公开(公告)号：US4916126A

公开(公告)日：1990-04-10

申请号：US270701

申请日：1988-11-14

申请人： Peter Traxler ,  Klaus Muller ,  Wilhelm Kump

发明人： Peter Traxler ,  Klaus Muller ,  Wilhelm Kump

IPC分类号： A61K31/495 ,  A61P3/06 ,  C07D498/08

CPC分类号： C07D498/08

摘要： Compounds of the formula ##STR1## in which R represents lower alkyl, R.sub.1 represents tri-lower alkylmethylcarbonyl, and one of the radicals R.sub.2 and R.sub.3 represents tri-lower alkylmethylcarbonyl and the other represents hydrogen, and salts thereof, exhibit hypo-lipidaemic properties.

摘要翻译： PCT No.PCT / CH87 / 00123 Sec。 371日期：1988年11月14日 102（e）日期1988年11月14日PCT提交1987年9月25日PCT公布。 公开号WO89 / 02894 日期：1989年4月6日。其中R表示低级烷基，R 1表示三低级烷基甲基羰基，式中R 1和R 3之一表示三低级烷基甲基羰基，另一方式 代表氢，及其盐表现出低脂血症特性。

公开(公告)号：US20090247548A1

公开(公告)日：2009-10-01

申请号：US10597298

申请日：2005-01-28

申请人： Giorgio Caravatti ,  Peter Traxler ,  Thomas Esser ,  Handan He

发明人： Giorgio Caravatti ,  Peter Traxler ,  Thomas Esser ,  Handan He

IPC分类号： A61K31/496 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to a compound of formula I wherein R1 is a heterocyclic radical or an unsubstituted or substituted aromatic radical; G is C1-C7-alkylene, —C(═O)—, or C1-C6-alkylene-C(═O)— wherein the carbonyl group is attached to the piperazine moiety; Q is —NH— or —O—, with the proviso that Q is —O— if G is —C(═O)— or C1-C6-alkylene-C(═O)—; and X is either not present or C1-C7-alkylene, with the proviso that a heterocyclic radical R1 is bonded via a ring carbon atom if X is not present; or a salt thereof, which is useful for treating anti-proliferative diseases.

摘要翻译： 本发明涉及式Ⅰ化合物，其中R 1是杂环基或未取代或取代的芳族基; G是C 1 -C 7 - 亚烷基，-C（-O） - 或C 1 -C 6亚烷基-C（-O） - ，其中羰基连接到哌嗪部分; Q是-NH-或-O-，条件是如果G是-C（-O） - 或C 1 -C 6 - 亚烷基-C（-O） - ，则Q是-O-。 并且X不存在或者C 1 -C 7 - 亚烷基，条件是如果X不存在，则杂环基R1经由环碳原子键合; 或其盐，其可用于治疗抗增殖性疾病。

公开(公告)号：US06180636B2

公开(公告)日：2001-01-30

申请号：US09242592

申请日：1999-02-19

申请人： Peter Traxler ,  Guido Bold ,  Marc Lang ,  Jörg Frei

发明人： Peter Traxler ,  Guido Bold ,  Marc Lang ,  Jörg Frei

IPC分类号： A61K31519

CPC分类号： C07D487/04

摘要： There are described 7H-pyrrolo[2,3-d]pyrimidine derivatives of the formula I in which the substituents are as defined in claim 1. These compounds inhibit the tyrosine kinase activity of the receptor for the epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumor agents.

