公开(公告)号：WO2013163239A1

公开(公告)日：2013-10-31

申请号：PCT/US2013/037878

申请日：2013-04-24

Applicant: TAVARES, Francis Xavier

Inventor： TAVARES, Francis Xavier

IPC: C07D205/08 ,  C07D487/14 ,  A61K31/397 ,  A61P35/00

CPC classification number: C07D487/14 ,  C07D205/08

Abstract: Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC------OR---NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam.

Abstract translation: 提出了合成内酰胺的方法，其中式HOOC ------ OR --- NH-LG的羧酸（其中OR为有机部分，LG为离去基团）与酸例如 作为有机酸，特别是强酸，和脱水剂，其可以是相同的，例如强酸酐，使得加入的酸的量可以进行所需的转化而不损失 在环化前离开组（LG），并回收内酰胺。

公开(公告)号：WO2013148748A1

公开(公告)日：2013-10-03

申请号：PCT/US2013/033971

申请日：2013-03-27

Applicant: TAVARES, Francis Xavier

Inventor： TAVARES, Francis Xavier

IPC: C07D487/14 ,  C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D487/14 ,  C07D487/20 ,  C07D498/14

Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.

Abstract translation: 本文提供了可用作激酶抑制剂的化合物，以及盐，药物组合物，医学治疗方法及其合成方法。

公开(公告)号：WO03051886A8

公开(公告)日：2004-08-19

申请号：PCT/US0239672

申请日：2002-12-11

Applicant: SMITHKLINE BEECHAM CORP ,  HARRIS PHILIP ANTHONY ,  JUNG DAVID KENDALL ,  PEEL MICHAEL ROBERT ,  RENO MICHAEL JOHN ,  RHEAULT TARA RENAE ,  BADIANG JENNIFER G ,  STEVENS KIRK LAWRENCE ,  VEAL JAMES MARVIN ,  DICKERSON SCOTT HOWARD ,  TAVARES FRANCIS XAVIER

Inventor： HARRIS PHILIP ANTHONY ,  JUNG DAVID KENDALL ,  PEEL MICHAEL ROBERT ,  RENO MICHAEL JOHN ,  RHEAULT TARA RENAE ,  BADIANG JENNIFER G ,  STEVENS KIRK LAWRENCE ,  VEAL JAMES MARVIN ,  DICKERSON SCOTT HOWARD ,  TAVARES FRANCIS XAVIER

IPC: A61K31/506 ,  A61K31/5377 ,  A61K45/00 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04 ,  A61K31/5025

CPC classification number: C07D487/04

Abstract: Fused pyradazine derivatives, which are useful as CDK inhibitors are described herein. The described invention also includes methods of making such fused pyradazines derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

Abstract translation: 本文描述了可用作CDK抑制剂的稠合的哒嗪衍生物。 所述的发明还包括制备这种稠合吡嗪嗪衍生物的方法以及使用它们在治疗过度增殖性疾病中的方法。

公开(公告)号：WO2003013518A1

公开(公告)日：2003-02-20

申请号：PCT/US2002/023255

申请日：2002-07-23

Applicant: SMITHKLINE BEECHAM CORPORATION ,  SAMANO, Vicente ,  BARRETT, David, Gene ,  DEATON, David, Norman ,  MCFADYEN, Robert, Blount ,  MILLER, Aaron, Bayne ,  RAY, John, Albert ,  TAVARES, Francis, Xavier ,  ZHOU, Huiqiang

Inventor： BARRETT, David, Gene ,  DEATON, David, Norman ,  MCFADYEN, Robert, Blount ,  MILLER, Aaron, Bayne ,  RAY, John, Albert ,  TAVARES, Francis, Xavier ,  ZHOU, Huiqiang

IPC: A61K31/4245

CPC classification number: C07D233/64 ,  C04B35/632 ,  C07D231/12 ,  C07D231/40 ,  C07D233/56 ,  C07D249/08 ,  C07D271/10 ,  C07D285/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Biaryl ketoamide derivatives (I), which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such biaryl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.

Abstract translation: 本文描述了可用作组织蛋白酶K抑制剂的双芳酮酮酰胺衍生物（I）。 所描述的发明还包括制备这种联芳基酮酰胺衍生物的方法以及用于治疗与骨质疏松增加相关的障碍（包括骨质疏松症）的方法，其可能最终导致骨折。

公开(公告)号：WO2015061407A1

公开(公告)日：2015-04-30

申请号：PCT/US2014/061712

申请日：2014-10-22

Applicant: TAVARES, Francis Xavier

Inventor： TAVARES, Francis Xavier

IPC: C07D201/08 ,  C07D205/08 ,  C07D207/24

CPC classification number: C07D487/04 ,  C07D201/08 ,  C07D205/08 ,  C07D207/24 ,  C07D487/10

Abstract: Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC------OR---NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam such as that of the formula (a), provided herein, wherein G represents the atom(s) needed to form a closed ring.

