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    Novel nitrogenous polymers
    4.
    发明授权
    Novel nitrogenous polymers 失效

    公开(公告)号：US3342786A

    公开(公告)日：1967-09-19

    申请号：US57041766

    申请日：1966-08-05

    Applicant: ROHM & HAAS

    Inventor： EMMONS WILLIAM D

    IPC: C07D265/32 ,  C07D267/08 ,  C08F20/34 ,  C08F20/36 ,  C10L1/14 ,  C10L1/22 ,  C10L1/24 ,  C10M149/10 ,  D04H1/64 ,  D06M15/267 ,  H01B3/44

    CPC classification number: H01B3/44 ,  C07D265/32 ,  C07D267/08 ,  C08F20/34 ,  C08F20/36 ,  C10L1/146 ,  C10L1/2368 ,  C10L1/2468 ,  C10M149/10 ,  C10M2205/026 ,  C10M2207/023 ,  C10M2207/026 ,  C10M2207/123 ,  C10M2207/125 ,  C10M2207/129 ,  C10M2207/144 ,  C10M2207/146 ,  C10M2207/22 ,  C10M2207/282 ,  C10M2207/34 ,  C10M2209/00 ,  C10M2209/02 ,  C10M2209/084 ,  C10M2209/10 ,  C10M2209/101 ,  C10M2209/108 ,  C10M2209/109 ,  C10M2215/04 ,  C10M2215/06 ,  C10M2215/066 ,  C10M2215/224 ,  C10M2215/26 ,  C10M2217/028 ,  C10M2217/06 ,  C10M2219/022 ,  C10M2219/024 ,  C10M2219/044 ,  C10M2219/087 ,  C10M2219/088 ,  C10M2219/089 ,  C10M2219/108 ,  C10M2223/041 ,  C10M2223/045 ,  C10M2227/061 ,  C10M2229/02 ,  C10M2229/05 ,  C10M2290/02 ,  C10N2210/02 ,  C10N2210/08 ,  C10N2240/02 ,  C10N2240/08 ,  C10N2250/10 ,  D04H1/587 ,  D04H1/64 ,  D06M15/267 ,  Y10S424/02

