公开(公告)号：US20130281463A1

公开(公告)日：2013-10-24

申请号：US13880994

申请日：2011-10-25

Applicant: Sangamesh Badiger ,  Dirk Behnke ,  Claudia Betschart ,  Simona Cotesta ,  Samuel Hintermann ,  Silvio Ofner ,  Chetan Pandit ,  Bernard Lucien Roy

Inventor： Sangamesh Badiger ,  Dirk Behnke ,  Claudia Betschart ,  Simona Cotesta ,  Samuel Hintermann ,  Silvio Ofner ,  Chetan Pandit ,  Bernard Lucien Roy

IPC: C07D471/10 ,  A61K45/06 ,  A61K31/444 ,  A61K31/506

CPC classification number: C07D471/10 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06 ,  C07D519/00

Abstract: The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract translation: 本发明涉及式（I）化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

公开(公告)号：US20120165331A1

公开(公告)日：2012-06-28

申请号：US13329868

申请日：2011-12-19

Applicant: Sangamesh BADIGER ,  Dirk BEHNKE ,  Claudia BETSCHART ,  Vinod CHAUDHARI ,  Simona COTESTA ,  Samuel HINTERMANN ,  Andreas LERCHNER ,  Fatma LIMAM ,  Silvio OFNER ,  Chetan PANDIT ,  Jürgen WAGNER

Inventor： Sangamesh BADIGER ,  Dirk BEHNKE ,  Claudia BETSCHART ,  Vinod CHAUDHARI ,  Simona COTESTA ,  Samuel HINTERMANN ,  Andreas LERCHNER ,  Fatma LIMAM ,  Silvio OFNER ,  Chetan PANDIT ,  Jürgen WAGNER

IPC: A61K31/5386 ,  A61K31/498 ,  A61K31/501 ,  A61K31/499 ,  A61K31/497 ,  A61K31/517 ,  A61K31/506 ,  A61K31/438 ,  A61K31/427 ,  A61K31/423 ,  C07D487/10 ,  C07D498/04 ,  C07D471/10 ,  A61P25/28 ,  C07D498/10 ,  A61K31/502

CPC classification number: C07D471/10

Abstract: The invention relates to compounds of the formula I A-D-C(R1)2—B  (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract translation: 本发明涉及式I A-D-C（R 1）2 -B（I）的化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

公开(公告)号：US07550146B2

公开(公告)日：2009-06-23

申请号：US10898410

申请日：2004-07-23

Applicant: Samuel J. Danishefsky ,  Dalibor Sames ,  Samuel Hintermann ,  Peter Glunz ,  Govindaswami Ragupathi ,  Philip O. Livingston ,  Kenneth O. Lloyd ,  Valery Kudryashov

Inventor： Samuel J. Danishefsky ,  Dalibor Sames ,  Samuel Hintermann ,  Peter Glunz ,  Govindaswami Ragupathi ,  Philip O. Livingston ,  Kenneth O. Lloyd ,  Valery Kudryashov

IPC: A61K38/14 ,  A61K39/385 ,  C07K9/00

CPC classification number: C07H5/06

Abstract: The present invention provides novel glycoconjugates such as glycopeptides, as well as convergent methods for the synthesis thereof. An exemplary preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the glycoconjugates of the invention.

Abstract translation: 本发明提供了新的糖缀合物，如糖肽，以及其合成方法。 通过合成通常在上皮肿瘤细胞表面上发现的粘蛋白基序来举例说明一个示例性的制备方法。 本发明还提供了使用本发明的糖缀合物治疗癌症的组合物和方法。

公开(公告)号：US07087756B2

公开(公告)日：2006-08-08

申请号：US10486569

申请日：2002-08-14

Applicant: Samuel Hintermann ,  Bastian Hengerer ,  Ulrike Von Krosigk

Inventor： Samuel Hintermann ,  Bastian Hengerer ,  Ulrike Von Krosigk

IPC: C07D471/02

CPC classification number: C07D498/04

Abstract: The invention provides compounds of formula I, wherein X, Y, R1, R2, and R3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.

