340962-84-7Relevant academic research and scientific papers
PYRIDAZINONES AS PARP7 INHIBITORS
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Page/Page column 93, (2021/05/07)
The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
CARBAMATE COMPOUNDS AND OF MAKING AND USING SAME
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Paragraph 00506, (2013/10/08)
Provided herein are carbamate compounds which may be useful in the treatment of, for example, pain, solid tumors and/or obesity.
Discovery of a tetrahydropyrimidin-2(1 H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor
Fujimoto, Takuya,Imaeda, Yasuhiro,Konishi, Noriko,Hiroe, Katsuhiko,Kawamura, Masaki,Textor, Garret P.,Aertgeerts, Kathleen,Kubo, Keiji
experimental part, p. 3517 - 3531 (2010/09/10)
Coagulation enzyme factor Xa (FXa) is a particularly promising target for the development of new anticoagulant agents. We previously reported the imidazo[1,5-c]imidazol-3-one derivative 1 as a potent and orally active FXa inhibitor. However, it was found that 1 predominantly undergoes hydrolysis upon incubation with human liver microsomes, and the human specific metabolic pathway made it difficult to predict the human pharmacokinetics. To address this issue, our synthetic efforts were focused on modification of the imidazo[1,5-c] imidazol-3-one moiety of the active metabolite 3a, derived from 1, which resulted in the discovery of the tetrahydropyrimidin-2(1H)-one derivative 5k as a highly potent and selective FXa inhibitor. Compound 5k showed no detectable amide bond cleavage in human liver microsomes, exhibited a good pharmacokinetic profile in monkeys, and had a potent antithrombotic efficacy in a rabbit model without prolongation of bleeding time. Compound 5k is currently under clinical development with the code name TAK-442.
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues
Qiao, Jennifer X.,Cheng, Xuhong,Smallheer, Joanne M.,Galemmo, Robert A.,Drummond, Spencer,Pinto, Donald J.P.,Cheney, Daniel L.,He, Kan,Wong, Pancras C.,Luettgen, Joseph M.,Knabb, Robert M.,Wexler, Ruth R.,Lam, Patrick Y.S.
, p. 1432 - 1437 (2007/10/03)
The synthesis, SAR, pharmacokinetic profile, and modeling studies of both monocyclic and fused pyrazoles containing substituted N-arylpiperidinyl P4 moieties that are potent and selective factor Xa inhibitors will be discussed. Fused pyrazole analog 16a,
High-yielding syntheses of 1-piperidin-4-yl butyro- and valerolactams through a tandem reductive animation-lactamization (reductive lactamization)
Mapes, Christopher M.,Mani, Neelakandha S.
supporting information, p. 482 - 486 (2012/12/31)
We report a procedure for the concise and high-yielding syntheses of 1-piperidin-4-yl-substituted butyro- and valero-lactams. Beginning with 1-benzyl-4-piperidone and γ- or δ-amino esters or acids, we have effected a tandem reductive animation lactamizati
SUBSTITUTED OXIMES AS NEUROKININ ANTAGONISTS
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Page 13, (2010/02/05)
Compounds within the genus represented by structural formula (I) or a pharmaceutically acceptable salt thereof, wherein: T is substituted phenyl or substituted pyridyl; R is H, methyl, ethyl, -CH2CN, -CH2C(O)NH2, -(CH2)3SO3H, -CH2C(O)NHCH3, -CH2C(O)NHOH, -CH2C(O)NHOCH3, -CH2C(O)NHCH2CN, -CH2F, -CH2C(O)NHCH2SO3H, (a), (b), (c), (d) or (e); R is methyl or ethyl; and Z is substituted piperidinyl.
Substituted amino methyl factor Xa inhibitors
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, (2008/06/13)
The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors
Ting, Pauline C,Lee, Joe F,Anthes, John C,Shih, Neng-Yang,Piwinski, John J
, p. 491 - 494 (2007/10/03)
The NK1 and NK2 receptor activity of a series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4(Z)- (methoxyimino)pentyl-1-piperidines was evaluated. Compounds 11d, 11e, 11f, 12a, and 12k were found to be our most potent inhibitors.
