公开(公告)号：US09993470B2

公开(公告)日：2018-06-12

申请号：US15627238

申请日：2017-06-19

Applicant: AERIE PHARMACEUTICALS, INC.

Inventor： Casey Kopczynski ,  Cheng-Wen Lin ,  Jill Marie Sturdivant ,  Mitchell A. deLong

IPC: A61K31/472 ,  A61K47/48 ,  C07D409/12 ,  C07D217/22 ,  A61K31/557 ,  A61K9/00 ,  A61K9/08 ,  A61K31/559 ,  A61K31/5575 ,  A61K31/4725

CPC classification number: A61K31/472 ,  A61K9/0048 ,  A61K9/08 ,  A61K31/4725 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/559 ,  A61K47/54 ,  A61K47/55 ,  C07D217/22 ,  C07D409/12 ,  A61K2300/00

Abstract: Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.

公开(公告)号：US09981041B2

公开(公告)日：2018-05-29

申请号：US15244617

申请日：2016-08-23

Applicant: Ira Jason Salzman

Inventor： Ira Jason Salzman

IPC: A61K47/38 ,  A61K31/7036 ,  A61M11/00 ,  A61F9/00 ,  A61K38/13 ,  A61K31/4725 ,  A61D7/00 ,  A61K31/56 ,  A61K9/12 ,  A61K47/06 ,  A61K9/00

CPC classification number: A61K47/38 ,  A61D7/00 ,  A61K9/0048 ,  A61K9/12 ,  A61K31/4725 ,  A61K31/56 ,  A61K31/7036 ,  A61K38/13

Abstract: An ophthalmic composition for administration as a spray to the eye is provided. The ophthalmic composition comprises a lubricant comprising hydroxypropyl methylcellulose (HPMC), mineral oil, and sterile water. The ophthalmic composition is also configured as a delivery vehicle for administration of ophthalmic pharmaceuticals to the eye. A method of treating keratoconjunctivitis sicca by administering the ophthalmic composition is also provided.

公开(公告)号：US09968630B2

公开(公告)日：2018-05-15

申请号：US15254312

申请日：2016-09-01

Applicant: Turun yliopisto

Inventor： Jukka Westermarck ,  Anna Cvrljevic

IPC: C07H21/02 ,  A61K31/713 ,  A61K31/436 ,  A61K31/337 ,  A61K31/404 ,  A61K31/4188 ,  A61K31/517 ,  A61K31/553 ,  A61K45/06 ,  A61K31/15 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/7068 ,  A61K33/24 ,  A61K38/00 ,  A61K31/00 ,  A61K31/09 ,  A61K31/165 ,  A61K31/166 ,  A61K31/245 ,  A61K31/282 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/4406 ,  A61K31/444 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/498 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/551 ,  A61K31/7105 ,  A61K31/7088 ,  C12N15/113 ,  C12Q1/68 ,  G01N33/574 ,  A61K31/502

CPC classification number: A61K31/713 ,  A61K31/00 ,  A61K31/09 ,  A61K31/15 ,  A61K31/165 ,  A61K31/166 ,  A61K31/245 ,  A61K31/282 ,  A61K31/337 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/436 ,  A61K31/4406 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/498 ,  A61K31/502 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/7068 ,  A61K31/7088 ,  A61K31/7105 ,  A61K33/24 ,  A61K38/00 ,  A61K45/06 ,  C12N15/113 ,  C12N2310/14 ,  C12N2320/30 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N33/57496 ,  G01N2333/4704 ,  G01N2333/4748 ,  A61K2300/00

Abstract: The invention is based on a finding that silencing CIP2A (KIAA1524) gene sensitizes cancer cells for apoptosis-inducing activity of certain small molecule chemotherapeutic agents. Thus, the invention is directed to a respective combination therapy, sensitization method and pharmaceutical compositions. The invention further relates to a method of selecting cancer therapy for a subject on the basis of CIP2A and p53 expression and/or protein activity in a sample obtained from said subject.

