公开(公告)号：US20190247388A1

公开(公告)日：2019-08-15

申请号：US16393383

申请日：2019-04-24

Applicant: Nektar Therapeutics

Inventor： Jennifer Riggs-Sauthier ,  Bo-Liang Deng ,  Timothy A. Riley

IPC: A61K31/485 ,  A61K31/4468 ,  A61K31/4025 ,  A61K31/402 ,  C07D489/02 ,  A61K47/60 ,  A61K47/10 ,  A61K31/439

CPC classification number: A61K31/485 ,  A61K31/402 ,  A61K31/4025 ,  A61K31/439 ,  A61K31/4468 ,  A61K47/10 ,  A61K47/60 ,  C07D489/02

Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.

公开(公告)号：US20190046523A1

公开(公告)日：2019-02-14

申请号：US16165364

申请日：2018-10-19

Applicant: Nektar Therapeutics

Inventor： Jennifer Riggs-Sauthier ,  Bo-Liang Deng ,  Timothy A. Riley

IPC: A61K31/485 ,  A61K31/4468 ,  A61K31/4025 ,  A61K31/402 ,  C07D489/02 ,  A61K47/60 ,  A61K47/10 ,  A61K31/439

CPC classification number: A61K31/485 ,  A61K31/402 ,  A61K31/4025 ,  A61K31/439 ,  A61K31/4468 ,  A61K47/10 ,  A61K47/60 ,  C07D489/02

Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.

公开(公告)号：US20180327769A1

公开(公告)日：2018-11-15

申请号：US15893202

申请日：2018-02-09

Applicant: Tasmanian Alkaloids Pty. Ltd.

Inventor： Anthony J. FIST

IPC: C12N15/82 ,  C07D489/02 ,  A01H5/00 ,  A01H1/06 ,  A01H5/02

CPC classification number: C12N15/8257 ,  A01H1/06 ,  A01H5/00 ,  A01H5/02 ,  A01H6/64 ,  C07D489/02

Abstract: The present invention is directed to an improved poppy straw, concentrate of poppy straw and opium of Papaver somniferum for the production of thebaine containing little or no oripavine, codeine or morphine. The present invention also provides plants, stands and seeds of Papaver somniferum and methods for the production of thebaine.

公开(公告)号：US10028945B2

公开(公告)日：2018-07-24

申请号：US15285818

申请日：2016-10-05

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC: A01N43/42 ,  A61K31/44 ,  A61K31/485 ,  A61K31/495 ,  A61K31/445 ,  A61K38/05 ,  A61K47/48

CPC classification number: A61K31/485 ,  A61K31/445 ,  A61K31/495 ,  A61K38/05 ,  A61K47/54 ,  A61K47/542 ,  C07D489/02 ,  C07D489/08

Abstract: A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing the ketone-containing opioid is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of the ketone-containing opioid from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.

公开(公告)号：US09932349B2

公开(公告)日：2018-04-03

申请号：US15260610

申请日：2016-09-09

Applicant: Rensselaer Polytechnic Institute

Inventor： Mark P. Wentland

IPC: C07D491/18 ,  C07D489/12 ,  C07D489/08 ,  C07D489/00

CPC classification number: C07D489/12 ,  A61K31/485 ,  C07D221/22 ,  C07D221/26 ,  C07D401/04 ,  C07D405/06 ,  C07D489/00 ,  C07D489/02 ,  C07D489/08 ,  C07D489/10 ,  C07D491/18

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.

公开(公告)号：US20170296654A1

公开(公告)日：2017-10-19

申请号：US15640781

申请日：2017-07-03

Applicant: ALERE SAN DIEGO, INC.

