1624258-63-4Relevant academic research and scientific papers
Stereoelectronic substituent effects in polyhydroxylated piperidines and hexahydropyridazines
Jensen, Henrik Helligso,Lyngbye, Laila,Jensen, Astrid,Bols, Mikael
, p. 1218 - 1226 (2002)
From the pKa values of the conjugate acids of a large series of hydroxylated piperidines and hexahydropyridazines, a consistent difference in basicity was found between stereo-isomers having an axial or equatorial hydroxyl (OH) group either β o
Straightforward and scalable synthesis of orthogonally protected 3,7-diazabicyclo[4.1.0]heptane
Schramm, Heiko,Pavlova, Maria,Hoenke, Christoph,Christoffers, Jens
, p. 1659 - 1662 (2009)
Orthogonally N-protected (Boc and Cbz) 3,4-aziridinopiperidine is a versatile building block for the synthesis of 4-substituted 3-aminopiperidines, which are compounds with a high potential for biological activity. A multigram synthesis over five steps, starting with extraordinarily simple materials (pyridine and benzyl chloride), was developed. Georg Thieme Verlag Stuttgart.
Regio- and stereo-controlled copper organometallic addition to a piperidinyl aziridine: Synthesis of trans 3-amino-4-alkyl-piperidines
Hu, X.Eric,Kim, Nick K,Ledoussal, Benoit,Colson, Anny-Odile
, p. 4289 - 4293 (2002)
3,4-Piperidinyl aziridine N-phosphonate underwent ring opening in Grignard addition catalyzed by a copper reagent to yield trans 3-amino-4-alkyl-piperidines. The nucleophilic addition occurred trans to the aziridine group and regioselectively at C-4 position of the piperidine ring. The high regioselectivity was rationalized by steric argument based on conformational analysis.
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases
Epple, Robert,Urbina, Hugo D.,Russo, Ross,Liu, Hong,Mason, Daniel,Bursulaya, Badry,Tumanut, Christine,Li, Jun,Harris, Jennifer L.
, p. 1254 - 1259 (2007)
A 6-oxa-1-aza-bicyclo[3.2.1]octan-7-one system inhibits the proteolytic activity of several cysteine proteases belonging to the papain family. In vitro mechanistic studies and in silico calculations suggest that the minimal π-overlap between the bridgehea
HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Page/Page column 81-83, (2021/06/26)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
ANTIBACTERIAL COMPOUNDS
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Page/Page column 52-53, (2017/09/05)
This invention relates to antibacterial drug compounds containing a bicyclic core, typically a bicycle in which one of the rings is an oxazolidinone. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections and in methods of treating bacterial infections.
BENZOIMIDAZOLE DERIVATIVES AS PAD4 INHIBITORS
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Page/Page column 98; 99, (2016/12/07)
Compounds of formula (I): wherein X, Y, R1 and R3-R11 are as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
PROTEIN KINASE C INHIBITORS AND METHODS OF THEIR USE
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Paragraph 0160, (2016/04/20)
PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absor
1H-PYRROLO[2,3-B] PYRIDINE DERIVATIVES AND THEIR USE AS KINASE INHIBITORS
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Paragraph 0408, (2015/02/18)
The inventions relates to compounds of (I) and therapeutic uses thereof: (I) The terms Z, Y, and R1 are as defined in the claims.
2-(AZAINDOL-2-YL)BENZIMIDAZOLES AS PAD4 INHIBITORS
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Paragraph 0443; 0444; 0445, (2015/07/02)
Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl;R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy;R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl;R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6 alkyl;A is C—R5 or N;B is C—R6 or N;D is C—R7 or N;with the proviso that at least one of A, B, and D, is N;R5 is hydrogen or C1-6alkyl;R6 is hydrogen or C1-6alkyl;R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy;R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen;R9 is hydrogen or hydroxy;R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
