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21 条记录 (耗时 0.051 秒)

    Liquid phase process for the preparation of GNRH peptides
    13.
    发明授权
    Liquid phase process for the preparation of GNRH peptides 有权
    用于制备GNRH肽的液相方法

    公开(公告)号：US06235876B1

    公开(公告)日：2001-05-22

    申请号：US09350231

    申请日：1999-07-08

    申请人： David C. Palmer ,  Ahmed Abdel-Magid ,  Urs P. Eggmann ,  Bruce Harris ,  Kirk L. Sorgi

    发明人： David C. Palmer ,  Ahmed Abdel-Magid ,  Urs P. Eggmann ,  Bruce Harris ,  Kirk L. Sorgi

    IPC分类号： C07K704

    CPC分类号： C07K5/0815 ,  C07K5/101 ,  C07K5/1013 ,  C07K5/1016 ,  C07K7/23 ,  Y02P20/55

    摘要： A liquid phase process for preparing GnRH peptide analogs of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2-AA5-AA6-AA7-AA8-Pro-AA10-NH2   Formula 1 which comprises: (a) reacting a peptide of the formula: T-(R2)AA5-AA6-X  where T is (P2) AA4 orP2 and X is AA7-OH or is —OH, with a peptide of the formula: X′-AA8-Pro-AA10-NH2  or acid-addition salt form thereof, where X′ is AA7 when X is absent and X′ is absent when X is AA7-OH;  in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula: T-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2 (b) removing the P2 protecting group at the N-terminus, and (c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula: G-AA1-(R1)D-Phe-AA3-T′  or acid-addition salt form thereof, where T′ is AA4-OH when T is absent and is absent when T is P2-AA4, in a liquid reaction medium to obtain a GnRH peptide of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2.

    摘要翻译： 用于制备下式的GnRH肽类似物的液相方法：其包括：（a）使下式的肽与其中T是（P2）AA4或P2，X是AA7-OH或-OH的肽反应， 式：或其酸加成盐形式，其中当X不存在时X'为AA 7，X为AA 7 -OH时X'不存在; 在液体反应介质中，在肽偶联剂和强有机胺碱存在下，得到下式的产物：（b）在N末端除去P2保护基，和（c）使步骤 （b）或其酸加成盐与下式的肽或其酸加成盐形式，当T不存在时T'为AA4-OH，当T为P2-AA4时不存在，在液体反应中 培养基以获得下式的GnRH肽：

    Benzotriazapinone salts and methods for using same
    20.
    发明申请
    Benzotriazapinone salts and methods for using same 有权
    苯并三氮杂酮盐及其使用方法

    公开(公告)号：US20050026911A1

    公开(公告)日：2005-02-03

    申请号：US10833232

    申请日：2004-04-27

    申请人： Ahmed Abdel-Magid ,  Judith Cohen

    发明人： Ahmed Abdel-Magid ,  Judith Cohen

    IPC分类号： C07D255/04 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  A61K31/5513 ,  C07D257/10

    CPC分类号： C07D401/04 ,  C07D255/04 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12

