公开(公告)号：US08697730B2

公开(公告)日：2014-04-15

申请号：US12257876

申请日：2008-10-24

Applicant: Melissa Virginia Rewolinski ,  Kevin Murray Schaab ,  Christopher David King ,  Nicholas Simon Stock

Inventor： Melissa Virginia Rewolinski ,  Kevin Murray Schaab ,  Christopher David King ,  Nicholas Simon Stock

IPC: A61K31/44 ,  A61K31/405 ,  C07D401/00 ,  C07D209/02

CPC classification number: C07D401/10 ,  C07D401/14

Abstract: Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

Abstract translation: 本文描述的是合成3- [5-（吡啶-2-基甲氧基）-3-（2-甲基-2-丙硫基）-1- [4-（2-甲氧基吡啶-5-基）苄基] - 吲哚-2-基] -2,2-二甲基 - 丙酸，其药学上可接受的盐，药学上可接受的溶剂合物。 还描述了适用于哺乳动物的口服给药的药物组合物，以及使用这些口服药物组合物治疗呼吸道疾病或其它白三烯依赖性或白细胞三烯介导的病症或疾病的方法。

公开(公告)号：US09688624B2

公开(公告)日：2017-06-27

申请号：US13519292

申请日：2011-01-05

Applicant: Jason Edward Brittain ,  Christopher David King ,  Brian Andrew Stearns

Inventor： Jason Edward Brittain ,  Christopher David King ,  Brian Andrew Stearns

IPC: C07C323/41

CPC classification number: C07C323/41 ,  C07B2200/13

Abstract: Described herein is the DP2 antagonist 2-(3-(2-((tert-butylthio)methyl)-4-(2,2-dimethyl-propionylamino)phenoxy)-4-methoxyphenyl)acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.

公开(公告)号：US20090291981A1

公开(公告)日：2009-11-26

申请号：US12471106

申请日：2009-05-22

Applicant: Kevin Murray SCHAAB ,  Christopher David KING ,  Nicholas Simon STOCK

Inventor： Kevin Murray SCHAAB ,  Christopher David KING ,  Nicholas Simon STOCK

IPC: A61K31/444 ,  C07D401/14 ,  A61P11/06

CPC classification number: C07D401/14 ,  A61K31/444

Abstract: Described herein is the FLAP inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, including solvates, and polymorphs thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

Abstract translation: 本文描述的是FLAP抑制剂3- [3-叔丁基硫烷基-1- [4-（6-乙氧基 - 吡啶-3-基） - 苄基] -5-（5-甲基 - 吡啶-2-基甲氧基）-1H - 吲哚-2-基] -2,2-二甲基 - 丙酸或其药学上可接受的盐。 还描述了制备FLAP抑制剂或其药学上可接受的盐，包括溶剂化物及其多晶型物的方法。 本文还描述了适用于向包括FLAP抑制剂或其药学上可接受的盐的哺乳动物施用的药物组合物，以及使用这些药物组合物治疗呼吸道疾病或其它白三烯依赖性或白细胞三烯介导的病症的方法 或疾病。

公开(公告)号：US09556133B2

公开(公告)日：2017-01-31

申请号：US13992022

申请日：2011-12-07

Applicant: Jason Edward Brittain ,  Thomas Jon Seiders ,  Christopher David King ,  Victor W. Rosso

Inventor： Jason Edward Brittain ,  Thomas Jon Seiders ,  Christopher David King ,  Victor W. Rosso

IPC: C07D261/14

CPC classification number: C07D261/14 ,  C07B2200/13

Abstract: Described herein is the LPA1 antagonist 1-{4′-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid (Compound 1), or pharmaceutically acceptable salts thereof. Also described are methods of preparing the LPA1 antagonist, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions suitable for administration to a mammal that include the LPA1 antagonist, or pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating LPA-dependent or LPA-mediated diseases or conditions.

