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    Novel interleukin-1 and tumor necrosis factor-alpha modulators, synthesis of said modulators and their enantiomers and methods of using said modulators
    24.
    发明申请
    Novel interleukin-1 and tumor necrosis factor-alpha modulators, synthesis of said modulators and their enantiomers and methods of using said modulators 有权

    公开(公告)号：US20060252832A1

    公开(公告)日：2006-11-09

    申请号：US11417906

    申请日：2006-05-03

    申请人： Michael Palladino ,  Emmanuel Theodorakis

    发明人： Michael Palladino ,  Emmanuel Theodorakis

    IPC分类号： A61K31/20 ,  C07C69/74 ,  C07C61/29

    CPC分类号： C07C33/14 ,  A61K31/12 ,  A61K31/16 ,  A61K31/215 ,  C07B2200/05 ,  C07B2200/07 ,  C07C57/26 ,  C07C61/29 ,  C07C61/35 ,  C07C62/30 ,  C07C62/32 ,  C07C69/753 ,  C07C69/757 ,  C07C233/58 ,  C07C2603/26 ,  C07D295/15 ,  C07D295/185 ,  C07D295/26 ,  Y02A50/463

    摘要： Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-α modulators, and thus are useful in the treatment of various diseases. wherein the R groups are defined as follows: if any R3—R5, R7, R8, R11—R13 is not hydrogen, R2 or R6 or R9 is not methyl, or R10 is not CH2, then R1 is selected from the group consisting of hydrogen, a halogen, COOH, C1-C12 carboxylic acids, C1-C12 acyl halides, C1-C12 acyl residues, C1-C12 esters, C1-C12 secondary amides, (C1-C12)(C1-C12) tertiary amides, (C1-C12)(C1-C12) cyclic amides, (C1-C12) amines, C1-C12 alcohols, (C1-C12)(C1-C12) ethers, C1-C12 alkyls, C1-C12 substituted alkyls, C2-C12 alkenyls, C2-C12 substituted alkenyls, and C5-C12 aryls. If all R3—R5, R7, R8, R11—R13 are hydrogen, R2, R6, and R9 are each methyl, and R10 is CH2, then R1 is selected from hydrogen, a halogen, C1-C12 carboxylic acids, C1-C12 acyl halides, C1-C12 acyl residues, C2-C12 esters, C2-C12 secondary amides, (C1-C12)(C1-C12) tertiary amides, C2-C12 alcohols, (C1-C12)(C1-C12) ethers other than methyl-acetyl ether, C2-C12 alkyls, C1-C12 substituted alkyls, C2-C12 alkenyls, C2-C12 substituted alkenyls, and C2-C12 aryls. R2 and R9 are each separately selected from hydrogen, a halogen, C1-C12 alkyl, C1-C12 substituted alkyls, C2-C12 alkenyl, C2-C12 substituted alkenyl, C2-C12 alkynyl, C1-C12 acyl, C1-C12 alcohol, and C5-C12 aryl. R3—R5, R7, R8, and R11—R13 are each separately selected from hydrogen, a halogen, C1-C12 alkyl, C1-C12 substituted alkyls, C2-C12 alkenyl, C2-C12 substituted alkenyl, C2-C12 alkynyl, and C5-C12 aryl. R6 is selected from hydrogen, a halogen, C1-C12 alkyl, C1-C12 substituted alkyls, C2-C12 alkenyl, C2-C12 substituted alkenyl, and C2-C12 alkynyl. Rio is selected from hydrogen, a halogen, CH2, C1-C6 alkyl, C1-C6 substituted alkyl, C2-C6 alkenyl, C2-C6 substituted alkenyl, C1-C12 alcohol, and C5-C12 aryl. Pharmaceutical compositions comprising, and uses of, therapeutically effective amounts of the aove compounds and their prodrug esters, and a pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds and their analogs, are also disclosed.

    Coating compositions
    26.
    发明授权
    Coating compositions 失效
    涂料组合物

    公开(公告)号：US5277709A

    公开(公告)日：1994-01-11

    申请号：US822446

    申请日：1992-01-16

    申请人： William P. Armstrong ,  Emyr Phillips

    发明人： William P. Armstrong ,  Emyr Phillips

    IPC分类号： C09D5/00 ,  C07C59/185 ,  C07C59/347 ,  C07C59/80 ,  C07C59/84 ,  C07C59/90 ,  C07C61/22 ,  C07C62/30 ,  C07C65/34 ,  C07C69/738 ,  C07F9/38 ,  C09D5/08 ,  C09D5/44 ,  C09D7/12 ,  C04B9/02

