A61K31/527

Modulators of toll-like receptors for the treatment of HIV

Provided are methods, uses, pharmaceutical regimens, pharmaceutical compositions, and kits comprising modulators of TLR7, including those of Formula II: ##STR00001##
and pharmaceutically acceptable salts thereof, useful in treating HIV infections.

Modulators of toll-like receptors for the treatment of HIV

Provided are methods, uses, pharmaceutical regimens, pharmaceutical compositions, and kits comprising modulators of TLR7, including those of Formula II: ##STR00001##
and pharmaceutically acceptable salts thereof, useful in treating HIV infections.

Ethynyl derivatives

The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

THERAPEUTIC REGIMENS FOR TREATMENT OF CANCER USING ERIBULIN AND SELECTIVE CDK4/6 INHIBITOR COMBINATIONS

The present invention provides methods and compositions for treating cancers with a combination of eribulin and a selective CDK4/6 inhibitor, wherein the selective CDK4/6 inhibitor reduces eribulin's effects on myelosuppression and/or myeloablation without reducing the efficacy of eribulin therapy.

THERAPEUTIC REGIMENS FOR TREATMENT OF CANCER USING ERIBULIN AND SELECTIVE CDK4/6 INHIBITOR COMBINATIONS

The present invention provides methods and compositions for treating cancers with a combination of eribulin and a selective CDK4/6 inhibitor, wherein the selective CDK4/6 inhibitor reduces eribulin's effects on myelosuppression and/or myeloablation without reducing the efficacy of eribulin therapy.

INDOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS

The present invention relates inter alia to a compound of formula (I)

##STR00001##

wherein R.sub.1, R.sub.2 and R.sub.3, are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.

INDOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS

The present invention relates inter alia to a compound of formula (I)

##STR00001##

wherein R.sub.1, R.sub.2 and R.sub.3, are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.

CYSTEINE-DEPENDENT INVERSE AGONISTS OF NUCLEAR RECEPTORS ROR-GAMMA/ROR-GAMMA-T AND METHODS OF TREATING DISEASES OR DISORDERS THEREWITH
20210147380 · 2021-05-20 · ·

Provided herein are compounds, compositions and methods for treating and preventing diseases and disorders, comprising administering to patients therapeutically effective amounts of cysteine-dependent inverse agonists of the nuclear receptor RORγ/RORγt. In some such embodiments, the inverse agonists bind to cysteine 476 of a nuclear receptor RORγ in the patient. Also provided are methods, as well as compounds and compositions, for modulating the activity of RORγ and RORγt by binding to the allosteric binding site through a covalent bond. In some aspects, the present disclosure relates to using compounds containing Michael acceptor groups which bind to a cysteine residue in the allosteric binding site such as cysteine 476 in RORγ.

Transient protection of normal cells during chemotherapy

This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.

Transient protection of normal cells during chemotherapy

This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.