1648 results about "Depressant" patented technology

Provided herein, in part, is a compound of Formula (I)or a hydrate thereof,essentially free of one or more impurities, compositions thereof, and methods of use thereof.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

Provided are a fused tricyclic compound, a preparation method therefor and a pharmaceutical use thereof. Specifically, provided are a compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as a therapeutic agent, particularly a use as an RAS inhibitor and a use in the preparation of a drug for treating and / or preventing RAS-mediated or RAS-dependent diseases or disorders. The groups in general formula (I) are as defined in the description.

The present invention belongs to the technical field of chemical drugs, and relates to a PCSK9 and HMG-CoA dual-target compound, or an isomer thereof, or a racemate thereof, or a pharmaceutically acceptable salt thereof, a preparation method therefor, the use thereof as a PCSK9 inhibitor and / or HMG-CoA reductase inhibitor, and a method for using same to treat a plurality of specific diseases or disorders.

Disclosed are methods of treating cancer comprising administering to a subject a treatment regimen comprising a compound of Formula (I): Formula (I), or a pharmaceutically acceptable salt thereof, and a PD-1 or PD-L1 antagonist.

Provided are pyrazole-containing polycyclic derivative inhibitors, preparation methods therefor, and uses thereof. In particular, provided are compounds represented by formula (I), preparation methods therefor, pharmaceutical compositions containing the compounds, and uses thereof as P2X3 inhibitors in the treatment of P2X3 receptor dysfunction, particularly in the treatment of neurological diseases, wherein the substituents in formula (I) are the same as those described in the definitions. TIFF2023506436000188.tif48169

The present embodiments provide compounds of Formula (I), compositions of the compounds, and methods for treating diseases such as cancer.

The present invention relates to an azacyclic derivative, a preparation method therefor and a use of a pharmaceutical composition containing the derivative in medicine. Specifically, the present invention relates to a cyclic derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and a use thereof as a therapeutic agent, especially as a WRN inhibitor. The definition of each substituent in general formula (I) is the same as that in the description.

Provided herein are compounds of formulae (I)-(IX), or pharmaceutically acceptable salts or deuterated forms thereof as defined herein. Also provided herein are pharmaceutical compositions comprising a compound of formula (I)-(IX) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of formula (I)-(IX) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

Provided herein are novel DPP1 inhibitor compounds having the general structure of Formula (I), (II) or (III), or a pharmaceutically acceptable salt thereof. Also provided are certain methods of treatment, e.g., a method for treating an obstructive disease of the airway or a method of treating an inflammatory condition with a composition comprising an effective amount of one of the compounds provided herein.

The invention belongs to the field of flotation, and particularly relates to a composite inhibitor for copper sulphide ore, an inhibition method, a copper-molybdenum separation method and a flotation reagent thereof.The composite inhibitor for the copper sulphide ore comprises a component A, a component B, a component C and a component D according to the weight ratio of (3-7): (1-2): (1-2): (1-3); wherein the component A is a compound shown in a formula 1 (1); the component B is a compound shown in a formula 2; the component C is konjac mannan; component D is a compound represented by formula 3. The research shows that the component A and the component D are innovatively combined, and flotation of the copper sulphide ore can be accidentally inhibited with high selectivity on the basis of combination and synergy of special groups between the component A and the component D.

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts or deuterated forms thereof, wherein R0, L and R1 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

The present application relates to novel substituted heterocyclic carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and / or prevention of diseases and to their use for producing medicaments for the treatment and / or prevention of diseases, in particular for the treatment and / or prevention of breathing difficulties including sleep-induced breathing difficulties such as central and obstructive sleep apnoea, snoring (primary and obstructive snoring), dysphagia, peripheral and cardiac vascular disorders including diabetic microangiopathies and disorders of the peripheral and central nervous system including neurodegenerative and neuroinflammatory disorders.

The present invention relates to a substituted pyrimidine-fused ring inhibitor, a method for preparing same, and use thereof. Specifically, the compound of the present invention has a structure represented by formula (I). Further disclosed are a method for preparing the compound, and use of the compound as a KRAS mutation inhibitor. The compound has a good selective inhibition effect on KRAS mutation and has better pharmacodynamic and pharmacokinetic performance and lower toxic and side effects.

The invention provides a compound as shown in a formula I which can be used as a sodium channel regulator, and a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition containing the compound and the stereoisomer, the tautomer or the pharmaceutically acceptable salt thereof and a carrier or excipient, and a pharmaceutical application of the pharmaceutical composition as a NaV1.8 inhibitor (such as pain, respiratory diseases, neurological disorders, mental diseases and the like).

