公开(公告)号：US20050119288A1

公开(公告)日：2005-06-02

申请号：US10919831

申请日：2004-08-17

Applicant: Samit Bhattacharya ,  Richard Connell ,  Jitesh Jani ,  James Moyer ,  Dennis Noe ,  Stefanus Steyn

Inventor： Samit Bhattacharya ,  Richard Connell ,  Jitesh Jani ,  James Moyer ,  Dennis Noe ,  Stefanus Steyn

IPC: A61K31/00 ,  A61K31/506 ,  A61K31/517 ,  A61P35/00

CPC classification number: A61K31/00 ,  A61K31/506 ,  A61K31/517 ,  A61K2300/00

Abstract: The invention is directed to methods for the a method for treating overexpression of the erbB2 in a mammal in need of treatment by administering to the mammal a therapeutically effective amount of a first inhibitor of an erbB2 receptor and then, after an interval of less than 24 hours, administering to the mammal from one to six therapeutically effective amounts of the same or different inhibitor of the erbB2 receptor. The invention is also directed to a slow daily infusion of the erbB2 inhibitor. The overexpression of the erbB2 receptor can result in abnormal cell growth and lead to cancer. By the methods of the invention, the efficacy and safety of the inhibitors is increased. The invention is also directed to kits for facilitating the dose administration method of the invention.

Abstract translation: 本发明涉及用于治疗需要治疗的哺乳动物中erbB2的过度表达的方法，其通过向哺乳动物施用治疗有效量的第一种erbB2受体抑制剂，然后在间隔小于24 小时，向哺乳动物施用1至6个治疗有效量的相同或不同的erbB2受体抑制剂。 本发明还涉及缓慢的每日输注erbB2抑制剂。 erbB2受体的过度表达可导致细胞生长异常并导致癌症。 通过本发明的方法，抑制剂的功效和安全性增加。 本发明还涉及用于促进本发明的剂量给药方法的试剂盒。

公开(公告)号：US20070072885A1

公开(公告)日：2007-03-29

申请号：US11422235

申请日：2006-06-05

Applicant: Samit Bhattacharya ,  Chandra Prakash

Inventor： Samit Bhattacharya ,  Chandra Prakash

IPC: A61K31/517 ,  C07D403/02

CPC classification number: C07D239/94 ,  C07D401/12

Abstract: The invention relates to substantially pure compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R5, and X are as defined herein, and wherein the compound of formula 1 optionally further comprises a hydroxy substituent, an O-glucuronic acid, or an N−>O (N-oxide) moiety. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders that contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Abstract translation: 本发明涉及基本上纯的式1化合物及其药学上可接受的盐，前药和溶剂化物，其中R 1，R 2，R 3， R 5，R 5如本文所定义，并且其中式1化合物任选地进一步包含羟基取代基，O-葡萄糖醛酸或N-（O-氧化物） ）部分。 本发明还涉及通过施用式1的化合物和用于治疗含有式1化合物的这种病症的药物组合物来治疗哺乳动物异常细胞生长的方法。本发明还涉及制备式1化合物的方法。

公开(公告)号：US20080234303A1

公开(公告)日：2008-09-25

申请号：US11613390

申请日：2006-12-20

Applicant: Samit Bhattacharya ,  Michael Luzzio ,  Donn Wishka ,  Gonghua Pan ,  Arthur Brosius ,  Joel Arcari ,  James Southers ,  Kendra Nelson ,  Jun Xiao

Inventor： Samit Bhattacharya ,  Michael Luzzio ,  Donn Wishka ,  Gonghua Pan ,  Arthur Brosius ,  Joel Arcari ,  James Southers ,  Kendra Nelson ,  Jun Xiao

IPC: A61K31/506 ,  C07D487/04

CPC classification number: C07D471/08 ,  C07D487/08 ,  C07D495/08

Abstract: The present invention relates to a compound of the formula 1 or a pharmaceutically acceptable salt thereof, wherein Ar is a group of formula and R1, R2, R13, A, K, M, L1, L2, X, Y1, Y2, Q, salt thereof, wherein R1, R2, R13, A, K, L1, L2, W, X, Z1, Z2, Y1, Y2, Z1, Z2, M, Q, W, X, m, p and q are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

Abstract translation: 本发明涉及式1化合物或其药学上可接受的盐，其中Ar是式的基团，R 1，R 2，R 2， 13，A，K，M，L 1，L 2，X，Y 1，Y 2， 其中R 1，R 2，R 13，A，K，L 1， L，2，...，W，X，Z 1，Z 2，Y 1，Y 2， Z 1，Z 2，Z 2，M，Q，W，X，m，p和q如本文所定义。 这种新型的嘧啶衍生物可用于治疗哺乳动物中异常细胞生长，如癌症。 本发明还涉及使用这些化合物治疗哺乳动物，特别是人类异常细胞生长的方法，以及含有这些化合物的药物组合物。

公开(公告)号：US20070270438A1

公开(公告)日：2007-11-22

申请号：US11746314

申请日：2007-05-09

Applicant: Samit Bhattacharya ,  Matthew Brown ,  Peter Dorff ,  Susan LaGreca ,  Robert Maguire

Inventor： Samit Bhattacharya ,  Matthew Brown ,  Peter Dorff ,  Susan LaGreca ,  Robert Maguire

IPC: A61K31/497 ,  A61K31/4439 ,  A61K31/4245 ,  C07D413/02

CPC classification number: C07D213/38 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

Abstract: The invention relates to compounds of formula I and to pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof; wherein B, D, E, R1, R2, R3, R4, R5, R8, m, n, p, q, r, s, t and u are as defined herein. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases and autoimmune diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐，前体药物，溶剂合物或水合物; 其中B，D，E，R 1，R 2，R 3，R 4，R SUP R 5，R 8，m，n，p，q，r，s，t和u如本文所定义。 本发明还涉及使用这些化合物治疗哺乳动物，特别是人类的过度增殖性疾病和自身免疫性疾病的方法，以及含有这些化合物的药物组合物。

公开(公告)号：US20050159435A1

公开(公告)日：2005-07-21

申请号：US11079648

申请日：2005-03-14

Applicant: John Kath ,  Joel Morris ,  Samit Bhattacharya

Inventor： John Kath ,  Joel Morris ,  Samit Bhattacharya

IPC: A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61K39/395 ,  A61K45/00 ,  A61P5/00 ,  A61P5/28 ,  A61P35/00 ,  A61P43/00 ,  C07D239/00 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D43/02

CPC classification number: C07D401/12 ,  C07D239/94 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12

Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Abstract translation: 本发明涉及式1的化合物及其药学上可接受的盐，前药和溶剂合物，其中R 1，R 3，R 4， R 5，R 11，m和p如本文所定义。 本发明还涉及通过施用式1的化合物和用于治疗含有式1化合物的这种病症的药物组合物来治疗哺乳动物异常细胞生长的方法。本发明还涉及制备式1化合物的方法。