公开(公告)号：US20070082902A1

公开(公告)日：2007-04-12

申请号：US11542902

申请日：2006-10-04

Applicant: Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer

Inventor： Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer

IPC: A61K31/5377 ,  A61K31/519 ,  C07D487/10 ,  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：US20070072880A1

公开(公告)日：2007-03-29

申请号：US11542833

申请日：2006-10-04

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer

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：US20070032495A1

公开(公告)日：2007-02-08

申请号：US11546766

申请日：2006-10-12

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.

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]三嗪化合物作为激酶抑制剂，例如细胞周期蛋白依赖性激酶，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物 化合物，制备包含一种或多种这样的化合物的药物制剂的方法，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与激酶相关的一种或多种疾病的方法。

公开(公告)号：US20060173016A1

公开(公告)日：2006-08-03

申请号：US11395824

申请日：2006-03-31

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

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

IPC: A61K31/517 ,  C07D487/04

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.

公开(公告)号：US20060148816A1

公开(公告)日：2006-07-06

申请号：US11362217

申请日：2006-02-24

Applicant: Kamil Paruch ,  Timothy Guzi

Inventor： Kamil Paruch ,  Timothy Guzi

IPC: A61K31/496 ,  A61K31/4545 ,  C07D403/14 ,  C07D401/02

CPC classification number: C07D211/46 ,  C07D211/58

Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, 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 type 3 17β-hydroxysteroid dehydrogenase 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型化合物作为3β17β-羟基类固醇脱氢酶的抑制剂，制备此类化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法 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3型17β-羟类固醇脱氢酶相关的一种或多种疾病的方法。

公开(公告)号：US20060094706A1

公开(公告)日：2006-05-04

申请号：US11244628

申请日：2005-10-06

Applicant: Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  Gerald Shipps

Inventor： Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  Gerald Shipps

IPC: A61K31/554 ,  A61K31/553 ,  A61K31/551 ,  A61K31/541 ,  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. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.

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。 本发明还涉及丙型肝炎病毒（HCV）复制的抑制。 特别地，本发明的实施方案提供了用于抑制HCV RNA依赖性RNA聚合酶酶活性的化合物和方法。 本发明还提供了预防和治疗HCV感染的组合物和方法。

公开(公告)号：US20060040958A1

公开(公告)日：2006-02-23

申请号：US11244776

申请日：2005-10-06

Applicant: Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer

Inventor： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer

IPC: 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 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：US06372747B1

公开(公告)日：2002-04-16

申请号：US09465553

申请日：1999-12-16

Applicant: Arthur G. Taveras ,  Ronald J. Doll ,  Alan B. Cooper ,  Johan A. Ferreira ,  Timothy Guzi ,  Dinanath F. Rane ,  Viyyoor M. Girijavallabhan ,  Cynthia J. Aki ,  Jianping Chao ,  Carmen Alvarez ,  Joseph M. Kelly ,  Tarik Lalwani ,  Jagdish A. Desai ,  James J-S Wang

Inventor： Arthur G. Taveras ,  Ronald J. Doll ,  Alan B. Cooper ,  Johan A. Ferreira ,  Timothy Guzi ,  Dinanath F. Rane ,  Viyyoor M. Girijavallabhan ,  Cynthia J. Aki ,  Jianping Chao ,  Carmen Alvarez ,  Joseph M. Kelly ,  Tarik Lalwani ,  Jagdish A. Desai ,  James J-S Wang

IPC: A61K31496

CPC classification number: C07D401/04 ,  C07D401/14

Abstract: Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alkyl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

Abstract translation: 公开了下式的化合物：其中R 13表示咪唑环; R14表示氨基甲酸酯，脲，酰胺或磺酰胺基; 当酰胺基和R 13咪唑基之间的烷基链被取代时，R8表示H，或R8表示芳基烷基，杂芳基烷基或环烷基等取代基; 并且其余的取代基如本文所定义。 还公开了其中R 8为H，酰胺基和R 13咪唑基之间的烷基链未被取代的化合物。 还公开了使用所公开的化合物治疗癌症的方法和抑制法呢基蛋白转移酶的方法。

公开(公告)号：US20150353552A1

公开(公告)日：2015-12-10

申请号：US14443294

申请日：2013-11-15

Applicant: Abdelghani Abe ACHAB ,  Michael D. ALTMAN ,  Yongqi DENG ,  Timothy GUZI ,  Solomon KATTAR ,  Jason D. KATZ ,  Joey L. METHOT ,  Hua ZHOU ,  Meredeth MCGOWAN ,  Matthew P. CHRISTOPHER ,  Yudith GARCIA ,  Neville John THONY ,  Francesc Xavier FRADERA LLINAS ,  Changwei MU ,  Sixing ZHANG ,  Rong ZHANG ,  Kin Chiu FONG ,  Xiansheng LENG ,  MERCK SHARP & DOHME CORP.

Inventor： Abdelghani Abe Achab ,  Michael D. Altman ,  Yongqi Deng ,  Timothy Guzi ,  Solomon Kattar ,  Jason D. Katz ,  Joey L. Methot ,  Hua Zhou ,  Meredeth McGowan ,  Matthew P. Christopher ,  Yudith Garcia ,  Neville John Anthony ,  Francesc Xavier Fradera Llinas ,  Kin Chiu Fong ,  Xiansheng Leng ,  Changwei Mu ,  Sixing Zhang ,  Rong Zhang

IPC: C07D473/30 ,  A61K31/5377 ,  A61K31/52

CPC classification number: A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D473/00 ,  C07D473/06 ,  C07D473/30 ,  C07D473/38 ,  C07D519/00 ,  A61K2300/00

Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

Abstract translation: 本发明提供了作为PI3K-δ抑制剂的式I化合物，因此可用于治疗PI3K-δ介导的疾病如炎症，哮喘，COPD和癌症。

公开(公告)号：US07432268B2

公开(公告)日：2008-10-07

申请号：US11273712

申请日：2005-11-14

Applicant: Timothy Guzi ,  Kamil Paruch ,  Alan Mallams ,  Jocelyn D. Rivera ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Jonathan A. Pachter ,  Yi-Tsung Liu ,  Anil K. Saksena

Inventor： Timothy Guzi ,  Kamil Paruch ,  Alan Mallams ,  Jocelyn D. Rivera ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Jonathan A. Pachter ,  Yi-Tsung Liu ,  Anil K. Saksena

IPC: A61K31/497 ,  A61K31/445 ,  A01N43/40 ,  C07D241/02 ,  C07D211/70 ,  C07D211/82 ,  C07D213/06

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: 公开了可用作3型17β-羟基甾体脱氢酶抑制剂的式（I）化合物：其前药或化合物或所述前药的药学上可接受的盐。 还公开了含有所述化合物及其用于治疗或预防雄激素依赖性疾病的药物组合物。