    摘要： This invention relates to pharmaceutically acceptable salts of compounds of formula (I) wherein: W is N or N+—O−; R1 and R5 are independently H, C1 to C6 alkyl, (C1 to C6 alkyl)oxy, thio, (C1 to C6 alkyl)thio, carboxy, carboxy(C1 to C6 alkyl), formyl, (C1 to C6 alkyl)carbonyl, (C1 to C6 alkyl)oxycarbonyl, (C1 to C6 alkyl)carbonyloxy, nitro, trihalomethyl, hydroxy, hydroxy(C1 to C6 alkyl), amino, (C1 to C6 alkyl)amino, di(C1 to C6 alkyl)amino, aminocarbonyl, halo, halo(C1 to C6 alkyl), aminosulfonyl, (C1 to C6 alkyl)sulfonylamino, (C1 to C6 alkyl)aminocarbonyl, di(C1 to C6 alkyl)aminocarbonyl, [N-Z](C1 to C6 alkyl)carbonylamino, formyloxy, formamido, (C1 to C6 alkyl)aminosulfonyl, di(C1 to C6 alkyl)aminosulfonyl, [N-Z](C1 to C6 alkyl)sulfonylamino or cyano; or R1 and R5 together form a methylenedioxy group; R2 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms. R3 is —(CR11R12)n—X_(CR13R14)—R9; m is 0, 1, 2, 3 or 4; p is 0, 1 or 2; X is a bond, —CR15═CR16—, —C≡C—, C(O)NH, NHC(O), C(O)NMe, NMeC(O), C(O)O, NHC(O)NH, NHC(O)O, OC(O)NH, NH, O, CO, SO2, SO2NH, C(O)NHNH, R9 is H; C1 to C6 alkyl; or phenyl, naphthyl, pyridyl, benzimidazolyl, indazolyl, quinolinyl, isoquinolinyl, indolinyl, isoindolinyl, indolyl or isoindolyl all optionally substituted with 1, 2 or 3 groups independently selected from -L-Q wherein: L is a bond, or a group of the formula —(CR17R18)v—Y—(CR17R18)w, wherein v and w are independently 0, 1, 2 or 3, and Y is a bond, —CR15═CR16—, phenyl, furanyl, thiophenyl, pyrrolyl, thiazolyl, imidazolyl, oxazolyl, isoxazolyl, pyrazolyl, isoxazolonyl, piperazinyl, piperidinyl, morpholinyl, pyrrolidinyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyridyl or pyridazyl; and Q is H, (C1 to C6 alkyl)oxy, [N-Z](C1 to C6 alkyl)oxy(C1 to C6 alkyl)amino, thio, (C1 to C6 alkyl)thio, carboxy(C1 to C6 alkyl)thio, carboxy, carboxy(C1 to C6 alkyl), carboxy(C1 to C6 alkenyl), [N-Z]carboxy(C1 to C6 alkyl)amino, carboxy(C1 to C6 alkyl)oxy, formyl, (C1 to C6 alkyl)carbonyl, (C1 to C6 alkyl)oxycarbonyl, (C1 to C6 alkyl)carbonyloxy, nitro, trihalomethyl, hydroxy, amino, [N-Z](C1 to C6 alkyl)amino, aminocarbonyl, (C1 to C6 alkyl)aminocarbonyl, di(C1 to C6 alkyl)aminocarbonyl, [N-Z] (C1 to C6 alkyl)carbonylamino, C5 to C8 cycloalkyl, [N-Z](C1 to C6 alkyl)carbonyl(C1 to C6 alkyl)amino, halo, halo(C1 to C6 alkyl), sulfamoyl, [N-Z](C1 to C6 alkyl)sulfonylamino, (C1 to C6 alkyl)sulfonylaminocarbonyl, carboxy(C1 to C6 alkyl)sulfonyl, carboxy(C1 to C6 alkyl)sulfinyl, tetrazolyl, [N-Z]tetrazolylamino, cyano, amidino, amidinothio, SO3H, formyloxy, formamido, C3 to C8 cycloalkyl, (C1 to C6 alkyl)sulphamoyl, di(C1 to C6 alkyl)sulphamoyl, (C1 to C6 alkyl)carbonylaminosulfonyl, 5-oxo-2,5-dihydro[1,2,4]oxadiazolyl, carboxy(C1 to C6 alkyl)carbonylamino, tetrazolyl(C1 to C6 alkyl)thio, [N-Z]tetrazolyl(C1 to C6 alkyl)amino, 5-oxo-2,5-dihydro[1,2,4]thiadiazolyl, 5-oxo-1,2-dihydro[1,2,4]triazolyl, [N-Z](C1 to C6 alkyl)amino(C1 to C6 alkyl)amino, or a group of the formula  wherein P is O, S or NR19; Z is H, C1 to C6 alkyl, t-butoxycarbonyl, acetyl, benzoyl or benzyl; R4 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may nally be replaced by N, O and/or S atoms; and R11, R12, R13, R14, R15, R16, R17, R18 and R19 are independently H or C1 to C3alkyl. Such salts are useful, for example, for the treatment of gastrin related disorders.

    摘要翻译： 本发明涉及式（I）化合物的药学上可接受的盐，其中：W是N或N + O - ; R 1和R 5独立地是H，C 1 -C 6烷基，（C 1 -C 6烷基）氧基，硫代，（C 1 -C 6烷基）硫代，羧基，羧基（C 1 -C 6烷基），甲酰基，（C 1 C 1 -C 6烷基）羰基，（C 1 -C 6烷基）氧羰基，（C 1 -C 6烷基）羰基氧基，硝基，三卤代甲基，羟基，羟基（C 1 -C 6烷基），氨基，（C 1 -C 6烷基）氨基， C 1 -C 6烷基）氨基羰基，卤素（C 1 -C 6烷基），氨基磺酰基，（C 1 -C 6烷基）磺酰基氨基，（C 1 -C 6烷基）氨基羰基，二（C 1至C 6烷基）氨基羰基，[NZ] C 1 -C 6烷基）羰基氨基，甲酰氧基，甲酰氨基，（C 1至C 6烷基）氨基磺酰基，二（C 1至C 6烷基）氨基磺酰基，[NZ]（C 1至C 6烷基）磺酰基氨基或氰基; 或R 1和R 5一起形成亚甲二氧基; R 2是任选取代的C 1 -C 18烃基，其中最多三个C原子可以任选地被N，O和/或S原子替代。 R 3是 - （CR 11 R 12）n -X（CR 13 R 14）-R 9; m为0,1,2,3或4; p为0,1或2; X是一个键，-CR 15 = CR 16 - ，-C = C - ，C（O）NH，NHC（O），C（O）NMe，NMeC（O），C（O）O ，NHC（O）NH，NHC（O）O，OC（O）NH，NH，O，CO，SO 2，SO 2 NH，C（O）NHNH，R 9是H; C1至C6烷基; 或苯基，萘甲酸