Patent classifications
C07D215/02
AGENT FOR INTRODUCING PROTECTING GROUP FOR HYDROXY GROUP AND/OR MERCAPTO GROUP
A novel agent for introducing a protecting group for a hydroxy group and/or a mercapto group that can be introduced and removed under mild conditions is provided. The agent for introducing a protecting group for a hydroxy group and/or mercapto group of a substrate compound having the hydroxy group and/or mercapto group is represented by the following formula (I), wherein A represents a ring structure having 1 to 5 rings in which two carbon atoms of an adjacent benzene ring are included, the ring structure comprises a substituted or unsubstituted five-membered ring or six-membered ring and optionally include a heterocycle; each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 is independently a hydrogen atom or a linear or branched alkyl group having 1 to 5 carbon atoms; and X is a halogen atom or OSO.sub.2R.sup.5 (R.sup.5=an aryl group or an alkyl group).
AGENT FOR INTRODUCING PROTECTING GROUP FOR HYDROXY GROUP AND/OR MERCAPTO GROUP
A novel agent for introducing a protecting group for a hydroxy group and/or a mercapto group that can be introduced and removed under mild conditions is provided. The agent for introducing a protecting group for a hydroxy group and/or mercapto group of a substrate compound having the hydroxy group and/or mercapto group is represented by the following formula (I), wherein A represents a ring structure having 1 to 5 rings in which two carbon atoms of an adjacent benzene ring are included, the ring structure comprises a substituted or unsubstituted five-membered ring or six-membered ring and optionally include a heterocycle; each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 is independently a hydrogen atom or a linear or branched alkyl group having 1 to 5 carbon atoms; and X is a halogen atom or OSO.sub.2R.sup.5 (R.sup.5=an aryl group or an alkyl group).
Aryl-quinoline derivatives
The invention provides novel compounds having the general formula (I) ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
Aryl-quinoline derivatives
The invention provides novel compounds having the general formula (I) ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
Compounds for inhibition of α4β7 integrin
- Peter A. Blomgren ,
- Taryn Campbell ,
- Jayaraman Chandrasekhar ,
- Christopher T. Clark ,
- Julian A. Codelli ,
- Kevin S. Currie ,
- Jeffrey E. Kropf ,
- Yasamin Moazami ,
- Nicole Nava ,
- Leena Patel ,
- Stephane Perreault ,
- Jason K. Perry ,
- Kassandra F. Sedillo ,
- Natalie Seeger ,
- Kirk L. Stevens ,
- Jennifer Anne Treiberg ,
- Suet C. Yeung ,
- Zhongdong Zhao
The present disclosure provides a compound of Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
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. ##STR00001##
Indoleamine 2,3-dioxygenase inhibitors and use of same in medicine
The present invention relates to a compound represented by formula I, a pharmaceutical composition containing the compound of formula I, a method for inhibiting indoleamine 2,3-dioxygenase, and its use in medicine. ##STR00001##
SUBSTITUTED 2-PYRIDONE TRICYCLIC COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME
The present invention includes in one aspect substituted 2-oxo-1,2,5,6-tetrahydrobenzo[h]quinoline-3-carboxylic acids, analogues thereof, and compositions comprising the same, which can be used to treat and/or prevent hepatitis B virus (HBV) infection and/or hepatitis D virus (HDV) in a patient. In certain embodiments, the invention provides a compound of formula (I), or a salt, solvate, geometric isomer, stereoisomer, tautomer, and any mixtures thereof:
##STR00001##
SUBSTITUTED 2-PYRIDONE TRICYCLIC COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME
The present invention includes in one aspect substituted 2-oxo-1,2,5,6-tetrahydrobenzo[h]quinoline-3-carboxylic acids, analogues thereof, and compositions comprising the same, which can be used to treat and/or prevent hepatitis B virus (HBV) infection and/or hepatitis D virus (HDV) in a patient. In certain embodiments, the invention provides a compound of formula (I), or a salt, solvate, geometric isomer, stereoisomer, tautomer, and any mixtures thereof:
##STR00001##
Novel Amide Compound, and Pin1 Inhibitor, Therapeutic Agent for Inflammatory Diseases and Therapeutic Agent for Cancer That Use the Same
The purpose of the invention is to develop, as drug-candidate compounds, a group of novel compounds having the activity of inhibiting functions of Pin1. The invention provides: a compound represented by formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic or prophylactic agent for inflammatory diseases, a therapeutic or prophylactic agent for cancer, and a therapeutic or prophylactic agent for adiposity that use said compound/salt.
##STR00001##