公开(公告)号：US20120196792A1

公开(公告)日：2012-08-02

申请号：US13439551

申请日：2012-04-04

Applicant: Yiyin Ku ,  Keith F. McDaniel ,  Hui-Ju Chen ,  Jason P. Shanley ,  Dale J. Kempf ,  David J. Grampovnik ,  Ying Sun ,  Dong Liu ,  Yonghua Gai ,  Yat Sun Or ,  Seble H. Wagaw ,  Ken Engstrom ,  Tim Grieme ,  Ahmad Sheikh ,  Jianzhang Mei

Inventor： Yiyin Ku ,  Keith F. McDaniel ,  Hui-Ju Chen ,  Jason P. Shanley ,  Dale J. Kempf ,  David J. Grampovnik ,  Ying Sun ,  Dong Liu ,  Yonghua Gai ,  Yat Sun Or ,  Seble H. Wagaw ,  Ken Engstrom ,  Tim Grieme ,  Ahmad Sheikh ,  Jianzhang Mei

IPC: A61K38/12 ,  A61P31/12 ,  C07K5/12

CPC classification number: C07K1/113 ,  C07D487/04

Abstract: The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

公开(公告)号：US08232246B2

公开(公告)日：2012-07-31

申请号：US12495299

申请日：2009-06-30

Applicant: Keith F. McDaniel ,  Dale J. Kempf

Inventor： Keith F. McDaniel ,  Dale J. Kempf

IPC: A61K38/00

CPC classification number: C07K5/0804 ,  C07K5/0802

Abstract: Compounds capable of inhibiting replication of the hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract translation: 描述了能够抑制丙型肝炎病毒（“HCV”）复制的化合物。 本发明还涉及制备这种化合物的方法，包含这些化合物的组合物，以及使用这些化合物治疗HCV感染的方法。

公开(公告)号：US20120184559A1

公开(公告)日：2012-07-19

申请号：US13362833

申请日：2012-01-31

Applicant: Dale J. Kempf ,  Charles A. Flentge ,  John T. Randolph ,  Peggy Huang ,  Larry L. Klein

Inventor： Dale J. Kempf ,  Charles A. Flentge ,  John T. Randolph ,  Peggy Huang ,  Larry L. Klein

IPC: A61K31/4965 ,  A61K31/4439 ,  A61K31/425 ,  C12N9/99 ,  A61K31/27

CPC classification number: C07D277/30 ,  A61K31/426 ,  A61K31/427 ,  A61K45/06 ,  C07C53/18 ,  C07D213/30 ,  C07D231/12 ,  C07D233/64 ,  C07D263/32 ,  C07D277/24 ,  C07D277/38 ,  C07D277/587 ,  C07D333/16 ,  C07D417/04

Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.

Abstract translation: 新的式1化合物或其药学上可接受的盐抑制细胞色素P450单加氧酶。

公开(公告)号：US20120083490A1

公开(公告)日：2012-04-05

申请号：US13315137

申请日：2011-12-08

Applicant: Larry L. Klein ,  Hui-Ju Chen ,  Ming C. Yeung ,  Charles A. Flentge ,  John T. Randolph ,  Peggy P. Huang ,  Douglas K. Hutchinson ,  Dale J. Kempf

Inventor： Larry L. Klein ,  Hui-Ju Chen ,  Ming C. Yeung ,  Charles A. Flentge ,  John T. Randolph ,  Peggy P. Huang ,  Douglas K. Hutchinson ,  Dale J. Kempf

IPC: A61K31/5355 ,  C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  C12N9/99 ,  A61K31/4439 ,  A61K31/513 ,  C07D417/14 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4535 ,  A61P31/12 ,  A61P31/14 ,  A61P43/00 ,  C07D277/30

CPC classification number: A61K31/5377 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/506 ,  A61K45/06 ,  C07D213/79 ,  C07D277/24 ,  C07D277/30 ,  C07D277/593 ,  C07D417/12

Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.

