公开(公告)号：US20130109705A1

公开(公告)日：2013-05-02

申请号：US13699077

申请日：2011-05-19

Applicant: Tona M. Gilmer ,  Rakesh Kumar

Inventor： Tona M. Gilmer ,  Rakesh Kumar

IPC: A61K31/519 ,  A61K31/517

CPC classification number: A61K31/519 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4858 ,  A61K31/517 ,  A61K2300/00

Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.

Abstract translation: 本发明涉及一种治疗人类癌症的方法和用于治疗的药物组合物。 特别地，该方法涉及一种癌症治疗方法，其包括给予N- {3-氯-4 - [（3-氟苄基）氧基]苯基} -6- [5 - （{[2-（甲磺酰基）乙基]氨基 }甲基）-2-呋喃基] -4-喹唑啉胺或其药学上可接受的水合物和/或盐和N- {3- [3-环丙基-5-（2-氟-4-碘 - 苯基氨基） -2,4,7-三氧代-3,4,6,7-四氢-2H-吡啶并[4,3-d]嘧啶-1-基]苯基}乙酰胺或其药学上可接受的盐或溶剂化物 对有需要的人。

公开(公告)号：US20090274693A1

公开(公告)日：2009-11-05

申请号：US12435473

申请日：2009-05-05

Applicant: Tona M. Gilmer ,  James G. Greger, JR. ,  Li Liu ,  Hong Shi

Inventor： Tona M. Gilmer ,  James G. Greger, JR. ,  Li Liu ,  Hong Shi

IPC: A61K31/5377 ,  A61K31/47 ,  A61K39/395 ,  A61P35/04

CPC classification number: A61K31/5377 ,  A61K31/47 ,  A61K31/517 ,  A61K39/39558 ,  C07K16/32 ,  C07K2317/24 ,  C07K2317/73 ,  A61K2300/00

Abstract: The present invention relates to a method of treating cancer in a patient comprising administering to the patient therapeutically effective amounts of:a) a compound of formula A: or a pharmaceutically acceptable salt thereof, wherein R1-R4, p, and q are as defined; and(b) an erbB inhibitor that inhibits erbB-1 or erbB-2 or erbB-3 receptor or a combination thereof. The method of the present invention addresses a need in the art with the discovery of a combination therapy that shows evidence of being a more effective therapy than previously disclosed therapies.

Abstract translation: 本发明涉及一种治疗患者的癌症的方法，包括向患者施用治疗有效量的：a）式A化合物或其药学上可接受的盐，其中R 1 -R 4，p和q如上所定义 ; 和（b）抑制erbB-1或erbB-2或erbB-3受体的erbB抑制剂或其组合。 本发明的方法解决了本领域的需要，发现了组合疗法，该组合治疗显示出比先前公开的疗法更有效的治疗的证据。

公开(公告)号：US09180129B2

公开(公告)日：2015-11-10

申请号：US13699077

申请日：2011-05-19

Applicant: Tona M. Gilmer ,  Rakesh Kumar

Inventor： Tona M. Gilmer ,  Rakesh Kumar

IPC: A61K31/519 ,  A61K31/517 ,  A01N43/90 ,  A01N43/54 ,  A61K9/20 ,  A61K9/48

CPC classification number: A61K31/519 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4858 ,  A61K31/517 ,  A61K2300/00

Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.

Abstract translation: 本发明涉及一种治疗人类癌症的方法和用于治疗的药物组合物。 特别地，该方法涉及一种癌症治疗方法，其包括给予N- {3-氯-4 - [（3-氟苄基）氧基]苯基} -6- [5 - （{[2-（甲磺酰基）乙基]氨基 }甲基）-2-呋喃基] -4-喹唑啉胺或其药学上可接受的水合物和/或盐和N- {3- [3-环丙基-5-（2-氟-4-碘 - 苯基氨基） -2,4,7-三氧代-3,4,6,7-四氢-2H-吡啶并[4,3-d]嘧啶-1-基]苯基}乙酰胺或其药学上可接受的盐或溶剂化物 对有需要的人。