Abstract translation: 本发明提供式I化合物，其中X，Y，R 1，R 2和R 3是如说明书中所定义的， 及其制备。 式I的化合物可用作药物。

公开(公告)号：US20090281077A1

公开(公告)日：2009-11-12

申请号：US12440440

申请日：2007-09-07

Applicant: Samuel Hintermann ,  Michele Chiesi

Inventor： Samuel Hintermann ,  Michele Chiesi

IPC: A61K31/554 ,  C07D281/02 ,  A61P25/00 ,  A61P9/00

CPC classification number: C07D281/10

Abstract: The invention relates to novel heterocyclic compounds of the formula in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

Abstract translation: 本发明涉及游离碱形式或酸加成盐形式的新颖的式杂环化合物，其制备方法，其用作药物和包含它们的药物。

公开(公告)号：US07160856B2

公开(公告)日：2007-01-09

申请号：US10205021

申请日：2002-07-25

Applicant: Samuel J. Danishefsky ,  Dalibor Sames ,  Samuel Hintermann ,  Xiao Tao Chen ,  Jacob B. Schwarz ,  Peter Glunz ,  Govindaswami Ragupathi ,  Philip O. Livingston ,  Scott Kuduk ,  Lawrence Williams

Inventor： Samuel J. Danishefsky ,  Dalibor Sames ,  Samuel Hintermann ,  Xiao Tao Chen ,  Jacob B. Schwarz ,  Peter Glunz ,  Govindaswami Ragupathi ,  Philip O. Livingston ,  Scott Kuduk ,  Lawrence Williams

IPC: A61K38/14 ,  A61K39/385 ,  C07K9/00

CPC classification number: C07K14/4727 ,  A61K38/00 ,  A61K39/00 ,  C07K9/001

Abstract: The present invention provides novel α-O-linked glycoconjugates such as α-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the α-O-linked glycoconjugates.

Abstract translation: 本发明提供了新的α-O-连接的糖缀合物，例如α-O-连接的糖肽，以及用于合成它们的收敛方法。 通常的制备方法通过上皮肿瘤细胞表面上通常发现的粘蛋白基序的合成来举例说明。 本发明还提供了使用α-O-连接的糖缀合物治疗癌症的组合物和方法。

公开(公告)号：US20120258973A1

公开(公告)日：2012-10-11

申请号：US13517115

申请日：2010-12-20

Applicant: Sangamesh Babiger ,  Dirk Behnke ,  Claudia Betschart ,  Vinod Chaudhari ,  Murali Chebrolu ,  Simona Cotesta ,  Samuel Hintermann ,  Arndt Meyer ,  Chetan Pandit

Inventor： Sangamesh Babiger ,  Dirk Behnke ,  Claudia Betschart ,  Vinod Chaudhari ,  Murali Chebrolu ,  Simona Cotesta ,  Samuel Hintermann ,  Arndt Meyer ,  Chetan Pandit

IPC: A61K31/437 ,  A61P3/00 ,  A61P25/30 ,  A61P25/28 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/497 ,  C07D519/00 ,  C07D498/04 ,  A61K31/444 ,  A61P25/00 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D498/04 ,  C07D519/00

Abstract: The invention relates to compound of the formula (I′) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract translation: 本发明涉及式（I'）的化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

公开(公告)号：US20110294799A1

公开(公告)日：2011-12-01

申请号：US12673394

申请日：2008-08-12

Applicant: Samuel Hintermann ,  Konstanze Hurth ,  Joachim Nozulak ,  Marina Tintelnot-Blomley

Inventor： Samuel Hintermann ,  Konstanze Hurth ,  Joachim Nozulak ,  Marina Tintelnot-Blomley

