412299-83-3Relevant academic research and scientific papers
Synthesis of isoindoles by one-electron reductions of dibenzo[1,4]diazocines
Bovenkerk, Marcel,Esser, Birgit
, p. 775 - 785 (2015/01/30)
A synthetic protocol to isoindoles is reported through one-electron reductions of dibenzo[1,4]diazocines. The utility of the approach has been demonstrated through the synthesis of six novel isoindole derivatives. Photophysical measurements revealed emissions between 440 and 460 nm. A reaction mechanism, supported by experimental results and quantum chemical calculations, is postulated.
INDOLINONE ANALOGUES
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Paragraph 0161; 0162; 0163; 0237; 0238, (2014/10/16)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
INDOLINONE ANALOGUES AS BRD4 INHIBITORS
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Page/Page column 52, (2014/10/15)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
Development of Large-Scale Synthesis using a Palladium-Catalyzed Cross-Coupling Reaction for an Isoquinolone Derivative as a Potent DPP-4 Inhibitor
Sera, Misayo,Yamashita, Makoto,Ono, Yuujirou,Tabata, Takashi,Muto, Eigo,Ouchi, Takashi,Tawada, Hiroyuki
, p. 446 - 453 (2014/04/17)
An efficient large-scale synthesis of a novel DPP-4 inhibitor 1, an isoquinolone derivative bearing an aminomethyl group at the 3-position and carbamoylmethoxy group at the 6-position, is described. We have developed an effective and convenient synthetic
Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: A new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554
Banno, Yoshihiro,Miyamoto, Yasufumi,Sasaki, Mitsuru,Oi, Satoru,Asakawa, Tomoko,Kataoka, Osamu,Takeuchi, Koji,Suzuki, Nobuhiro,Ikedo, Koji,Kosaka, Takuo,Tsubotani, Shigetoshi,Tani, Akiyoshi,Funami, Miyuki,Tawada, Michiko,Yamamoto, Yoshio,Aertgeerts, Kathleen,Yano, Jason,Maezaki, Hironobu
experimental part, p. 4953 - 4970 (2011/10/04)
The design, synthesis, and structure-activity relationships of a new class of potent and orally active non-peptide dipeptidyl peptidase IV (DPP-4) inhibitors, 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones, are described. We hypothesized that the 4-ph
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1)
Asano, Yasutomi,Kitamura, Shuji,Ohra, Taiichi,Aso, Kazuyoshi,Igata, Hideki,Tamura, Tomoko,Kawamoto, Tomohiro,Tanaka, Toshimasa,Sogabe, Satoshi,Matsumoto, Shin-ichi,Yamaguchi, Masashi,Kimura, Hiroyuki,Itoh, Fumio
, p. 4715 - 4732 (2008/09/21)
A novel series of 4-phenylisoquinolones were synthesized and evaluated as c-Jun N-terminal kinase (JNK) inhibitors. Initial modification at the 2- and 3-positions of the isoquinolone ring of hit compound 4, identified from high-throughput screening, led to the lead compound 6b. The optimization was carried out using a JNK1-binding model of 6b and several compounds exhibited potent JNK inhibition. Among them, 11g significantly inhibited cardiac hypertrophy in rat pressure-overload models without affecting blood pressure and the concept of JNK inhibitors as novel therapeutic agents for heart failure was confirmed.
Fused heterocyclic compounds
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, (2008/06/13)
The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
BENZOXAZOCINES AND THEIR USE AS MONOAMINE-REUPTAKE INHIBITORS
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Page 19, (2010/02/07)
Compounds of the general formula (1), wherein one of W, X, Y and Z is N or CR4 and the others are each CH; and R4 is a specified substituent. These compounds inhibit monoamine reuptake, and are useful in the treatment of pain, emesis depression, post traumatic stress disorders, attention deficit disorders, obsessive compulsive disorders, pre-menstrual syndrome, substance abuse and sexual dysfunction.
JNK INHIBITOR
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Page 44, (2010/02/09)
A JNK inhibitor containing a compound having an isoquinolinone skeleton or a salt thereof, such as a compound represented by the formula wherein ring A and ring B are each an optionally substituted benzene ring, X is -O-, -N=, -NR3- or -CHR3-, R2 is an acyl group, an optionally esterified or thioesterified carboxyl group, an optionally substituted carbamoyl group or an optionally substituted amino group and the like, a broken line shows a single bond or a double bond, and R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like, and the like.