摘要翻译： 描述了式Iin的7H-吡咯并[2,3-d]嘧啶衍生物，其取代基如权利要求1中所定义。这些化合物抑制表皮生长因子（EGF）受体的酪氨酸激酶活性和c- erbB2激酶，可用作抗肿瘤剂。

公开(公告)号：US4876258A

公开(公告)日：1989-10-24

申请号：US226487

申请日：1988-08-01

申请人： Wilhelm Kump ,  Peter Traxler

发明人： Wilhelm Kump ,  Peter Traxler

IPC分类号： A61K31/395 ,  A61P31/04 ,  A61P31/06 ,  C07D498/08

CPC分类号： C07D498/08

摘要： Rifamycin derivatives of formula ##STR1## wherein R is a radical of the formula ##STR2## in which R.sub.1 is an unsubstituted or substituted biphenylyl radical, and wherein X--X, Y--Y and Z--Z are each vinylene of the formula CH.dbd.CH, or wherein X--X and Y--Y are each ethylene of the formula CH.sub.2 --CH.sub.2 and Z--Z is ethylene or vinylene, and processes for the preparation thereof are described. These compounds can be used as antibacterial and antiviral medicaments.

摘要翻译： 其中R是下式的基团，其中R 1是未取代或取代的联苯基，其中XX，YY和ZZ各自是式 CH = CH，或其中XX和YY各自是式CH 2 -CH 2的乙烯，ZZ是乙烯或亚乙烯基，并且其制备方法进行了描述。 这些化合物可以用作抗菌和抗病毒药物。

公开(公告)号：US4551450A

公开(公告)日：1985-11-05

申请号：US644886

申请日：1984-08-27

申请人： Peter Traxler

发明人： Peter Traxler

IPC分类号： C07D498/08 ,  C07D519/00 ,  A61K31/395

CPC分类号： C07D498/08 ,  C07D519/00

摘要： Novel hydrazones derived from 3-formylrifamycin S or SV as the aldehydo component and a bi- or tri-cyclic N-aminopiperazine as the hydrazino component and having the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6, independently of one another, each represents a hydrogen atom or C.sub.1-4 -alkyl,m and n, independently of one another, each represents an integer from 0 to 5,X represents C.sub.1-5 -alkylidene, benzylidene or C.sub.1-4 -alkoxymethylene,Y represents C.sub.1-5 -alkylidene, C.sub.1-4 -alkoxymethylene, oxy, thio or optionally substituted imino of the formula --N(R)-- wherein R represents hydrogen, C.sub.1-4 -alkyl, C.sub.3-5 -alkenyl, C.sub.3-12 -cycloalkyl or phenyl, orX and Y together represent 1,2-cycloalkylene or o-phenylene each of which can be substituted by from one to three C.sub.1-4 -alkyl radicals, andRif represents a radical of rifamycin S or SV that is bonded in the 3-position by the free valency,are distinguished by a high and long-lasting antituberculotic activity. They are manufactured in conventional manner, for example by condensation of their components.

摘要翻译： 衍生自作为醛组分的3-甲酰基叶绿素S或SV的新型腙和作为肼基组分的双环或三环N-氨基哌嗪，并具有式（Ⅰ）的R1，R2，R3，R4，R5 和R 6彼此独立地表示氢原子或C 1-4 - 烷基，m和n彼此独立地表示0-5的整数，X表示C1-5亚烷基，亚苄基或C1- 4-烷氧基亚甲基，Y代表C1-5亚烷基，C1-4烷氧基亚甲基，氧基，硫代或式-N（R） - 的任选取代的亚氨基，其中R表示氢，C 1-4 - 烷基，C 3-5 - 烯基 ，C 3-8 - 环烷基或苯基，或X和Y一起代表1,2-亚环烷基或邻亚苯基，其各自可被一至三个C 1-4 - 烷基取代，Rif代表利福霉素S 或通过自由价键合在3位上的SV被高度和持久的抗结核活性区分。 它们以常规方式制造，例如通过其组分的冷凝。

