1466-74-6Relevant academic research and scientific papers
TRICYCLIC COMPOUND SERVING AS IMMUNOMODULATOR
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, (2019/01/04)
Provided are compounds of formula I and formula II or pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The compounds of formula I and formula II or the pharmaceutically acceptable salts of the compounds provide indole 2,3-dioxygenase (IDO) inhibitory activity and are capable of treating IDO-mediated immunosuppressive diseases, such as infectious diseases or cancer.
PARTIALLY SATURATED NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
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, (2015/06/17)
There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I'): (in the above-mentioned general formula (I'), W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.
Discovery of 6-phenylpyrimido[4,5- B ][1,4]oxazines as potent and selective Acyl CoA: Diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents
Fox, Brian M.,Sugimoto, Kazuyuki,Iio, Kiyosei,Yoshida, Atsuhito,Zhang, Jian,Li, Kexue,Hao, Xiaolin,Labelle, Marc,Smith, Marie-Louise,Rubenstein, Steven M.,Ye, Guosen,McMinn, Dustin,Jackson, Simon,Choi, Rebekah,Shan, Bei,Ma, Ji,Miao, Shichang,Matsui, Takuya,Ogawa, Nobuya,Suzuki, Masahiro,Kobayashi, Akio,Ozeki, Hidekazu,Okuma, Chihiro,Ishii, Yukihito,Tomimoto, Daisuke,Furakawa, Noboru,Tanaka, Masahiro,Matsushita, Mutsuyoshi,Takahashi, Mitsuru,Inaba, Takashi,Sagawa, Shoichi,Kayser, Frank
, p. 3464 - 3483 (2014/05/20)
The discovery and optimization of a series of acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors based on a pyrimido[4,5-b][1,4]oxazine scaffold is described. The SAR of a moderately potent HTS hit was investigated resulting in the discovery of phenylcyclohexylacetic acid 1, which displayed good DGAT1 inhibitory activity, selectivity, and PK properties. During preclinical toxicity studies a metabolite of 1 was observed that was responsible for elevating the levels of liver enzymes ALT and AST. Subsequently, analogues were synthesized to preclude the formation of the toxic metabolite. This effort resulted in the discovery of spiroindane 42, which displayed significantly improved DGAT1 inhibition compared to 1. Spiroindane 42 was well tolerated in rodents in vivo, demonstrated efficacy in an oral triglyceride uptake study in mice, and had an acceptable safety profile in preclinical toxicity studies.
AMINE COMPOUNDS
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Page 226, (2010/02/07)
The present invention provide a compound of the formula:wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.
Potassium dodecatangestocobaltate trihydrate (K5CoW12O40·3H2O): A mild and efficient catalyst for deprotection of dioxolanes and trimethylsilyl ethers
Habibi, Mohammad H,Tangestaninejad, Shahram,Mohammadpoor-Baltork, Iraj,Mirkhani, Valiollah,Yadollahi, Bahram
, p. 6771 - 6774 (2007/10/03)
Mild and easy deprotection of benzylic dioxolanes to carbonyl compounds (in refluxing dry acetone) and trimethylsilyl ethers to alcohols in acetonitrile at ambient temperature has been carried out in excellent yields under K5CoW12O40·3H2O (0.01 molar equiv.) catalysis.
Penicillins having a substituted acrylamido side chain
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, (2008/06/13)
Compounds of formula (I) and their salts and esters: STR1 wherein X is hydrogen or a group NHR1, wherein R1 is hydrogen or an amino protecting group, and R is optionally substituted C5-8 cycloalkyl or cycloalkenyl, are useful in the treatment of bacterial infections.
