You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Details for Patent: 8,716,310


✉ Email this page to a colleague

« Back to Dashboard


Title:Dual mechanism inhibitors for the treatment of disease
Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
Inventor(s): deLong; Mitchell A. (Chapel Hill, NC), Sturdivant; Jill Marie (Chapel Hill, NC), Royalty; Susan M. (Davis, CA)
Assignee: Aerie Pharmaceuticals, Inc. (Research Triangle Park, NC)
Filing Date:Feb 15, 2013
Application Number:13/768,594
Claims:1. A compound according to Formula II: ##STR00238## and salts thereof, wherein R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-C.sub.4 alkyl, aryl, C.sub.1-C.sub.4 alkyl aryl, C.sub.1-C.sub.4 alkyl heteroaryl, C.sub.1-C.sub.4 alkyl heterocyclyl, C.sub.2-C.sub.4 alkenyl, C.sub.2-C.sub.4 alkynyl, C.sub.1-C.sub.4 carbonyl, C.sub.1-C.sub.4 carbonylamino, C.sub.1-C.sub.4 alkoxy, C.sub.1-C.sub.4 sulfonyl, C.sub.1-C.sub.4 sulfonylamino, C.sub.1-C.sub.4 thioalkyl, C.sub.1-C.sub.4 carboxyl, or form a ring with each other or with A; wherein R.sup.3 is hydrogen; wherein A is C.sub.1-C.sub.4 alkyl; wherein B is hydrogen, an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, C.sub.1-C.sub.22 alkyl, C.sub.1-C.sub.22 alkyl aryl, C.sub.1-C.sub.22 alkyl heteroaryl, C.sub.2-C.sub.22 alkenyl, C.sub.2-C.sub.22 alkynyl, C.sub.1-C.sub.22 carbonyl, C.sub.1-C.sub.22 carbonylamino, C.sub.1-C.sub.22 alkoxy, C.sub.1-C.sub.22 sulfonyl, C.sub.1-C.sub.22 sulfonylamino, C.sub.1-C.sub.22 thioalkyl, or C.sub.1-C.sub.22 carboxyl; wherein X.sup.1, X.sup.2, and X.sup.3 are, independently, hydrogen, halogen, or C.sub.1-C.sub.4 alkyl; wherein the double circle indicates a phenyl ring; and wherein each Z is independently a bond or C.sub.1-C.sub.4 alkyl.

2. A compound according to claim 1, wherein R.sup.1 is hydrogen or C.sub.1-C.sub.4 alkyl; B is C.sub.1-C.sub.22 carbonyl; and X.sub.1, X.sub.2, and X.sub.3 are hydrogen.

3. A compound according to claim 1, wherein Z is a bond or --CH.sub.2--.

4. A compound according to claim 1, wherein X.sup.1, X.sup.2 and X.sup.3 are each hydrogen.

5. A compound according to claim 1, wherein A is --CH.sub.2CH.sub.2--.

6. A compound according to claim 1, wherein R.sup.1 and R.sup.2 are independently hydrogen or methyl.

7. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.

8. A method for treating a disease in a subject comprising: administering to a subject an effective amount of a compound according to claim 1; wherein the disease comprises glaucoma or dry eye.

9. The method of claim 8, wherein intraocular pressure is reduced.

10. A method of modulating kinase activity comprising: contacting a cell with a compound according to claim 1 in an amount effective to modulate kinase activity.

11. The method of claim 10, wherein the cell is in a subject.

12. A method of reducing intraocular pressure in a patient in need using: a compound according to claim 1.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.