公开(公告)号：US4411896A

公开(公告)日：1983-10-25

申请号：US397379

申请日：1982-07-12

申请人： Thomas Schupp ,  Peter Traxler ,  Jakob Nuesch

发明人： Thomas Schupp ,  Peter Traxler ,  Jakob Nuesch

IPC分类号： C07D498/08 ,  C07D498/18 ,  C12P17/18 ,  A61K31/395 ,  C07D491/08

CPC分类号： C07D498/08 ,  C07D498/18 ,  C12P17/189 ,  C12R1/365 ,  Y10S435/872 ,  Y10S435/886

摘要： New antibiotically active compounds having the basic structure of rifamycin S, namely 3-hydroxyrifamycin S (formula A: X=>C.dbd.O; R.sup.1 =OH; R.sup.2 =H), 3,31-dihydroxy-rifamycin S (formula A: X=>C.dbd.O; R.sup.1 =R.sup.2 =OH) and 1-desoxy-1-oxarifamycin S (formula A: X=--O--; R.sup.1 =R.sup.2 =H) ##STR1## are formed by cultivating, under aerobic conditions, a strain of Nocardia mediterranei which is derived from Streptomyces mediterranei ATCC 13 685 as the parent strain and is characterized by the ability to produce at least one of the mentioned compounds. The recombinant strain Nocardia mediterranei DSM 1415 has proved suitable. The mentioned rifamycin S analogues have analogous antibiotic properties to this but have a wider range of action, especially against gram-negative bacteria.

摘要翻译： 具有利福霉素S的基本结构的新的抗生素活性化合物即3-羟基喜树碱S（式A：X => C = O; R1 = OH; R2 = H），3,31-二羟基利福霉素S（式A：X （A = X = -O-; R 1 = R 2 = H）通过在有氧下培养形成（A），（C = O; R1 = R2 = OH）和1-脱氧-1-氧硫霉素S 条件，来自地衣链霉菌（Streptomyces mediterranei）ATCC13685作为亲本菌株的诺卡氏菌（Nocardia mediterranei）菌株，其特征在于产生至少一种所述化合物的能力。 重组菌诺卡氏菌DSM 1415已证明是合适的。 所提到的利福霉素S类似物具有类似的抗生素特性，但具有更广泛的作用范围，特别是针对革兰氏阴性细菌。

公开(公告)号：US4374129A

公开(公告)日：1983-02-15

申请号：US330409

申请日：1981-12-14

申请人： Peter Traxler

发明人： Peter Traxler

IPC分类号： C07H15/18 ,  A61K31/70 ,  A61K31/7028 ,  A61P31/04 ,  A61P31/10 ,  C07H19/01 ,  A61K31/71 ,  C07H13/04

CPC分类号： C07H19/01

摘要： N-acylated 11-amino derivatives of papulacandin A or B of the formula I ##STR1## in which Pap is the remainder of papulacandin A or B, R represents methyl or hydrogen and Ac represents the acyl radical of an organic acid, including salts of compounds with salt-forming properties, are distinguished by their antibiotic, especially antimycotic, action and can be used for combating infections of that type, especially those caused by Candida albicans. The compounds are produced according to conventional processes from corresponding 11-unsubstituted papulacandin derivatives.

摘要翻译： 其中Pap是其余的papulacandin A或B，R表示甲基或氢，Ac表示有机酸的酰基，其中式（I）的帕拉可质素A或B的N-酰化的11-氨基衍生物， 包括具有成盐性质的化合物的盐通过其抗生素特别是抗真菌作用来区分，并且可用于对抗那种类型的感染，特别是由白色念珠菌引起的感染。 根据常规方法从相应的11-未取代的帕拉可坎因衍生物制备化合物。

公开(公告)号：US06710047B2

公开(公告)日：2004-03-23

申请号：US10338062

申请日：2003-01-07

申请人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

发明人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

IPC分类号： A61K31495

CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etheritied or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are as defined, then G is selected from the group comprising lower alkylene, —CH2—O—, —CH2—S—, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.