Abstract translation: 本发明的特征在于式I化合物或其药学上可接受的盐，溶剂合物或前药，以及使用该化合物抑制CYP酶代谢活性的方法。 本发明还涉及使用这些化合物，盐，溶剂合物或前药来改善由CYP酶代谢的药物的药代动力学的方法。

公开(公告)号：US20110091423A1

公开(公告)日：2011-04-21

申请号：US12958899

申请日：2010-12-02

Applicant: Dale J. Kempf ,  Kennan C. Marsh

Inventor： Dale J. Kempf ,  Kennan C. Marsh

IPC: A61K38/21 ,  A61K31/497 ,  A61K31/403 ,  A61K31/427 ,  A61K31/7056 ,  A61P31/14

CPC classification number: A61K38/212 ,  A61K31/407 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/7056 ,  A61K2300/00

Abstract: The present invention discloses compositions and a method of improving the pharmacokinetics of pharmaceutical agents (or pharmaceutically acceptable salts, esters, and prodrugs thereof) which are metabolized by cytochrome P450 monoxygenase comprising coadministering ritonavir or a pharmaceutically acceptable salt, ester, and prodrug thereof.

Abstract translation: 本发明公开了通过包含联合利托那韦或其药学上可接受的盐，酯和前药的细胞色素P450单加氧酶代谢的药物（或其药学上可接受的盐，酯和前体药物）的药代动力学的组合物和方法。

公开(公告)号：US07915411B2

公开(公告)日：2011-03-29

申请号：US11613825

申请日：2006-12-20

Applicant: David A. Betebenner ,  David A. DeGoey ,  Clarence J. Maring ,  Allan C. Krueger ,  Nobuhiko Iwasaki ,  Todd W. Rockway ,  Curt S. Cooper ,  David D. Anderson ,  Pamela L. Donner ,  Brian E. Green ,  Dale J. Kempf ,  Dachun Liu ,  Keith F. McDaniel ,  Darold L. Madigan ,  Christopher E. Motter ,  John K. Pratt ,  Jason P. Shanley ,  Michael D. Tufano ,  Rolf Wagner ,  Rong Zhang ,  Akhteruzzaman Molla ,  Hongmei Mo ,  Tami J. Pilot-Matias ,  Sherie V L. Masse ,  Robert J. Carrick ,  Wenping He ,  Liangjun Lu ,  David J. Grampovnik

Inventor： David A. Betebenner ,  David A. DeGoey ,  Clarence J. Maring ,  Allan C. Krueger ,  Nobuhiko Iwasaki ,  Todd W. Rockway ,  Curt S. Cooper ,  David D. Anderson ,  Pamela L. Donner ,  Brian E. Green ,  Dale J. Kempf ,  Dachun Liu ,  Keith F. McDaniel ,  Darold L. Madigan ,  Christopher E. Motter ,  John K. Pratt ,  Jason P. Shanley ,  Michael D. Tufano ,  Rolf Wagner ,  Rong Zhang ,  Akhteruzzaman Molla ,  Hongmei Mo ,  Tami J. Pilot-Matias ,  Sherie V L. Masse ,  Robert J. Carrick ,  Wenping He ,  Liangjun Lu ,  David J. Grampovnik

IPC: C07D471/04 ,  A61P1/16

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D475/06 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.

公开(公告)号：US20110003827A1

公开(公告)日：2011-01-06

申请号：US11009841

申请日：2004-12-10

Applicant: Charles A. Flentge ,  Hui-Ju Chen ,  David A. DeGoey ,  William J. Flosi ,  David J. Grampovnik ,  Peggy P. Huang ,  Dale J. Kempf ,  Larry L. Klein ,  Allan C. Krueger ,  Darold L. Madigan ,  John T. Randolph ,  Minghua Sun ,  Ming C. Yeung ,  Chen Zhao

Inventor： Charles A. Flentge ,  Hui-Ju Chen ,  David A. DeGoey ,  William J. Flosi ,  David J. Grampovnik ,  Peggy P. Huang ,  Dale J. Kempf ,  Larry L. Klein ,  Allan C. Krueger ,  Darold L. Madigan ,  John T. Randolph ,  Minghua Sun ,  Ming C. Yeung ,  Chen Zhao

IPC: A61K31/501 ,  C07C317/48 ,  C07C311/37 ,  C07D213/46 ,  C07D307/14 ,  C07D333/22 ,  C07D417/12 ,  C07D409/06 ,  C07D403/06 ,  C07D471/04 ,  A61K31/216 ,  A61K31/18 ,  A61K31/4402 ,  A61K31/341 ,  A61K31/381 ,  A61K31/427 ,  A61K31/4178 ,  A61K31/4709 ,  A61K31/437 ,  A61K31/506 ,  A61P31/18

