公开(公告)号：US20170095462A1

公开(公告)日：2017-04-06

申请号：US15387537

申请日：2016-12-21

Applicant: InterMune, Inc.

Inventor： Lawrence M. Blatt ,  Scott D. Seiwert ,  Leonid D. Beigelman ,  Ramachandran Radhakrishnan ,  Karl Kossen ,  Vladimir Serebryany

IPC: A61K31/4412 ,  A61K31/444 ,  A61K31/44

CPC classification number: A61K31/4412 ,  A61K31/44 ,  A61K31/444 ,  A61K31/45 ,  A61K31/4704 ,  A61K31/7052 ,  A61K47/56 ,  A61K47/58 ,  C07D213/16 ,  C07D213/26 ,  C07D213/63 ,  C07D213/64 ,  C07D213/69 ,  C07D215/227 ,  C07H15/26 ,  C07K1/1077 ,  C08F289/00 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/475

Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.

公开(公告)号：US09527816B2

公开(公告)日：2016-12-27

申请号：US14263787

申请日：2014-04-28

Applicant: InterMune, Inc.

Inventor： Lawrence M. Blatt ,  Scott D. Seiwert ,  Leonid D. Beigelman ,  Ramachandran Radhakrishnan ,  Karl Kossen ,  Vladimir Serebryany

IPC: A61K31/44 ,  A61K31/4412 ,  C07D213/26 ,  C07D213/63 ,  C07D213/16 ,  C07D213/64 ,  C07D215/227 ,  A61K31/4704 ,  A61K31/7052 ,  A61K31/45 ,  C07D213/69 ,  C07H15/26

CPC classification number: A61K31/4412 ,  A61K31/44 ,  A61K31/444 ,  A61K31/45 ,  A61K31/4704 ,  A61K31/7052 ,  A61K47/56 ,  A61K47/58 ,  C07D213/16 ,  C07D213/26 ,  C07D213/63 ,  C07D213/64 ,  C07D213/69 ,  C07D215/227 ,  C07H15/26 ,  C07K1/1077 ,  C08F289/00 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/475

Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.

公开(公告)号：US20160022654A1

公开(公告)日：2016-01-28

申请号：US14772241

申请日：2014-03-13

Applicant: INTERMUNE, INC. ,  THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY ,  THE U.S. GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS

Inventor： Mark R. Nicolls ,  Karl Kossen ,  Alan Cohen

IPC: A61K31/4418 ,  A61K45/06

CPC classification number: A61K31/4418 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/4427 ,  A61K45/06

Abstract: The disclosure relates to methods of preserving or improving microvascular integrity in a patient in need thereof comprising administering pirfenidone therapy to the patient.

Abstract translation: 本公开涉及在有需要的患者中保存或改善微血管完整性的方法，包括向患者施用吡非尼酮治疗。

公开(公告)号：US20140235637A1

公开(公告)日：2014-08-21

申请号：US14263822

申请日：2014-04-28

Applicant: InterMune, Inc.

Inventor： Karl Kossen ,  Scott D. Seiwert ,  Vladimir Serebryany ,  Donald Ruhrmund ,  Leonid D. Beigelman ,  Luca Francesco Mario Raveglia ,  Stefania Vallese ,  Ivana Bianchi ,  Tao Hu

IPC: C07D213/64 ,  C07D417/04 ,  C07D409/04 ,  C07D405/04 ,  C07D213/85

CPC classification number: C07D213/63 ,  C07D213/22 ,  C07D213/64 ,  C07D213/69 ,  C07D213/71 ,  C07D213/85 ,  C07D237/14 ,  C07D239/36 ,  C07D239/54 ,  C07D241/18 ,  C07D251/10 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

Abstract translation: 公开了用于治疗炎症和纤维化疾病的化合物和方法，包括用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物表现出低的抑制p38MAPK的能力; 并且其中所述接触以对所述化合物抑制p38MAPK的抑制浓度低的SAPK调节浓度进行。 还公开了吡非尼酮的衍生物和类似物，其可用于调节应激活化蛋白激酶（SAPK）系统。

公开(公告)号：US20140228310A1

公开(公告)日：2014-08-14

申请号：US14263787

申请日：2014-04-28

Applicant: InterMune, Inc.

Inventor： Lawrence M. Blatt ,  Scott D. Seiwert ,  Leonid D. Beigelman ,  Ramachandran Radhakrishnan ,  Karl Kossen ,  Vladimir Serebryany

IPC: C07D213/64 ,  C07D213/69 ,  C07D215/227 ,  C07H15/26

CPC classification number: A61K31/4412 ,  A61K31/44 ,  A61K31/444 ,  A61K31/45 ,  A61K31/4704 ,  A61K31/7052 ,  A61K47/56 ,  A61K47/58 ,  C07D213/16 ,  C07D213/26 ,  C07D213/63 ,  C07D213/64 ,  C07D213/69 ,  C07D215/227 ,  C07H15/26 ,  C07K1/1077 ,  C08F289/00 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/475

Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.

Abstract translation: 公开了用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物表现出低的抑制至少一种p38MAPK的能力; 并且其中所述接触以对所述化合物抑制至少一种p38MAPK的低百分比抑制浓度的SAPK-调节浓度进行。 还公开了吡非尼酮的衍生物。 这些衍生物可以调节应激活化蛋白激酶（SAPK）系统。

公开(公告)号：US09290450B2

公开(公告)日：2016-03-22

申请号：US14263822

申请日：2014-04-28

Applicant: InterMune, Inc.