公开(公告)号：US09944666B2

公开(公告)日：2018-04-17

申请号：US15368454

申请日：2016-12-02

Applicant: BIOGEN MA INC.

Inventor： Kevin M. Guckian ,  Gnanasambandam Kumaravel ,  Bin Ma ,  Sha Mi ,  Hairuo Peng ,  Zhaohui Shao ,  Lihong Sun ,  Arthur G. Taveras ,  Zhili Xin ,  Lei Zhang

IPC: C07D401/04 ,  C07D215/38 ,  C07D217/12 ,  A61K31/47 ,  C07F7/08 ,  A61K45/06 ,  C07C229/50 ,  A61K31/196 ,  C07D215/12 ,  A61K31/4545 ,  A61K31/506 ,  C07D295/096 ,  A61K31/495 ,  C07D213/74 ,  A61K31/496 ,  A61K31/551 ,  C07D239/42 ,  C07D241/20 ,  A61K31/497 ,  C07D211/14 ,  A61K31/451 ,  C07D205/04 ,  A61K31/397 ,  C07D401/06 ,  A61K31/4709 ,  C07D491/107 ,  C07D209/52 ,  A61K31/403 ,  C07D451/02 ,  A61K31/439 ,  A61K31/695 ,  C07C233/60 ,  C07D451/14

CPC classification number: C07F7/081 ,  A61K31/195 ,  A61K31/196 ,  A61K31/397 ,  A61K31/403 ,  A61K31/41 ,  A61K31/439 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/695 ,  A61K45/06 ,  C07C211/38 ,  C07C217/58 ,  C07C229/46 ,  C07C229/50 ,  C07C233/60 ,  C07C233/61 ,  C07C235/66 ,  C07C2102/10 ,  C07C2102/42 ,  C07C2102/44 ,  C07C2102/50 ,  C07C2103/62 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2602/46 ,  C07C2602/50 ,  C07C2603/62 ,  C07C2603/74 ,  C07D205/04 ,  C07D209/52 ,  C07D211/14 ,  C07D213/74 ,  C07D215/12 ,  C07D215/20 ,  C07D215/38 ,  C07D217/22 ,  C07D239/42 ,  C07D241/20 ,  C07D295/096 ,  C07D401/04 ,  C07D401/06 ,  C07D451/02 ,  C07D451/14 ,  C07D471/08 ,  C07D491/107 ,  C07F7/0805 ,  A61K2300/00

Abstract: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

公开(公告)号：US09944620B2

公开(公告)日：2018-04-17

申请号：US14906330

申请日：2014-07-22

Applicant: LES LABORATOIRES SERVIER ,  VERNALIS (R&D) LTD

Inventor： Arnaud Le Tiran ,  Thierry Le Diguarher ,  Jéròme-Benoît Starck ,  Jean-Michel Henlin ,  Guillaume De Nanteuil ,  Olivier Geneste ,  James Edward Paul Davidson ,  James Brooke Murray ,  I-Jen Chen

IPC: C07D401/14 ,  C07D471/04 ,  A61K31/4985 ,  C07D487/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/4725 ,  A61K31/475 ,  A61K31/5377 ,  A61K9/20 ,  A61K31/4709 ,  A61N5/10

CPC classification number: C07D401/14 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/475 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K2300/00

Abstract: Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

公开(公告)号：US09931336B2

公开(公告)日：2018-04-03

申请号：US15236625

申请日：2016-08-15

Applicant: AERIE PHARMACEUTICALS, INC.

Inventor： Casey Kopczynski ,  Cheng-Wen Lin ,  Jill Marie Sturdivant ,  Mitchell A. deLong

IPC: A61K31/472 ,  A61K31/4725 ,  C07D409/12 ,  C07D217/22 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/559 ,  A61K9/00 ,  A61K9/08 ,  A61K47/48

CPC classification number: A61K31/472 ,  A61K9/0048 ,  A61K9/08 ,  A61K31/4725 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/559 ,  A61K47/54 ,  A61K47/55 ,  C07D217/22 ,  C07D409/12 ,  A61K2300/00

Abstract: Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.