The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and / or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g., neurosurgery, endovascular clot removal, spinal tap, aneurysm repair, or deep brain stimulation, as well as retinal edema), as well as hyponatremia and excess fluid retention, and diseases such as epilepsy, retinal ischemia and other diseases of the eye associated with abnormalities in intraocular pressure and / or tissue hydration, myocardial ischemia, myocardial ischemia / reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines, as well as to novel assays for identifying aquaporin inhibitors.

The invention discloses application of an Hspa5 inhibitor in preparation of a medicine for preventing or treating anxiety disorder. An anxiety mouse model is constructed through chronic constraint stress (CRS), and in combination with medial amygdala kernel (MeA) transcriptome sequencing and qPCR verification, it is found that the endoplasmic reticulum molecular chaperone Hspa5 is remarkably up-regulated in the anxiety state. Furthermore, an Hspa5 specific inhibitor HA15 is locally injected into a MeA brain region, so that the anxiety-like behavior induced by the CRS is remarkably improved, and the exploration time of an open field experiment central region, the exploration time of an open arm of an elevated cross labyrinth and the exploration time of a bright box of a bright-dark box experiment are prolonged. The invention discloses the function of Hspa5 as a novel anti-anxiety target for the first time, and provides a direct experimental basis and a transformation direction for developing a novel anti-anxiety drug which is non-monoamine and targets an endoplasmic reticulum homeostasis.

The invention relates to a polycyclic compound, a preparation method thereof and application of the polycyclic compound in medicine. Specifically, the invention relates to a polycyclic compound as shown in a general formula (I), a preparation method of the polycyclic compound, a pharmaceutical composition containing the polycyclic compound and application of the polycyclic compound as a therapeutic agent, especially application of the polycyclic compound as a BTK inhibitor or degradation agent and application of the polycyclic compound in preparation of drugs for treating and / or preventing BTK-mediated or dependent diseases or symptoms. Wherein each group in the general formula (I) is defined in the specification.

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts or deuterated forms thereof, wherein R0, L and R1 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

The present invention relates to a compound of the formula (i) wherein Ar represents a phenyl or a 6-membered heteroaryl group, R1 and R2 represent independently a hydrogen atom or a deuterium atom, R3 represents (1) a —COR4 group, (2) a —BOR5OR6 group, (3) a —X—Z group, (4) a (C1-C6)alkyl group or a (C1-C6)alkenyl group, (5) a —X—S(O)n(R7)p(R8)q group, (6) a halogen atom, a —NH2 group or a —CN group, (7) a —O—R11 group, (8) a —NH—COR9 group, (9) a —C(═NH)NHOH group, (10) a —NH—C(NH)—R9′ group, or (11) a —NHCOCOOR12 group or a —NHCOCONR12′R12″ group, X represents a bond, a —NH— group, a —CONH— group or a —CO— group, Z represents a 4 or 5-membered cycloalkyl, a 4 or 5-membered heterocylcloalkyl group, a 4 or 5-membered heteroaryl group or a phenyl group or a pharmaceutically acceptable salt thereof. The present invention further relates to a medicament comprising said compound of formula (I) and to said compound of formula (I) for use as an inhibitor and degrader of estrogen receptors.

The present application relates to a heteroaryl compound, a preparation method therefor, and the pharmaceutical use thereof. Specifically, the present application relates to a heteroaryl compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the heteroaryl compound, the use thereof as a therapeutic agent, particularly as a BTK inhibitor or degrader, and the use thereof in the preparation of a drug for treating and / or preventing BTK-mediated or dependent diseases or conditions. Each group in general formula (I) is as defined in the description.

The present invention belongs to the field of medical technology and specifically disclosed is a compound represented by formula (I′), or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and each symbol therein is as defined in the claims. The compound of the present invention may be used as a drug for regulating RET kinase activity or treating RET-related diseases, and has better pharmacokinetic properties.

The present disclosure provides compounds of Formula (I), (II), and (III). The provided compounds are able to bind protein kinases (e.g., SIK) and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase (e.g., SIK, (e.g., SIK1, SIK2, or SIK3)) in a subject or cell. The provided compounds may be useful in treating or preventing a disease (e.g., proliferative disease, musculoskeletal disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.

Solid pharmaceutical compositions containing an active pharmaceutical ingredient, such as a JAK inhibitor, and methods of treatment using such pharmaceutical compositions are described.

The present invention provides SETD2 protein inhibitors, as well as methods, compositions and kits for treating a disease, disorder or condition in a subject using a SETD2 protein inhibitor and optionally a second therapeutic agent, wherein the second therapeutic agent comprises one or more glycocortin receptor agonists, one or more immunomodulatory drugs, one or more proteasome inhibitors, one or more Bcl-2 inhibitors, one or more multi-effect pathway modulators, one or more XPO1 inhibitors, and one or more pharmaceutically acceptable salts thereof, one or more histone deacetylase inhibitors or one or more EZH2 inhibitors, or a combination thereof.