cas 266690-48-6, 1-Amino-6-methoxyisoquinoline

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Method for synthesizing 1-aminoisoquinoline skeleton by rhodium-catalyzed 4-phenyl oxadiazolone and vinylene carbonate
The invention discloses a method for generating 1-aminoisoquinoline and a derivative thereof through a rhodium-catalyzed reaction of a 4-phenyl oxadiazolone compound and vinylene carbonate. According to the invention, a 4-phenyl oxadiazolone compound is used as a raw material and reacts with vinylene carbonate under the catalysis of transition metal rhodium to generate an isoquinoline ring. The synthesis operation steps are simple, the atom economy is high, the application range of the substrate is wide, the post-treatment operation is simpler, the implementation feasibility is high, and a foundation is laid for industrial production and wide application of the aminoisoquinoline compound.
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Paragraph 0016-0017

(2021/12/07)

Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors
Fragment-based NMR screening of a small literature focused library led to identification of a historical thrombin/FactorXa building block, 17A, that was found to be a ROCK-I inhibitor. In the absence of an X-ray structure, fragment growth afforded 6-substituted isoquinolin-1-amine derivatives which were profiled in the primary ROCK-I IMAP assay. Compounds 23A and 23E were selected as fragment optimized hits for further profiling. Compound 23A has similar ROCK-1 affinity, potency and cell based efficacy to the first generation ROCK inhibitors, however, it has a superior PK profile in C57 mouse. Compound 23E demonstrates the feasibility of improving ROCK-1 affinity, potency and cell based efficacy for the series, however, it has a poor PK profile relative to 23A.
Ray, Peter,Wright, Jane,Adam, Julia,Bennett, Johnathan,Boucharens, Sylviane,Black, Darcey,Cook, Andrew,Brown, Angus R.,Epemolu, Ola,Fletcher, Dan,Haunso, Anders,Huggett, Margaret,Jones, Phil,Laats, Steven,Lyons, Amanda,Mestres, Jordi,De Man, Jos,Morphy, Richard,Rankovic, Zoran,Sherborne, Brad,Sherry, Lorcan,Van Straten, Nicole,Westwood, Paul,Zaman, Guido Z.R.
supporting information; scheme or table
p. 97 - 101
(2011/02/28)

6-SUBSTITUTED ISOQUINOLINE DERIVATIVES
The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.
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Page/Page column 5

(2008/06/13)

2-(ARYLOXY)ACETAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.
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(2008/06/13)

PHENYLGLYCINAMIDE DERIVATIVES USEFUL AS ANTICOAGULANTS
The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it is directed to novel phenylglycinamide derivatives, and analogues thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
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Page/Page column 150-153

(2008/06/13)

Serine protease inhibitor
A serine protease inhibitor having the formula (I), in which J is H, R1, R1—O—C(O)—, R1—C(O—, R1—SO2—, R3OOC—(CHR2)p—, (R2a,R2b)N—CO—(CHR2)p— or Het-CO—(CHR2)p—;W is an amino-acid of the formula —NH—CHR1—C(O)—, —NR4—CH((CH2)qC(O)OR1)—C(O)—, —NR4—CH((CH2)qC(O)N(R2a,R2b))—C(O)—, —NR4—CH((CH2)qC(O)Het)-C(O)—, D-1-Tiq, D-3-Tiq, D-Atc, Aic, D-1-Piq, D-3 Piq, glutanyl or a (C1-C6) alkylester thereof;E is —NR2—CH2— or the fragment ?which is unsubstituted or substituted with (1-6C)alkyl, (1-6C)alkoxy or benzyloxy;R1 is selected form (1-12C)alkyl, (2-12C)alkenyl, (2-12C)alkynyl, (3-12C)cycloalkyl and (3-12C)cycloalkyl(1-6C)alkylene, which groups are unsubstituted or substituted with (3-12C)cycloalkyl, (1-6C)alkoxy, oxo, OH, CF3 or halogen, and from (6-14C)aryl, (7-15C)aralkyl, (8-16C)aralkenyl and (14-20C)(bisary)alkyl, wherein the aryl groups are unsubstituted or substituted with (1-6C)alkyl, (3-12C)cycloalkyl, (1-6C)alkoxy, OH, CF3 or halogen;R2, R2a and R2b are each independently selected from H, (1-C)alkyl, (3-8C)alkenyl, (3-8C)alkynyl, (3-8C)cycloalkyl and (3-6C)cycloalkyl(1-4C)alkylene, which are unsubstituted or substituted with (3-6C)cycloalkyl, (1-6C)alkoxy, CF3 or halogen, and from (6-14C)aryl and (7-15C)aralkyl, wherein the aryl groups are unsubstituted or substituted with (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)alkoxy, CF3 or halogen;R3 is the same as R2 or is Het-(1-6C)alkyl;R4 is H or (1-3C)alkyl;X and Y are CH or N, with the proviso that they are not both N;Het is a 4-, 5- or 6-membered heterocycle containing one or more heteroatoms selected from O, N and S;m is 1 or 2;p is 1, 2 or 3;q is 1, 2 or 3;t is 2, 3 or 4;or a pharmaceutically acceptable addition salt or solvate thereof.
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Page/Page column 10

(2010/02/11)