- Preparation method of 4-oxo-8-azaspiro [4.5] dec-2-ene-8-carboxylic acid tert-butyl ester (benzyl ester)
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The invention discloses a preparation method of 4-oxo-8-azaspiro [4.5] dec-2-ene-8-carboxylic acid tert-butyl ester (benzyl ester) and an intermediate thereof. The preparation method comprises the following steps: reacting a compound II with 3-bromopropylene under the action of alkali 1 to generate a compound III; dissolving the compound III in a solvent, carrying out cyclization under the action of lithium diisopropylamide, and reacting to generate a compound IV; and under the action of alkali 2, carrying out double bond shift on the compound IV to generate a compound I. The method has the advantages of easily available raw materials, simple operation and high yield, the total yield can reach more than 65%, and the method is suitable for large-scale preparation.
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Paragraph 0039-0042
(2021/07/08)
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- INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
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Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions.
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Paragraph 0371; 0372
(2018/09/16)
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- Spirocyclic derivatives
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The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter); and methods of treating patients with such compounds; wherein R1, R2, R3, R4, R5, R6, R9, R10, Q, X, Y, Z, A, L, B, m, n and p are as defined herein.
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Page/Page column 203
(2016/04/09)
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- 2-[BIS(4-FLUOROPHENYL)METHYL]-2,7-DIAZASPIRO[4.5]DECAN-10-ONE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE HUMAN DOPAMINE-ACTIVE-TRANSPORTER (DAT) PROTEIN FOR THE TREATMENT OF E.G. ATTENTION DEFICIT DISORDER (ADD)
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The present invention provides compounds of formula (I) and in particular 2-[bis(4-fluorophenyl)methyl]-2,7- diazaspiro[4.5]decan-10-one derivatives and related compounds as inhibitors of human dopamine-active-transporter (DAT) protein for the treatment of sexual dysfunction, affective disorders, anxiety, depression, chronic fatigue, Tourette syndrome, Angelman syndrome, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), obesity, pain, obsessive-compulsive disorder, movement disorders, CNS disorders, sleep disorders, narcolepsy, conduct disorder, substance abuse (including smoking cessation), eating disorders, and impulse control disorders.
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Page/Page column 92
(2016/04/09)
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- ANTIBACTERIAL COMPOUNDS
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The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
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Page/Page column 35
(2012/04/18)
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- COMPOUND HAVING SPIRO-BONDED CYCLIC GROUP AND USE THEREOF
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The invention relates to a compound represented by formula (I): a salt thereof, an N-oxide thereof, or a solvate thereof (symbols in the formula are as described in the specification). The compound of the present invention exhibits very low risk of side effects and also has persistent and strong antagonistic activity against CXCR4, and is therefore useful as for example, preventive and/or therapeutic agent for inflammatory and immune diseases, infections (for example, HIV infection), diseases associated with HIV infection (for example, acquired immunodeficiency syndrome (AIDS)), cancer, cancer metastasis, psychoneurotic diseases and cardiovascular diseases (for example, retinopathy), metabolic diseases, cancerous diseases, or an agent for regeneration therapy.
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Page/Page column 50
(2012/05/04)
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- Novel piperidinyl monocarboxylic acids as S1P1 receptor agonists
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The present invention relates to novel compounds acting as agonists at S1P (sphingosine-1-phosphate) receptors, compositions containing these compounds, use of these compounds in medicine and their process of preparation.
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Page/Page column 17-18
(2012/11/06)
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- NOVEL PIPERIDINYL MONOCARBOXYLIC ACIDS AS S1P1 RECEPTOR AGONISTS
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The present invention relates to novel compounds acting as agonists at S1P (sphingosine-1-phosphate) receptors, compositions containing these compounds, use of these compounds in medicine and their process of preparation.
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Page/Page column 34
(2012/11/06)
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- SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims respectively a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (I) (Ia) and formula (Ib) as described herein. More specifically, the compounds of this invention
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Page/Page column 33-34
(2011/12/02)
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- SUBSTITUTED N-HETEROARYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula ( Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described her
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Page/Page column 25-26
(2011/12/02)
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- Design, syntheses, and SAR of 2,8-diazaspiro[4.5]decanones as T-type calcium channel antagonists
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It was hypothesized that an appropriately substituted 2,8-diazaspiro[4.5] decan-1-one could effectively approximate a 5-feature T-type pharmacophore model published in the literature. Compounds were designed and synthesized to test our hypothesis and were found to be potent T-type calcium channel inhibitors with modest selectivity over L-type calcium channels. The synthesis and SAR of the series is described.
- Fritch, Paul C.,Krajewski, Jeffrey
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scheme or table
p. 6375 - 6378
(2010/11/18)
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- SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONES USED AS H3 MODULATORS
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The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I), wherein R1, R2, R3, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptor
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Page/Page column 34
(2010/06/20)
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- Amidine compounds
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A compound of the formula [I] wherein R1, R2and R3are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the presen
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- Cyclohexyl derivatives and their use as therapeutic agents
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The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
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- 4,4-Disubstituted cyclohexylamine NK1 receptor antagonists II
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A series of novel 4,4-disubstituted cyclohexylamines as NK1 receptor antagonists is described: modifications to the amine moiety retain NK1 receptor binding affinity whilst disrupting IKr affinity.
- Cooper, Laura C.,Carlson, Emma J.,Castro, Jose L.,Chicchi, Gary G.,Dinnell, Kevin,Di Salvo, Jerry,Elliott, Jason M.,Hollingworth, Gregory J.,Kurtz, Marc M.,Ridgill, Mark P.,Rycroft, Wayne,Tsao, Kwei-Lan,Swain, Christopher J.
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p. 1759 - 1762
(2007/10/03)
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- Heterocyclylalkylpiperidine derivatives, their preparation and compositions containing them
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Heterocyclylalkylpiperidine derivatives of general formula (I) in their enantiomeric or diastereoisomeric forms or mixtures of these forms, and/or, where appropriate, in their syn or anti form or a mixture thereof, as well as any salt thereof.
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- N-acyl cyclic amine derivatives
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The invention relates to compounds represented by the general formula [I][wherein Ar means an aryl group or a heteroaryl group which may have a substitutive group selected from a group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; R1 means a C3-C6 cycloalkyl group which is substitutable with a fluorine atom; R2 and R4 mean hydrogen atoms, groups represented by -(A1)m-NH-B or the like; R3 and R5 mean hydrogen atoms, C1-C6 aliphatic hydrocarbon groups or the like which are substitutable with a lower alkyl group(s); n means 0 or 1; and X means an oxygen atom or a sulfur atom]. Compounds according to the invention, since they not only have potent selective antagonistic activity against muscarinic M3 receptors but also exhibit excellent oral activity, durability of action and pharmacokinetics, are very useful as safe and effective remedies against respiratory, urinary and digestive diseases with little adverse side effects.
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