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US 11,078,161 B2Granted
Rock-inhibiting compound and uses thereof
AssigneeHitgen Inc.
InventorsJin Li, Dengyou Zhang, Jingchao Feng, Wei Liao, Li Lin, Si Li
Life of this patent
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Abstract
Disclosed herein are a compound of formula (I) and a preparation method and uses thereof. The compound shows a good inhibitory activity against ROCK, providing a new medicinal strategy to clinically treat the diseases associated with abnormal ROCK activity.
Claims9
A compound of formula (II) or a stereoisomer thereof:
- wherein:
- R1 is selected from the group consisting of hydrogen, hydroxyl, halogen, amino, carboxyl, trifluoromethyl, nitro, cyano and C1-C6 alkyl;
- m is 0, 1, 2 or 3;
- R2 and R2′ are independently selected from the group consisting of hydrogen and C1-C6 alkyl;
- A ring is selected from the group consisting of 5- to 6-membered aromatic ring, 5- to 6-membered heteroaromatic ring and
- B ring and C ring are independently selected from the group consisting of 5- to 6-membered aromatic ring and 5- to 6-membered heteroaromatic ring;
- R4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, 3- to 6-membered cycloalkyl, 3- to 6-membered heterocycloalkyl, —(CH2)mORa, —(CH2)mOC(O)Ra, —(CH2)mOC(O)NRaRb, —(CH2)mNRaRb, —(CH2)mNRaC(O)Rb, —(CH2)mNRaC(O)ORb, —(CH2)mC(O)Ra, —(CH2)mC(O)ORa and —(CH2)mC(O)NRaRb;
- and
- Ra and Rb are independently selected from the group consisting of hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, substituted and unsubstituted 3- to 6-membered cycloalkyl, substituted and unsubstituted 3- to 6-membered heterocycloalkyl, substituted and unsubstituted 5- to 6-membered aromatic ring and substituted and unsubstituted 5- to 6-membered heteroaromatic ring, wherein the substituted 3- to 6-membered cycloalkyl, substituted 3- to 6-membered heterocycloalkyl, substituted 5- to 6-membered aromatic ring and substituted 5- to 6-membered heteroaromatic ring each comprise 1-2 substituents independently selected from the group consisting of halogen and C1-C6 alkyl.
6 more elements
A compound of formula (III) or a stereoisomer thereof:
- wherein
- R1 is selected from the group consisting of hydrogen, hydroxyl, halogen, amino, carboxyl, trifluoromethyl, nitro, cyano and C1-C6 alkyl;
- m is 0, 1, 2 or 3;
- A ring is an unsubstituted phenyl;
- E ring is a substituted or unsubstituted 4- to 5-membered N-containing heterocycloalkyl;
- wherein the substituted N-containing heterocycloalkyl comprises 1-2 substituents independently selected from the group consisting of halogen and C1-C6 alkyl;
- and
- R4 is absent.
5 more elements
A method for treating a disease associated with abnormal ROCK activity in a patient in need thereof, comprising:
- administering an effective amount of a compound of formula (I), or a stereoisomer thereof to the patient;
- wherein:
- n is independently 0, 1 or 2;
- R1 is independently selected from the group consisting of hydrogen, hydroxyl, halogen, amino, carboxyl, trifluoromethyl, nitro, cyano and C1-C6 alkyl;
- m is 0, 1, 2, 3, 4 or 5;
- R3 is —NR2R2′ or a substituted or unsubstituted N-containing heterocycloalkyl, wherein the substituted N-containing heterocycloalkyl comprises 1-2 substituents independently selected from the group consisting of halogen and C1-C6 alkyl;
- R2 and R2′ are independently hydrogen or C1-C6 alkyl;
- A ring is selected from the group consisting of 5- to 6-membered aromatic ring, 5- to 6-membered heteroaromatic ring and
- wherein B ring and C ring are independently selected from the group consisting of 5- to 6-membered aromatic ring and 5- to 6-membered heteroaromatic ring;
- R4 is independently selected from the group consisting of hydrogen, halogen, nitro, cyano, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, 3- to 6-membered cycloalkyl, 3- to 6-membered heterocycloalkyl, —(CH2)mORa, —(CH2)mOC(O)Ra, —(CH2)mOC(O)NRaRb, —(CH2)mNRaRb, —(CH2)mNRaC(O)Rb, —(CH2)mNRaC(O)ORb, —(CH2)mC(O)Ra, —(CH2)mC(O)ORa and —(CH2)mC(O)NRaRb;
- and
- Ra and Rb are independently selected from the group consisting of hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, substituted and unsubstituted 3- to 6-membered cycloalkyl, substituted and unsubstituted 3- to 6-membered heterocycloalkyl, substituted and unsubstituted 5- to 6-membered aromatic ring and substituted and unsubstituted 5- to 6-membered heteroaromatic ring, wherein the substituted 3- to 6-membered cycloalkyl, substituted 3- to 6-membered heterocycloalkyl, substituted 5- to 6-membered aromatic ring and substituted 5- to 6-membered heteroaromatic ring each comprise 1-2 substituents independently selected from the group consisting of halogen and C1-C6 alkyl.
9 more elements
Dependencies are inferred from the claim text.