US 2021/0275677 A1Published application

B-cell immunotherapy in cancer treatment

AssigneeAlyssum Therapeutic s, Inc.

InventorsShiladitya Sengupta, Aniruddha Sengupta

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Abstract

The present disclosure provides methods for treating cancer in amount of a compound of formula (VIII), or a pharmaceutically acceptable salt thereof, wherein Q, linker, and lipid are defined herein, and (ii) a therapeutically effective amount of an immune checkpoint inhibitor. Q-linker-lipid (VIII) In some embodiments, the compound is the following structure (IO-125), or a pharmaceutically acceptable salt thereof; Pharmaceutical compositions comprising a compound of formula (VIII), such as IO-125, or a pharmaceutically acceptable salt thereof, an immune checkpoint inhibitor, and a pharmaceutically acceptable excipient are also described.

Claims23

Dependent claims

A method for treating cancer in a patient, comprising administering to the patient:

a therapeutically effective amount of a compound of formula (VIII) or a pharmaceutically acceptable salt thereof;
Q-linker-lipid (VIII)
wherein:
Q is a platinum containing moiety;
the lipid is a fat, wax, sterol, steroid, bile acid, fat-soluble vitamin, monoglyceride, diglyceride, phospholipid, glycolipid, sulpholipid, aminolipid, chromolipid, glycerophospholipid, sphingolipid, prenollipid, saccharolipid, polyketide, fatty acid, fatty alcohol, glycerolipid, or combination thereof;
and
(i) the linker is
(a) —X—CH2—X2—X1—, wherein:
X is NH;
X1 is C(O)O, C(O)NH, O(CH2)—, NH, or O;
X2 is (CH2)n, or C(O);
and
n is 0, 1, 2, 3, 4, or 5;
(b) —(CH2)nO—, —(CH2)nNHC(O)O, —(CH2)nOC(O)NH—, —(CH2)nC(O)NH(CH2)mO, —(CH2)nO(CH2)mO—, —(CH2)nO(O)—, —(CH2)nNHC(O)(CH2)mO—, or —(CH2)nC(O)O—, wherein:
n and m are, independently, 0, 1, 2, 3, 4, or 5;
or
(c) —X3—X4X5—X6—, wherein:
X3 is CH, CH2, or O;
and
X4, X5 and X6 are, independently, —CH2O— or O;
(d) or combinations of (a)-(c);
(ii) or the linker is a bond, —O—, NHCH2CH2NHC(O)—, —NHCH2CH2NHC(O)O—, —NHCH2CH2—, —NHCH2CH2O—, —NHCH2C(O)—, —NHCH2C(O)O—, —NHCH2C(O)OCH2CH2CH2—, —NHCH2C(O)OCH2CH2CH2O—, —NHCH2C(O)NH—, —CH2CH2—, —CH2CH2O—, —CH2CH2NHC(O)—, —CH2CH2NHC(O)O—, —CH2CH2O—, —CH2C(O)NHCH2CH2—, —CH2C(O)NHCH2CH2O—, —CH2CH2OCH2CH2—, —CH2CH2OCH2CH2O—, —CH2C(O)—, —CH2C(O)O—, —CH2CH2CH2—, —CH2CH2CH2O—, ═CHCH═CH2—, ═CHCH═CHCH2O—, —CH═CHCH2—, —CH═CHCH2O—, —OCH2CH2O—, —CH2—, —CH2O—, —NHC(O)CH2—, —NHC(O)CH2O—, —C(O)CH2—, —C(O)CH2O—, —OC(O)CH2—, —OC(O)CH2O—, —C(O)CH2CH2C(O)NHCH2CH2—, —OC(O)CH2CH2C(O)NHCH2CH2—, —C(O)CH2CH2C(O)NHCH2CH2O—, —OC(O)CH2CH2C(O)NHCH2CH2O—, —C(O)CH2CH2C(O)NHCH2CH2NHC(O)—, —OC(O)CH2CH2C(O)NHCH2CH2NHC(O)—, —C(O)CH2CH2C(O)NHCH2CH2NHC(O)O—, —OC(O)CH2CH2C(O)NHCH2CH2NHC(O)O—, or a combination thereof;
and
(ii) a therapeutically effective amount of an immune checkpoint inhibitor.

