Category: 362703-57-9

On April 22, 2004, King, Bryan W.; Sheppeck, James; Gilmore, John L. published a patent.Recommanded Product: 362703-57-9 The title of the patent was Preparation of triazolone and triazolethione inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme as anti-inflammatory agents. And the patent contained the following:

The present application describes novel hydantoin derivatives (shown as I; A = O, S; L-R11 represents a very large variety of substituents and is defined in the claims; e.g. II) or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof. Some examples of I exhibit Ki’s <10 μM but individual data are not presented. Although the methods of preparation are not claimed, 37 example preparations are included. For example, II was prepared in 4 steps (100, 66, 73 and 82%, resp.) starting with condensation of Et 4-aminobutyrate hydrochloride with 4-(2-methylquinolin-4-ylmethoxy)benzoyl chloride hydrochloride followed by base hydrolysis to the acid, followed by hydrazide formation with thiosemicarbazide followed by cyclization. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Recommanded Product: 362703-57-9

The Article related to triazolone triazolethione preparation inhibitor matrix metalloproteinase tace antiinflammatory, tnf alpha converting enzyme inhibitor triazolone triazolethione preparation, aggrecanase inhibitor triazolone triazolethione preparation and other aspects.Recommanded Product: 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 15, 2004, Duan, Jingwu; King, Bryan W.; Decicco, Carl; Maduskuie, Thomas P.; Voss, Mathew E. published a patent.Electric Literature of 362703-57-9 The title of the patent was Preparation of β-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-α. And the patent contained the following:

Novel β-amino acid derivatives A-CR3R4aCR2R4NR1CO-X-Z-Ua-Xa-Ya-Za [A = CO2H, SH, CH2SH, S(O)Ra:NH (Ra = H, alkyl), P(O)(OH)2, etc.; X, Xa is absent or alkylene, alkenylene or alkynylene; Z is absent or substituted C3-13 carbocycle or 5-14 membered heterocycle; Ua is absent or O, NRa1 [Ra1 = H, (un)substituted alkyl, alkenyl or alkynyl; Ra and Ra1 may form a ring], CO, CO2, O2C, CONRa1, S(O)p (p = 0-2), etc.; Ya is absent or O, NRa1, S(O)p or CO; Za is H, substituted C3-13 carbocycle or 5-14 membered heterocycle; R1 is H, alkyl, Ph, benzyl; R2 is Q (Q is H, substituted carbocycle or heterocycle), alkylene-Q, (CRaRa1)r1O(CRaRa1)r-Q (r, r1 = 0-4), (CRaRa1)r1NRa(CRaRa1)r-Q, etc.; R3 = Q1 (Q1 is any group given for Q), alkylene-Q1, (CRaRa1)r1O(CRaRa1)r-Q1, (CRaRa1)r1NRa(CRaRa1)r-Q1, etc.; R4, R4a = H, substituted alkyl, alkenyl or alkynyl; alternatively R1 and R2, R1 and R3, R3 and R4a may form rings (with provisos)] or a stereoisomer or pharmaceutically acceptable salt were prepared as metalloprotease and TNF-α inhibitors. Thus, N-hydroxy-1-[[4-[(2-methyl-4-quinolinyl)methoxy]phenyl]acetyl]-3-azetidinecarboxamide was prepared by a multistep procedure involving reactions of Me 4-hydroxyphenylacetate, 2-methyl-4-quinolinylmethanol, and 3-azetidinecarboxylic acid Me ester. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Electric Literature of 362703-57-9

The Article related to amino acid beta preparation inhibitor metalloprotease tnf, heterocyclyl beta amino acid preparation inhibitor metalloprotease tnf, cycloalkyl beta amino acid preparation inhibitor metalloprotease tnf and other aspects.Electric Literature of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 27, 2001, Duan, Jingwu; King, Bryan W.; Decicco, Carl; Maduskuie, Thomas P., Jr.; Voss, Matthew E. published a patent.Electric Literature of 362703-57-9 The title of the patent was Preparation of β-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-α. And the patent contained the following:

Novel β-amino acid derivatives A-CR3R4aCR2R4NR1CO-X-Z-Ua-Xa-Ya-Za [A = CO2H, SH, CH2SH, S(O)Ra:NH (Ra = H, alkyl), P(O)(OH)2, etc.; X, Xa is absent or alkylene, alkenylene or alkynylene; Z is absent or substituted C3-13 carbocycle or 5-14 membered heterocycle; Ua is absent or O, NRa1 [Ra1 = H, (un)substituted alkyl, alkenyl or alkynyl; Ra and Ra1 may form a ring], CO, CO2, O2C, CONRa1, S(O)p (p = 0-2), etc.; Ya is absent or O, NRa1, S(O)p or CO; Za is H, substituted C3-13 carbocycle or 5-14 membered heterocycle; R1 is H, alkyl, Ph, benzyl; R2 is Q (Q is H, substituted carbocycle or heterocycle), alkylene-Q, (CRaRa1)r1O(CRaRa1)r-Q (r, r1 = 0-4), (CRaRa1)r1NRa(CRaRa1)r-Q, etc.; R3 = Q1 (Q1 is any group given for Q), alkylene-Q1, (CRaRa1)r1O(CRaRa1)r-Q1, (CRaRa1)r1NRa(CRaRa1)r-Q1, etc.; R4, R4a = H, substituted alkyl, alkenyl or alkynyl; alternatively R1 and R2, R1 and R3, R3 and R4a may form rings (with provisos)] or a stereoisomer or pharmaceutically acceptable salt were prepared as metalloprotease and TNF-α inhibitors. Thus, N-hydroxy-1-[[4-[(2-methyl-4-quinolinyl)methoxy]phenyl]acetyl]-3-azetidinecarboxamide was prepared by a multistep procedure involving reactions of Me 4-hydroxyphenylacetate, 2-methyl-4-quinolinylmethanol, and 3-azetidinecarboxylic acid Me ester. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Electric Literature of 362703-57-9

The Article related to amino acid beta preparation inhibitor metalloprotease tnf, heterocyclyl beta amino acid preparation inhibitor metalloprotease tnf, cycloalkyl beta amino acid preparation inhibitor metalloprotease tnf and other aspects.Electric Literature of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem