38555-41-8Relevant academic research and scientific papers
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent
Kerns, Jeffrey K.,Busch-Petersen, Jakob,Fu, Wei,Boehm, Jeffrey C.,Nie, Hong,Muratore, Michael,Bullion, Ann,Lin, Guoliang,Li, Huijie,Davis, Roderick,Lin, Xichen,Lakdawala, Ami S.,Cousins, Rick,Field, Rita,Payne, Jeremy,Miller, David D.,Bamborough, Paul,Christopher, John A.,Baldwin, Ian,Osborn, Ruth R.,Yonchuk, John,Webb, Edward,Rumsey, William L.
supporting information, p. 1164 - 1169 (2018/11/23)
IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization of a series of 3,5-disubstituted-indole-7-carboxamides for oral activity. In doing so
Synthesis of Cyclic α-Diazo-β-keto Sulfoxides in Batch and Continuous Flow
McCaw, Patrick G.,Buckley, Naomi M.,Eccles, Kevin S.,Lawrence, Simon E.,Maguire, Anita R.,Collins, Stuart G.
, p. 3666 - 3679 (2017/04/11)
Diazo transfer to β-keto sulfoxides to form stable isolable α-diazo-β-keto sulfoxides has been achieved for the first time. Both monocyclic and benzofused ketone derived β-keto sulfoxides were successfully explored as substrates for diazo transfer. Use of continuous flow leads to isolation of the desired compounds in enhanced yields relative to standard batch conditions, with short reaction times, increased safety profile, and potential to scale up.
Tetrahydrothiopyran and pyrimidine derivatives and its preparation method and application (by machine translation)
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Paragraph 0043; 0048; 0049; 0050, (2017/01/19)
The invention discloses four diazanaphthylaone compound and its preparation method and application. The [...] and pyrimidines compound or its pharmaceutically acceptable salt or prodrug, has the following general formula I or II of the structure is shown, the invention also comprises four diazanaphthylaone compounds of preparation method and and containing one or more of such compounds in the preparation of the composition for the treatment and prevention of human immunodeficiency virus (HIV) application of the medicament. (by machine translation)
Identification of the 5,5-dioxo-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidine derivatives as highly selective PDE4B inhibitors
Goto, Taiji,Shiina, Akiko,Murata, Takeshi,Tomii, Masato,Yamazaki, Takanori,Yoshida, Ken-Ichi,Yoshino, Toshiharu,Suzuki, Osamu,Sogawa, Yoshitaka,Mizukami, Kiyoshi,Takagi, Nana,Yoshitomi, Tomomi,Etori, Maki,Tsuchida, Hiroshi,Mikkaichi, Tsuyoshi,Nakao, Naoki,Takahashi, Mizuki,Takahashi, Hisashi,Sasaki, Shigeki
supporting information, p. 893 - 899 (2014/02/14)
A PDE4B subtype selective inhibitor is expected to have a wider therapeutic window than non-selective PDE4 inhibitors. In this Letter, two series of 7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidine derivatives and 5,5-dioxo-7,8- dihydro-6H-thiopyrano[3,2-d]pyri
Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors
Goto, Taiji,Shiina, Akiko,Yoshino, Toshiharu,Mizukami, Kiyoshi,Hirahara, Kazuki,Suzuki, Osamu,Sogawa, Yoshitaka,Takahashi, Tomoko,Mikkaichi, Tsuyoshi,Nakao, Naoki,Takahashi, Mizuki,Hasegawa, Masashi,Sasaki, Shigeki
supporting information, p. 3325 - 3328 (2013/06/27)
2-Phenyl-4-piperidinyl-6,7-dihydrothieno[3,4-d]pyrimidine derivative (2) was found to be a new PDE4 inhibitor with moderate PDE4B activity (IC 50 = 150 nM). A number of derivatives with a variety of 4-amino substituents and fused bicyclic pyrim
INDOLE CARBOXAMIDES AS IKK2 INHIBITORS
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Page/Page column 95, (2008/12/04)
The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Beta-Amino-Acid derivatives as inhibitors of matrix metalloproteases and TNF-Alpha
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, (2008/06/13)
The present application describes novel β-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3, R4, and R4a are defined in the present specification, which are useful as metalloprotease and/or as TNF-α inhibitors.
Anesthesia methods using benzopyrans and esters thereof as pre-anesthesia medication
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, (2008/06/13)
Improved anesthesia methods comprising pretreating a patient to be anesthetized with a benzopyran of formula I STR1 wherein, in the C ring, X is NR1, S, CH2 or STR2 R1 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, loweralkanoyl, cycloalkyloweralkyl, cycloalkylloweralkanoyl, cycloalkyl, haloloweralkyl, haloloweralkenyl, phenylloweralkyl, phenyloweralkenyl or phenyloweralkylnyl; m is an integer from 0 to 3, n is an integer from 0 to 3 and n + m = 2 or 3; or the C ring is quinuclidine ring STR3 R2 is loweralkyl; R3 is hydrogen or STR4 wherein Y is a straight or branched chain alkylene group having from one to eight carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4, Z is CH2, O, S or NR6, R6 being hydrogen or loweralkyl, with the limitation that when Z is O, S or NR5, the sum of a and b is 3 or 4, and R5 is hydrogen or loweralkyl; R4 is C1 -C20 straight or branched chain alkyl, cycloalkyl, or STR5 wherein Y is a straight or branched chain alkylene group having from one to ten carbon atoms, and each R7, R8 and R9 are the same or different members of the group consisting of hydrogen, halo, trifluoromethyl or loweralkyl; and the pharmaceutically acceptable salts thereof, with the limitation that when X is STR6 m = 2 and n = 2, R3 cannot be hydrogen.
Method of producing analgesia and compositions useful therein
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, (2008/06/13)
A method of relieving pain in a mammalian patient suffering therefrom by administering 1,2-dihydro-5,5-dimethyl-10-hydroxy-8-(3-methyl-2-octyl)-3H,5H-thiopyrano[2,3-c][1]benzopyran.
Method of treating hypertension with, and compositions useful therein containing, a 4H-thieno[2,3-c][1]benzopyran or a 3H,5H-thiopyrano[2,3-c][1]
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, (2008/06/13)
A method of reducing blood pressure in a hypertensive mammalian patient by administering 1,2-dihydro-4,4-dimethyl-9-hydroxy-7-(3-methyl-2-octyl)-4H-thieno[2,3-c][1]benzopyran or 1,2-dihydro-5,5-dimethyl-10-hydroxy-8-(3-methyl-2-octyl)-3H,5H-thiopyrano-8 2,3-c][1]benzopyran. Pharmaceutical compositions containing 1,2-dihydro-4,4-dimethyl-9-hydroxy-7-(3-methyl-2-octyl)-4H-thieno[2,3-c][1]benzopyran or 1,2-dihydro-5,5-dimethyl-10-hydroxy-8-(3-methyl-2-octyl)-3H,5H-thiopyrano[2,3-c][1]benzopyran dispersed in a pharmaceutical carrier.