IPC: A61K31/4745 ,  C07D471/14 ,  A61K31/5377 ,  A61K31/4375 ,  A61K31/496 ,  A61P25/00 ,  A61P25/22 ,  A61P25/08 ,  A61P25/06 ,  A61P25/24 ,  A61P25/28 ,  A61P25/16 ,  A61P25/18 ,  A61P1/08 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D471/14

Abstract: The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract translation: 本发明涉及式I化合物，其中取代基如说明书中所定义; 游离碱形式或酸加成盐形式; 作为其制备，用作药物和包含它的药物。

公开(公告)号：US20100222396A1

公开(公告)日：2010-09-02

申请号：US12695462

申请日：2010-01-28

Applicant: Dirk BEHNKE ,  Claudia Betschart ,  Simona Cotesta ,  Marc Gerspacher ,  Samuel Hintermann ,  Bernard Lucien Roy ,  Anette Von Matt ,  Jürgen Wagner

Inventor： Dirk BEHNKE ,  Claudia Betschart ,  Simona Cotesta ,  Marc Gerspacher ,  Samuel Hintermann ,  Bernard Lucien Roy ,  Anette Von Matt ,  Jürgen Wagner

IPC: A61K31/44 ,  C07D207/30 ,  A61K31/40 ,  C07D213/81

CPC classification number: C07C233/78 ,  C07D207/416 ,  C07D209/08 ,  C07D213/81 ,  C07D215/48 ,  C07D215/50 ,  C07D217/26 ,  C07D233/66 ,  C07D235/24 ,  C07D277/56 ,  C07D307/79 ,  C07D317/68 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

Abstract: The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract translation: 本发明涉及式I化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

公开(公告)号：US07432293B2

公开(公告)日：2008-10-07

申请号：US10545245

申请日：2004-02-13

Applicant: Samuel Hintermann ,  Bastian Hengerer ,  Boris Schmidt

Inventor： Samuel Hintermann ,  Bastian Hengerer ,  Boris Schmidt

IPC: A61K31/42 ,  A61K31/4245 ,  C07D263/30 ,  C07D271/06

CPC classification number: C07D271/06 ,  C07D261/08 ,  C07D263/32 ,  C07D413/04

Abstract: The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy C1-4alkoxy, CF3, halogen, C1-4alkylamino, di C1-4alkylamino, di C1-4 alkylamino C1-4 alkoxy or N—C1-4 alkoxy C1-4 alkyl-N—C1-4 alkylamino, N—C1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C1-4 alkoxy, wherein the C1-4 alkyl radicals in R2 are optionally further substituted by C1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3, X is O, Y is CH, Z is N and W is CH, (b) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R1 is not hydroxy when R2 is CF3, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.

Abstract translation: 本发明涉及式（I）的化合物：其中R 1是羟基，C 1-4烷氧基，氨基，C 1-4 烷基 - 氨基，二C 1-4烷基氨基，苄氧基或C 2 -C 7烷酰基，R 2 为C 1-4烷基，C 1-4烷氧基，C 1-4烷氧基C 1-4烷基 烷氧基，CF 3，卤素，C 1-4烷基氨基，二C 1-4烷基氨基，二C 1-4 烷基氨基C 1-4烷氧基或NC 1-4烷氧基C 1-4烷基-NC 1-4 烷基氨基，NC 1-4烷基 - 哌嗪基，吗啉基或吡咯烷基-C 1-4烷氧基，其中C 1-4 - R 2中的烷基任选进一步被C 1-4烷基，卤素，氰基，氨基，烷氧基或烷硫基取代，X是N或O，Y是N ，O或CH，Z是N或CH，W是N或CH，条件是当R（R）不为羟基或C 1-4烷氧基时， 2是CF 3，X是O，Y是C H，Z是N，W是CH，（b）当R 2是CF时，R 1不是羟基或C 1-4烷氧基 3是或氯，X是N，Y是O，Z是CH，W是CH，（c）R 1不是羟基， SUB>是CF 3，X是O，Y是N，Z是CH，W是CH，（d）X和Y不同时为O，其盐; 它们的制备，它们的用途和含有它们的药物组合物。