公开(公告)号：US10208064B2

公开(公告)日：2019-02-19

申请号：US15323989

申请日：2015-07-09

Applicant: MERCK SHARP & DOHME CORP. ,  Alexander Pasternak ,  Ian Davies ,  Fa-Xiang Ding ,  Jinlong Jiang ,  Shuzhi Dong ,  Xin Gu ,  Takao Suzuki ,  Joseph P. Vacca ,  Zhifa Pu ,  Shouning Xu

Inventor： Alexander Pasternak ,  Ian Davies ,  Fa-Xiang Ding ,  Jinlong Jiang ,  Shuzhi Dong ,  Xin Gu ,  Takao Suzuki ,  Joseph P. Vacca ,  Zhifa Pu ,  Shouning Xu

IPC: C07D513/10 ,  C07D519/00 ,  A61K45/06 ,  A61K31/435 ,  A61K31/4745 ,  A61K31/4375

Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

公开(公告)号：US20170197989A1

公开(公告)日：2017-07-13

申请号：US15323989

申请日：2015-07-09

Applicant: Alexander PASTERNAK ,  Ian DAVIES ,  Fa-Xiang DING ,  Jinlong JIANG ,  Shuzhi DONG ,  Xin GU ,  Takao SUZUKI ,  Joseph P. VACCA ,  Zhifa PU ,  Shouning XU ,  Merck Sharp & Dohme Corp.

Inventor： Alexander Pasternak ,  Ian Davies ,  Fa-Xiang Ding ,  Jinlong Jiang ,  Shuzhi Dong ,  Xin Gu ,  Takao Suzuki ,  Joseph P. Vacca ,  Zhifa Pu ,  Shouning Xu

IPC: C07D519/00 ,  A61K31/4745 ,  A61K31/4375 ,  A61K31/435

CPC classification number: C07D519/00 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/4745 ,  A61K45/06

Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

公开(公告)号：US08377874B2

公开(公告)日：2013-02-19

申请号：US12446789

申请日：2007-10-23

Applicant: Nigel J. Liverton ,  Joseph P. Vacca ,  John A. McCauley ,  Michael T. Rudd

Inventor： Nigel J. Liverton ,  Joseph P. Vacca ,  John A. McCauley ,  Michael T. Rudd

IPC: A61K38/00 ,  A01N37/18

CPC classification number: C07K5/0802 ,  A61K38/00 ,  C07D519/00

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

公开(公告)号：US08133891B2

公开(公告)日：2012-03-13

申请号：US12718386

申请日：2010-03-05

Applicant: Ian M. Bell ,  Steven N. Gallicchio ,  Craig A. Stump ,  Cory R. Theberge ,  Joseph P. Vacca ,  C. Blair Zartman ,  Xufang Zhang

Inventor： Ian M. Bell ,  Steven N. Gallicchio ,  Craig A. Stump ,  Cory R. Theberge ,  Joseph P. Vacca ,  C. Blair Zartman ,  Xufang Zhang

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

CPC classification number: C07D519/00 ,  C07D209/96 ,  C07D471/06 ,  C07D471/16 ,  C07D487/06

Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract translation: 本发明涉及式I化合物：其中A1，A2，B1，B2，B3，B4，D1，D2，J，K，T，U，V，W，X，Y，Z， R5a，R5b，R5c，m和n在本文中定义），其可用作CGRP受体的拮抗剂，并且可用于治疗或预防涉及CGRP的疾病，例如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US07879797B2

公开(公告)日：2011-02-01

申请号：US11919783

申请日：2006-04-28

Applicant: M. Katharine Holloway ,  Nigel J. Liverton ,  Steven W. Ludmerer ,  John A. McCauley ,  David Olsen ,  Michael T. Rudd ,  Joseph P. Vacca

Inventor： M. Katharine Holloway ,  Nigel J. Liverton ,  Steven W. Ludmerer ,  John A. McCauley ,  David Olsen ,  Michael T. Rudd ,  Joseph P. Vacca

IPC: A61K38/00

CPC classification number: C07K5/0808 ,  C07K5/0806 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0821

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。

公开(公告)号：US20100298210A1

公开(公告)日：2010-11-25

申请号：US12446296

申请日：2007-10-19

Applicant: Nigel J. Liverton ,  Vincenzo Summa ,  Joseph P. Vacca ,  Maria Emilia Di Francesco ,  Marco Pompei

Inventor： Nigel J. Liverton ,  Vincenzo Summa ,  Joseph P. Vacca ,  Maria Emilia Di Francesco ,  Marco Pompei

IPC: A61K38/12 ,  C07K5/12 ,  A61P31/14

CPC classification number: C07K5/0812 ,  A61K38/00 ,  C07K5/0808

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use treating or preventing HCV infections.

