- 1-CYANO-PYRROLIDINE DERIVATIVES AS DUB INHIBITORS
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The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The novel compounds have formula (I): (Formula (I)) or are pharmaceutically acceptable salts thereof, wherein: R1a, R1b, R1c, R1d, R1e and R1f each independently represent hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C3-C4 cycloalkyl, or R1b and R1c together form an optionally substituted C3-C6 cycloalkyl ring, or R1d and R1e together form an optionally substituted C3-C6 cycloalkyl ring; R2 represents hydrogen or optionally substituted C1-C6 alkyl; A represents an optionally further substituted 5 to 10 membered monocyclic or bicyclic heteroaryl, heterocyclyl or aryl ring; L represents a covalent bond or linker; B represents an optionally substituted 3 to 10 membered monocyclic or bicyclic heterocyclyl, heteroaryl, cycloalkyl or aryl ring; and when -A-L-B is at position x attachment to A is via a carbon ring atom of A, and either: A cannot be triazolopyridazinyl, triazolopyridinyl, imidazotriazinyl, imidazopyrazinyl or pyrrolopyrimidinyl; or B cannot be substituted with phenoxyl; or B cannot be cyclopentyl when L is an oxygen atom.
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Paragraph 0847-0848
(2020/11/30)
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- A Bifunctional Reagent Designed for the Mild, Nucleophilic Functionalization of Pyridines
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Herein is reported the design and application of a reagent for the direct functionalization of pyridines. These reactions occur under mild conditions and exhibit broad functional group tolerance, enabling the late-stage functionalization of drug-like molecules. The reagent can be easily prepared on large scale from inexpensive reagents, and reacts in the title reaction with acetonitrile, sodium chloride, and sodium methanesulfonate as the sole byproducts. Although this Communication focuses primarily on reactions with cyanide as nucleophile, preliminary experiments with other nucleophiles foreshadow the broad reaching synthetic utility of this approach.
- Fier, Patrick S.
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p. 9499 - 9502
(2017/07/24)
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- SILICON-BASED CROSS COUPLING AGENTS AND METHODS OF THEIR USE
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Compositions and methods using silicon-based cross-coupling agents in the formation of carbon-carbon and carbon-nitrogen bonds are described.
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Paragraph 0055
(2016/02/10)
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- SILICON-BASED CROSS COUPLING AGENTS AND METHODS OF THEIR USE
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Compositions and methods using silicon-based cross-coupling agents in the formation of carbon-carbon and carbon-nitrogen bonds are described.
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Paragraph 0049
(2014/01/08)
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- Unification of anion relay chemistry with the Takeda and Hiyama cross-coupling reactions: Identification of an effective silicon-based transfer agent
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The unification of Anion Relay Chemistry (ARC) with the Takeda and Hiyama palladium-mediated cross-coupling processes to provide aryl-aryl, alkenyl-aryl, and alkenyl-alkenyl coupled products by exploiting a common silicon-based transfer agent has been achieved. These results provide a practical solution for intermolecular cross-coupling of organolithium reagents without the problematic lithium-halogen exchange and/or undesired homocoupling that has kept organolithium cross-couplings from achieving the same level of utility asother palladium-mediated methods (e.g., Suzuki organoboron, Negishi organozinc, Stille organotin, Kumada organomagnesium, etc.).