Abstract translation: 本文描述的是LPA1拮抗剂1- {4' - [3-甲基-4 - （（R）-1-苯基 - 乙氧基羰基氨基） - 异恶唑-5-基] - 联苯-4-基} - 环丙烷羧酸（化合物1 ）或其药学上可接受的盐。 还描述了制备LPA1拮抗剂或其药学上可接受的盐的方法，以及适用于给予包括LPA1拮抗剂的哺乳动物或其药学上可接受的盐的药物组合物，以及使用该药物组合物治疗LPA- 依赖或LPA介导的疾病或病症。

公开(公告)号：US08815917B2

公开(公告)日：2014-08-26

申请号：US12846690

申请日：2010-07-29

Applicant: Jason Edward Brittain ,  Brian Andrew Stearns ,  Christopher David King ,  Kevin Ross Holme

Inventor： Jason Edward Brittain ,  Brian Andrew Stearns ,  Christopher David King ,  Kevin Ross Holme

IPC: A61K31/4418 ,  A61K31/195 ,  C07D213/64 ,  C07C229/00

CPC classification number: A61K31/195

Abstract: Described herein is the DP2 antagonist [2′-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4′-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.

Abstract translation: 本文描述的是DP2拮抗剂[2' - （3-苄基-1-乙基 - 脲基甲基）-6-甲氧基-4'-三氟甲基 - 联苯-3-基] - 乙酸或其药学上可接受的盐。 还描述了制备DP2拮抗剂或其药学上可接受的盐的方法。 本文还描述了适用于给予哺乳动物包括DP2拮抗剂或其药学上可接受的盐的药物组合物，以及使用这些药物组合物治疗呼吸系统疾病或病症，过敏性疾病或病症，炎性疾病或病症的方法，如 以及其他前列腺素D2依赖性或前列腺素D2介导的疾病或病症。

公开(公告)号：US20130253023A1

公开(公告)日：2013-09-26

申请号：US13992022

申请日：2011-12-07

Applicant: Jason Edward Brittain ,  Thomas Jon Seiders ,  Christopher David King ,  Victor W. Rosso

Inventor： Jason Edward Brittain ,  Thomas Jon Seiders ,  Christopher David King ,  Victor W. Rosso

IPC: C07D261/14

CPC classification number: C07D261/14 ,  C07B2200/13

Abstract: Described herein is the LPA1 antagonist 1-{4′-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-bi-phenyl-4-yl}-cyclopropanecarboxylic acid (Compound 1), or pharmaceutically acceptable salts thereof. Also described are methods of preparing the LPA1 antagonist, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions suitable for administration to a mammal that include the LPA1 antagonist, or pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating LPA-dependent or LPA-mediated diseases or conditions.

Abstract translation: 本文描述的是LPA1拮抗剂1- {4' - [3-甲基-4 - （（R）-1-苯基 - 乙氧基羰基氨基） - 异恶唑-5-基] - 邻 - 苯基-4-基} - 环丙烷羧酸 化合物1）或其药学上可接受的盐。 还描述了制备LPA1拮抗剂或其药学上可接受的盐的方法，以及适用于给予包括LPA1拮抗剂的哺乳动物或其药学上可接受的盐的药物组合物，以及使用该药物组合物治疗LPA- 依赖或LPA介导的疾病或病症。

公开(公告)号：US20130053444A1

公开(公告)日：2013-02-28

申请号：US13519292

申请日：2011-01-05

Applicant: Jason Edward Brittain ,  Christopher David King ,  Brian Andrew Stearns

Inventor： Jason Edward Brittain ,  Christopher David King ,  Brian Andrew Stearns

IPC: A61K31/196 ,  A61P11/00 ,  A61P29/00 ,  A61P11/02 ,  A61P11/06 ,  A61P37/00 ,  A61P27/02 ,  A61P17/00 ,  C07C321/10 ,  A61P37/08

CPC classification number: C07C323/41 ,  C07B2200/13

Abstract: Described herein is the DP2 anatgonist 2-(3-(2-((tert-butylthio)methyl)-4-(2,2-dimethyl-propionylamino)phenoxy)-4-methoxyphenyl)acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 anatgonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 anatgonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.