21 more elements

A pharmaceutical composition comprising:

i. a compound of the Formula (VIII), or a pharmaceutically acceptable salt thereof;
Q-linker-lipid (VIII)
wherein:
Q is a platinum containing moiety;
the lipid is a fat, wax, sterol, steroid, bile acid, fat-soluble vitamin, monoglyceride, diglyceride, phospholipid, glycolipid, sulpholipid, aminolipid, chromolipid, glycerophospholipid, sphingolipid, prenollipid, saccharolipid, polyketide, fatty acid, fatty alcohol, glycerolipid, or combination thereof;
and
(i) the linker is
(a) —X—CH2—X2—X1—, wherein:
X is NH;
X1 is C(O)O, C(O)NH, O(CH2)—O, NH, or O;
X2 is (CH2), or C(O);
and
n is 0, 1, 2, 3, 4, or 5;
(b) —(CH2)nO—, —(CH2)nNHC(O)O—, —(CH2)nOC(O)NH—, —(CH2)nC(O)NH(CH2)mO—, —(CH2)nO(CH2)mO—, —(CH2)nO(O)—, —(CH2)nNHC(O)(CH2)mO—, or —(CH2)nC(O)O—, wherein:
n and m are, independently, 0, 1, 2, 3, 4, or 5;
or
(c) —X3—X4X5—X6—, wherein:
X3 is CH, CH2, or O;
and
X4, X5 and X6 are, independently, —CH2O— or O;
or
(ii) or the linker is a bond, —O—, NHCH2CH2NHC(O)—, —NHCH2CH2NHC(O)O—, —NHCH2CH2—, —NHCH2CH2O—, —NHCH2C(O)—, —NHCH2C(O)O—, —NHCH2C(O)OCH2CH2CH2—, —NHCH2C(O)OCH2CH2CH2O—, —NHCH2C(O)NH—, —CH2CH2—, —CH2CH2O—, —CH2CH2NHC(O)—, —CH2CH2NHC(O)O—, —CH2CH2O—, —CH2C(O)NHCH2CH2—, —CH2C(O)NHCH2CH2O—, —CH2CH2OCH2CH2—, —CH2CH2OCH2CH2O—, —CH2C(O) CH2C(O)O—, —CH2CH2CH2—, —CH2CH2CH2O—, ═CHCH═CH2—, ═CHCH═CHCH2O—, —CH═CHCH2—, —CH═CHCH2O—, OCH2CH2O—, —CH2—, —CH2O—, —NHC(O)CH2—, —NHC(O)CH2O—, —C(O)CH2—, —C(O)CH2O—, —OC(O)CH2—, —OC(O)CH2O—, —C(O)CH2CH2C(O)NHCH2CH2—, —OC(O)CH2CH2C(O)NHCH2CH2—, —C(O)CH2CH2C(O)NHCH2CH2O—, —OC(O)CH2CH2C(O)NHCH2CH2O—, —C(O)CH2CH2C(O)NHCH2CH2NHC(O)—, —OC(O)CH2CH2C(O)NHCH2CH2NHC(O)—, —C(O)CH2CH2C(O)NHCH2CH2NHC(O)O—, —OC(O)CH2CH2C(O)NHCH2CH2NHC(O)O—, or a combination thereof;
ii. an immune checkpoint inhibitor;
and
iii. a pharmaceutically acceptable excipient.

22 more elements

Dependencies are inferred from the claim text.

Facts

Application: 17/258,610Filed 10 Jul 2019
Priority: 10 Jul 2018
Published: 9 Sep 2021
Term ends: Not estimatedThe source records don’t support an estimate.

Classification12 codes

A61K 47/551
The modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug: one of the codrug's…
A61K 39/3955
Against materials from animals: against proteinaceous materials, e.g. enzymes, hormones, lymphokines
A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…
A61K 47/554
The modifying agent being an organic compound: the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid

Family

Application62/695,946Us provisional application · filed 10 Jul 2018
US 12,357,699 B2Related patent
US 2021/0275677 A1This patent

From the US filing history. Foreign family members aren’t listed.

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