US2023321050A1PendingUtilityA1
Heterocyclic Compounds and Uses Thereof
Est. expiryAug 17, 2029(~3.1 yrs left)· nominal 20-yr term from priority
A61K 31/423A61K 31/444A61K 31/437A61K 31/517A61K 31/5025A61K 31/496A61K 31/4709A61K 31/5377A61K 31/498A61K 31/541A61K 31/551A61K 31/497A61K 31/428C12N 9/1205C07D 413/04C07D 413/14C07D 417/04C07D 417/14C07D 471/04C07D 487/04C07D 519/00C07D 401/14Y02A50/30A61P 1/00A61P 1/04A61P 1/16A61P 1/18A61P 11/00A61P 11/06A61P 11/08A61P 13/08A61P 13/12A61P 15/00A61P 15/08A61P 17/00A61P 17/02A61P 17/06A61P 17/16A61P 19/00A61P 19/02A61P 21/00A61P 25/00A61P 25/02A61P 25/04A61P 25/14A61P 25/28A61P 27/02A61P 29/00A61P 29/02A61P 3/00A61P 31/04A61P 31/12A61P 35/00A61P 35/04A61P 37/02A61P 37/06A61P 37/08A61P 43/00A61P 7/00A61P 7/04A61P 9/00A61P 9/10A61P 3/10A61K 31/422C07D 519/06
81
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
Claims
exact text as granted — not AI-modified1 - 53 . (canceled)
54 . A method of inhibiting a phosphatidyl inositol-3 kinase (PI3 kinase), comprising: contacting the PI3 kinase with a therapeutically effective amount of a compound of the following formula:
or a pharmaceutically acceptable salt thereof, wherein
W 1 is CR 3 ;
W 2 is CR 4 ;
W 3 is N;
W 4 is N;
W 5 is CR 7 ;
W 6 is CR 8 ;
R 1 and R 2 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, alkoxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, halo, cyano, hydroxy, nitro, phosphate, urea, carbonate, or NR′R″ wherein R′ and R″ are taken together with nitrogen to form a cyclic moiety;
R 3 is amido of formula —C(O)N(R) 2 or —NHC(O)R, wherein R is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, or heteroalicyclic; or wherein said (R) 2 may be taken together with the nitrogen to which they are attached to form an optionally substituted 4-, 5-, 6-, or 8-membered ring;
R 4 is hydrogen, alkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxy, heterocycloalkyloxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, halo, cyano, hydroxy, nitro, phosphate, urea, carbonate, or NR′R″, wherein R′ and R″ are taken together with nitrogen to form a cyclic moiety;
or R 3 and R 4 taken together form a cyclic moiety; and
R 5 , R 7 , and R 8 are independently hydrogen, alkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxy, heterocycloalkyloxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, halo, cyano, hydroxy, nitro, phosphate, urea, carbonate, or NR′R″, wherein R′ and R″ are taken together with nitrogen to form a cyclic moiety.
55 . The method of claim 54 , wherein the contacting of the PI3 kinase with the compound comprises contacting a cell that expresses the PI3 kinase.
56 . The method of claim 54 , wherein the PI3 kinase is PI3 kinase alpha.
57 . The method of claim 55 , further comprising administering a second therapeutic agent to the cell.
58 . The method of claim 54 , wherein the contacting of the PI3 kinase with the compound is in a subject suffering from a cancer selected from the group consisting of: breast invasive carcinoma, prostate adenocarcinoma, colon adenocarcinoma, thyroid carcinoma, bladder urothelial carcinoma, lung adenocarcinoma, uterine carcinosarcoma, cervical squamous cell carcinoma and endocervical adenocarcinoma, testicular germ cell tumors, lung squamous cell carcinoma, stomach adenocarcinoma, glioblastoma multiforme, liver hepatocellular carcinoma, pancreatic adenocarcinoma, esophageal carcinoma, brain lower grade glioma, head and neck squamous cell carcinoma, rectum adenocarcinoma, cholangiocarcinoma, and mesothelioma.
59 . The method of claim 54 , wherein the contacting of the PI3 kinase with the compound is in a subject suffering from breast cancer, lung cancer, gastric cancer, colorectal cancer, ovarian cancer, or uterine cancer.
