公开(公告)号：US20070225270A1

公开(公告)日：2007-09-27

申请号：US11710644

申请日：2007-02-23

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Marc Labroli ,  Kartik Keertikar

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Marc Labroli ,  Kartik Keertikar

IPC: A61K31/551 ,  A61K31/5377 ,  A61K31/519 ,  C07D487/04 ,  A61K31/541

CPC classification number: C07D487/04 ,  Y02P20/582

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

公开(公告)号：US20070082901A1

公开(公告)日：2007-04-12

申请号：US11542852

申请日：2006-10-04

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer

IPC: A61K31/5377 ,  A61K31/519 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a] pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种这类化合物的药物组合物， 制备包括一种或多种这样的化合物的药物制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。

公开(公告)号：US20070082900A1

公开(公告)日：2007-04-12

申请号：US11542801

申请日：2006-10-04

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  David Parry

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  David Parry

IPC: A61K31/5377 ,  A61K31/519

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.

Abstract translation: 本发明提供使用吡唑并[1,5-a]嘧啶化合物抑制选自AKT，检查点激酶，极光激酶，Pim激酶和酪氨酸激酶的蛋白激酶的方法，以及治疗，预防，抑制或 使用这种化合物改善与蛋白激酶相关的一种或多种疾病。

公开(公告)号：US20070072882A1

公开(公告)日：2007-03-29

申请号：US11543182

申请日：2006-10-04

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  M. Siddiqui ,  Panduranga Reddy ,  David Belanger ,  Blake Hamann ,  Patrick Curran

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  M. Siddiqui ,  Panduranga Reddy ,  David Belanger ,  Blake Hamann ,  Patrick Curran

IPC: A61K31/519 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类作为细胞周期蛋白依赖性激酶（CDK）抑制剂的吡唑并[1,5-a]嘧啶化合物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备方法 包含一种或多种这样的化合物的药物制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

公开(公告)号：US20070072881A1

公开(公告)日：2007-03-29

申请号：US11542920

申请日：2006-10-04

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Marc Labroli ,  Kartik Keertikar

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Marc Labroli ,  Kartik Keertikar

IPC: A61K31/519 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

公开(公告)号：US20060122389A1

公开(公告)日：2006-06-08

申请号：US11335383

申请日：2006-01-19

Applicant: Timothy Guzi ,  Kamil Paruch

Inventor： Timothy Guzi ,  Kamil Paruch

IPC: A61K31/53 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the kinases using such compounds or pharmaceutical compositions.

公开(公告)号：US20060069103A1

公开(公告)日：2006-03-30

申请号：US11273712

申请日：2005-11-14

Applicant: Timothy Guzi ,  Kamil Paruch ,  Alan Mallams ,  Jocelyn Rivera ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Jonathan Pachter ,  Yi-Tsung Liu ,  Anil Saksena

Inventor： Timothy Guzi ,  Kamil Paruch ,  Alan Mallams ,  Jocelyn Rivera ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Jonathan Pachter ,  Yi-Tsung Liu ,  Anil Saksena

IPC: A61K31/496 ,  C07D403/02

CPC classification number: C07D211/34 ,  C07D211/48 ,  C07D295/185 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/02 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

Abstract: There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17β-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.

Abstract translation: 公开了式（I）的化合物：

公开(公告)号：US20070275983A1

公开(公告)日：2007-11-29

申请号：US11779050

申请日：2007-07-17

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Lawrence Dillard ,  Vinh Tran ,  Zhenmin He ,  Ray James ,  Haengsoon Park

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Lawrence Dillard ,  Vinh Tran ,  Zhenmin He ,  Ray James ,  Haengsoon Park

IPC: A61K31/519 ,  A61K38/14 ,  A61K31/704 ,  A61K31/7072 ,  A61K31/52

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/52 ,  A61K31/704 ,  A61K31/7072 ,  A61K45/06 ,  A61K2300/00

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法 包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

公开(公告)号：US20070117804A1

公开(公告)日：2007-05-24

申请号：US11598186

申请日：2006-11-08

Applicant: Lianyun Zhao ,  Patrick Curran ,  David Belanger ,  Blake Hamann ,  Panduranga Reddy ,  Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  M. Siddiqui ,  Praveen Tadikonda

Inventor： Lianyun Zhao ,  Patrick Curran ,  David Belanger ,  Blake Hamann ,  Panduranga Reddy ,  Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  M. Siddiqui ,  Praveen Tadikonda

IPC: A61K31/498 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的咪唑并吡嗪化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种此类化合物的药物组合物，制备药物制剂的方法，包括一种或多种 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。

公开(公告)号：US20070083044A1

公开(公告)日：2007-04-12

申请号：US11542921

申请日：2006-10-04

Applicant: Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  Carmen Alvarez

Inventor： Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  Carmen Alvarez

IPC: C07D487/12 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of amino-substituted pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的氨基取代的吡唑并[1,5-a]嘧啶化合物作为蛋白质和/或检查点激酶的抑制剂，制备这些化合物的方法，药物组合物包括一种或多种这样的化合物 制备药物制剂的方法，包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。