Inventor： Karl Kossen ,  Scott D. Seiwert ,  Vladimir Serebryany ,  Donald Ruhrmund ,  Leonid D. Beigelman ,  Luca Francesco Mario Raveglia ,  Stefania Vallese ,  Ivana Bianchi ,  Tao Hu

IPC: C07D213/22 ,  C07D241/18 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D213/63 ,  C07D213/64 ,  C07D213/71 ,  C07D237/14 ,  C07D417/14 ,  C07D471/04 ,  C07D213/69 ,  C07D213/85 ,  C07D239/36 ,  C07D239/54 ,  C07D251/10 ,  C07D405/14 ,  C07D409/04 ,  C07D413/14

CPC classification number: C07D213/63 ,  C07D213/22 ,  C07D213/64 ,  C07D213/69 ,  C07D213/71 ,  C07D213/85 ,  C07D237/14 ,  C07D239/36 ,  C07D239/54 ,  C07D241/18 ,  C07D251/10 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

公开(公告)号：US08969347B2

公开(公告)日：2015-03-03

申请号：US13652247

申请日：2012-10-15

Applicant: Intermune, Inc.

Inventor： Karl Kossen ,  Scott D. Seiwert ,  Vladimir Serebryany ,  Donald Ruhrmund ,  Leonid Beigelman ,  Luca Francesco Mario Raveglia ,  Stefania Vallese ,  Ivana Bianchi ,  Tao Hu

IPC: A61K31/44 ,  C07D213/64 ,  C07D401/04 ,  C07D213/63 ,  C07D213/22 ,  C07D213/71 ,  C07D237/14 ,  C07D241/18 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D213/69 ,  C07D213/85 ,  C07D239/36 ,  C07D239/54 ,  C07D251/10 ,  C07D405/14 ,  C07D409/04 ,  C07D413/14

CPC classification number: C07D213/63 ,  C07D213/22 ,  C07D213/64 ,  C07D213/69 ,  C07D213/71 ,  C07D213/85 ,  C07D237/14 ,  C07D239/36 ,  C07D239/54 ,  C07D241/18 ,  C07D251/10 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

Abstract translation: 公开了用于治疗炎症和纤维化疾病的化合物和方法，包括用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物表现出低的抑制p38MAPK的能力; 并且其中所述接触以对所述化合物抑制p38MAPK的抑制浓度低的SAPK调节浓度进行。 还公开了吡非尼酮的衍生物和类似物，其可用于调节应激活化蛋白激酶（SAPK）系统。

公开(公告)号：US20140286929A1

公开(公告)日：2014-09-25

申请号：US14213970

申请日：2014-03-14

Applicant: Intermune, Inc.

Inventor： Karl Kossen ,  Xiaoli Qin ,  Sharlene R. Lim ,  Scott S. Seiwert ,  Donald Ruhrmund

IPC: G01N33/543 ,  A61K38/45 ,  A61K38/46 ,  A61K38/17 ,  A61K38/48

CPC classification number: G01N33/6893 ,  C12Q1/6883 ,  C12Q2600/118 ,  C12Q2600/158 ,  G01N33/6854 ,  G01N2800/12

Abstract: Provided herein are novel biomarkers for the identification, prediction or monitoring of fibrotic pulmonary diseases (e.g. idiopathic pulmonary fibrosis (IPF)). The biomarkers provided herein may further be used for therapeutic treatment of IPF.

Abstract translation: 本文提供了用于鉴定，预测或监测纤维化性肺疾病（例如特发性肺纤维化（IPF））的新型生物标志物。 本文提供的生物标志物可进一步用于IPF的治疗性治疗。

公开(公告)号：US10010536B2

公开(公告)日：2018-07-03

申请号：US15387537

申请日：2016-12-21

Applicant: InterMune, Inc.

Inventor： Lawrence M. Blatt ,  Scott D. Seiwert ,  Leonid D. Beigelman ,  Ramachandran Radhakrishnan ,  Karl Kossen ,  Vladimir Serebryany

IPC: A61K31/4412 ,  A61K31/44 ,  A61K31/444

CPC classification number: A61K31/4412 ,  A61K31/44 ,  A61K31/444 ,  A61K31/45 ,  A61K31/4704 ,  A61K31/7052 ,  A61K47/56 ,  A61K47/58 ,  C07D213/16 ,  C07D213/26 ,  C07D213/63 ,  C07D213/64 ,  C07D213/69 ,  C07D215/227 ,  C07H15/26 ,  C07K1/1077 ,  C08F289/00 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/475

Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.

公开(公告)号：US20170314074A1

公开(公告)日：2017-11-02

申请号：US15351719

申请日：2016-11-15

Applicant: Intermune, Inc.

Inventor： Karl Kossen ,  Sharlene R. Lim ,  Scott D. Seiwert ,  Donald Ruhrmund

IPC: C12Q1/68

CPC classification number: C12Q1/6883 ,  A61K31/7088 ,  A61K45/06 ,  C12Q2600/118 ,  C12Q2600/158 ,  G16B99/00 ,  Y02A50/411 ,  Y02A90/24 ,  Y02A90/26

Abstract: Provided herein are, inter alia, methods and biomarkers to determine if a patient has or is at risk for developing an LPA-associated disease, to indicate the progressiveness of the disease, and/or to facilitate evaluation of responsiveness to therapy. Compositions and kits including the biomarker proteins and biomarker RNAs provided herein are further provided.