CPC classification number: C07D417/12 ,  C07C311/18 ,  C07C311/29 ,  C07C311/41 ,  C07C311/47 ,  C07C317/18 ,  C07D209/14 ,  C07D213/30 ,  C07D213/40 ,  C07D233/36 ,  C07D233/64 ,  C07D233/72 ,  C07D277/24 ,  C07D277/28 ,  C07D307/14 ,  C07D307/20 ,  C07D307/52 ,  C07D333/20 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/10 ,  C07D409/06 ,  C07D409/10 ,  C07D417/06 ,  C07D417/10 ,  C07D471/04 ,  C07D493/04

Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract translation: 公开了式的化合物作为HIV蛋白酶抑制剂。 还公开了用于抑制HIV感染的方法和组合物。

公开(公告)号：US20100280248A1

公开(公告)日：2010-11-04

申请号：US12834315

申请日：2010-07-12

Applicant: Dale J. Kempf

Inventor： Dale J. Kempf

IPC: C07D215/02 ,  C07D277/20 ,  C07D261/02 ,  C07D213/04 ,  C07D233/54 ,  C07D207/30

CPC classification number: C07D277/30 ,  A61K31/426 ,  A61K31/427 ,  A61K45/06 ,  C07C53/18 ,  C07D213/30 ,  C07D231/12 ,  C07D233/64 ,  C07D263/32 ,  C07D277/24 ,  C07D277/38 ,  C07D277/587 ,  C07D333/16 ,  C07D417/04

Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.

Abstract translation: 新的式1化合物或其药学上可接受的盐抑制细胞色素P450单加氧酶。

公开(公告)号：US20100144608A1

公开(公告)日：2010-06-10

申请号：US12584716

申请日：2009-09-10

Applicant: Yiyin Ku ,  Keith F. McDaniel ,  Hui-Ju Chen ,  Jason P. Shanley ,  Dale J. Kempf ,  David J. Grampovnik ,  Ying Sun ,  Dong Liu ,  Yonghua Gai ,  Yat Sun Or ,  Seble H. Wagaw ,  Ken Engstrom ,  Tim Grieme ,  Ahmad Sheikh ,  Jianzhang Mei

Inventor： Yiyin Ku ,  Keith F. McDaniel ,  Hui-Ju Chen ,  Jason P. Shanley ,  Dale J. Kempf ,  David J. Grampovnik ,  Ying Sun ,  Dong Liu ,  Yonghua Gai ,  Yat Sun Or ,  Seble H. Wagaw ,  Ken Engstrom ,  Tim Grieme ,  Ahmad Sheikh ,  Jianzhang Mei

IPC: A61K38/12 ,  C07D487/04 ,  A61P31/12

CPC classification number: C07K1/113 ,  C07D487/04

Abstract: The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

Abstract translation: 本发明涉及新的大环化合物和在需要用所述大环化合物进行这种治疗的受试者中治疗丙型肝炎感染的方法。 本发明还涉及包含本发明化合物或其药学上可接受的盐，酯或前药与药学上可接受的载体或赋形剂组合的药物组合物。

公开(公告)号：US07320961B2

公开(公告)日：2008-01-22

申请号：US10802829

申请日：2004-03-18

Applicant: Dale J. Kempf ,  Richard J. Bertz ,  Jeffrey F. Waring

Inventor： Dale J. Kempf ,  Richard J. Bertz ,  Jeffrey F. Waring

IPC: A61K31/425 ,  A61K38/00

CPC classification number: A61K31/436 ,  A61K31/167 ,  A61K31/282 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/496 ,  A61K31/506 ,  A61K31/565 ,  A61K31/7048 ,  A61K31/7068 ,  A61K31/708

Abstract: The present invention is directed to a method for inducing UGT1A1 isoform expression for treatment of a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate comprising the step of administering to a subject an effective amount of ritonavir. In particular, the present invention is directed to a method of treating unconjugated hyperbilirubinemia by UGT1A1 induction comprising the step of administering to a subject an effective amount of ritonavir.

Abstract translation: 本发明涉及一种用于诱导UGT1A1同种型表达的方法，用于治疗由UGT1A1底物升高的血清浓度引起的疾病，障碍或不良反应，包括向受试者施用有效量的利托那韦的步骤。 特别地，本发明涉及一种通过UGT1A1诱导处理未结合的高胆红素血症的方法，其包括向受试者施用有效量的利托那韦的步骤。