146603-99-8Relevant articles and documents
Preparation method of 4-oxo-8-azaspiro [4.5] dec-2-ene-8-carboxylic acid tert-butyl ester (benzyl ester)
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Paragraph 0039-0042, (2021/07/08)
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.
INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
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Paragraph 0371; 0372, (2018/09/16)
Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions.
Spirocyclic derivatives
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Page/Page column 203, (2016/04/09)
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.
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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Page/Page column 92, (2016/04/09)
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.
ANTIBACTERIAL COMPOUNDS
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Page/Page column 35, (2012/04/18)
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.
COMPOUND HAVING SPIRO-BONDED CYCLIC GROUP AND USE THEREOF
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Page/Page column 50, (2012/05/04)
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.
Novel piperidinyl monocarboxylic acids as S1P1 receptor agonists
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Page/Page column 17-18, (2012/11/06)
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.
NOVEL PIPERIDINYL MONOCARBOXYLIC ACIDS AS S1P1 RECEPTOR AGONISTS
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Page/Page column 34, (2012/11/06)
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.
SUBSTITUTED N-HETEROARYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF
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Page/Page column 25-26, (2011/12/02)
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
SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF
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Page/Page column 33-34, (2011/12/02)
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