Inventor： Mariusz BANASZCZYK ,  Normand HÉBERT ,  Neil STOWE

IPC: A61K39/385 ,  C08L25/06 ,  C07D489/04 ,  A61K39/39 ,  C07D489/00 ,  C07K16/06 ,  C07F9/6561 ,  A61K39/00 ,  C07D489/02 ,  G01N33/94 ,  C07K16/44

CPC classification number: A61K39/385 ,  A61K39/0013 ,  A61K39/39 ,  A61K2039/6081 ,  A61K2039/627 ,  C07D489/00 ,  C07D489/02 ,  C07D489/04 ,  C07F9/6561 ,  C07K16/06 ,  C07K16/44 ,  C07K2317/33 ,  C08L25/06 ,  G01N33/9486

Abstract: The present invention relates to novel 6-acetylmorphine analogs, and methods for their synthesis and use. Such analogs are designed to provide a convenient linkage chemistry for coupling under mild conditions to a suitable group on a target protein, polypeptide, solid phase or detectable label.

公开(公告)号：US20170267686A1

公开(公告)日：2017-09-21

申请号：US15505625

申请日：2015-08-21

Applicant: EPIMERON INC.

Inventor： Peter James Facchini

IPC: C07D489/02 ,  C12P17/18

CPC classification number: C07D489/02 ,  C07D489/08 ,  C12N9/0006 ,  C12N9/90 ,  C12P17/18 ,  C12P17/188 ,  C12Y101/01247

Abstract: Methods that may be used for the manufacture of a class of chemical compounds known as morphinans, including neopine, are provided. Compositions useful for the synthesis of morphinans, including neopine, are also provided.

公开(公告)号：US09732096B2

公开(公告)日：2017-08-15

申请号：US15074960

申请日：2016-03-18

Applicant: OrphoMed, Inc.

Inventor： Nikhilesh Nihala Singh

IPC: C07D489/12 ,  A61K31/485 ,  C07D519/00 ,  C07D489/02 ,  C07C217/64 ,  C07C217/70 ,  C07C233/43 ,  C07D489/08 ,  A61K31/137 ,  A61K31/167 ,  C07C233/16 ,  C07D489/00 ,  C07C233/25 ,  C07C217/74

CPC classification number: A61K31/167 ,  A61K9/0053 ,  A61K9/20 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K31/137 ,  A61K31/485 ,  A61K45/06 ,  C07C217/64 ,  C07C217/70 ,  C07C217/74 ,  C07C233/16 ,  C07C233/25 ,  C07C233/43 ,  C07C2601/14 ,  C07D489/00 ,  C07D489/02 ,  C07D489/08 ,  C07D489/12 ,  C07D519/00

Abstract: The present invention provides a buprenorphine dimer compound, wherein the two buprenorphine portions are linked via an ethylene spacer, wherein the spacer is bonded to the two opioid molecules via an ether bond. Pharmaceutical compositions comprising such a buprenorphine dimer drug are also disclosed, and the use of such compounds in the treatment of gastrointestinal hyperalgesia generally and in particular diarrhea-predominant irritable bowel syndrome.

公开(公告)号：US20170217977A1

公开(公告)日：2017-08-03

申请号：US15260610

申请日：2016-09-09

Applicant: Rensselaer Polytechnic Institute

Inventor： Mark P. WENTLAND

IPC: C07D489/12 ,  C07D489/00 ,  C07D489/08

CPC classification number: C07D489/12 ,  A61K31/485 ,  C07D221/22 ,  C07D221/26 ,  C07D401/04 ,  C07D405/06 ,  C07D489/00 ,  C07D489/02 ,  C07D489/08 ,  C07D489/10 ,  C07D491/18

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.

公开(公告)号：US09657028B2

公开(公告)日：2017-05-23

申请号：US15004380

申请日：2016-01-22

Applicant: Johnson Matthey Public Limited Company

Inventor： Saroop Singh Matharu ,  Ewart Grant ,  Brian W. Heinrich

IPC: C07D489/02 ,  A61K31/485 ,  C07D489/04

CPC classification number: C07D489/02 ,  C07D489/04

Abstract: Improved processes for making hydrocodone and hydromorphone as well as their 8,14-dihydrothebaine and 8,14-dihydrooripavine derivatives and salts are disclosed.