US2017114019A1PendingUtilityA1
18-20 member bi-polycyclic compounds
Est. expiryJun 4, 2034(~7.9 yrs left)· nominal 20-yr term from priority
A61P 35/00C07D 209/42C07D 409/04C07D 215/48C07D 215/54C07C 2602/10C07C 259/10C07D 209/08C07C 2102/10
43
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Claims
Abstract
The invention relates to 18-20 member bi-polycyclic compounds, methods of making these compounds, and methods of using them in treating hyperproliferative disorders (e.g., cancer) and non-malignant tumors; promoting muscle formation; inhibiting muscle degeneration or the loss of muscle mass or muscle function; and myofibers ex vivo.
Claims
exact text as granted — not AI-modified1 . A compound of Formula I:
A-W—Z (I)
or a pharmaceutically acceptable salt thereof, wherein
A is
W is a heterocyclylene, arylene, heteroarylene, alkenylenearylene, arylenealkenylene alkenyleneheteroarylene, or heteroarylenealkenylene; and
Z is a hydrogen bond donor, with the proviso that the compound is not
where R is —OH, —OCH 3 and —NHOH; and R′ is —OH or —OCH 3 .
2 . The compound of claim 1 , wherein W is an indolinylene linked to A at any one of positions 2, 3, 4, 5, 6 or 7 of the indolinylene; a quinolinene linked to A at any one of positions 2, 3, 4, 5, 6, 7, or 8; or an isoquinolinene linked to A at any one of positions 1, 3, 4, 5, 6, 7, or 8.
3 . The compound of claim 1 , wherein W is -propylene-phenylene-.
4 . The compound of claim 1 , wherein Z is —C(O)NR 1 R 2 or —C(O)OR 3 , wherein R 1 and R 2 are each independently hydrogen (H), hydroxyl (OH), C 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, or aminoaryl; and R 3 is H or C 1-6 alkyl.
5 . The compound of claim 2 , wherein Z is linked to the indolinylene, quinolinene, or isoquinolinene at any one of the positions that is not linked to A.
6 . The compound of claim 4 , wherein W is
7 . The compound of claim 1 , wherein W is an indolinylene linked to A at any one of positions 2, 3, 4, 5, 6 or 7 of the indolinylene; Z is —C(O)NR 1 R 2 or —C(O)OR 3 , wherein R 1 and R 2 are each independently hydrogen, hydroxyl, C 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, or aminoaryl; and R 3 is H or C 1-6 alkyl, and wherein Z is linked to the indolinylene at any one of positions 2, 3, 4, 5, 6 or 7 of the indolinylene not linked to A.
8 . The compound of claim 1 , wherein W is a quinolinene linked to A at any one of positions 2, 3, 4, 5, 6, 7 or 8 of the quinolinene; Z is —C(O)NR 1 R 2 or —C(O)OR 3 , wherein R 1 and R 2 are each independently hydrogen, hydroxyl, C 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, or aminoaryl; and R 3 is H or C 1-6 alkyl, and wherein Z is linked to the quinolinene at any one of positions 2, 3, 4, 5, 6, 7 or 8 of the quinolinene.
9 . The compound of claim 1 , W is a isoquinolinene linked to A at one of positions 1, 3, 4, 5, 6, 7 or 8 of the isoquinolinene moiety; Z is —C(O)NR 1 R 2 or —C(O)OR 3 , wherein R 1 and R 2 are each independently hydrogen, hydroxyl, C 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, or aminoaryl; and R 3 is H or C 1-6 alkyl, and wherein Z is linked to the quinoline ring at any one of positions 2, 3, 4, 5, 6, 7 or 8 of the isoquinolinene.
10 . The compound of claim 7 , wherein Z is —C(O)NR 1 R 2 ; R 1 is H; and R 2 is OH.
11 . The compound of claim 7 , wherein Z is —C(O)NR 1 R 2 ; R 1 is H; and R 2 is aminoaryl.
12 . The compound of claim 7 , wherein Z is —C(O)OR 3 ; and R 3 is H.
13 . The compound of claim 7 , wherein Z is —C(O)OR 3 ; and R 3 is C 1-6 alkyl.
14 . The compound of claim 1 , wherein the compound is
15 . A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable carrier.
16 . A method of treating a subject who has cancer or a non-malignant tumor, the method comprising administering to the subject a therapeutically effective amount of a compound of claim 1 .
17 . The method of claim 16 , wherein the cancer is non-small cell lung cancer, colon cancer, melanoma, breast cancer, renal cancer, ovarian cancer, prostate cancer, cancer of the central nervous system, a blood cancer, or a neuroblastoma.
18 . (canceled)
19 . A method of inhibiting loss of muscle mass or muscle function in a subject, the method comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I:
A-W—Z (I)
or a pharmaceutically acceptable salt thereof, wherein
A is
W is a heterocyclylene, arylene, heteroarylene, alkenylenearylene, arylenealkenylene or alkenyleneheteroarylene, heteroarylenealkenylene; and
Z is a hydrogen bond donor.
20 .- 21 . (canceled)
22 . The method of claim 19 , wherein the loss of muscle mass is associated with intensive care unit-acquired weakness (ICUAW), chronic obstructive pulmonary disease (COPD), heart failure, traumatic injury or malignancy.
23 . A method for treating myofibers ex vivo, the method comprising:
providing an ex vivo preparation of myofibers, optionally comprising a natural or synthetic biological matrix; and contacting the preparation with an amount of a compound of Formula I:
A-W—Z (I)
or a pharmaceutically acceptable salt thereof, wherein the amount of the compound is sufficient to promote muscle mass or muscle function and
A is
W is a heterocyclylene, arylene, heteroarylene, alkenylenearylene, arylenealkenylene alkenyleneheteroarylene, or heteroarylenealkenylene; and
Z is a hydrogen bond donor.Join the waitlist — get patent alerts
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