公开(公告)号：US09758538B2

公开(公告)日：2017-09-12

申请号：US15209574

申请日：2016-07-13

Applicant: PFIZER INC.

Inventor： Ping Chen ,  Hengmiao Cheng ,  Gary Michael Gallego ,  Mehran Jalaie ,  John Charles Kath ,  Suvi Tuula Marjukka Orr ,  Mason Alan Pairish

IPC: C07F9/6558 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14 ,  C07D405/14 ,  A61K31/5377 ,  C07D401/04 ,  C07D403/04

CPC classification number: C07F9/65583 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1-R11, m, n, and p are defined herein. The novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

公开(公告)号：US08680111B2

公开(公告)日：2014-03-25

申请号：US13786106

申请日：2013-03-05

Applicant: Pfizer Inc.

Inventor： Simon Bailey ,  Benjamin Joseph Burke ,  Michael Raymond Collins ,  Jingrong Jean Cui ,  Judith Gail Deal ,  Robert Louis Hoffman ,  Qinhua Huang ,  Ted William Johnson ,  Robert Steven Kania ,  John Charles Kath ,  Phuong Thi Quy Le ,  Michele Ann McTigue ,  Cynthia Louise Palmer ,  Paul Francis Richardson ,  Neal William Sach

IPC: A01N43/42 ,  A61K31/44 ,  A01N43/02 ,  A61K31/335 ,  C07D471/00 ,  C07D491/00 ,  C07D498/00 ,  C07D513/00 ,  C07D515/00 ,  C07D313/00

CPC classification number: C07D498/08 ,  C07D273/02 ,  C07D413/04 ,  C07D413/14 ,  C07D491/08 ,  C07D491/18 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18

Abstract: The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.

Abstract translation: 本发明涉及本文进一步定义的式（Φ）化合物及其药学上可接受的盐，涉及包含这些化合物和盐的药物组合物及其用途。 本发明的化合物和盐抑制间变性淋巴瘤激酶（ALK）和/或EML4-ALK，并且可用于治疗或改善异常细胞增殖性疾病如癌症。

公开(公告)号：US20150141402A1

公开(公告)日：2015-05-21

申请号：US14548749

申请日：2014-11-20

Applicant: PFIZER INC.

Inventor： Douglas Carl Behenna ,  Hengmiao Cheng ,  Sujin Cho-Schultz ,  Theodore Otto Johnson, JR. ,  John Charles Kath ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Simon Paul Planken

IPC: C07D473/16

CPC classification number: C07D473/16 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/5386 ,  C07D473/18 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, G, ring A, ring B, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, and m are defined herein. The novel purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中Q，G，环A，环B，R1，R2，R3，R4，R5，R5a，R6，R7，R8，R9， R 11，R 12，R 13，R 14，R 15，R 16，R 17，R 18，R 19，R 20，R 21，R 22，R 23，R 24和m如本文所定义。 新型嘌呤衍生物可用于治疗哺乳动物中异常细胞生长，如癌症。 另外的实施方案涉及含有化合物的药物组合物和使用化合物和组合物治疗哺乳动物异常细胞生长的方法。

公开(公告)号：US09260439B2

公开(公告)日：2016-02-16

申请号：US14677112

申请日：2015-04-02

Applicant: PFIZER INC.

Inventor： Ping Chen ,  Hengmiao Cheng ,  Judith Gail Deal ,  Gary Michael Gallego ,  Mehran Jalaie ,  John Charles Kath ,  Suvi Tuula Marjukka Orr ,  Hong Shen ,  Luke Raymond Zehnder

IPC: A61K31/5377 ,  C07D487/04 ,  C07F9/6561 ,  A61K45/06 ,  A61N5/10

CPC classification number: C07D487/04 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  C07F9/65616

Abstract: The present invention relates to compounds of formula (X) or pharmaceutically acceptable salts thereof, wherein R1-R50, a, b, d, e, f, g, h, i, j, k, l, o, p, q, r, s, t, u, y, and z are defined herein. The novel dihydropyrrolopyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Abstract translation: 本发明涉及式（X）化合物或其药学上可接受的盐，其中R 1 -R 50，a，b，d，e，f，g，h，i，j，k，l，o，p，q， r，s，t，u，y和z在本文中定义。 新型二氢吡咯并嘧啶衍生物可用于治疗哺乳动物中异常细胞生长，如癌症。 另外的实施方案涉及含有化合物的药物组合物和使用化合物和组合物治疗哺乳动物异常细胞生长的方法。

公开(公告)号：US20140135339A1

公开(公告)日：2014-05-15

申请号：US14156144

申请日：2014-01-15

Applicant: PFIZER INC.

Inventor： Simon Bailey ,  Benjamin Joseph Burke ,  Michael Raymond Collins ,  Jingrong Jean Cui ,  Judith Gail Deal ,  Robert Louis Hoffman ,  Qinhua Huang ,  Ted William Johnson ,  Robert Steven Kania ,  John Charles Kath ,  Phuong Thi Quy Le ,  Michele Ann McTigue ,  Cynthia Louise Palmer ,  Paul Francis Richardson ,  Neal William Sach

IPC: C07D498/18 ,  C07D498/22

CPC classification number: C07D498/08 ,  C07D273/02 ,  C07D413/04 ,  C07D413/14 ,  C07D491/08 ,  C07D491/18 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18

Abstract: The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.