    CPC分类号： C09D5/448 ,  C07C59/185 ,  C07C59/347 ,  C07C59/80 ,  C07C59/84 ,  C07C59/90 ,  C07C61/22 ,  C07C62/30 ,  C07C65/34 ,  C07C69/738 ,  C07F9/3808 ,  C07F9/3882 ,  C09D5/086

    摘要： A coating composition comprising a) an organic film-forming binder; and b) a corrosion-inhibiting amount of a substantially water-insoluble mono- or poly-basic salt of:i) a ketoacid having the formula I: ##STR1## in which m and n, independently, are 0 or an integer from 1 to 10 provided that the sum of m and n is at least 1; A is C.sub.1 -C.sub.15 alkyl, C.sub.2 -C.sub.15 alkenyl, optionally substituted C.sub.3 -C.sub.12 cycloalkyl, C.sub.2 -C.sub.15 alkyl interrupted by one or more O-, N- or S-atoms, optionally substituted C.sub.6 -C.sub.10 aryl, optionally substituted C.sub.7 -C.sub.12 aralkyl, optionally substituted C.sub.7 -C.sub.12 aralkenyl, a heterocyclic residue or a ferrocenyl residue; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each is a substituent A, hydrogen, OH, O-C.sub.1 -C.sub.15 alkyl, NH.sub.2, NH(C.sub.1 -C.sub.15 alkyl), N(C.sub.1 -C.sub.15 alkyl).sub.2, CO.sub.2 H, CO.sub.2 (C.sub.1 -C.sub.15 alkyl), SO.sub.3 H, P(O) (OH).sub.2 P(O)(OH)(O-C.sub.1 -C.sub.15 alkyl), P(O) (O-C.sub.1 -C.sub.15 alkyl).sub.2, SH, S(C.sub.1 -C.sub.15 alkyl), nitro, cyano, halogen or two of R.sub.1, R.sub.2 R.sub.3 and R.sub.4, together with the carbon atoms to which they are attached, form a C.sub.3 -C.sub.12 cycloalkyl ring or C.sub.6 - or C.sub.10 aryl ring, or one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 together with the carbon atom to which it is attached, and with the group A--C(.dbd.O)--, forms a ring, or R.sub.1 and R.sub.2, R.sub.3 and R.sub.4 form a carbonyl group or a C.dbd.C double bond, provided that A is not optionally substituted C.sub.6 -C.sub.10 aryl when R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are simultaneously hydrogen and provided that R.sub.1 and R.sub.2, or R.sub.3 and R.sub.4, respectively, are not simultaneously both OH or both NH.sub.2 ; and ii) a base selected from a) a cation of Group Ia, Ib, IIa, IIb, IIIa, IIIb, IVa, IVb, Va, VIa, VIIa or VIIIa of the Periodic Table of Elements;b) an amine of formula II which is specified herein.

    摘要翻译： 一种涂料组合物，其包含a）有机成膜粘合剂; 和b）基本上不溶于水的不溶性单碱金属或多碱性盐的腐蚀抑制量：i）具有式I的酮酸：（*化学结构*）I，其中m和n独立地为0或 1到10的整数，只要m和n之和至少为1; A是C 1 -C 15烷基，C 2 -C 15烯基，任选取代的C 3 -C 12环烷基，被一个或多个O-，N-或S-原子间隔的C 2 -C 15烷基，任选取代的C 6 -C 10芳基，任选取代的C 7 -C 12 芳烷基，任选取代的C 7 -C 12芳烯基，杂环残基或二茂铁基残基; R 1，R 2，R 3和R 4相同或不同，各自为取代基A，氢，OH，O-C 1 -C 15烷基，NH 2，NH（C 1 -C 15烷基），N（C 1 -C 15烷基）2，CO 2 H ，CO（C 1 -C 15烷基），SO 3 H，P（O）（OH）2 P（O）（OH）（O-C 1 -C 15烷基），P（O）（O-C 1 -C 15烷基） ，S（C 1 -C 15烷基），硝基，氰基，卤素或R 2，R 3，R 3和R 4中的两个与它们所连接的碳原子一起形成C 3 -C 12环烷基环或C 6 - 或C 10芳环， 或R 1，R 2，R 3和R 4中的一个与其所连接的碳原子一起，并与基团AC（= O） - 形成环，或者R 1和R 2，R 3和R 4形成羰基或 C = C双键，条件是当R 1，R 2，R 3和R 4同时为氢时，A不是任选取代的C 6 -C 10芳基，条件是R 1和R 2或R 3和R 4分别不同时为OH或NH 2 ; 和ii）选自a）元素周期表的Ia，Ib，IIa，IIb，IIIa，IIIb，IVa，IVb，Va，VIa，VIIa或VIIIa族的阳离子的碱; b）本文所述的式II的胺。

