公开(公告)号：US20180185489A1

公开(公告)日：2018-07-05

申请号：US15740219

申请日：2016-06-30

Applicant: Santen Pharmaceutical Co., Ltd.

Inventor： Tatsuya MIYAZAKI ,  Kenji MASAKI ,  Kyohei TAKAHASHI ,  Kazuhito YAMADA

IPC: A61K47/14 ,  A61K31/444 ,  A61K9/00 ,  A61K47/34 ,  A61P27/02

CPC classification number: A61K47/14 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/06 ,  A61K31/165 ,  A61K31/196 ,  A61K31/335 ,  A61K31/405 ,  A61K31/436 ,  A61K31/444 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5575 ,  A61K31/573 ,  A61K31/58 ,  A61K31/585 ,  A61K38/13 ,  A61K47/34 ,  A61P27/02 ,  A61P27/06

Abstract: To provide a depot formulation for which depot formation is easy, and is capable of maintaining the depot form for a long period as desired, and in the case of containing a drug, to provide a depot formulation that sustained-releases the drug over a long period after being administered into the body. The present invention relates to a depot formulation containing a trialkyl citrate and/or an acetyl trialkyl citrate, in which the alkyl groups possessed by each of the trialkyl citrate and the acetyl trialkyl citrate are the same or different, and have a carbon number of 3 to 5.

公开(公告)号：US10005767B2

公开(公告)日：2018-06-26

申请号：US15419660

申请日：2017-01-30

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Vanessa Taylor ,  Hui Li ,  Rajinder Singh

IPC: A01N43/54 ,  A61K31/505 ,  C07D413/12 ,  A61K31/155 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D487/08 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D419/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/08 ,  A61K31/538 ,  A61K31/55 ,  A61K31/675 ,  C07D413/14 ,  C07D471/04 ,  C07D487/10 ,  C07D498/04 ,  C07F9/6558 ,  A61K31/5415 ,  A61K31/635 ,  C07D451/02

CPC classification number: C07D413/12 ,  A61K31/155 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/635 ,  A61K31/675 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D413/14 ,  C07D419/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D498/04 ,  C07F9/65583

Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

公开(公告)号：US09993491B2

公开(公告)日：2018-06-12

申请号：US14616164

申请日：2015-02-06

Applicant: SOCPRA—SCIENCES ET GENIE S.E.C.

Inventor： Jerome Mulhbacher ,  Daniel Lafontaine ,  Francois Malouin ,  Marianne Allard ,  Eric Marsault

IPC: A61K31/505 ,  A61K31/513 ,  A61K31/675 ,  A61K31/54 ,  A61K31/535 ,  A61K31/542 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/4412 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D498/04 ,  C07D513/04

CPC classification number: A61K31/675 ,  A61K31/4412 ,  A61K31/505 ,  A61K31/513 ,  A61K31/519 ,  A61K31/535 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/542 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D498/04 ,  C07D513/04 ,  Y10T436/141111 ,  Y10T436/143333

Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.

公开(公告)号：US20180155360A1

公开(公告)日：2018-06-07

申请号：US15578589

申请日：2016-06-02

Applicant: Glactone Pharma Development AB

Inventor： Johansson Martin ,  Olov Sterner ,  Anders Bjartell ,  Rebecka Hellsten ,  Zilma Escobar

IPC: C07D493/18 ,  A61K31/4433 ,  A61P35/00 ,  A61P37/06 ,  A61P25/28 ,  A61P31/12 ,  A61K31/365 ,  A61K31/497 ,  C07D519/00 ,  A61K31/5383 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/4184 ,  A61K31/437

CPC classification number: C07D493/18 ,  A61K31/365 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/5383 ,  A61P25/28 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  C07D307/937 ,  C07D519/00

Abstract: Ether analogues of galiellalactone, methods of preparing the analogues, and use of the analogues in the treatment of cancer are disclosed. The analogues are of formula (I) or (II):

公开(公告)号：US09988369B2

公开(公告)日：2018-06-05

申请号：US15584109

申请日：2017-05-02

Applicant: AMGEN INC.

