Patent classifications
C07D207/14
Heterocyclic compound and application thereof
- Tatsuhiko Fujimoto ,
- Kentaro Rikimaru ,
- Koichiro FUKUDA ,
- Hiromichi Sugimoto ,
- Takahiro Matsumoto ,
- Yuichi KAJITA ,
- Satoshi Mikami ,
- Yuhei MIYANOHANA ,
- Tatsuki KOIKE ,
- Masaki Daini ,
- Masaki Ogino ,
- Kohei TAKEUCHI ,
- Tohru Miyazaki ,
- Yoshiteru ITO ,
- Norihito Tokunaga ,
- Takahiro SUGIMOTO ,
- Tsuneo ODA ,
- Yasutaka HOASHI ,
- Yasushi Hattori ,
- Keisuke IMAMURA
The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the specification, or a salt thereof, has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.
Heterocyclic compound and application thereof
- Tatsuhiko Fujimoto ,
- Kentaro Rikimaru ,
- Koichiro FUKUDA ,
- Hiromichi Sugimoto ,
- Takahiro Matsumoto ,
- Yuichi KAJITA ,
- Satoshi Mikami ,
- Yuhei MIYANOHANA ,
- Tatsuki KOIKE ,
- Masaki Daini ,
- Masaki Ogino ,
- Kohei TAKEUCHI ,
- Tohru Miyazaki ,
- Yoshiteru ITO ,
- Norihito Tokunaga ,
- Takahiro SUGIMOTO ,
- Tsuneo ODA ,
- Yasutaka HOASHI ,
- Yasushi Hattori ,
- Keisuke IMAMURA
The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the specification, or a salt thereof, has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.
COMPOSITIONS AND METHODS FOR TREATING CANCER
K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
COMPOSITIONS AND METHODS FOR TREATING CANCER
K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
Nitrogen-containing heterocyclic compound and use of same
The present invention relates to a compound represented by the formula ##STR00001##
wherein ring A is a nitrogen-containing heterocycle;
ring B is an aromatic ring optionally having substituent(s);
ring D is an aromatic ring optionally having substituent(s);
L is a group represented by the formula ##STR00002## R.sup.2, R.sup.3, R.sup.4a ′ and R.sup.4b are each independently a hydrogen atom, an optionally halogenated C.sub.1-6 alkyl group or an optionally halogenated C.sub.3-6 cycloalkyl group, or R.sup.2 and R.sup.3 are optionally bonded via an alkylene chain or an alkenylene chain, or R.sup.4a and R.sup.4b are optionally bonded via an alkylene chain or an alkenylene chain; R.sup.1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like. The compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, digestive tract diseases, central neurological disease and the like.
Nitrogen-containing heterocyclic compound and use of same
The present invention relates to a compound represented by the formula ##STR00001##
wherein ring A is a nitrogen-containing heterocycle;
ring B is an aromatic ring optionally having substituent(s);
ring D is an aromatic ring optionally having substituent(s);
L is a group represented by the formula ##STR00002## R.sup.2, R.sup.3, R.sup.4a ′ and R.sup.4b are each independently a hydrogen atom, an optionally halogenated C.sub.1-6 alkyl group or an optionally halogenated C.sub.3-6 cycloalkyl group, or R.sup.2 and R.sup.3 are optionally bonded via an alkylene chain or an alkenylene chain, or R.sup.4a and R.sup.4b are optionally bonded via an alkylene chain or an alkenylene chain; R.sup.1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like. The compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, digestive tract diseases, central neurological disease and the like.
SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS
Substituted cyclohexyl chemical entities of Formula (I): wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.
##STR00001##
SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS
Substituted cyclohexyl chemical entities of Formula (I): wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.
##STR00001##
BROAD SPECTRUM ANTI-CANCER COMPOUNDS
Described herein, inter alia, are compounds for treating cancer and methods of use. This disclosure features chemical entities (e.g., small hairpin RNAs (shRNAs), micro RNA (miRNAs), small interfering RNA (siRNAs), small molecule inhibitors, antisense nucleic acids, peptides, viruses, CRISPR-sgRNAs, or combinations thereof) that inhibit one or more of m6A writers (e.g., methyltransferase like 3 (Mettl3 or MT-A70) or methyltransferase like-14 (Mettl14)), m6Am writers (e.g., phosphorylated CTD interacting factor I (PCIF 1), or Mettl3/14), m6A erasers (e.g., fat-mass and obesity-associated protein (FTO) or ALKB homolog 5 (ALKBH5)), m6Am erasers (e.g., FTO), m6A readers (e.g., YTH domain-containing family proteins (YTHs)), YTF domain family member 1 (YTHDF 1), YTF domain family member 2 (YTHDF 2), YTF domain family member 3 (YTHDF 3), or tyrosine-protein phosphatase non-receptor type 2 (PTPN2).
INHIBITORS OF SPINSTER HOMOLOG 2 (SPNS2) FOR USE IN THERAPY
The present disclosure provides SPNS2 inhibitor compounds according to Formula (IA) and Formula (I), and their pharmaceutically acceptable salts, and/or tautomers as described in the disclosure, and the disclosure provides their pharmaceutical compositions and methods of use in therapy.