- Smith III, Amos B.,Hoye, Adam T.,Martinez-Solorio, Dionicio,Kim, Won-Suk,Tong, Rongbiao
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supporting information; experimental part
p. 4533 - 4536
(2012/04/23)
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- Synthesis of biaryls through a one-pot tandem borylation/Suzuki-Miyaura cross-coupling reaction catalyzed by a palladacycle
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The tricyclohexylphosphane adduct of cyclopalladated ferrocenylimine I exhibited high catalytic activity in the one-pot borylation/Suzuki-Miyaura coupling (BSC) reaction with low catalyst loading (2 mol-%). Various biaryls were obtained in good to excellent yields for 37 examples. This process was applied to aryl and heteroaryl halides (Br and Cl) containing a variety of functional groups and did not require an excess amount of phosphane ligand and the addition of the palladium catalyst in the second step. Cyclopalladated ferrocenylimine I exhibited high catalytic activity in the borylation/Suzuki- Miyaura coupling (BSC) reaction with low catalyst loading. Various unsymmetrical biaryls were obtained ingood to excellent yields in one pot. This protocol was applied to aryl and heteroaryl halides (Br and Cl) containing a variety of functional groups without adding catalyst in the second step. Copyright
- Wang, Lianhui,Cui, Xiuling,Li, Jingya,Wu, Yusheng,Zhu, Zhiwu,Wu, Yangjie
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p. 595 - 603
(2012/03/09)
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- SUBSTITUTED 2-PHENYL-PYRIDINE DERIVATIVES
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The present invention relates to compounds of formula I wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
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Page/Page column 25
(2011/04/14)
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- PYRIDINE COMPOUND AND USE THEREOF FOR PEST CONTROL
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A pyridine compound represented by general formula (I): (wherein, R1 represents a C1-C7 alkyl group optionally substituted by halogen, or the like, m represents an integer of 1 to 5, A represents a single bond, an oxygen atom, a sulfur atom, or the like, R2 represents a C1-C7 alkyl group optionally substituted by halogen, or the like.); a pest controlling composition comprising as an active ingredient the pyridine compound; a pest controlling method comprising applying the pyridine compound to a pest or a place where a pest inhabits.
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Page/Page column 55
(2011/06/26)
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- SUBSTITUTED 2-PHENYL-PYRIDINE DERIVATIVES
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The present invention relates to compounds of formula (I) wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
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Page/Page column 61
(2009/11/29)
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- 2-AMINOCARBONYL-PYRIDINE DERIVATIVES
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The present invention relates to 2-aminocarbonyl-pyridine derivatives and their use as P2Yi2 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
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Page/Page column 80
(2008/06/13)
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- 1,3-BENZOTHIAZINONE DERIVATIVES AND USE THEREOF
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This invention provides a compound represented by the formula (I) :wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents;R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents;n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I) , which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
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- Novel chiral oxazoline ligands for potential charge-transfer effects in the Rh(I)-catalysed enantioselective hydrosilylation
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Novel 2-(4,4′-bipyridin-2-yl)oxazolines, bearing a chiral oxazoline moiety, were synthesised starting from 4,4′-bipyridine and selectively monomethylated in the N′-position. After coordination to rhodium these electron-poor ligands are supposed to exhibit charge-transfer effects with electron-donating substrates in the Rh(I)-catalysed enantioselective hydrosilylation (see next publication). Similar effects were expected from 4,4′-bipyridine- and pyrazine-bisoxazolines after complexation with rhodium. For comparison 2-(4-phenylpyridin-2-yl)oxazoline ligands were synthesised. Rh(I)-complexes of selected ligands were prepared and characterised, including an X-ray structure analysis.
- Brunner, Henri,Stoeriko, Reinhard,Rominger, Frank
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p. 771 - 781
(2007/10/03)
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- 28. Novel thiazole-containing complexing agents and luminescence of their europium(III) and terbium(III) chelates
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The synthesis of novel thiazole-containing complexing agents and their luminescence properties with EuIII and TbIII ions are reported. One of these terpyridine analogues was also tested as an EuIII labelling reagent, and its luminescence properties as an antibody conjugate were studied.
- Mukkala, Veli-Matti,Liitti, Paeivi,Hemmilae, Ilkka,Takalo, Harri,Matachescu, Cristina,Kankare, Jouko
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p. 295 - 306
(2007/10/03)
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- 2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
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The present invention is directed to certain piperidine, pyrrolidine, and hexahydro-1H-azepine compounds of the general structural formula: STR1 wherein R1, R3, R4, R5, A, W, X, Y, and n axe as defined herein. T
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- 2-Pyridylcarboxamides which inhibit arachidonic acid release
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2-Pyridylcarboxamides are provided having the structure STR1 wherein n is 1 to 10; R is hydrogen, lower alkyl, alkali metal or an amine salt; and R1 is C6 -C20 alkyl, C6 -C20 alkenyl, C6 to C20 alkoxy or phenyl. These compounds are useful as inhibitors of arachidonic acid release and as such are useful as antiallergy agents.
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