公开(公告)号：US20130231347A1

公开(公告)日：2013-09-05

申请号：US13988116

申请日：2011-11-18

Applicant: Maureen Bleam ,  Tona M. Gilmer ,  James G. Greger ,  Sylvie G. Laquerre ,  Li Liu

Inventor： Maureen Bleam ,  Tona M. Gilmer ,  James G. Greger ,  Sylvie G. Laquerre ,  Li Liu

IPC: A61K31/519 ,  A61K45/06 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506

CPC classification number: A61K31/519 ,  A61K31/437 ,  A61K31/44 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D417/14 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/156 ,  A61K2300/00

Abstract: The disclosure is directed to a method of treating humans suffering from V600 mutant melanoma that incorporates the detection of the presence or absence of at least one mutation in at least one NRAS protein and/or at least one MEK1 protein, or a gene encoding said protein, and subsequently initiating treatment, modifying treatment, or discontinuing treatment with a chemo-therapeutic agent selected from a BRaf inhibitor or other suitable agent based upon the presence or absence of said mutation.

Abstract translation: 本公开涉及一种治疗患有V600突变黑素瘤的人的方法，该方法包括检测至少一种NRAS蛋白和/或至少一种MEK1蛋白中至少一个突变的存在或不存在，或编码所述蛋白的基因 并且随后基于所述突变的存在或不存在，用选自BRaf抑制剂或其它合适的试剂的化学治疗剂开始治疗，改变治疗或停止治疗。

公开(公告)号：US20130165456A1

公开(公告)日：2013-06-27

申请号：US13819091

申请日：2011-08-24

Applicant: Tona M. Gilmer ,  Rakesh Kumar ,  Li Liu

Inventor： Tona M. Gilmer ,  Rakesh Kumar ,  Li Liu

IPC: A61K31/519 ,  A61K31/506

CPC classification number: A61K31/519 ,  A61K9/20 ,  A61K9/2054 ,  A61K9/4858 ,  A61K31/506 ,  A61K2300/00

Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.

Abstract translation: 本发明涉及一种治疗人类癌症的方法和用于治疗的药物组合物。 特别地，该方法涉及一种包括给予5 - [[4 - [（2,3-二甲基-2H-吲唑-6-基）甲基氨基] -2-嘧啶基]氨基] -2-甲基苯磺酰胺的癌症治疗方法， 或其药学上可接受的盐和N- {3- [3-环丙基-5-（2-氟-4-碘 - 苯基氨基）6,8-二甲基; -2,4,7-三氧代-3,4,6,7-四氢-2H-吡啶并[4,3-d]嘧啶-1-基]苯基}乙酰胺或其药学上可接受的盐或溶剂化物 有需要的人。

公开(公告)号：US20120035183A1

公开(公告)日：2012-02-09

申请号：US12921793

申请日：2009-03-16

Applicant: Tona M. Gilmer ,  Li Liu ,  James Greger

Inventor： Tona M. Gilmer ,  Li Liu ,  James Greger

IPC: A61K31/517 ,  A61P35/00

CPC classification number: A61K31/519 ,  A61K31/506 ,  A61K2300/00

Abstract: The present invention relates to a method of treating cancer in a mammal by administration of 4-quinazolinamines and at least one additional anti-neoplastic compound. In particular, the method relates to a methods of treating cancers by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof in combination with at least one additional anti-neoplastic compound.