Abstract translation: 本文描述的是DP2阴离子表面活性剂2-（3-（2 - （（叔丁硫基）甲基）-4-（2,2-二甲基 - 丙酰基氨基）苯氧基）-4-甲氧基苯基）乙酸或其药学上可接受的盐 。 还描述了制备DP2拮抗剂或其药学上可接受的盐的方法。 本文还描述了适用于给予哺乳动物的药物组合物，其包括DP2拮抗剂或其药学上可接受的盐，以及使用这些药物组合物治疗呼吸系统疾病或病症，过敏性疾病或病症，炎性疾病或病症的方法，如 以及其他前列腺素D2依赖性或前列腺素D2介导的疾病或病症。

公开(公告)号：US20110034558A1

公开(公告)日：2011-02-10

申请号：US12846690

申请日：2010-07-29

Applicant: Jason Edward BRITTAIN ,  Brian Andrew STEARNS ,  Christopher David KING ,  Kevin Ross HOLME

Inventor： Jason Edward BRITTAIN ,  Brian Andrew STEARNS ,  Christopher David KING ,  Kevin Ross HOLME

IPC: A61K31/195 ,  C07C59/135 ,  A61P29/00 ,  A61P37/08 ,  A61P27/02 ,  A61P17/00 ,  A61P11/00

CPC classification number: A61K31/195

Abstract: Described herein is the DP2 antagonist [2′-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4′-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.

Abstract translation: 本文描述的是DP2拮抗剂[2' - （3-苄基-1-乙基 - 脲基甲基）-6-甲氧基-4'-三氟甲基 - 联苯-3-基] - 乙酸或其药学上可接受的盐。 还描述了制备DP2拮抗剂或其药学上可接受的盐的方法。 本文还描述了适用于给予哺乳动物包括DP2拮抗剂或其药学上可接受的盐的药物组合物，以及使用这些药物组合物治疗呼吸系统疾病或病症，过敏性疾病或病症，炎性疾病或病症的方法，如 以及其他前列腺素D2依赖性或前列腺素D2介导的疾病或病症。

公开(公告)号：US20110160249A1

公开(公告)日：2011-06-30

申请号：US12993319

申请日：2009-05-22

Applicant: Kevin Murray Schaab ,  Christopher David King ,  Nicholas Simon Stock

Inventor： Kevin Murray Schaab ,  Christopher David King ,  Nicholas Simon Stock

IPC: A61K31/444 ,  C07D401/14 ,  A61P11/06 ,  A61P11/00 ,  A61P9/00

CPC classification number: C07D401/14 ,  A61K31/444

Abstract: A pharmaceutically acceptable salt comprising 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionate as the anion and a cation selected from Na+, K+, Li+, Ca2+, NH4+, the protonated form of dicyclohexylamine, the protonated form of N-methyl-D-glucamine, the protonated form of tris(hydroxymethyl)methylamine, the protonated form of arginine, and the protonated form of lysine is disclosed, along with formulations and methods of using the same.

Abstract translation: 包含3- [3-叔丁基硫烷基-1- [4-（6-乙氧基 - 吡啶-3-基） - 苄基] -5-（5-甲基 - 吡啶-2-基甲氧基） 吲哚-2-基] -2,2-二甲基 - 丙酸酯和选自Na +，K +，Li +，Ca 2+，NH 4 +，质子化形式的二环己基胺，质子化形式的N-甲基-D-葡萄糖胺， 公开了三（羟甲基）甲胺的质子化形式，精氨酸的质子化形式和赖氨酸的质子化形式，以及使用它们的制剂和方法。

公开(公告)号：US20100075934A1

公开(公告)日：2010-03-25

申请号：US12257876

申请日：2008-10-24

Applicant: Melissa Virginia REWOLINSKI ,  Kevin Murray SCHAAB ,  Christopher David KING ,  Jillian F. EVANS ,  Petpiboon Peppi PRASIT ,  John Howard HUTCHINSON ,  Nicholas Simon STOCK

Inventor： Melissa Virginia REWOLINSKI ,  Kevin Murray SCHAAB ,  Christopher David KING ,  Jillian F. EVANS ,  Petpiboon Peppi PRASIT ,  John Howard HUTCHINSON ,  Nicholas Simon STOCK

IPC: A61K31/444 ,  A61K31/56 ,  C07D401/14 ,  A61P11/00

CPC classification number: C07D401/10 ,  C07D401/14

Abstract: Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

Abstract translation: 本文描述的是合成3- [5-（吡啶-2-基甲氧基）-3-（2-甲基-2-丙硫基）-1- [4-（2-甲氧基吡啶-5-基）苄基] - 吲哚-2-基] -2,2-二甲基 - 丙酸，其药学上可接受的盐，药学上可接受的溶剂合物。 还描述了适用于哺乳动物的口服给药的药物组合物，以及使用这些口服药物组合物治疗呼吸道疾病或其它白三烯依赖性或白细胞三烯介导的病症或疾病的方法。