    Abstract: Polymers or copolymers of the unsaturated carboxylic esters of formula in which R is a hydrogen atom or methyl group, m is 1, 2 or 3, p is 1, 2, 3 or 4, x is 1, 2, 3 or 4, A is an alkylene group (2-4C) and Z is a substituted morpholinone group or a substituted glycine group in which Y is an alkylene group (2 or 3C); either R1 is a hydrogen atom, an alkyl group (1-8C), or a phenyl group and R2 is hydrogen, an alkyl group (1-8C) or R1 and R2 are joined in a ring of 5 to 7 C atoms with the proviso that when p is greater than 1 then m is 1, and when m is greater than 1 then R is hydrogen (see Division C2) are prepared by vinyl addition processes. Hydrolysis of the cyclic radical to form the glycine radical during the polymerization in aqueous media varies with the temperature and acidity or alkalinity of the medium, or the hydrolysis may be brought about after polymerization by heating in aqueous medium. Conventional free-radical catalysts may be used and copolymers with H2C=C in which R is a hydrogen atom or a methyl group, m is 1,2, or 3; p is 1,2,3 or 4; #c is 1,2,3 or 4; A is an alkylene group (2-4 C); and Z is a substituted morpholinone group or a substituted glycine group in which Y is an alkylene group (2-3 C); R1 is hydrogen, alkyl (1-8 C), or phenyl group; R2 is hydrogen, alkyl (1-8 C) or R1 and R2 may be joined to form a 5-7 C ring; providing that when p is greater than 1 then m is 1, and when m is greater than 1 R is hydrogen, specifically N - (b - methacryloxyethyl) - 2 - morpholinone, N - (b - acyloxyethyl) - 2 - morpholinone, N - [b - (4 - pentenoyloxy)ethyl] - 2 - morpholinone or mixtures thereof. The esters are prepared by reacting in which R0 is an alkyl group with an N-substituted morpholinone-2 under transesterifying conditions e.g. in presence of tetra alkyl titanate or an alkali metal (C1-C4)-alkoxide. Alternatively, an acyl halide may be reacted with the N-substituted morpholinone-2, e.g. in the presence of a hydrogen halide acceptor. The ester may be hydrolysed to form a compound with Z a substituted glycine group. The N-substituted-morpholinone-2 may be prepared by reacting an alkylene oxide (2-4 C) with a compound where M is an alkali metal and acidifying and dehydrating the intermediate formed, or by reacting the alkylene oxide with a hydroxy-(poly)-alkoxyamine H(OA)#c-NH2 (#c=2-4), followed by reaction with an alkali metal a -chloro-acetate. The ester products are normally stable, colourless liquids which may form addition linear polymers, or copolymers with vinyl monomers. Examples describe the preparation of the compounds specified above and N - [b - (3 - pentenoyloxy)propyl] - 3,3 - dimethyl - 2 - morpholinone, N - [3 - (crotonoxypropyl] - 5 - methyl - 2 morpholinone, N - (acyloxyethoxyethyl) - 2 - morpholinone, N - (methacryloxypropoxypropyl) - 3 - phenyl - 2 - morpholinone, and N-(5-hexenoyloxyethoxyethoxyethoxyethyl) -2-morpholinone and their hydrolysis to the corresponding glycines.ALSO:Polymers or copolymers of the unsaturated carboxylic esters of formula in which R is a hydrogen atom or a methyl group; m is 1, 2 or 3; p is 1, 2, 3 or 4; x is 1, 2, 3 or 4; A is an alkylene group (2-4C) and Z is a substituted morpholinone group or a substituted glycine group which Y is an alkylene group (2 or 3C); either R1 is a hydrogen atom, an alkyl group (1-8c) or a phenyl group and R2 is hydrogen-an alkyl group (1-8C) or R1 and R2 are joined in a ring of 5 to 7C atoms with the proviso that when p is greater than 1 then m is 1, and when m is greater than 1 then R is a hydrogen atom (see Divns C2 and C3) may be used to coat substrates much as wood or metal, e.g. steel plate, a copper wire or glass. Conventional comonomers are specified together with usual additives and the coatings which may be on either bare or primed surfaces (with alkyd, epoxy or aminoplast primers) may be cured by heating with or without a catalyst. Examples describe the coating of steel with a copolymer of methyl methacrylate, ethyl acrylate and N-(B-methacryloxyethyl)-2-morpholinone; methyl methacrylate, butyl methacrylate, N-[B-(4-pentenoyl-oxy) ethyl]-2-morpholinone; methyl methacrylate, vinyl toluene, 2-ethylhexyl methacrylate and N-[3-(crolonoxy) propyl]-5-methyl-2-morpholinone; and vinyl acetate, vinyl chloride, styrene, butyl acrylate and N-[B-(3-pentenoyloxy)propyl]-3, 3-di-methyl-2-morpholinone; aluminium or wood with a copolymer of methyl and butyl methacrylate and N-(B-methacryloxyethyl)-2-morpholinone; and the enamelling of copper wire by passing through a latex prepared by polymerising a solution of the hydrolysis product of N-(diglycol)-2-morpholinone with N-methoxymethyl-methacrylamide, acrylonitrile and butyl acrylate, to which is added dimethyl formamide.ALSO:Polymers or copolymers of the unsaturated carboxylic esters of formula: in which R is a hydrogen atom or a methyl group; m is 1, 2 or 3; p is 1, 2, 3 or 4; x is 1, 2, 3 or 4; A is an alkylene group (2-4C) and Z is a substituted morpholine group: or a substituted glycine group: in which Y is an alkylene group (2 or 3C); either R1 is a hydrogen atom, an alkyl group (1-8c) or a phenyl group and R2 is hydrogen, an alkyl group (1-8c) or R1 and R2 are joined in a ring of 5 to 7C atoms with the proviso that when p is greater than 1 then m is 1, and when m is greater than 1 then R is a hydrogen atom (see Divisions C2 and C3) may be used to treat textiles, (e.g. bonding non-woven fabrics, shrink proofing wool and crease-proofing cotton and rayon), paper (e.g. p to increase wet strength or as a binder in mineral coating. Conventional comonomers are specified together with usual additives and the compositions may be cured in situ with heat and with or without a catalyst. Examples describe the bonding of non-woven fabric of carded viscose fibres with an aqueous dispersion of a copolymer from N-(5-hexenoyloxyethoxy ethoxyethoxyethyl) - 2 - morpholinone, ethyl acrylate, acrylamide and N-methylolacrylamide which is cured thereon; the sizing of yarns of cotton, rayon, wool, nylon and cellulose acetate with aqueous solutions of hydrolysis products of N-(B-methacryloxyethyl)2-morpholinone, N-(B-acryloxyethyl)-2-morpholinone, N-[B-(3-pentenoyloxy) propyl]-3, 3-di-methyl-2-morpholinone, N-[3-(crotonxy) propyl]-5-methyl-2-morpholinone, N-(acyloxyethoxyethyl)-2-morpholinone, N-(methacryloxypro poxypropyl))-3-phenyl-2-morpholinone, and N-(5-hexenoyloxyethoxyethoxyethoxyethyl) - 2 - morpholinone which are directly polymerised without isolation of the hydrolysed monomer. The size is water-soluble, and may be removed by normal scouring.

