51 results about "Neurocatin" patented technology

Pharmaceutical compositions for intravenous administration comprising the compound of Formula Ior pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and / or emesis with the pharmaceutical compositions are also described herein.

Pharmaceutical compositions for intravenous administration comprising the compound of Formula Ior pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and / or emesis with the pharmaceutical compositions are also described herein.

The disclosure relates to the use of neurokinin-1 (NK-1) antagonists, such as serlopitant, MK-0303 or MK-8478, in alleviating or suppressing cough (including acute, subacute and chronic cough) and urge to cough. The cough can have an unknown cause (idiopathic cough) or can be associated with any type of medical condition, such as a respiratory disorder. The NK-1 antagonist can be delivered by oral inhalation for more rapid peripheral and central antitussive action. Another antitussive agent in addition to the NK-1 antagonist can optionally be administered for the treatment of the cough or urge to cough, or the cough-associated medical condition.

The present invention relates compounds of Formula (A) as NK-1 receptor antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to NK-1 receptor in humans. More specifically, the compounds and / or pharmaceutical compositions of the present invention are believed to potentially offer therapeutic benefits to patients who suffer, among others, chemotherapy-induced nausea and vomit (CINV) and / or post-operative nausea and vomit (PONV).

The invention provides a medicinal composition containing a neurokinin 1(NK-1) receptor antagonist, a 5-hydroxytryptamine 3 (5HT-3) receptor antagonist and adrenocortical hormone. The medicinal composition adopts a NK-1 receptor antagonist, a 5HT-3 receptor antagonist and adrenocortical hormone as active components, is added with certain auxiliaries with specific spices and proportion to prepare and develop an oral preparation according to a technical means specified in the invention. The medicinal composition can be used for preventing and treating nausea and emesis caused by cancer radiotherapy, chemotherapy and operation. The invention aims to provide a medicinal composition preparation which can prevent and treat emesis more conveniently by utilizing the NK-1 receptor antagonist, the 5HT-3 receptor antagonist and adrenocortical hormone, thereby improving the compliance of a patient.

The invention relates to an anti-hepatoma effect of an antagonist SR140333 of a neurokinin receptor 1, in particular to a method for treating hepatoma of a subject, relieving a hepatoma symptom of the subject or inhibiting hepatoma cell proliferation, an application of the antagonist of the neurokinin receptor 1 in preparing medicine, an reagent or a medicine composition for treating the hepatoma, relieving the hepatoma symptom or inhibiting the hepatoma cell proliferation, and a pharmaceutical product. The pharmaceutical product comprises the antagonist SR140333 of the neurokinin receptor 1 as an active ingredient and a specification of the pharmaceutical product.

The invention relates to compounds of general Formula I: wherein the variables are as defined herein. Also provided are pharmaceutical compositions comprising such compounds, and methods for treating patients suffering from a disorder responsive to neurokinin-3 receptor modulation. NK-3 receptor modulators provided herein are also useful as probes for the localization of NK-3 receptors.

A method and solution for perioperatively inhibiting tumor cell adhesion and a variety of pain and inflammation processes at wounds from general surgical procedures including oral / dental procedures. The solution preferably includes at least one anti-tumor cell adhesion agent and multiple pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for preemptive inhibition of pain and while avoiding undesirable side effects associated with oral, intramuscular, subcutaneous or intravenous application of larger doses of the agents. One preferred solution to inhibit tumor cell adhesion, pain and inflammation includes at least one anti-tumor cell adhesion agent, a serotonin2 antagonist, a serotonin3 antagonist, a histamine antagonist, a serotonin agonist, a cyclooxygenase inhibitor, a neurokininl antagonist, a neurokinin2 antagonist, a purinoceptor antagonist, an ATP-sensitive potassium channel opener, a calcium channel antagonist, a bradykininl antagonist, a bradykinin2 antagonist and a mu -opioid agonist.

Compounds and methods for the prevention and / or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor, based on 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)3yridine-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium and pharmaceutically acceptable salts thereof.

