170097-67-3

Usage

Uses

Used in Pharmaceutical Industry:
2-(TERT-BUTOXYCARBONYL)-1,2,3,4-TETRAHYDROISOQUINOLINE-6-CARBOXYLIC ACID is used as a starting material for the synthesis of benzazole derivatives. These derivatives have potential applications as β-secretase inhibitors, which are important in the treatment and prevention of diseases, particularly those related to the central nervous system.
In the context of pharmaceutical research and development, 2-(TERT-BUTOXYCARBONYL)-1,2,3,4-TETRAHYDROISOQUINOLINE-6-CARBOXYLIC ACID serves as a key intermediate in the synthesis of novel therapeutic agents. The benzazole derivatives, which are derived from N-Boc-1,2,3,4-Tetrahydroisoquinoline-6-carboxylic Acid, are of particular interest due to their potential to modulate the activity of β-secretase, an enzyme implicated in the pathogenesis of various neurodegenerative diseases. By inhibiting this enzyme, these derivatives may help slow down or halt the progression of these diseases, offering new treatment options for patients.

InChI:InChI=1/C15H19NO4/c1-15(2,3)20-14(19)16-7-6-10-8-11(13(17)18)4-5-12(10)9-16/h4-5,8H,6-7,9H2,1-3H3,(H,17,18)

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 893566-74-0 6-bromo-2-(tert-butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline 
• 124-38-9 carbon dioxide 
• 877861-62-6 methyl 1,2,3,4-tetrahydroisoquinoline-6-carboxylate hydrochloride 
• 158984-84-0 6-trifluoromethanesulfonyloxy-3,4-dihydro-1H-isoquinoline-2-carboxylic acid tert-butyl ester 
• 158984-83-9 N-tert-butoxycarbonyl-6-hydroxy-1,2,3,4-tetrahydroisoquinoline 
• 63905-73-7 6-hydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride 
• 170097-66-2 3,4-Dihydro-1H-isoquinoline-2.6-dicarboxylic acid 2-tert-butyl ester-6-methyl ester 
• 173089-82-2 isoquinoline-6-carboxylic acid methyl ester 
• 106778-42-1 isoquinoline-6-carbonitrile 
• 185057-00-5 methyl 1,2,3,4-tetrahydroisoquinoline-6-carboxylate 
• 1194550-56-5 5,7-dichloro-2-trityl-1,2,3,4-tetrahydroisoquinoline-6-carboxylic acid 
• 226942-29-6 6-bromo-1,2,3,4-tetrahydroisoquinoline 
• 34784-05-9 6-bromo-isoquinoline 

Downstream Products

• 1111882-14-4 1,1-dimethylethyl 6-[({1-[(3,4-dichlorophenyl)methyl]-5-methyl-1H-1,2,3-triazol-4-yl}amino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinecarboxylate 
• 947672-49-3 3-(4-(2-(cyclopropylsulfonyl)-1,2,3,4-tetrahydroisoquinolin-6-ylamino)-5-methylpyrimidin-2-ylamino)benzenesulfonamide 
• 1202755-95-0 3-(4-(2-(2-chloroacetyl)-1,2,3,4-tetrahydroisoquinolin-6-ylamino)-5-methylpyrimidin-2-ylamino)benzenesulfonamide 
• 1202759-69-0 C₂₀H₂₂N₆O₂S 
• 164148-92-9 tert-butyl 6-amino-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 1200399-64-9 N-{5-[(4-chlorophenyl)methyl]-1,3-thiazol-2-yl}-1,2,3,4-tetrahydro-6-isoquinolinecarboxamide hydrochloride 
• 1200399-90-1 N-{2-[(4-chlorophenyl)methyl]-4-methyl-1,3-thiazol-5-yl}-1,2,3,4-tetrahydro-6-isoquinolinecarboxamide hydrochloride 
• 1200399-91-2 N-{4-[(3-nitrophenyl)methyl]-1,3-thiazol-2-yl}-1,2,3,4-tetrahydro-6-isoquinolinecarboxamide hydrochloride 
• 1200399-98-9 N-(4-methyl-5-{[(phenylmethyl)amino]carbonyl}-1,3-thiazol-2-yl)-1,2,3,4-tetrahydro-6-isoquinolinecarboxamide 
• 1035189-06-0 N-(5-methyl-1-{[2-(methyloxy)phenyl]methyl}-1H-pyrazol-3-yl)-1,2,3,4-tetrahydro-6-isoquinolinecarboxamide hydrochloride 
• 949922-27-4 1-(1,2,3,4-tetrahydroisoquinolin-6-yl)ethanone 
• 1598386-37-8 4-(5-bromo-2-(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinoline-6-carbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxamido)benzoic acid trifluoroacetate 
• 1579517-52-4 C₃₁H₃₄N₄O₄ 
• 1579517-50-2 C₃₆H₄₂N₄O₆ 