公开(公告)号：US20180086756A1

公开(公告)日：2018-03-29

申请号：US15692811

申请日：2017-08-31

Applicant: CHEMOCENTRYX, INC.

Inventor： Junfa FAN ,  Jaroslaw KALISIAK ,  Rebecca M. LUI ,  Venkat Reddy MALI ,  Jeffrey P. McMAHON ,  Jay P. POWERS ,  Hiroko TANAKA ,  Yibin ZENG ,  Penglie ZHANG

IPC: C07D471/04 ,  A61K31/4725 ,  C07D405/14 ,  A61K31/536 ,  C07D413/14 ,  A61K31/453 ,  C07D405/04 ,  A61K31/4545 ,  A61K31/496

CPC classification number: C07D471/04 ,  A61K31/453 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/536 ,  A61K45/06 ,  A61P35/00 ,  A61P37/00 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14

Abstract: Compounds are provided that are modulators of the CCR2 receptor. The compounds have the general formula (I): and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of CCR2 receptors.

公开(公告)号：US20180085348A1

公开(公告)日：2018-03-29

申请号：US15701122

申请日：2017-09-11

Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

Inventor： Hongwu Chen ,  June X. Zou ,  Junjian Wang

IPC: A61K31/403 ,  A61K31/655 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4166 ,  A61K31/713 ,  C12N15/113 ,  A61K31/185 ,  A61K31/18

CPC classification number: A61K31/403 ,  A61K31/18 ,  A61K31/185 ,  A61K31/4166 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/655 ,  A61K31/713 ,  C07D209/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D419/12 ,  C07K14/70567 ,  C12N15/1138 ,  C12N2310/14 ,  C12N2320/31

Abstract: The present invention provides compositions, methods, and kits comprising one or more RORγ inhibitors, alone or in combination with one or more anticancer drugs, such as an anti-androgen drug, that are useful for treating cancer, e.g., prostate cancer, such as castration-resistant prostate cancer (CRPC), and numerous other types of cancer including lung cancer, breast cancer, liver cancer, ovarian cancer, endometrial cancer, bladder cancer, colon cancer, lymphoma, and glioma.

公开(公告)号：US20180064690A1

公开(公告)日：2018-03-08

申请号：US15812528

申请日：2017-11-14

Applicant: Janssen Pharmaceutica NV

Inventor： Steven Goldberg ,  Christoph Steeneck ,  Christian Gege ,  Olaf Kinzel ,  Gerald Kleymann ,  Thomas Hoffmann ,  Anne M. Fourie ,  Xiaohua Xue

IPC: A61K31/426 ,  A61K31/506 ,  C07D277/30 ,  A61K31/433 ,  A61K31/454 ,  A61K31/4725 ,  C07D417/14 ,  A61K45/06 ,  A61K31/427 ,  C07D417/04 ,  A61K31/5377

CPC classification number: A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D277/30 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention comprises compounds of Formula I wherein:R1, R2, R3, R4, R5, R7, R8, and are defined in the specification.The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

公开(公告)号：US20180042919A1

公开(公告)日：2018-02-15

申请号：US15674717

申请日：2017-08-11

Applicant: East Tennessee State University Research Foundation

Inventor： Gregory A. Ordway ,  Attila Szebeni ,  Russell Brown

IPC: A61K31/4725 ,  A61K31/138 ,  A61K31/166

CPC classification number: A61K31/4725 ,  A61K31/138 ,  A61K31/166 ,  A61K31/472 ,  A61K45/06 ,  A61K2300/00

Abstract: Pharmaceutical formulations comprising an inhibitor of poly(ADP)-ribose) polymerase-1 (PARP1) and their use for the treatment of major depressive disorder and conditions that share at least one of the two major defining symptoms of major depressive disorder.