公开(公告)号：US20240343755A1

公开(公告)日：2024-10-17

申请号：US18557899

申请日：2022-04-29

Applicant: ALCON INC.

Inventor： Mitchell A. deLong ,  Jill M. Sturdivant ,  Cynthia L. Lichorowic

IPC: C07J43/00 ,  A61K31/573 ,  A61K31/58 ,  A61K47/55 ,  A61P27/02 ,  C07J5/00 ,  C07J71/00

CPC classification number: C07J43/003 ,  A61K31/573 ,  A61K31/58 ,  A61K47/55 ,  A61P27/02 ,  C07J5/0053 ,  C07J5/0076 ,  C07J71/0031

Abstract: Provided herein are compounds and pharmaceutical compositions useful in modulating kinase activity, and related diseases. These compounds are conjugates of glucocorticoids with rho-kinase inhibitors. Also provided herein are methods of treating an eye disease or disorder in a subject. Also provided herein are methods of reducing intraocular pressure in a subject. Also provided herein are methods of modulating kinase activity in a cell. Also provided herein are methods of making the compounds provided herein, and compounds useful for the preparation of the compounds provided herein.

公开(公告)号：US20240360075A1

公开(公告)日：2024-10-31

申请号：US18640931

申请日：2024-04-19

Applicant: ALCON INC.

Inventor： Heeren M. Gordhan ,  Mitchell A. deLong ,  Jill M. Sturdivant ,  David Archer Ellis ,  Cynthia L. Lichorowic

IPC: C07C233/60 ,  A61K9/00 ,  A61K31/16 ,  A61K31/165 ,  A61K31/167 ,  A61K31/175 ,  A61K31/192 ,  A61K31/27 ,  A61K31/277 ,  A61K31/337 ,  A61K31/341 ,  A61K31/343 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/425 ,  A61K31/4465 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/69 ,  A61K47/12 ,  A61K47/18 ,  A61K47/38 ,  C07C231/02 ,  C07C233/58 ,  C07C233/59 ,  C07C233/62 ,  C07C233/63 ,  C07C235/14 ,  C07C235/56 ,  C07C237/24 ,  C07C271/20 ,  C07C271/24 ,  C07C279/22 ,  C07C315/04 ,  C07C317/30 ,  C07D205/04 ,  C07D207/09 ,  C07D209/54 ,  C07D211/58 ,  C07D213/75 ,  C07D213/79 ,  C07D231/40 ,  C07D239/42 ,  C07D263/04 ,  C07D263/56 ,  C07D265/36 ,  C07D275/03 ,  C07D277/46 ,  C07D295/088 ,  C07D295/135 ,  C07D295/32 ,  C07D305/06 ,  C07D305/08 ,  C07D305/14 ,  C07D307/22 ,  C07D307/94 ,  C07D309/14 ,  C07D311/58 ,  C07D335/02 ,  C07F5/02

CPC classification number: C07C233/60 ,  A61K9/0048 ,  A61K31/16 ,  A61K31/165 ,  A61K31/167 ,  A61K31/175 ,  A61K31/192 ,  A61K31/27 ,  A61K31/277 ,  A61K31/337 ,  A61K31/341 ,  A61K31/343 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/425 ,  A61K31/4465 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/69 ,  A61K47/12 ,  A61K47/183 ,  A61K47/186 ,  A61K47/38 ,  C07C231/02 ,  C07C233/58 ,  C07C233/59 ,  C07C233/62 ,  C07C233/63 ,  C07C235/14 ,  C07C235/56 ,  C07C237/24 ,  C07C271/20 ,  C07C271/24 ,  C07C279/22 ,  C07C315/04 ,  C07C317/30 ,  C07D205/04 ,  C07D207/09 ,  C07D209/54 ,  C07D211/58 ,  C07D213/75 ,  C07D213/79 ,  C07D231/40 ,  C07D239/42 ,  C07D263/04 ,  C07D263/56 ,  C07D265/36 ,  C07D275/03 ,  C07D277/46 ,  C07D295/088 ,  C07D295/135 ,  C07D295/32 ,  C07D305/06 ,  C07D305/08 ,  C07D305/14 ,  C07D307/22 ,  C07D307/94 ,  C07D309/14 ,  C07D311/58 ,  C07D335/02 ,  C07F5/025 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/18 ,  C07C2602/38 ,  C07C2602/42 ,  C07C2602/50

Abstract: Described herein are modified monoterpene TRPM8 activating compounds. In particular, provided herein are compounds that affect the function of ion channels in a cell, and are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including inflammatory eye diseases such as uveitis, cardiovascular diseases, inflammatory diseases, and diseases characterized by abnormal growth, such as cancers.