37 results about "P2y1 receptor" patented technology

The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.

The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.

The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.

The present invention provides novel urea mimics and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, W, and R6 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.

The present invention provides novel urea mimics and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, W, and R6 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

The present invention provides indole compounds of Formula (I) or (II):or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables ring A, X1, X2, X3, X4, R6, and R15 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

The present invention provides novel C-linked cyclic compounds and analogues of Formula (I):or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.

The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.

The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.

The present invention provides compounds of Formula (I) that are useful for binding and / or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and / or conditions in which modulation of MC1R is beneficial. Such diseases and / or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.

Y4 receptor agonist peptide selected from the group consisting of: [Ala30]PP2-36, [Thr30]PP2-36, [Asn30]PP2-36, [Gln30]PP2-36, [Glu10]PP2-36, [Glu10,Leu17,Thr30]PP2-36, [Nle17,Nle30]PP2-36, [Glu10,Nle17,Nle30]PP2-36, their PP1-36 equivalents, and analogues and derivatives thereof as described in the specification, are selective agonists of the Y4 receptor relative to the Y1 and Y2 receptors, and are useful in the treatment, for example, of obesity and overweight, and conditions in which these are considered contributory factors, and in the treatment of diarrhoea and intestinal hypersecretion.

A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.

The invention provides a reagent card for detecting the therapeutic effect of thienopyridine antiplatelet drugs and an application method and application of the reagent card. The reagent card comprises four detection channels which are sequentially arranged in parallel and are independent of one another, the detection channel I contains channel I detection reagent, and the channel I detection reagent contains a lyophilized agent, wherein the lyophilized agent is obtained by firmly bonding activated dye microspheres with receptor ligand of blood platelets GpIIb / IIIa through amido bonds, then adding blood coagulation factors, and conducting freeze-drying; the detection channel II contains channel II detection reagent, and the channel II detection reagent contains a lyophilized agent serving as a blood platelet maximum activating agent; the detection channel III contains no detection reagent, the detection channel IV contains channel IV detection reagent, and the channel IV detection reagent contains a lyophilized agent serving as a blood platelet P2Y12 receptor activating agent and P2Y1 receptor antagonist. By means of the reagent card, the therapeutic effect of thienopyridine antiplatelet drugs can be detected easily, fast, conveniently and accurately.

Novel p75 receptor antagonist compounds and compositions and uses thereof for the prevention and treatment of p75-associated disorders, such as neurodegenerative diseases, are described.

The present invention provides methods for treating inflammation in the lungs of a subject in need of such treatment, comprising the step of administering an effective amount of a composition comprising b-nicotinamide adenine dinucleotide to the subject. Also provided is a method of increasing integrity of a vascular barrier in a subject, comprising the step of contacting one or both of human P2Y1 receptors or P2Y11 receptors in the subject with an amount of a composition comprising beta-nicotinamide adenine dinucleotide effective to activate the receptors; wherein activation thereof increases the integrity of the vascular barrier in the subject.

The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and / or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.

The invention discloses a P2Y1 / U2OS cell strain and a preparation method and application thereof and belongs to the technical field of high throughput screening and detection of drugs. The P2Y1 / U2OS cell strain is prepared by the following steps: firstly establishing a human P2Y1 receptor fluorescin eukaryotic expression vector P2Y1 / pCMV6 and then transfecting a U2SO cell according to a Lipofectamine2000 operating manual; and screening the G418 (400 mu g / ml) in a pressurized manner for 2 weeks to obtain the P2Y1 / U2OS cell strain. The P2Y1 / U2OS cell strain disclosed by the invention and used for determining the biological activity of a P2Y1 receptor stimulant or an antagonist is easy to standardize and good in repeatability, has the characteristics of high specificity and sensitivity, low using cost and convenient operation for the P2Y1 receptor, and has a good application prospect in drug screening and efficacy evaluation.

The present invention provides novel ureas containing N / -aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are defined herein. These compounds are selective inhibitors of the human P2Y, receptor which can be used as medicaments for treating thromboembolic disorders.

The invention provides a P2Y12 receptor platelet aggregation detection reagent card and a production method thereof. The P2Y12 receptor platelet aggregation detection reagent card comprises four detection channels, the first channel contains a lyophilized reagent coated with BSA and fibrinogen and contains no activators, the second channel contains a lyophilized reagent coated with the BSA and fibrinogen and also contains a platelet maximum activator iso-TRAP (thrombin receptor activating peptide), the third channel contains no lyophilized reagents, and the fourth channel contains the lyophilized reagent coated with the BSA and fibrinogen, and also contains a platelet P2Y12 receptor activator ADP (adenosine diphosphate) and a P2Y1 receptor antagonist PGE1 (prostaglandin E1). The patient'sP2Y12 receptor pathway-correlated platelet aggregation function is rapidly and effectively detected through optical nephelometry by using the detection reagent card. The card has the advantages of high sensitivity, strong specificity, easiness in operation, and suitableness for bedside fast detection, and can well predict the future thrombus or bleeding risk in patients treated with the P2Y12 receptor antagonists.

The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor and may be used as medicaments in the treatment and / or prophylaxis of thromboembolic disorders.

The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used as medicaments.

The present invention provides compounds of Formula (I): Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used medicaments.

The present invention provides novel heteroaryl compounds of formula (Ia) which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity. (Ia) or a stereoisomer, tautomer, pharmaceutically acceptable salt, or solvate thereof, wherein: ring A is a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-4 ringheteroatoms selected from N, NR11, S(O)p, and O, wherein said heteroaryl is substituted with 0-4 R1; ring B is phenyl substituted with 0-4 R7, pyridyl substituted with 0-3 R7, or thienyi substituted with 0-2 R7; X is NH or NMe; Y is O or S; R5 is a -(CRfRf)n-C3-10 carbocycle substituted with 1-4 R5a, or a -(CRfRf)n-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NR11, O, and S(O)p, wherein said heterocycle is substituted with 0-4 R5a; the other substituents and variables are defined in the claims.