摘要翻译： 本发明涉及式I化合物，其中r为0至2，n为0至2; m为0〜4; R1和R2（i）在每种情况下都是低级烷基，或（ii）一起在子式I *中形成桥，或（iii）一起形成子式I **中的桥，其中一个或两个环成员T1，T2 ，T3和T4是氮，余数分别为CH; A，B，D和E是N或CH，其中不多于2个这些基团是N; G是低级亚烷基，酰氧基或羟基 - 低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂，硫杂或亚氨基; Q是甲基; R是H或低级烷基; X是亚氨基，氧杂或硫杂; Y是芳基，吡啶基或（未）取代的环烷基; 羟基，醚基或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二取代的氨基甲酰基，脒基， 胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基。 并且其中以波浪线表征的键是单键或双键; 或所述化合物的N-氧化物，其规定如果Y是吡啶基或未取代的环烷基，则X是亚氨基，剩余的基团如所定义，则G选自低级亚烷基，-CH 2 -O-， -CH 2 -S-，氧杂和硫杂; 或其盐。 该化合物抑制血管发生。

公开(公告)号：US06258812B1

公开(公告)日：2001-07-10

申请号：US09367273

申请日：1999-10-20

申请人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

发明人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

IPC分类号： A61K31498

CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* (I*) or (iii) together form a bridge in subformula I** (I**), wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; c is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are a s defined, then G is selected from the group comprising lower alkylene, —CH2—O—, CH2—S—, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.

摘要翻译： 本发明涉及式I化合物，其中r为0至2，n为0至2; m为0〜4; R1和R2（i）在每种情况下都是低级烷基，或（ii）一起在子式I *（I *）中形成桥，或（iii）一起形成子式I **（I **）中的桥，其中 环成员T1，T2，T3和T4中的一个或两个是氮，余下的都是CH; A，B，D和E是N或CH，其中不多于2个这些基团是N; G是低级亚烷基，酰氧基或羟基 - 低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂，硫杂或亚氨基; Q是甲基; c是H或低级烷基; X是亚氨基，氧杂或硫杂; Y是芳基，吡啶基或（未）取代的环烷基; 羟基，醚化或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二取代的氨基甲酰基，脒基， 胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基。 并且其中以波浪线表征的键是单键或双键; 或所述化合物的N-氧化物，其规定如果Y是吡啶基或未取代的环烷基，则X是亚氨基，剩余的基团如所定义，则G选自低级亚烷基，-CH 2 -O-， CH2-S-，氧杂和硫杂; 或其盐。 该化合物抑制血管发生。

公开(公告)号：US6096749A

公开(公告)日：2000-08-01

申请号：US53266

申请日：1998-04-01

申请人： Peter Traxler ,  Pascal Furet ,  Wolfgang K.-D. Brill

发明人： Peter Traxler ,  Pascal Furet ,  Wolfgang K.-D. Brill

IPC分类号： C07D498/02 ,  A61K31/495 ,  A61K31/505 ,  A61K31/519 ,  A61P17/06 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D20060101 ,  C07D207/18 ,  C07D239/42 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumor diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0,R is one or more substituents selected from halogen, alkyl, trifluoromethyl and alkoxy; andR.sub.1 and R.sub.2 are each independently of the other alkyl, or phenyl that is unsubstituted or substituted by halogen, trifluoromethyl, alkyl or by alkoxy, it also being possible for one of the two radicals R.sub.1 and R.sub.2 to be hydrogen, or R.sub.1 and R.sub.2 together form an alkylene chain having from 2 to 5 carbon atoms that is unsubstituted or substituted by alkyl;or salts thereof. Compounds of formula I inhibit protein kinases, for example the tyrosine protein kinase of the receptor for the epidermal growth factor, EGF.

摘要翻译： 本发明涉及下述化合物在肿瘤疾病和其它增殖性疾病如牛皮癣的治疗性治疗中的用途，以及该类型的新型化合物。 化合物是其中n为0至5的式I化合物，当n不为0时，R为一个或多个选自卤素，烷基，三氟甲基和烷氧基的取代基; 并且R 1和R 2各自独立地为未被取代或被卤素，三氟甲基，烷基或烷氧基取代的苯基，也可以是两个基团R 1和R 2中的一个为氢，或者R 1和R 2 一起形成未被取代或被烷基取代的具有2至5个碳原子的亚烷基链; 或其盐。 式I的化合物抑制蛋白激酶，例如表皮生长因子受体的酪氨酸蛋白激酶EGF。