307313-03-7

Usage

Uses

Used in Pharmaceutical Industry:
Pyrazolo[1,5-a]pyridine-2-carboxylic acid, 4,5,6,7-tetrahydro(9CI) is used as a potential pharmaceutical compound for its possible biological activities. Its heterocyclic structure, which includes both a pyrazole and a pyridine ring, suggests that it may have therapeutic applications, although the specific uses and mechanisms of action are yet to be determined through further research and development.

Upstream product

• 63237-88-7 pyrazolo[1,5-a]pyridine-2-carboxylic acid 
• 105786-95-6 4,5,6,7-tetrahydro<1.2.3>oxadiazolo<3,4-a>pyridin-3-one 
• 4043-87-2 pipecolic Acid 
• 307307-82-0 methyl 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-2-carboxylate 
• 98303-20-9 1-(tert-butoxycarbonyl)piperidine-2-carboxylic acid 
• 132910-79-3 (+/-) methyl N-tert-butyloxycarbonyl 2-piperidinecarboxylate 
• 4515-18-8 1-nitroso-piperidine-2-carboxylic acid 
• 307307-84-2 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-2-carboxylic acid ethyl ester 

Downstream Products

• 307313-04-8 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-carboxylic acid chloride 
• 1367714-07-5 C₂₀H₂₄F₂N₄O 
• 623564-49-8 (4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yl)methanol 

Relevant academic research and scientific papers

Focal adhesion kinase inhibitor and use

The invention belongs to the field of medicines, relates to a focal adhesion kinase inhibitor and use, in particular relates to a novel focal adhesion kinase inhibitor compound, or stereoisomers, geometric isomers, tautomers, oxynitrides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, further relates to the use of the compound and pharmaceutical compositions as medicines, in particular the use of the compound and pharmaceutical compositions in manufacture of medicines for treatment or prevention of cancer, pulmonary hypertension, and pathological angiogenesis-related diseases.

A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core

A series of potent non-acetylinic negative allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5 NAMs) was developed starting from HTS screening hit 1. Potency was improved via iterative SAR, and physicochemical properties were optimized to deliver orally bioavailable compounds acceptable for in vivo testing. A lead molecule from the series demonstrated dose-dependent activity in the second phase of the rat formalin test from 30 mg/kg, and a preliminary PK/PD relationship was established.

Identification of fused bicyclic heterocycles as potent and selective 5-HT2A receptor antagonists for the treatment of insomnia

A series of fused bicyclic heterocycles was identified as potent and selective 5-HT2A receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties, and significant improvements on deep sleep (delta power) and sleep consolidation.

The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics

This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and good oral bioavailability in man. Optimisation of the preclinical profile resulted in the identification of UK-369003 (19a) and its nomination as a clinical candidate. The clinical pharmacokinetic and safety profile has enabled us to progress the compound to test its efficacy in patients with lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH) and a paper describing its efficacy has recently been published.2,3.

PYRAZOLE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS

The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10- alkenyl, C2-C10-alkynyl, etc.; n is 0 to 4; or two radicals Rpx bound to the same ring- member may form an oxo substituent, or two radicals Rpx bound to adjacent ring- members may form a 3- to 7-membered fused cyclic radical; B is N or CR4, wherein R4 is H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, etc.; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkyl, etc.; X2 is O2a, NR2bR2c or S(O)mR2d, wherein m is 0, 1 or 2; R2a is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R1 is H, CN, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, etc.; R2, R3 and R5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, etc.; to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material comprising at least one compound of formulae I or II, to a method for treating or protecting an animal from infestation or infection by parasites, to novel pyrazole compounds of formulae I or Il and agricultural composition containing those compounds.

INDOLIZINE CARBOXAMIDES AND THE AZA AND DIAZA DERIVATIVES THEREOF

The invention relates to neuroreceptor-active carboxamide-substituted indolizine derivatives of general formula (I) wherein X represents a group of general formula (X1).

Pyrazolopyrimidine derivatives

The present invention provides a compound of formula (I): where Q is a group of formula: These compounds inhibit cyclic guanosine 3',5'-monophosphate phosphodiesterases (cGMP PDEs). More notably, the compounds are potent and selective inhibitors of the type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases and have utility therefore in a variety of therapeutic areas. In particular, the present compounds are of value for the curative or prophylactic treatment of mammalian sexual disorders.