60 . The method of claim 54 , wherein
W 1 is CR 3 ; W 2 is CR 4 ; W 3 is N; W 4 is N; W 5 is CR 7 ; W 6 is CR 8 ; R 1 and R 2 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, alkoxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, halo, cyano, hydroxy, nitro, phosphate, urea, or carbonate; R 3 is amido of formula —C(O)N(R) 2 or —NHC(O)R, wherein R is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, or heteroalicyclic; or wherein said (R) 2 may be taken together with the nitrogen to which they are attached to form an optionally substituted 4-, 5-, 6-, or 7-membered ring, and R 4 , R 7 , and R 8 are each hydrogen.
61 . The method of claim 54 , wherein the compound is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
62 . The method of claim 54 , wherein
W 1 is CR 3 ; W 2 is CR 4 ; W 3 is N; W 4 is N; W 5 is CR 7 ; W 6 is CR 8 ; R 1 and R 2 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, alkoxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, halo, cyano, hydroxy, nitro, phosphate, urea, or carbonate; R 3 is amido of formula —C(O)N(R) 2 or —NHC(O)R, wherein R is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, or heteroalicyclic; or wherein said (R) 2 may be taken together with the nitrogen to which they are attached to form an optionally substituted 4-, 5-, 6-, or 7-membered ring, and R 4 , R 7 , and R 8 are each hydrogen.
63 . The method of claim 54 , wherein the compound is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
64 . The method of claim 54 wherein the compound is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
65 . The method of claim 59 , wherein the compound is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
66 . The method of claim 59 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
67 . The method of claim 59 , wherein the lung cancer is non-small cell lung cancer.
68 . The method of claim 59 , wherein the lung cancer is squamous cell carcinoma.
69 . The method of claim 59 , wherein the lung cancer is small cell lung cancer.
70 . The method of claim 59 , wherein the uterine cancer is endometrial cancer.
71 . The method of claim 59 , wherein the uterine cancer is uterine carcinosarcoma.
72 . The method of claim 59 , wherein the uterine cancer is cervical squamous cell carcinoma.
73 . The method of claim 59 , wherein the colorectal cancer is colon adenocarcinoma.
74 . The method of claim 59 , wherein the colorectal cancer is rectum adenocarcinoma.
75 . The method of claim 64 , wherein the contacting of the PI3 kinase with the compound is in a subject suffering from breast cancer, lung cancer, gastric cancer, colorectal cancer, ovarian cancer, or uterine cancer.
76 . The method of claim 75 , wherein the lung cancer is non-small cell lung cancer.
77 . The method of claim 75 , wherein the lung cancer is squamous cell carcinoma.
78 . The method of claim 75 , wherein the lung cancer is small cell lung cancer.
79 . The method of claim 75 , wherein the uterine cancer is endometrial cancer.
80 . The method of claim 75 , wherein the cancer is uterine cancer.
81 . The method of claim 75 , wherein the uterine cancer is uterine carcinosarcoma.
82 . The method of claim 75 , wherein the uterine cancer is cervical squamous cell carcinoma.
83 . The method of claim 75 , wherein the cancer is colorectal cancer.
84 . The method of claim 75 , wherein the colorectal cancer is colon adenocarcinoma.
85 . The method of claim 75 , wherein the colorectal cancer is rectum adenocarcinoma.
86 . The method of claim 75 , wherein the cancer is breast cancer.
87 . The method of claim 75 , wherein the cancer is ovarian cancer.
88 . The method of claim 57 , wherein the second therapeutic agent is an inhibitor of Ras oncogenic isoforms.
89 . The method of claim 54 , wherein the therapeutically effective amount is from about 0.05 to about 7 g/day.
90 . The method of claim 54 , wherein the therapeutically effective amount is from about 0.05 to about 2.5 g/day.
91 . The method of claim 58 , further comprising administering a second therapeutic agent to the subject.
92 . The method of claim 91 , wherein the second therapeutic agent is a chemotherapeutic agent.Join the waitlist — get patent alerts
Track US2023321050A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.