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Cellular Signalling Inhibitors Their Formulations And Methods Thereof

Abstract: The present disclosure relates generally to Cellular Signalling inhibitors of compound of Formula (I) compositions and formulations comprising the same methods processes and uses thereof. In particular the present disclosure provides CSF-1R inhibitors demonstrating sustained inhibition of CSF/CSF1R signalling pathway with decreased toxicity. The present disclosure also provides supramolecular combinatorial therapeutics wherein a CSF-1R inhibitor is combined with one or more of a chemotherapeutic agent a kinase inhibitor and an immunoregulator each of which is optionally conjugated with a lipid. The present disclosure also provides a method for treating cancer allergy Systemic lupus erythematosus nephritis Chronic Obstructive Pulmonary Disease and abnormal macrophage functions or any combinations thereof.

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Patent Information

Application #
Filing Date
11 September 2018
Publication Number
39/2018
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
Parent Application

Applicants

INVICTUS ONCOLOGY PVT. LTD.
Plot 465, F.I.E., Patparganj Industrial Area Delhi 110092
THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
75 Francis Street Boston, Massachusetts 02115

Inventors

1. ROY, Monideepa
6 Buchan Road, Andover, MA-01810
2. BISWAS, Goutam
Plot 465, F.I.E., Patparganj Industrial Area Delhi 110092
3. SURYAVANSHI, Hemant
Plot 465, F.I.E., Patparganj Industrial Area Delhi 110092
4. MUKHERJEE, Anubhab
Plot 465, F.I.E., Patparganj Industrial Area Delhi 110092
5. KULKARNI, Ashish
42 Rockland Avenue Arlington, Massachusetts 02474
6. SENGUPTA, Shiladitya
3411 Chestnut street, Apt:602 Philadelphia, 19104

Specification

The compound of claim 1, wherein the linker is selected from the group consisting of a direct bond or an atom such as oxygen or sulfur, a unit such as NR1, C(O), C(O)O, C(O)NR1, SO, SO2, SO2NH or a chain of atoms, such as substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, aryl,

heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkylarylalkyl, alkylarylalkenyl,
alkylarylalkynyl, alkenylarylalkyl, alkenylarylalkenyl, alkenylarylalkynyl,
alkynylarylalkyl, alkynylarylalkenyl, alkynylarylalkynyl, alkylheteroarylalkyl,
alkylheteroarylalkenyl, alkylheteroarylalkynyl, alkenylheteroarylalkyl,
alkenylheteroarylalkenyl, alkenylheteroarylalkynyl, alkynylheteroarylalkyl, alkynylheteroarylalkenyl, alkynylheteroarylalkynyl, alkylheterocyclylalkyl, alkylheterocyclylalkenyl, alkylhererocyclylalkynyl, alkenylheterocyclylalkyl, alkenylheterocyclylalkenyl, alkenylheterocyclylalkynyl, alkynylheterocyclylalkyl, alkynylheterocyclylalkenyl, alkynylheterocyclylalkynyl, alkylaryl, alkenylaryl, alkynylaryl, alkylheteroaryl, alkenylheteroaryl, or alkynylhereroaryl, where one or more methylenes can be interrupted or terminated by O, S, S(O), SO2, N(R1)2, C(O), cleavable linking group, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic; where R1 is hydrogen, acyl, aliphatic or substituted aliphatic.
3. The compound of claim 1, wherein the linker is selected from the group consisting of a direct bond, ester, ether, amide or any functional group containing covalent linker.
4. The compound of claim 1, wherein the linker comprises at least one cleavable group.
5. The compound of claim 1, wherein the linker comprises succinic acid, fumaric acid, propargylic acid, ethylene glycol, diethylene glycol, or natural or unnatural amino

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