Patent classifications
C07D209/02
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds having the general Formula (I);
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and pharmaceutically acceptable salts thereof; wherein the variables R.sup.A, R.sup.AA, subscript n, subscript q, ring A, X.sup.2, L, subscript m, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Nrf and HIF activators/HDAC inhibitors and therapeutic methods using the same
Compounds that inhibit histone (HDACI) and/or activate Nrf2 and HIF, and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC and/or activation of Nrf2 and HIF provide a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
Bisamide sarcomere activating compounds and uses thereof
- Luke Ashcraft ,
- Alessandro Boezio ,
- John Butler ,
- Aroop CHANDRA ,
- Chihyuan Chuang ,
- Scott E. Collibee ,
- Mikkel V. Debenedetto ,
- Vincent Dimassa ,
- Russell Graceffa ,
- Justin Malinowski ,
- David Moebius ,
- Bradley Paul Morgan ,
- Joshua Payette ,
- Antonio ROMERO ,
- David St. Jean, Jr. ,
- Richard Vargas ,
- John Yeoman ,
- Hanmo Zhang ,
- Alan Cheng ,
- Felix Gonzalez Lopez De Turiso ,
- Michael Garrett Johnson
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof. ##STR00001##
Bisamide sarcomere activating compounds and uses thereof
- Luke Ashcraft ,
- Alessandro Boezio ,
- John Butler ,
- Aroop CHANDRA ,
- Chihyuan Chuang ,
- Scott E. Collibee ,
- Mikkel V. Debenedetto ,
- Vincent Dimassa ,
- Russell Graceffa ,
- Justin Malinowski ,
- David Moebius ,
- Bradley Paul Morgan ,
- Joshua Payette ,
- Antonio ROMERO ,
- David St. Jean, Jr. ,
- Richard Vargas ,
- John Yeoman ,
- Hanmo Zhang ,
- Alan Cheng ,
- Felix Gonzalez Lopez De Turiso ,
- Michael Garrett Johnson
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof. ##STR00001##
Compositions and methods for inhibiting M.SUP.pro .and PL.SUP.pro .protease activity and for preventing and treating SARS-CoV-2 infection
This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrrolidinone-acetamide (or similar) structure (e.g., ##STR00001##
Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PL.sup.pro), which function as inhibitors of the SARS-CoV-2 related viral 3CL protease (MP.sup.pro), which function as therapeutics for the treatment of viral infection characterized with PLP.sup.pro and/or M.sup.pro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLP.sup.pro and/or M.sup.pro protease activity and/or expression.
Compositions and methods for inhibiting M.SUP.pro .and PL.SUP.pro .protease activity and for preventing and treating SARS-CoV-2 infection
This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrrolidinone-acetamide (or similar) structure (e.g., ##STR00001##
Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PL.sup.pro), which function as inhibitors of the SARS-CoV-2 related viral 3CL protease (MP.sup.pro), which function as therapeutics for the treatment of viral infection characterized with PLP.sup.pro and/or M.sup.pro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLP.sup.pro and/or M.sup.pro protease activity and/or expression.
POLYCYCLIC COMPOUND ACTING AS IDO INHIBITOR AND/OR IDO-HDAC DUAL INHIBITOR
Compounds as IDO inhibitors and/or dual inhibitors of IDO-HDAC are described. Specifically, the compounds represented by the following formula (I) are described, wherein each group is defined as described in the specification. The compounds have IDO inhibitory activity or IDO-HDAC dual inhibitory activity and can be used for preventing or treating diseases associated with IDO and/or IDO-HDAC activity or expression levels. At the same time, the compounds of the present invention can be combined with an anti-tumor antibody such as PD-1 and PD-L1, and such a combination can greatly increase the anti-tumor response rate of the antibody and broaden the types of tumors to be treated.
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1-tetrahydropyranylcarbonyl-2,3-dihydro-1H-indole compounds for treating cancer
The present invention relates to certain novel 2,3-dihydro-1H-indole compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer selected from the group consisting of melanoma, acute myeloid leukemia, chronic lymphocytic leukemia, colorectal cancer, breast cancer, lung cancer, ovarian cancer, fallopian tube carcinoma, primary peritoneal carcinoma, cervical cancer, gastric cancer, liver cancer, pancreatic cancer, thyroid cancer, glioblastoma, non-Hodgkin's lymphoma, and Hodgkin's lymphoma. ##STR00001##
1-tetrahydropyranylcarbonyl-2,3-dihydro-1H-indole compounds for treating cancer
The present invention relates to certain novel 2,3-dihydro-1H-indole compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer selected from the group consisting of melanoma, acute myeloid leukemia, chronic lymphocytic leukemia, colorectal cancer, breast cancer, lung cancer, ovarian cancer, fallopian tube carcinoma, primary peritoneal carcinoma, cervical cancer, gastric cancer, liver cancer, pancreatic cancer, thyroid cancer, glioblastoma, non-Hodgkin's lymphoma, and Hodgkin's lymphoma. ##STR00001##
Aliphatic prolinamide derivatives
This invention is directed to novel aliphatic prolinamide derivatives of Formula I, and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention. The compounds of the invention are inhibitors of HTRA1. Thus, the compounds of the invention are useful in the prevention and treatment of a wide range of diseases mediated (in whole or in part) by HTRA1. The compounds of the invention are also useful for inhibiting HTRA1 protease activity in an eye or locus of an arthritis or related condition. ##STR00001##