    BENZOXAZEPIN OXAZOLIDINONE COMPOUNDS AND METHODS OF USE
    6.
    发明申请
    BENZOXAZEPIN OXAZOLIDINONE COMPOUNDS AND METHODS OF USE 审中-公开
    苯并噻唑氧杂环丁酮化合物及其使用方法

    公开(公告)号：US20170015678A1

    公开(公告)日：2017-01-19

    申请号：US15200301

    申请日：2016-07-01

    Applicant: Genentech, Inc.

    Inventor： Marie-Gabrielle Braun ,  Emily Hanan ,  Steven T. Staben ,  Robert Andrew Heald ,  Calum MacLeod ,  Richard Elliott

    IPC: C07D498/04 ,  A61K31/553

    CPC classification number: C07D413/14 ,  A61K31/553 ,  C07D267/08 ,  C07D498/04

    Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

    Abstract translation: 本文描述了具有式（I）结构的磷酸肌醇-3激酶（PI3K）调节活性或功能的苯并氧氮杂恶唑烷酮化合物：或其立体异构体，互变异构体或其药学上可接受的盐，以及本文所述的取代基和结构特征。 还描述了包括式I化合物的药物组合物和药物，以及将PI3K调节剂单独使用并与其它治疗剂联合用于治疗介导或依赖于PI3K调节异常的疾病或病症的方法。

    RECEPTOR ANTAGONIST
    9.
    发明申请
    RECEPTOR ANTAGONIST 审中-公开
    受体拮抗剂

    公开(公告)号：US20090239839A1

    公开(公告)日：2009-09-24

    申请号：US12391520

    申请日：2009-02-24

    Applicant: Fumio ITOH ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Hiroshi Mabuchi ,  Hiromi Yoshida ,  Hirokazu Matsumoto ,  Takeshi Wakabayashi

    Inventor： Fumio ITOH ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Hiroshi Mabuchi ,  Hiromi Yoshida ,  Hirokazu Matsumoto ,  Takeshi Wakabayashi

    IPC: A61K31/553 ,  A61P25/04

    CPC classification number: C07D267/08

    Abstract: An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I) [wherein ring A represents an optionally substituted aromatic ring; ring B represents an optionally substituted benzene ring; X represents oxygen, S(O)n (n is an integer of 0 to 2), or NR3 (R3 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group); and R1 and R2 each represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group] or a salt of the compound.

    Abstract translation: 用于调节RFRP受体功能的试剂，其特征在于含有由式（I）表示的化合物[其中环A表示任选取代的芳环; 环B表示任选取代的苯环; X表示氧，S（O）n（n为0〜2的整数）或NR 3（R 3表示氢，任选取代的烃基或任意取代的杂环基）。 并且R 1和R 2各自表示氢，任选取代的烃基或任选取代的杂环基]或该化合物的盐。

    Receptor antagonist
    10.
    发明申请
    Receptor antagonist 审中-公开
    受体拮抗剂

    公开(公告)号：US20070129348A1

    公开(公告)日：2007-06-07

    申请号：US10553273

    申请日：2004-04-15

    Applicant: Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Hiroshi Mabuchi ,  Hiromi Yoshida ,  Hirokazu Matsumoto ,  Takeshi Wakabayashi

    Inventor： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Hiroshi Mabuchi ,  Hiromi Yoshida ,  Hirokazu Matsumoto ,  Takeshi Wakabayashi

    IPC: A61K31/554 ,  A61K31/553 ,  A61K31/5513

    CPC classification number: C07D267/08

    Abstract: An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I) [wherein ring A represents an optionally substituted aromatic ring; ring B represents an optionally substituted benzene ring; X represents oxygen, S(O)n (n is an integer of 0 to 2), or NR3 (R3 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group); and R1 and R2 each represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group] or a salt of the compound.

    Abstract translation: 用于调节RFRP受体功能的试剂，其特征在于含有由式（I）表示的化合物[其中环A表示任选取代的芳环; 环B表示任选取代的苯环; X表示氧，S（O）n N（n为0〜2的整数）或NR 3（R 3）表示氢， 任选取代的烃基或任选取代的杂环基）; 和R 1和R 2各自表示氢，任选取代的烃基或任选取代的杂环基]或该化合物的盐。

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