The invention discloses an external preparation of a series of neurokinin-1 receptors (NK1 receptors) inhibitors and a preparation method of the external preparation. The NK1 receptor inhibitors comprise, but are not limited to, aprepitant, fosaprepitant, rolapitant, netupitant or pharmaceutically acceptable salts thereof. The external preparation comprises, but is not limited to, ointment, cream, gel, tincture, lotion, aerosol, spray, liniment, a foaming agent, patch, emplastrum and the like. The external preparation of the NK1 receptor inhibitors can slowly deliver the medicine at a constant speed, and reduce the blood concentration fluctuation caused by dissolution and absorption of the oral medicine; the pertinence to local lesions can be improved, and the side effects of the whole body are reduced; and meanwhile, a choice with high compliance is provided for patients inconvenient to take orally, and the external preparation has important significance in relieving the pain of cancer patients clinically.

The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and / or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Neurokinin 1 receptor (NK1R) agonist mediated protection of the eye is described. The protection can reduce dry eye and ocular infections, particularly in individuals with reduced NK1R activity.

Disclosed herein are novel pharmaceutical formulations of a neurokinin-1 (NK-1) receptor antagonist suitable for parenteral administration including intravenous administration. Also included are formulations including both the NK-1 receptor antagonist and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.

The invention relates to a crystal form of a neurokinin-1 antagonist and a preparation method of the crystal form. Specifically, the invention relates to an A crystal of a compound shown as a formula II and a preparation method thereof. The novel crystal form disclosed by the invention has good physicochemical properties and is more beneficial to clinical treatment.

The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(═O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(═O)R7, C(═O)OR7, C(═O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(═O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ═CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments.

The invention relates novel NK1 receptor antagonists represented in formula A, wherein R1 and R2 independently are selected from the group consisting of (C1-4)alkyl, (C1-4)haloalkyl, (C1-4)alkoxy, CD3 or halogen; R3 is selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)haloalkyl and (C1-4)hydroxyalkyl; R4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R5 and R6 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)hydroxyalkyl and (C1-4)haloalkyl and X and Y are independently selected from the group consisting of CH and N. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds.

The invention relates to a salt, a crystal form and a preparation method of a neurokinin-1 antagonist. Specifically, the invention relates to a sodium salt of a compound shown as a formula II, a crystal A of the sodium salt and a preparation method. The novel crystal form disclosed by the invention has good physicochemical properties and is more beneficial to clinical treatment.

Fertilized egg isolate, methods for preparing the fertilized egg isolate and uses thereof for treating mental health disorders and disease or conditions mediated by or associated with one or more glutamate receptors or by the neurokinin 2 (NK2) receptor.

A prophylactic or therapeutic agent for an IL-31 mediated disease, said agent comprising a neurokinin B signal blocker.

Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, R1 and R2 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.

The present invention relates to compounds and their uses. In particular, to compounds that inhibit the interaction between β-arrestin and the intracellular C-terminus of the activated NK1R and their use in the treatment of pain.

The present invention relates compounds of Formula (A) as NK-1 receptor antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to NK-1 receptor in humans. More specifically, the compounds and / or pharmaceutical compositions of the present invention are believed to potentially offer therapeutic benefits to patients who suffer, among others, chemotherapy-induced nausea and vomit (CINV) and / or post-operative nausea and vomit (PONV).

Compounds, pharmaceutical compositions and methods of treating a disorder or disease associated with neurokinin 2 (NK2) receptor activity.

The disclosure relates to the use of neurokinin-1 (NK-1) antagonists in treating pruritus in a subject, wherein i) the duration of the pruritus is about one year or longer, ii) the subject is about 40 years of age or older: iii) the subject has no inflammatory skin disease; and / or iv) the pruritus is idiopathic.

The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(═O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(═O)R7, C(═O)OR7, C(═O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(═O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ═CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments.

Fertilized egg isolate, methods for preparing the fertilized egg isolate and uses thereof for treating mental health disorders and disease or conditions mediated by or associated with one or more glutamate receptors or by the neurokinin 2 (NK2) receptor.