Inventor： Xiaoqi Chen ,  Yinhong Chen ,  Alan C. Cheng ,  Richard V. Connors ,  Mikkel V. Debenedetto ,  Paul John Dransfield ,  Zice Fu ,  James S. Harvey ,  Julie Anne Heath ,  Simon J. Hedley ,  Jonathan Houze ,  Ted C. Judd ,  Aarif Yusuf Khakoo ,  David John Kopecky ,  Su-Jen Lai ,  Zhihua Ma ,  Nobuko Nishimura ,  Steven H. Olson ,  Vatee Pattaropong ,  Gayathri Swaminath ,  Xiaodong Wang ,  Wen-Chen Yeh

IPC: C07D405/14 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5383 ,  A61K45/06 ,  C07D405/04 ,  C07D471/04 ,  C07D498/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D471/04 ,  C07D498/04

Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salts thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

公开(公告)号：US09975904B2

公开(公告)日：2018-05-22

申请号：US15460466

申请日：2017-03-16

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Akiharu Ishida ,  Takeshi Matsushita ,  Tetsuya Sekiguchi ,  Tatsuya Komagata ,  Takuya Nishio

IPC: C07D498/04 ,  C07D471/04 ,  A61K31/4418 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/517 ,  C07D213/82 ,  C07D235/18 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4184

CPC classification number: C07D498/04 ,  A61K31/4184 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/455 ,  A61K31/4709 ,  A61K31/48 ,  A61K31/4985 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5383 ,  A61K45/06 ,  C07D211/58 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D235/18 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04

Abstract: Provision of orally-available and low-toxic somatostatin receptor subtype 2 agonist. Since the compound represented by the general formula (I): wherein all symbols represent the same meanings as those described in the description, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof is non-peptidic low-molecular compound which has strong somatostatin receptor subtype 2 agonist activity, the compound is orally-available. Additionally, since the compound is low-toxic, the compound is useful for the prevention and/or treatment of the somatostatin related diseases such as acromegaly or gastrointestinal obstruction.

公开(公告)号：US20180118760A1

公开(公告)日：2018-05-03

申请号：US15569191

申请日：2016-04-27

Applicant: Shionogi & Co., Ltd.

Inventor： Makoto KAWAI ,  Kenji TOMITA ,  Toshiyuki AKIYAMA ,  Azusa OKANO ,  Masayoshi MIYAGAWA

IPC: C07D498/14 ,  A61P31/16 ,  C07F7/18 ,  C07F9/6561 ,  C07D519/00 ,  C07D471/14 ,  C07D491/22 ,  C07D471/20 ,  C07D513/14

CPC classification number: C07D498/14 ,  A61K31/53 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  A61K31/675 ,  A61P31/16 ,  C07C2601/08 ,  C07C2601/16 ,  C07D471/14 ,  C07D471/20 ,  C07D491/22 ,  C07D513/14 ,  C07D519/00 ,  C07F7/1804 ,  C07F9/6561

Abstract: The present invention provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.

公开(公告)号：US20180104252A1

公开(公告)日：2018-04-19

申请号：US15635818

申请日：2017-06-28

Applicant: Horizon Orphan LLC

Inventor： David C. Griffith ,  Michael N. Dudley ,  Mark W. Surber ,  Keith A. Bostian ,  Olga Rodny

IPC: A61K31/5383 ,  A61K31/536 ,  A61K9/00 ,  A61K31/538 ,  A61K31/47 ,  A61K31/4375 ,  A61K47/02

CPC classification number: A61K31/5383 ,  A61K9/0073 ,  A61K9/0078 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/536 ,  A61K31/538 ,  A61K47/02 ,  Y02A50/401 ,  Y02A50/406 ,  Y02A50/469 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/481 ,  Y02A50/483

Abstract: The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.

公开(公告)号：US20180037590A1

公开(公告)日：2018-02-08

申请号：US15787880

申请日：2017-10-19

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： John Emmerson Campbell ,  Michael Charles Hewitt ,  Philip Xinhe Jones ,  Linghong Xie

IPC: C07D498/06 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5383 ,  C07D233/58 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/4985 ,  C07D498/04 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/06 ,  C07D519/00 ,  C07D498/14 ,  C07D491/056 ,  C07D487/04 ,  C07D471/14 ,  C07D471/04 ,  C07D403/06 ,  C07D471/06 ,  C07D401/06

CPC classification number: C07D498/06 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5383 ,  C07D233/58 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D471/06 ,  C07D471/14 ,  C07D487/04 ,  C07D491/056 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00

Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

公开(公告)号：US20180002297A1

公开(公告)日：2018-01-04

申请号：US15617900

申请日：2017-06-08

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D257/04 ,  A61K31/41 ,  C07D487/04 ,  C07D471/04 ,  C07D413/10 ,  C07D403/14 ,  C07D403/12 ,  C07D403/06 ,  C07D401/14 ,  C07D401/12 ,  C07D401/10 ,  C07D401/04 ,  A61K31/58 ,  A61K31/55 ,  A61K31/546 ,  A61K31/519 ,  A61K31/506 ,  A61K31/496 ,  A61K31/4709 ,  A61K31/4245 ,  A61K31/4184 ,  C07D501/16 ,  C07J43/00

CPC classification number: C07D257/04 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/546 ,  A61K31/55 ,  A61K31/58 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/06 ,  C07D501/16 ,  C07D501/46 ,  C07J9/005 ,  C07J43/003

Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.