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。

公开(公告)号：US20100286185A1

公开(公告)日：2010-11-11

申请号：US12446789

申请日：2007-10-23

Applicant: Nigel J Liverton ,  Joseph P. Vacca ,  John A. McCauley ,  Joseph J. Romano ,  Michael T. Rudo

Inventor： Nigel J Liverton ,  Joseph P. Vacca ,  John A. McCauley ,  Joseph J. Romano ,  Michael T. Rudo

IPC: A61K31/4745 ,  C07D498/22 ,  A61P31/12

CPC classification number: C07K5/0802 ,  A61K38/00 ,  C07D519/00

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

公开(公告)号：US20100266714A1

公开(公告)日：2010-10-21

申请号：US12740105

申请日：2008-10-29

Applicant: Christopher S Burgey ,  Diem Nguyen ,  Zhengwu Deng ,  Daniel V. Paone ,  Craig M. Potteiger ,  Joseph P. Vacca

Inventor： Christopher S Burgey ,  Diem Nguyen ,  Zhengwu Deng ,  Daniel V. Paone ,  Craig M. Potteiger ,  Joseph P. Vacca

IPC: A61K33/00 ,  C07D401/12 ,  A61K31/444 ,  A61P25/08 ,  A61P25/04 ,  C07C235/42 ,  A61K31/166 ,  C07D239/26 ,  A61K31/505 ,  C07D403/12 ,  A61K31/506 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/5513

CPC classification number: C07C233/66 ,  C07C233/65 ,  C07C233/83 ,  C07C233/87 ,  C07D213/56 ,  C07D213/61 ,  C07D213/89 ,  C07D239/26 ,  C07D249/08 ,  C07D271/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

Abstract translation: 本发明涉及在治疗与疼痛有关的疾病状态，特别是外周疼痛，炎症性疼痛或可用P2X3受体亚基调节剂治疗的组织损伤疼痛中发挥关键作用的新型P2X3受体拮抗剂。

公开(公告)号：US07538112B2

公开(公告)日：2009-05-26

申请号：US11579772

申请日：2005-05-03

Applicant: John S. Wai ,  Joseph P. Vacca ,  Linghang Zhuang ,  Boyoung Kim ,  Terry A. Lyle ,  Catherine M. Wiscount ,  Melissa S. Egbertson ,  Lou Anne Neilson ,  Mark Embrey ,  Thorsten E. Fisher ,  Donnette D. Staas

Inventor： John S. Wai ,  Joseph P. Vacca ,  Linghang Zhuang ,  Boyoung Kim ,  Terry A. Lyle ,  Catherine M. Wiscount ,  Melissa S. Egbertson ,  Lou Anne Neilson ,  Mark Embrey ,  Thorsten E. Fisher ,  Donnette D. Staas

IPC: C07D487/14 ,  A61K31/5025 ,  A61K31/4985

CPC classification number: A61K31/5025 ,  C07D487/14 ,  Y02A50/414

Abstract: Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 羟基取代的吡嗪并吡咯并哒嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，二酮化合物具有式（I），其中R 1，R 2，R 3，R 4，R 5，R 6和R 7在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US20090124661A1

公开(公告)日：2009-05-14

申请号：US12325965

申请日：2008-12-01

Applicant: M. Katharine HOLLOWAY ,  Nigel J. LIVERTON ,  Steven W. LUDMERER ,  John A. MCCAULEY ,  David B. OLSEN ,  Michael T. RUDD ,  Joseph P. VACCA ,  Charles J. MCINTYRE

Inventor： M. Katharine HOLLOWAY ,  Nigel J. LIVERTON ,  Steven W. LUDMERER ,  John A. MCCAULEY ,  David B. OLSEN ,  Michael T. RUDD ,  Joseph P. VACCA ,  Charles J. MCINTYRE

IPC: A61K31/4523 ,  C07D498/18 ,  A61K31/407

CPC classification number: C07K5/0808 ,  A61K38/00 ,  C07K5/0812 ,  C07K5/0827

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。