- Corresponding amine nitrile and method of manufacturing thereof
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The invention relates to a manufacturing method of nitrile. Compared with the prior art, the manufacturing method has the characteristics of significantly reduced using amount of an ammonia source, low environmental pressure, low energy consumption, low production cost, high purity and yield of a nitrile product and the like, and nitrile with a more complex structure can be obtained. The invention also relates to a method for manufacturing corresponding amine from nitrile.
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- COSMETIC COMPOSITIONS WITH TRICYCLODECANE AMIDES
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The invention is directed to a cosmetic composition and the precursor thereof. The composition has solid agent and liquid agent, both of which are cosmetic benefit ingredients. The solubility of solid agents in liquid agents in the inventive compositions is enhanced in the presence of a tricyclodecane amide.
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Paragraph 0128-0129
(2016/02/26)
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- SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
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The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
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Paragraph 0460
(2015/07/22)
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- SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
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The present invention relates to Sulfonamide Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
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Page/Page column 102
(2014/01/17)
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- SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
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The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
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Page/Page column 102
(2014/01/17)
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- SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
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The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
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Paragraph 0459; 0460
(2014/02/15)
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- PHOTOPROTECTIVE COMPOSITIONS WITH TRICYCLODECANE AMIDES
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A personal care photoprotective composition is provided having a UV-A and UV-B sunscreen in conjunction with a tricyclodecane amide. The tricyclodecane amide functions to boost UV-A, UV-B and SPF performance when the personal care composition is applied to skin or hair of the human body.
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Page/Page column 27
(2014/09/29)
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- PROLONGED DELIVERY OF CERTAIN FRAGRANCE COMPONENTS FROM PERSONAL CARE COMPOSITIONS
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A personal care composition is provided having a highly volatile fragrance which incorporates alpha pinene, beta pinene, hexyl acetate, limonene, (+) –citronellal, dihydromyrcenol, alpha citronellol, beta citronellol, genaniol, lilial or combinations thereof in conjunction with tricyclodecane amide. The tricyclodecane amide functions to prevent fast volatilization of the highly volatile fragrance components when the personal care composition is applied to skin or hair of the human body.
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Page/Page column 25
(2014/09/29)
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- THIAZOLE SULFONAMIDE AND OXAZOLE SULFONAMIDE KINASE INHIBITORS
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The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents
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Page/Page column 155
(2010/10/03)
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- OCTAHYDROPYRROLO [3, 4-C] PYRROLE DERIVATIVES AN THEIR USE AS ANTIVIRAL AGENTS
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Chemokine receptor antagonists, in particular, 3,7-diazabicyclo [3.3.0] octane compounds according to formula (I) wherein R1-R3 and Ar are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula (I).
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Page/Page column 40; 66
(2008/06/13)
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- BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS
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Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
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Page/Page column 44-45
(2010/11/28)
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- HETEROARYL SUBSTITUTED PIPERAZINYL-PYRIDINE ANALOGUES
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Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful
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Page/Page column 49
(2008/06/13)
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- Process for producing cyanopiperidine
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The present invention relates to an improved and single step process for producing cyanopiperidine by dehydrating respective piperidine carboxamide employing a suitable dehydrating agent.
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Page/Page column 2
(2008/06/13)
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- INDAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF
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The present invention can provide a cancer treatment drug containing, as an active ingredient, a substance selected from the group consisting of an indazole compound of the following formula (I), a pharmaceutically acceptable salt, a hydrate, a water adduct and a solvate:
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Page/Page column 19
(2010/11/24)
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- CHEMICAL COMPOUNDS
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Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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- Syntheses and Binding Studies of New [(Aryl)(aryloxy)methyl]piperidine Derivatives and Related Compounds as Potential Antidepressant Drugs with High Affinity for Serotonin (5-HT) and Norepinephrine (NE) Transporters
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In a wide search program toward new, efficient, and fast-acting antidepressant drugs, we have prepared series of new compounds having an (aryl)(aryloxy)methyl moiety linked directly or through a methylene chain to different substituted and unsubstituted cycles (isoquinoline, piperazine, piperidine, tetrahydropyran, or cyclopentane). These compounds have been evaluated for their affinities for serotonin (5-HT) transporter (SERT) and 5-HT1A and 5-HT2A receptors. Racemic mixtures of 4-[(aryl)(aryloxy)methyl]piperidine derivatives showed much higher affinity values for SERT than fluoxetine and resulted in lack of affinity for 5-HT 1A and 5-HT2A receptors. Some of these racemic mixtures were resolved to their enantiomers and tested for binding to norepinephrine (NE) transporter (NET), dopamine (DA) transporter (DAT), and α2 receptor. Several of these enantiomers [(-)-15b, (-)-15j, (-)-15t, (+)-15u] displayed a dual binding profile with affinities for SERT and NET with K i i = 1.9 and 13.5 nM, respectively), and further pharmacological characterization is in progress for its evaluation as a antidepressant.
- Orjales, Aurelio,Mosquera, Ramón,Toledo, Antonio,Pumar, M. Carmen,García, Neftalí,Cortizo, Lourdes,Labeaga, Luis,Innerárity, Ana
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p. 5512 - 5532
(2007/10/03)
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- LTA4 Hydrolase inhibitors
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The present invention provides compounds of the formula Ar1-Q-Ar2-Y-R-Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as proriasis, ulcerative colitis, IBD and asthma.
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Page 185 - 186
(2010/01/31)
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- Pyrrolidine modulators of chemokine receptor activity
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The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R14and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
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- Studies on new platelet aggregation inhibitors 1. Synthesis of 7-nitro-3,4-dihydroquinoline-2(1H)-one derivatives
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A series of 6-cyclic aliphatic amino-7-nitro-3,4-dihydroquinoline-2(1H)-ones were prepared and tested for platelet aggregation inhibitory effect, cardiotonic activity and chronotropic activity. These compounds appeared to show selective inhibitory activity against platelet aggregation. Among them, 6-(4-ethoxycarbonylpiperidino)-7-nitro-3,4-dihydroquinoline-2(1H)-one (22f) showed the most potent inhibitory activity and high selectivity. A divergent synthetic route to 6-cyclic aliphatic amino-7-nitro-3,4-dihydroquinoline-2(1H)-one derivatives has also been investigated.
- Iyobe,Uchida,Kamata,Hotel,Kusama,Harada
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p. 822 - 829
(2007/10/03)
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- Aroylethenylpiperidinobutyrophenone antipsychotic agents
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4-Aroylethnyl-1-piperidinobutyrophenone derivatives and pharmaceutically acceptable salts thereof of the following general structure: STR1 wherein R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl; and R' is hydrogen or halogen, are useful as antipsychotic agents. The novel compounds are produced by aldol condensation of an acetophenone with a protected 4-(4-formyl-1-piperidino)-butyrophenone.
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- Cinnamoylpiperidinobutyrophenone antipsychotic agents
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Cinnamoylpiperidinobutyrophenone derivatives and pharmaceutically acceptable salts thereof of the following general structure: STR1 wherein R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl; and R' is hydrogen or halogen; are useful as antipsychoti
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