Abstract translation: 本发明涉及本文进一步定义的式（Φ）化合物及其药学上可接受的盐，涉及包含这些化合物和盐的药物组合物及其用途。 本发明的化合物和盐抑制间变性淋巴瘤激酶（ALK）和/或EML4-ALK，并且可用于治疗或改善异常细胞增殖性疾病如癌症。

公开(公告)号：US09290496B2

公开(公告)日：2016-03-22

申请号：US14548749

申请日：2014-11-20

Applicant: PFIZER INC.

Inventor： Douglas Carl Behenna ,  Hengmiao Cheng ,  Sujin Cho-Schultz ,  Theodore Otto Johnson, Jr. ,  John Charles Kath ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Simon Paul Planken

IPC: A61K31/519 ,  C07D473/18 ,  A61P35/00 ,  A61K31/5377 ,  C07D498/10 ,  A61K31/5386 ,  C07D487/04 ,  A61K31/52 ,  C07D473/16 ,  C07D519/00

CPC classification number: C07D473/16 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/5386 ,  C07D473/18 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, G, ring A, ring B, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, and m are defined herein. The novel purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中Q，G，环A，环B，R1，R2，R3，R4，R5，R5a，R6，R7，R8，R9， R 11，R 12，R 13，R 14，R 15，R 16，R 17，R 18，R 19，R 20，R 21，R 22，R 23，R 24和m如本文所定义。 新型嘌呤衍生物可用于治疗哺乳动物中异常细胞生长，如癌症。 另外的实施方案涉及含有化合物的药物组合物和使用化合物和组合物治疗哺乳动物异常细胞生长的方法。

公开(公告)号：US09133215B2

公开(公告)日：2015-09-15

申请号：US14156144

申请日：2014-01-15

Applicant: PFIZER INC.

Inventor： Simon Bailey ,  Benjamin Joseph Burke ,  Michael Raymond Collins ,  Jingrong Jean Cui ,  Judith Gail Deal ,  Robert Louis Hoffman ,  Qinhua Huang ,  Ted William Johnson ,  Robert Steven Kania ,  John Charles Kath ,  Phuong Thi Quy Le ,  Michele Ann McTigue ,  Cynthia Louise Palmer ,  Paul Francis Richardson ,  Neal William Sach

IPC: C07D273/02 ,  C07D413/04 ,  C07D413/14 ,  C07D491/08 ,  C07D491/18 ,  C07D498/08 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18

CPC classification number: C07D498/08 ,  C07D273/02 ,  C07D413/04 ,  C07D413/14 ,  C07D491/08 ,  C07D491/18 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18

Abstract: The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.

Abstract translation: 本发明涉及本文进一步定义的式（Φ）化合物及其药学上可接受的盐，涉及包含这些化合物和盐的药物组合物及其用途。 本发明的化合物和盐抑制间变性淋巴瘤激酶（ALK）和/或EML4-ALK，并且可用于治疗或改善异常细胞增殖性疾病如癌症。

公开(公告)号：US20130252961A1

公开(公告)日：2013-09-26

申请号：US13786106

申请日：2013-03-05

Applicant: PFIZER INC.

Inventor： Simon BAILEY ,  Benjamin Joseph Burke ,  Michael Raymond Collins ,  Jingrong Jean Cui ,  Judith Gail Deal ,  Robert Louis Hoffman ,  Qinhua Huang ,  Ted William Johnson ,  Robert Steven Kania ,  John Charles Kath ,  Phuong Thi Quy Le ,  Michele Ann McTigue ,  Cynthia Louise Palmer ,  Paul Francis Richardson ,  Neal William Sach

IPC: C07D498/08 ,  C07D513/18 ,  C07D498/22 ,  C07D498/18 ,  C07D491/18

CPC classification number: C07D498/08 ,  C07D273/02 ,  C07D413/04 ,  C07D413/14 ,  C07D491/08 ,  C07D491/18 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18

Abstract: The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.

Abstract translation: 本发明涉及本文进一步定义的式（Phi）化合物及其药学上可接受的盐，涉及包含这些化合物和盐的药物组合物及其用途。 本发明的化合物和盐抑制间变性淋巴瘤激酶（ALK）和/或EML4-ALK，并且可用于治疗或改善异常细胞增殖性疾病如癌症。

公开(公告)号：US20170015689A1

公开(公告)日：2017-01-19

申请号：US15209574

申请日：2016-07-13

Applicant: PFIZER INC.

Inventor： Ping Chen ,  Hengmiao CHENG ,  Gary Michael Gallego ,  Mehran Jalaie ,  John Charles Kath ,  Suvi Tuula Marjukka Orr ,  Mason Alan PAIRISH

IPC: C07F9/6558 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14

CPC classification number: C07F9/65583 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1-R11, m, n, and p are defined herein. The novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Abstract translation: 或其药学上可接受的盐，其中X，Y，Z，R 1 -R 11，m，n和p在本文中定义。 新型嘧啶衍生物可用于治疗哺乳动物中异常细胞生长，如癌症。 另外的实施方案涉及含有化合物的药物组合物和使用化合物和组合物治疗哺乳动物异常细胞生长的方法。