Relevant academic research and scientific papers

Discovery of HDAC6-Selective Inhibitor NN-390 with in Vitro Efficacy in Group 3 Medulloblastoma

Histone deacetylase 6 (HDAC6) has been targeted in clinical studies for anticancer effects due to its role in oncogenic transformation and metastasis. Through a second-generation structure–activity relationship (SAR) study, the design, and biological eval

INHIBITORS OF MLH1 AND/OR PMS2 FOR CANCER TREATMENT

The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process: Formula (I) wherein R1, R2, R3, R4, R6

Lifitegrast impurity and preparation method thereof

The invention discloses a lifitegrast impurity I and a preparation method thereof. The lifitegrast impurity I can be prepared by a directional synthesis method through structural analysis of the impurity, and the preparation method specifically comprises the following steps: taking I-2 as a starting raw material, and performing multi-step reaction to obtain the lifitegrast impurity I. The structural formula of the lifitegrast impurity I is as shown in the specification. The impurity prepared by the method is high in purity, the problem of difficulty in preparation of the lifitegrast impurity is solved, and the application of the impurity in quality control of a lifitegrast raw material and a preparation thereof is provided, so that the medication safety of lifitegrast is improved.

Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation

Protein arginine methyltransferases 5 (PRMT5) represents an attractive drug target in epigenetic field for the treatment of leukemia and lymphoma. Here, a series of N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)amide derivatives targeting PRMT5 were designed with structure-based approach and synthesized. Among them, compound 46 showed potent and selective PRMT5 inhibition activity with an IC50 of 8.5 nM, which was approximately equivalent with the phase I clinical trial PRMT5 inhibitor GSK-3326595 (IC50 = 5.5 nM). Compound 46 also displayed pronounced anti-proliferative activity in MV4-11 cells (GI50 = 18 nM) and antitumor activity in MV4-11 mouse xenografts model. This molecule can serve as an excellent tool compound for probing the biological function of PRMT5.

HETEROCYCLIC COMPOUND

The problem of the present invention is to provide a compound having a superior RORγt inhibitory action, and useful as a prophylactic or therapeutic agent for psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, rheumatoid arthritis, multiple sclerosis, uveitis, asthma, ankylopoietic spondylarthritis, systemic lupus erythematosus, chronic obstructive pulmonary disease or the like. The present invention relates to a compound represented by the formula (I): [wherein each symbol is as described in the DESCRIPTION] or a salt thereof, which has an RORγt inhibitory action, and useful as a prophylactic or therapeutic agent for psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, rheumatoid arthritis, multiple sclerosis, uveitis, asthma, ankylopoietic spondylarthritis, systemic lupus erythematosus, chronic obstructive pulmonary disease or the like.

NOVEL sEH INHIBITORS AND THEIR USE

The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R5a, R6a, A, B, Y, I, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

PYRAZOLE COMPOUNDS AS PROSTAGLANDIN RECEPTORS LIGANDS

Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein Z, R1 ,R2a, R2b, R10, R11 and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element

Our exploratory study was based on the concept that a non-amidine factor Xa (fXa) inhibitor is suitable for an orally available anticoagulant. We synthesized and evaluated a series of N-(6-chloronaphthalen-2-yl) sulfonylpiperazine derivatives incorporating various fused-bicyclic rings containing an aliphatic amine expected to be S4 binding element. Among this series, 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine type 61 displayed orally potent anti-fXa activity and evident prolongation of prothrombin time (PT) with the moderate bioavailability in rats. The X-ray crystal analysis afforded an obvious binding mode that 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c] pyridine and 6-chloronaphthalene respectively bound to S4 and S1 subsites. In this X-ray study, we discovered a novel intramolecular S-O close contact. Ab initio energy calculations of model compounds deduced that conformers with the most close S-O proximity were most stable. The Mulliken population analysis proposed that this energy profile was caused by both of electrostatic S-O affinity and N-O repulsion. The results of these calculations and X-ray analysis suggested a possibility that the restricted conformation effected the affinity to S4 subsite of fXa.

Dipeptides which promote release of growth hormone

Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis. STR1

Acetic acid derivatives

Acetic acid derivatives of the formula STR1 wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.