Abstract translation: 本发明涉及通过施用4-喹唑啉胺和至少一种另外的抗肿瘤化合物来治疗哺乳动物的癌症的方法。 特别地，该方法涉及通过给予N- {3-氯-4 - [（3-氟苄基）氧基]苯基} -6- [5 - （{[2-（甲磺酰基）乙基] 氨基}甲基）-2-呋喃基] -4-喹唑啉胺及其盐和溶剂化物与至少一种另外的抗肿瘤化合物的组合。

公开(公告)号：US20130231346A1

公开(公告)日：2013-09-05

申请号：US13988054

申请日：2011-11-17

Applicant: Tona M. Gilmer ,  Peter F. Lebowitz ,  Li Liu ,  Jolly Mazumdar

Inventor： Tona M. Gilmer ,  Peter F. Lebowitz ,  Li Liu ,  Jolly Mazumdar

IPC: A61K31/519 ,  A61K31/415 ,  A61K45/06 ,  A61K31/501 ,  A61K31/439

CPC classification number: A61K31/519 ,  A61K31/415 ,  A61K31/436 ,  A61K31/439 ,  A61K31/501 ,  A61K45/06 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/156 ,  A61K2300/00

Abstract: Methods for treating a human with cancer comprise administering a therapeutically effective amount of at least one MEK inhibitor and at least one mTOR inhibitor to said patient, wherein said patient has at least one mutation in at least one Ras protein or gene encoding at least one Ras protein and/or wherein said patient has at least one mutation, deletion or insertion in LKB1/STK11.

Abstract translation: 用癌症治疗人的方法包括向所述患者施用治疗有效量的至少一种MEK抑制剂和至少一种mTOR抑制剂，其中所述患者在至少一种Ras蛋白或编码至少一种Ras的基因中具有至少一个突变 蛋白质和/或其中所述患者在LKB1 / STK11中具有至少一个突变，缺失或插入。

公开(公告)号：US20130072507A1

公开(公告)日：2013-03-21

申请号：US13698847

申请日：2011-05-19

Applicant: Tona M. Gilmer ,  Rakesh Kumar

Inventor： Tona M. Gilmer ,  Rakesh Kumar

IPC: A61K31/517 ,  A61P35/02 ,  A61P35/00

CPC classification number: A61K31/517 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4858 ,  A61K31/4155 ,  A61K31/4375 ,  A61K2300/00

Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.

公开(公告)号：US20100010022A1

公开(公告)日：2010-01-14

申请号：US12536302

申请日：2009-08-05

Applicant: Rakesh KUMAR ,  Robert John MULLIN ,  Tona M. GILMER

Inventor： Rakesh KUMAR ,  Robert John MULLIN ,  Tona M. GILMER

IPC: A61K31/517 ,  A61K31/506 ,  A61P35/00

CPC classification number: A61K31/485 ,  A61K31/395 ,  A61K31/517 ,  A61K31/519 ,  A61K2300/00

Abstract: A method of treating cancer is described including administration of a pyrimidine derivative and a quinazoline derivative as well as a pharmaceutical composition including the same.

Abstract translation: 描述了治疗癌症的方法，包括施用嘧啶衍生物和喹唑啉衍生物以及包含其的药物组合物。

公开(公告)号：US20130137701A1

公开(公告)日：2013-05-30

申请号：US13814799

申请日：2011-08-09

Applicant: Tona M. Gilmer ,  James G. Greger, JR. ,  Li Liu

Inventor： Tona M. Gilmer ,  James G. Greger, JR. ,  Li Liu

IPC: A61K31/517 ,  A61K31/501

CPC classification number: A61K31/517 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4858 ,  A61K31/501 ,  A61K2300/00

Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.

Abstract translation: 本发明涉及一种治疗人类癌症的方法和用于治疗的药物组合物。 特别地，该方法涉及一种癌症治疗方法，其包括给予N- {3-氯-4 - [（3-氟苄基）氧基]苯基} -6- [5 - （{[2-（甲磺酰基）乙基]氨基 }甲基）-2-呋喃基] -4-喹唑啉胺或其药学上可接受的水合物和/或盐，和2,4-二氟-N- {2-（甲氧基）-5- [4-（4-哒嗪基） -6-喹啉基] -3-吡啶基}苯磺酰胺或其药学上可接受的盐。