公开(公告)号：US10751332B2

公开(公告)日：2020-08-25

申请号：US15183504

申请日：2016-06-15

Applicant: Asana Biosciences, LLC

Inventor： Aranapakam M. Venkatesan ,  Scott K. Thompson ,  Roger A. Smith ,  Sanjeeva P. Reddy ,  Raghava Reddy Kethiri ,  Purushottam M. Dewang ,  Gurulingappa Hallur ,  Chandrika Mulakala

IPC: A61K31/443 ,  A61K31/506 ,  C07D401/04 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/444

Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

公开(公告)号：US10471051B2

公开(公告)日：2019-11-12

申请号：US15694124

申请日：2017-09-01

Applicant: Asana Biosciences, LLC

Inventor： Aranapakam M. Venkatesan ,  Scott K. Thompson ,  Roger A. Smith ,  Sanjeeva P. Reddy ,  Raghava Reddy Kethiri ,  Purushottam M. Dewang ,  Gurulingappa Hallur ,  Chandrika Mulakala ,  Ramesh Mullangi ,  Mohd Zainuddin

IPC: A61K31/506 ,  A61K31/443 ,  C07D401/04 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/444

Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

公开(公告)号：US10188654B2

公开(公告)日：2019-01-29

申请号：US15365222

申请日：2016-11-30

Applicant: Asana Biosciences, LLC

Inventor： Sanjeeva P. Reddy ,  Sandeep Gupta ,  Roger Astbury Smith

IPC: A61K31/519 ,  A61K31/551 ,  A61K31/55 ,  A61K31/5377 ,  A61K9/00 ,  A61K31/541 ,  A61K31/675

Abstract: Disclosed are methods of treating cancer, which include administering a therapeutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt or ester thereof, to a subject in need thereof. Also disclosed are methods of inhibiting growth and proliferation of cancer cells in vitro or in vivo, which include contacting the cells with an amount of the compound of formula (I) effective to inhibit the growth or proliferation of the cancer cells. Further disclosed are methods of inhibiting tumor growth, which include contacting the tumor with an amount of the compound of formula (I) effective to inhibit the growth of the tumor.

公开(公告)号：US20190015337A1

公开(公告)日：2019-01-17

申请号：US16035771

申请日：2018-07-16

Applicant: Asana BioSciences, LLC

Inventor： Navnit Shah ,  Harpreet Sandhu ,  Ashish Chatterji ,  Helen Usansky ,  Louis Denis ,  Niranjan Rao ,  Sarper Toker

IPC: A61K9/16 ,  A61K9/50 ,  A61K9/28 ,  A61K9/20 ,  A61K9/48 ,  A61K9/00 ,  C07D471/04

Abstract: Embodiments of the disclosure relate generally to formulations, methods, kits, and dosage forms for improved stability of an active pharmaceutical ingredient, wherein the active ingredient comprises a compound of the formula: wherein X is N, Y is H or optionally substituted C1-C6 alkyl; R4 is morpholine optionally substituted with by C1-C6 alkyl; R7 is C1-C6 alkyl optionally substituted by one or more F; R8′ is halogen; and R6 is wherein R10 is H, C1-C6 alkyl, halogen, CN or CF3; R12 is H or halogen; R13 is H, halogen or C1-C6 alkyl; and R17 is H, C1-C6 alkyl, (C1-C6 alkyl)-NH2; and, pharmaceutically acceptable salts and free bases thereof, wherein the active ingredient remains in substantially amorphous form after storage of the pharmaceutical formulation for a predetermined time and conditions. In one embodiment the formulations, methods, kits and dosage forms comprising the active pharmaceutical ingredient with improved stability can be used in the treatment of a condition characterized by the dysregulation of one of both of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways.

公开(公告)号：US09896445B2

公开(公告)日：2018-02-20

申请号：US15183486

申请日：2016-06-15

Applicant: Asana Biosciences, LLC

Inventor： Aranapakam M. Venkatesan ,  Scott K. Thompson ,  Roger A. Smith ,  Sanjeeva P. Reddy ,  Raghava Reddy Kethiri ,  Purushottam M. Dewang ,  Gurulingappa Hallur ,  Chandrika Mulakala ,  Ramesh Mullangi ,  Mohd Zainuddin

IPC: A61K31/443 ,  C07D401/04 ,  C07D417/14 ,  C07D403/04 ,  A61K31/506 ,  C07D405/14 ,  C07D413/14 ,  A61K31/5377 ,  C07D409/14 ,  C07D403/14 ,  C07C309/30 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/444

CPC classification number: C07D417/14 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  C07C309/30 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

