947331-10-4

Usage

Uses

A Losartan derivative for treatment of hypertension

InChI:InChI=1/C41H35ClN6O2/c1-2-3-23-36-43-38(42)37(40(49)50)47(36)28-29-24-26-30(27-25-29)34-21-13-14-22-35(34)39-44-45-46-48(39)41(31-15-7-4-8-16-31,32-17-9-5-10-18-32)33-19-11-6-12-20-33/h4-22,24-27H,2-3,23,28H2,1H3,(H,49,50)

Upstream product

• 124750-99-8 cozaar 
• 76-83-5 trityl chloride 
• 124750-92-1 2-butyl-4-chloro-1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylic acid 
• 114798-26-4 lorsartan 

Downstream Products

• 1034453-10-5 1-[({[(5R)-5,6-bis(nitrooxy)hexyl]oxy}carbonyl)oxy]ethyl 2-butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylate 
• 947331-26-2 C₄₇H₄₅ClN₆O₅ 
• 947331-18-2 C₄₈H₄₇ClN₆O₅ 
• 947330-97-4 2-butyl-4-chloro-1-[2'-(1H-tetrazol-5-yl) 1,1'-biphenyl-methyl]imidazole-5-carboxylic acid ethyl ester 
• 947331-22-8 2-butyl-4-chloro-1-[(2'-(1-triphenylmethyl-1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl]imidazole-5-carboxylic acid 1-[(isopropoxy)carbonyloxy]methyl ester 
• 947331-24-0 C₄₅H₄₁ClN₆O₅ 
• 947331-12-6 C₄₉H₃₉ClN₆O₄ 
• 947331-16-0 C₄₇H₄₅ClN₆O₅ 
• 947331-15-9 C₄₇H₄₅ClN₆O₄ 
• 947331-20-6 C₅₀H₄₉ClN₆O₅ 
• 947331-14-8 C₄₆H₃₉ClN₆O₅ 
• 1173931-76-4 O⁽²⁾-(3-(((1-(((2-butyl-4-chloro-1-((2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1H-imidazol-5-yl)carbonyl)oxy)ethoxy)carbonyl)oxy)propyl) 1-(N,N-diethylamino)diazen-1-ium-1,2-diolate 
• 1177456-92-6 O₂-({[(2-butyl-4-chloro-1-{[2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)carbonyl]oxy}methyl) 1-[2S-(hydroxymethyl)pyrrolidin-1-yl]diazen-1-ium-1,2-diolate 
• 1207855-66-0 {5-[5-(nitrooxy)pentyl]-2-oxo-1,3-dioxol-4-yl}-2-butyl-4-chloro-1-[[2'-(1-triphenylmethyltetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylate 

Relevant academic research and scientific papers

A process for preparing a renin - angiotensin - aldosterone system dual inhibitor compound of intermediate

The invention relates to an intermediate compound for preparing RAAS (renin-angiotensin-aldosterone system) dual inhibitor compounds. RAAS dual inhibitors can be used for treating diseases related to an RAAS such as high blood pressure and heart diseases.

RAAS system as a dual inhibitor compounds

The invention discloses a compound used as a dual inhibitor for RAAS (rennin angiotensin aldosterone system) and particularly relates to a compound shown in formula (I), a stereisomer thereof or a pharmaceutically acceptable salt thereof. The compound can be used for treating and blocking RAS-associated diseases such as hypertension and heart disease, can be used for preventing or treating hypertension, congestive heart failure, pulmonary hypertension, renal insufficiency, renal ischemia, kidney failure, renal fibrosis, cardiac insufficiency, cardiac hypertrophy, cardiac fibrosis, myocardial ischemia, cardiomyopathy, glomerulonephritis, renal colic, complications such as nephropathy caused by diabetes, vasculopathy, vasculopathy, glaucoma, intraocular pressure elevation, atherosis, restenosis after revascularization, complications after blood vessel or cardiac operation, erectile dysfunction, hyperaldosteronism, lung fibrosis, scleroderma, anxiety, cognitive disorder, complications caused by immunosuppressor treatment as well as other known diseases associated with the rennin angiotensin aldosterone system.

ANGIOTENSIN II RECEPTOR ANTAGONISTS

The present invention relates to nitrooxyderivatives of angiotensin II receptor antagonist having the general formula (I): where in R is selected f rom the group consisting of (IIa) - (IIk): when R is selected from (Ilk), Y is selected from the group consisting of: 1) -C(O) (CH2) nR5; 2) -C(O)(CH2n-O-CH2-R5; 3) -C(O)-R6 wherein R6 is the following group: when R is selected from (IIa)-(IIh), Y is selected from the group consisting of: 4) -C(R1R2)OC(O)-(CH2)nR5; 5) -C(R1R2)OC(O)O-(CH2)nR5; 6) C(R1R2)OC(O)(CH2)n-O-CH2-R5; 7) C(R1R2)OC(O)O(CH2)n-O-CH2-R5; 8) -C(R1R2)OC(O)-R6 wherein R6 is as above defined; R1 and R2 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is -CH(ONO2)R7; R7 is CH3 or C1-4 alkyl; n is an integer from 1 to 4; or a pharmaceutically acceptable salt thereof.

ANGIOTENSIN II RECEPTOR ANTAGONISTS

A compound having the structure (I) wherein R is an angiotensin II receptor antagonist selected from the group consisting of (IIa)- (IIh); A is (Formula) wherein Rl and R2 are independently selected from the group consisting of hydrogen and C1-4 alkyl. Y is X0-Z wherein X0 is selected from the group consisting of: -O-, -O-CO-, -OCOO-, -OCONH- and -OSO2-; Z is a nitric oxide releasing moiety, or a pharmaceutically acceptable salt thereof.

Imidazole-5-Carboxylic Acid Derivatives, The Preparation Method Therefor and The Uses Thereof

The invention discloses imidazole-5-carboxylic acid derivatives, and their preparation methods. The derivatives of the invention are Angiotensin II receptor antagonists with angiotensin II antagonistic activity and antihypertensive activity, and thereby can be used as a therapeutical agent to treat hypertension.

ANGIOTENSIN II RECEPTOR ANTAGONISTS

A compound having the structure (A) wherein R is an angiotensin receptor antagonist active group, and Y is 1) -(CH2)3R5, 2) -C(O)(CH2)2R5, 3) -C(R1R2)OC(O)O(CH2)nR5, wherein n is 1 or 2, 4) -C(R1R2)OC(O)CH2CH2R5, 5) -C(R1R2)OC(O)OCH2CH2C(R3R4)R5, Formula (B), and Formula (C) provided that when Y is -C(O)(CH2)2R5, then R is Formula (D) R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is CH(ONO2)CH(ONO2)R6; R6 is selected from CH3, CH2CH3 and CH(CH3)2; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.

SALTS OF IMIDAZOLE-5-CARBOXYLIC ACID DERIVATIVES, A METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME

The present invention provides pharmaceutically acceptable salts of imidazole-5-carboxylic acid derivatives, methods for preparing same and pharmaceutical compositions comprising same. The salts obtained by the present invention can be easily dissolved in

IMIDAZOL-5-CARBOXYLIC ACID DERIVATIVES, PREPARATION METHODS AND USE THERROF

The invention discloses imidazole-5-carboxylic acid derivatives, and their preparation methods. The derivatives of the invention are Angiotensin II receptor antagonists with angiotensin II antagonistic activity and antihypertensive activity, and thereby can be used as a therapeutical agent to treat hypertension.