Abstract translation: 提出了合成内酰胺的方法，其中式HOOC ------ OR --- NH-LG的羧酸（其中OR为有机部分，LG为离去基团）与酸例如 作为有机酸，特别是强酸，和脱水剂，其可以是相同的，例如强酸酐，使得加入的酸的量可以进行所需的转化而不损失 在环化前离去基团（LG），并回收如本文提供的式（a）的内酰胺，其中G表示形成封闭环所需的原子。

公开(公告)号：WO2003062192A1

公开(公告)日：2003-07-31

申请号：PCT/US2003/001271

申请日：2003-01-15

Applicant: SMITHKLINE BEECHAM CORPORATION ,  CATALANO, John, George ,  DEATON, David, Norman ,  MILLER, Aaron, Bayne ,  TAVARES, Francis, Xavier

Inventor： CATALANO, John, George ,  DEATON, David, Norman ,  MILLER, Aaron, Bayne ,  TAVARES, Francis, Xavier

IPC: C07C271/34

CPC classification number: C07D213/30 ,  C07C271/22 ,  C07C271/34 ,  C07C275/16 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/40 ,  C07D231/40 ,  C07D233/84 ,  C07D237/14 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D263/58 ,  C07D277/24 ,  C07D277/34 ,  C07D285/08 ,  C07D295/215 ,  C07D417/12 ,  C07D495/04

Abstract: Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.

Abstract translation: 本文描述了可用作组织蛋白酶K抑制剂的环烷基酮酰胺衍生物。 所描述的发明还包括制备这种环烷酮酮酰胺衍生物的方法以及使用该方法来治疗与骨质疏松增加相关的障碍（包括骨质疏松症）的方法，其可能最终导致骨折。

公开(公告)号：WO2016168118A1

公开(公告)日：2016-10-20

申请号：PCT/US2016/026951

申请日：2016-04-11

Applicant: TAVARES, Francis Xavier ,  VITEK, Michael Peter

Inventor： TAVARES, Francis Xavier ,  VITEK, Michael Peter

IPC: C07C229/26 ,  A61K31/22 ,  A61K31/60 ,  A61K31/195 ,  C07C69/76 ,  C07C229/02

CPC classification number: C07C229/46 ,  A61K31/195 ,  A61K31/22 ,  A61K31/223 ,  A61K31/27 ,  A61K31/357 ,  A61K31/395 ,  A61K31/421 ,  A61K31/4422 ,  A61K31/549 ,  A61K31/661 ,  A61K31/6615 ,  A61K45/06 ,  A61P25/00 ,  A61P25/28 ,  A61P35/00 ,  C07C229/26 ,  C07C235/34 ,  C07C235/78 ,  C07C251/24 ,  C07C271/16 ,  C07C271/22 ,  C07C275/16 ,  C07C381/00 ,  C07C2602/08 ,  C07D211/86 ,  C07D211/90 ,  C07D263/44 ,  C07D269/00 ,  C07D285/34 ,  C07D317/36 ,  C07D317/40 ,  C07F9/06 ,  C07F9/09 ,  A61K2300/00

Abstract: Novel compounds of formula (II) are disclosed. Compounds of formula (II) comprise ornithine derivatives or compounds that may metabolize to ornithine. Also disclosed are methods for the treatment of neurodegenerative diseases such as Alzheimer's Disease using compounds of formula (II).

Abstract translation: 公开了新的式（II）化合物。 式（II）的化合物包含可以代谢为鸟氨酸的鸟氨酸衍生物或化合物。 还公开了使用式（II）化合物治疗神经变性疾病如阿尔茨海默病的方法。

公开(公告)号：WO2004035588A1

公开(公告)日：2004-04-29

申请号：PCT/US2003/032473

申请日：2003-10-14

Applicant: SMITHKLINE BEECHAM CORPORATION ,  DICKERSON, Scott, Howard ,  TAVARES, Francis, Xavier ,  ZHOU, Huiqiang

Inventor： DICKERSON, Scott, Howard ,  TAVARES, Francis, Xavier ,  ZHOU, Huiqiang

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K31/5025

Abstract: The present invention relates generally to inhibitors of the kinases, such as GSK3, and more particularly to fused pyradazine compounds according to formula (I) and methods of their use.

Abstract translation: 本发明一般涉及激酶抑制剂，例如GSK3，更具体地涉及根据式（I）的稠合哒嗪化合物及其使用方法。