A61K31/4409

SUBSTITUTED BICYCLIC COMPOUNDS

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):

##STR00001##

and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

SKIN COMPOSITION
20220331389 · 2022-10-20 ·

The present invention pertains to: the provision of a method for promoting skin wound healing and a composition to be used for promoting skin wound healing; the provision of a method useful for preventing or ameliorating ulcers and bedsores or a composition therefor; the provision of a method for preventing skin aging and a composition to be used for preventing skin aging; the provision of a composition useful for preventing or ameliorating skin damage caused by an anticancer agent; and, furthermore, the provision of a method for enhancing the regeneration ability of epidermal stem cells and a composition for enhancing the regeneration ability of epidermal stem cells. More specifically, use of a composition, said composition being characterized by comprising, as an active ingredient, a substance selected from the group consisting of a substance which induces or maintains the expression of COL17A1 in cells, a substance which inhibits the degradation of COL17A1 in cells, a substance which promotes the competitive amplification ability of epidermal stem cells, a substance which suppresses genomic stress or oxidative stress in cells and a substance which prevents DNA damage in cells, enables the promotion of skin wound healing, protection from an anticancer agent and prevention of skin aging. Thus, the regeneration ability of epidermal stem cells can be enhanced.

A Combined Inhibition of EGFR and NRF2 in The Treatment of Malignant Glioma
20230130791 · 2023-04-27 ·

The present disclosure is concerned with modulators of EGFR and modulators of Nrf2 for treating various cancers such as, for example, sarcomas, carcinomas, hematological cancers, solid tumors, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, bladder cancer, thyroid cancer, testicular cancer, pancreatic cancer, endometrial cancer, melanomas, gliomas, leukemias, lymphomas, chronic myeloproliferative disorders, myelodysplastic syndromes, myeloproliferative neoplasms, and plasma cell neoplasms (myelomas). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

A Combined Inhibition of EGFR and NRF2 in The Treatment of Malignant Glioma
20230130791 · 2023-04-27 ·

The present disclosure is concerned with modulators of EGFR and modulators of Nrf2 for treating various cancers such as, for example, sarcomas, carcinomas, hematological cancers, solid tumors, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, bladder cancer, thyroid cancer, testicular cancer, pancreatic cancer, endometrial cancer, melanomas, gliomas, leukemias, lymphomas, chronic myeloproliferative disorders, myelodysplastic syndromes, myeloproliferative neoplasms, and plasma cell neoplasms (myelomas). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

A Combined Inhibition of EGFR and NRF2 in The Treatment of Malignant Glioma
20230130791 · 2023-04-27 ·

The present disclosure is concerned with modulators of EGFR and modulators of Nrf2 for treating various cancers such as, for example, sarcomas, carcinomas, hematological cancers, solid tumors, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, bladder cancer, thyroid cancer, testicular cancer, pancreatic cancer, endometrial cancer, melanomas, gliomas, leukemias, lymphomas, chronic myeloproliferative disorders, myelodysplastic syndromes, myeloproliferative neoplasms, and plasma cell neoplasms (myelomas). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

DETECTION OF GENE POLYMORPHISMS

Provided herein, inter alia, are methods of detecting single polypeptide polymorphisms in a subject by detecting a G191A NAT2 SNP, a C282T NAT2 SNP, a T341C NAT2 SNP, a G590A NAT2 SNP and a G857A NAT2 SNP in a biological sample, wherein the subject is taking an arylamine drug or a hydrazine drug or the subject is in need of an arylamine drug or a hydrazine drug. The subject can have a tuberculosis infection and the drug can be isoniazid. Also provided are related kits.

DETECTION OF GENE POLYMORPHISMS

Provided herein, inter alia, are methods of detecting single polypeptide polymorphisms in a subject by detecting a G191A NAT2 SNP, a C282T NAT2 SNP, a T341C NAT2 SNP, a G590A NAT2 SNP and a G857A NAT2 SNP in a biological sample, wherein the subject is taking an arylamine drug or a hydrazine drug or the subject is in need of an arylamine drug or a hydrazine drug. The subject can have a tuberculosis infection and the drug can be isoniazid. Also provided are related kits.

Agent for promoting corneal endothelial cell adhesion

The invention provides an agent for promoting adhesion of a corneal endothelial cell, containing a Rho kinase inhibitor, as well as a culture medium for a corneal endothelial cell, a solution for preservation of cornea, and a method of producing a corneal endothelial preparation, which includes culturing the corneal endothelial cell using the aforementioned culture medium.

Agent for promoting corneal endothelial cell adhesion

The invention provides an agent for promoting adhesion of a corneal endothelial cell, containing a Rho kinase inhibitor, as well as a culture medium for a corneal endothelial cell, a solution for preservation of cornea, and a method of producing a corneal endothelial preparation, which includes culturing the corneal endothelial cell using the aforementioned culture medium.

Anti-cancer compounds

The present invention relates to new pharmaceutical agents, and to their use in the treatment of proliferative diseases, such as cancer (in particular, brain cancer). In some embodiments, the present invention relates to compounds of formula (I): ##STR00001## or pharmaceutically acceptable salts or prodrugs thereof.