公开(公告)号：US20170290838A1

公开(公告)日：2017-10-12

申请号：US15581330

申请日：2017-04-28

Applicant: Asana BioSciences, LLC

Inventor： Scott K. Thompson ,  Roger A. Smith ,  Sanjeeva Reddy ,  Tyler M. John ,  Vijay Kumar Nyavanandi ,  Hosahalli Subramanya ,  Vijay Potluri ,  Sunil Kumar Panigrahi ,  Prabhakara Rao Nadipalli ,  Saumitra Sengupta

IPC: A61K31/5377

CPC classification number: A61K31/5377 ,  A61K45/06 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D519/00 ,  G01N33/5011 ,  G01N33/57496

Abstract: The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8′ are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

公开(公告)号：US20170157126A1

公开(公告)日：2017-06-08

申请号：US15365222

申请日：2016-11-30

Applicant: Asana Biosciences, LLC

Inventor： Sanjeeva P. Reddy ,  Sandeep Gupta ,  Roger Astbury Smith

IPC: A61K31/519 ,  A61K31/551 ,  A61K31/55 ,  A61K31/5377 ,  A61K9/00

CPC classification number: A61K31/519 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61K31/675

Abstract: Disclosed are methods of treating cancer, which include administering a therapeutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt or ester thereof, to a subject in need thereof. Also disclosed are methods of inhibiting growth and proliferation of cancer cells in vitro or in vivo, which include contacting the cells with an amount of the compound of formula (I) effective to inhibit the growth or proliferation of the cancer cells. Further disclosed are methods of inhibiting tumor growth, which include contacting the tumor with an amount of the compound of formula (I) effective to inhibit the growth of the tumor.

公开(公告)号：US20160362407A1

公开(公告)日：2016-12-15

申请号：US15183504

申请日：2016-06-15

Applicant: Asana Biosciences, LLC

Inventor： Aranapakam M. Venkatesan ,  Scott K. Thompson ,  Roger A. Smith ,  Sanjeeva P. Reddy

IPC: C07D417/14 ,  C07C309/30 ,  A61K31/506 ,  C07D405/14 ,  C07D401/04 ,  C07D413/14 ,  C07D401/14 ,  C07D403/14 ,  A61K31/444 ,  A61K31/5377 ,  C07D409/14 ,  C07D403/04 ,  A61K31/4439

Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

公开(公告)号：US20160296501A1

公开(公告)日：2016-10-13

申请号：US15184800

申请日：2016-06-16

Applicant: Asana Biosciences, LLC

Inventor： Scott K. Thompson ,  Aranapakam Venkatesan ,  Tony Priestley ,  Mrinal Kundu ,  Ashis Saha

IPC: A61K31/437 ,  A61K31/497 ,  A61K31/496 ,  A61K31/506 ,  A61K31/444 ,  A61K31/4545

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  C07D471/22

Abstract: The present application provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R4 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient. In another embodiment, these compounds are useful for treating respiratory dysfunction in patients by administering one or more of the compounds to a patient.

Abstract translation: 本申请提供了用于制备和使用这些化合物的新型化合物和方法。 在一个实施方案中，化合物具有式（I）的结构，其中R 1 -R 4在本文中定义。 在另一个实施方案中，这些化合物可用于调节P2X3或P2X2 / 3受体中的一种或两种的方法。 在另一个实施方案中，这些化合物可用于通过向患者施用一种或多种化合物来治疗患者的疼痛。

公开(公告)号：US09371316B2

公开(公告)日：2016-06-21

申请号：US14461964

申请日：2014-08-18

Applicant: Asana Biosciences, LLC

Inventor： Roger Astbury Smith ,  Nicholas James Laping ,  Aranapakam M. Venkatesan ,  Raghava Reddy Kethiri ,  Chandregowda Venkateshappa ,  Bheemashankar Kulkarni ,  Purushottam Dewang ,  Rajendra Kristam ,  Rajesh Devraj

IPC: A61K31/4439 ,  C07D417/06 ,  C07D401/14 ,  C07D401/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/14 ,  C07D405/14 ,  C07D213/30 ,  C07D213/84

CPC classification number: C07D417/06 ,  C07D213/30 ,  C07D213/84 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D417/04 ,  C07D417/14

Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CYP17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.

Abstract translation: 本申请提供了新颖的吡啶化合物及其药学上可接受的盐或前药。 还提供了制备这些化合物的方法。 通过向患者施用治疗有效量的一种或多种化合物，这些化合物可用于抑制CYP17活性。 通过这样做，这些化合物在治疗与CYP17活性相关的病症中是有效的。 可以使用这些化合物治疗多种病症，并且包括以异常细胞增殖为特征的疾病。 在一个实施方案中，该疾病是癌症，例如前列腺癌。