, R3 and R4 have the meanings given for the general formula (I), to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.

Abstract: An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects. The present invention provides a compound represented by Formula (I) below, or a salt thereof.

Abstract: The present invention relates to novel polymorphic forms of alcaftadine, processes of preparing novel polymorphic forms of alcaftadine and pharmaceutical compositions thereof.

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.

Abstract: This invention is directed to a method for pre-screening an opioid-addicted patient to determine the patient's tolerance for a therapeutic dose of noribogaine.

Abstract: This invention relates generally to prodrugs of noribogaine. This invention also relates to pharmaceutical compositions comprising the prodrugs of noribogaine as well as method of treating pain, addiction and/or stress using such compounds and/or pharmaceutical compositions.

Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1, R2, R4, R5, R6 and R7 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.

Abstract: The present invention relates to novel polymorphic forms of alcaftadine, processes of preparing novel polymorphic forms of alcaftadine and pharmaceutical compositions thereof.

Abstract: The present invention concerns a premix composition for feeding cattle, comprising: a) a premix carrier having an overall particle size comprised between 300 and 400 ?m, b) zilpaterol, and c) a surface agent. The present invention is also related to a method of increasing the rate of weight gain in cattle, comprising the administration to the cattle of feed additives consisting of a premix composition such as described, over a period of at least two weeks.

Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.

Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.

Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B—The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain.

Abstract: This invention relates noribogaine derivatives, compositions and methods of use thereof.

Abstract: The invention provides methods for selecting and administering antidepressant medications to a patient based upon the patient's combination genotype and phenotype for a panel of genes.

Abstract: Stable noribogaine salt ansolvates are useful for preparing pharmaceutical compositions and for alleviating nociceptive pain in a patient. Such ansolvates can be prepared by slurrying solvated forms, preferably MeOH solvated noribogaine hydrochloride in EtOH/water.

Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.

Abstract: The present invention relates to a method of treating obesity in a subject by administering to the subject a compound having the formula: wherein n is from 0 to 8; R1 is CH2OH, CH(OH)R5, CH2OR5, CO2R5, C(O)NH2, C(O)NHR5, C(O)NR5R6, C(O)NHNH2, C(O)NHNHR5, C(O)NHNR5R6, C(O)NR5NH2, C(O)NR5NHR6, C(O)NR5NR6R7, C(O)NHNH(C(O)R5), C(O)NHNR5(C(O)R6), C(O)NR5NH(C(O)R6), C(O)NR5NR6(C(O)R7), CN, or C(O)R5; R2 is H, unsubstituted or substituted alkyl, YH, YR8, YR8R9, YR8YR9YR10, YC(O)R8, C(O)YR8, C(O)NH2, C(O)NHR8, C(O)NR8R9, NH2, NHR8, NR8R9, NHC(O)R8, or NR8C(O)R9; R3 and R4 are the same or different and are selected from the group consisting of H, halogens, unsubstituted or substituted alkyl, OH, OR10, NH2, NHR10, NR10R11, NHC(O)R10, or NR10C(O)R11; R5, R6, R7, R8, R9, R10, and R11 are the same or different and are selected from the group consisting of H, unsubstituted alkyl, substituted alkyl, unsubstituted aryl and substituted aryl; R12 is selected from the group consisting of H, unsubstituted alkyl, and substitu

Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.