    Carboxylic acid therapeutic agents
    27.
    发明授权
    Carboxylic acid therapeutic agents 失效
    羧酸治疗剂

    公开(公告)号：US4530919A

    公开(公告)日：1985-07-23

    申请号：US574765

    申请日：1984-01-27

    申请人： John L. Belletire

    发明人： John L. Belletire

    IPC分类号： C07C57/30 ,  C07C57/58 ,  C07C59/64 ,  C07C59/66 ,  C07C62/30 ,  C07C62/32 ,  C07C62/34 ,  C07D311/58 ,  C07D335/06 ,  C07F7/18 ,  A61K31/35

    CPC分类号： C07C62/30 ,  C07C57/30 ,  C07C57/58 ,  C07C59/64 ,  C07C59/66 ,  C07C62/32 ,  C07C62/34 ,  C07D311/58 ,  C07D335/06 ,  C07F7/18

    摘要： A series of substituted phenylacetic acid compounds and their derivatives, including the pharmacologically acceptable base salts of said acids, have been found to be active as oral hypoglycemic agents. Preferred member compounds include 6-ethoxy-1,2,3,4-tetrahydronaphthalene-1-carboxylic acid, 6-benzyloxy-1,2,3,4-tetrahydronaphthalene-1-carboxylic acid, chroman-4-carboxylic acid, p-chlorophenylacetic acid, o-methylphenylacetic acid, o-methoxyphenylacetic acid, p-methoxyphenylacetic acid and .alpha., .alpha.-di(4-methoxyphenyl)acetic acid. Synthetic routes leading to those member compounds which are novel per se are described in some detail.

    摘要翻译： 已经发现一系列取代的苯乙酸化合物及其衍生物，包括所述酸的药理学上可接受的碱盐，其作为口服降糖药具有活性。 优选的成员化合物包括6-乙氧基-1,2,3,4-四氢化萘-1-羧酸，6-苄氧基-1,2,3,4-四氢萘-1-羧酸，苯并二氢吡喃-4-羧酸，p 邻苯甲基苯乙酸，邻甲氧基苯基乙酸，对甲氧基苯基乙酸和α，α-二（4-甲氧基苯基）乙酸。 导致本身是新颖的那些成员化合物的合成路线被详细描述。

    SMALL MOLECULE INHIBITORS OF TRPA1
    30.
    发明申请
    SMALL MOLECULE INHIBITORS OF TRPA1 有权
    TRPA1小分子抑制剂

    公开(公告)号：US20160340288A1

    公开(公告)日：2016-11-24

    申请号：US15226829

    申请日：2016-08-02

    申请人： B.R.A.I.N. Biotechnology Research and Information Network AG

    发明人： Michael KROHN ,  Dirk SOMBROEK

    IPC分类号： C07C62/30 ,  A61K31/235 ,  A61Q19/00 ,  A61K8/36

    CPC分类号： C07C62/30 ,  A23L27/86 ,  A23L27/88 ,  A61K8/36 ,  A61K8/37 ,  A61K8/49 ,  A61K8/496 ,  A61K8/69 ,  A61K31/192 ,  A61K31/235 ,  A61K2800/782 ,  A61Q19/00 ,  C07C69/78 ,  C07C255/44 ,  C07D249/08 ,  C07D513/04

    摘要： The present invention relates to the use of compounds which are capable of attenuating skin irritation when they are applied to the skin. Skin irritation can be caused, inter alia, by ingredients of cosmetic or pharmaceutical compositions and/or environmental irritants. In particular, the present invention relates to compounds having the property of antagonizing the activation of the transient receptor potential (TRP) ankyrin 1 (TRPA1) ion channel and the use of said compounds as soothing agents. Such compounds can be used in many fields, particularly in personal-care products, cosmetics, textile and packaging products, pharmaceutical compositions, medical devices, and foodstuffs. The present invention further relates to products and/or pharmaceutical compositions containing said compounds. The present invention also relates to the use of the compounds described herein for the modulation of the taste of a food product.

    摘要翻译： 本发明涉及当它们施用于皮肤时能够减轻皮肤刺激性的化合物的用途。 特别是由化妆品或药物组合物和/或环境刺激物的成分引起皮肤刺激。 特别地，本发明涉及具有拮抗瞬时受体电位（TRP）锚蛋白1（TRPA1）离子通道的活化和使用所述化合物作为舒缓剂的性质的化合物。 这些化合物可用于许多领域，特别是在个人护理产品，化妆品，纺织和包装产品，药物组合物，医疗装置和食品中。 本发明还涉及含有所述化合物的产品和/或药物组合物。 本发明还涉及本文所述的化合物用于调节食品味道的用途。