公开(公告)号：US20240254162A1

公开(公告)日：2024-08-01

申请号：US18527402

申请日：2023-12-04

Applicant: The Second People's Hospital of Shenzhen(Shenzhen Institute of Geriatrics)

Inventor： Zhengzhi Wu ,  Bohua Long ,  Liuyang Pu ,  Zhiyue Li ,  Shengquan Hu ,  Limin Li

IPC: C07K5/02 ,  C07C227/20 ,  C07K1/107 ,  C07K5/062

CPC classification number: C07K5/0202 ,  C07C227/20 ,  C07K1/107 ,  C07K5/06026 ,  A61K38/00

Abstract: A CyclotheonellazoleA, a synthesis method therefor, and an application method thereof are provided, and a compound with a structure of formula (I) and a pharmaceutically acceptable salt thereof are provided, the structure of formula (I) is as follows:




R1, R2, R3 and R4 are independently selected form the group consisting of a hydrogen group (H), an alkyl group with carbon atoms in a range of 1-6, an alkoxy group with carbon atoms in a range of 1-6, a halogen group, a hydroxyl group, an amino group, a nitro group, a cyano group and a sulfydryl group. A CyclotheonellazoleA natural product is successfully synthesized by a classical retrosynthesis analysis, a stereoscopic structure of the CyclotheonellazoleA natural product is confirmed, extremely excellent protease inhibitory activity of the CyclotheonellazoleA natural product is confirmed by combining a protease inhibition activity experiment, and the CyclotheonellazoleA has a strong application prospect in a pharmaceutical industry.

公开(公告)号：US20180355055A1

公开(公告)日：2018-12-13

申请号：US15974089

申请日：2018-05-08

Applicant: ImmunoGen, Inc.

Inventor： Wei Li ,  Nathan Elliott Fishkin ,  Robert Yongxin Zhao ,  Michael Louis Miller ,  Ravi V.J. Chari

IPC: C07K16/28 ,  C07K19/00 ,  A61K47/60 ,  C07K5/103 ,  C07K5/02 ,  C07D519/00 ,  C07D498/04 ,  C07D487/04 ,  A61K45/06 ,  A61K38/07 ,  A61K31/5517 ,  A61P35/00 ,  A61K47/68 ,  C07K16/46

CPC classification number: C07K16/2896 ,  A61K31/5517 ,  A61K38/07 ,  A61K45/06 ,  A61K47/60 ,  A61K47/6835 ,  A61K47/6849 ,  A61K47/6863 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  C07K5/0202 ,  C07K5/1008 ,  C07K16/2803 ,  C07K16/46 ,  C07K19/00

Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

公开(公告)号：US09994613B2

公开(公告)日：2018-06-12

申请号：US15288863

申请日：2016-10-07

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Marion W. Wannamaker ,  Robert J. Davies

IPC: C07K5/062 ,  A61K38/00 ,  A61P17/00 ,  C07K5/06 ,  C07D307/02 ,  C07D477/02 ,  C07D477/20 ,  C07K5/02 ,  C07K5/08 ,  C07D207/16 ,  C07K5/083

CPC classification number: C07K5/06034 ,  A61K38/00 ,  C07D207/16 ,  C07D307/02 ,  C07D477/02 ,  C07D477/20 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06 ,  C07K5/06008 ,  C07K5/06191 ,  C07K5/08 ,  C07K5/0808 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/475

Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

公开(公告)号：US09975921B2

公开(公告)日：2018-05-22

申请号：US14927669

申请日：2015-10-30

Applicant: Helsinn Healthcare SA

Inventor： Keith Lorimer ,  Seemon H Pines ,  Bernhard Paul ,  Benjamin Littler

IPC: C07D401/00 ,  C07K5/062 ,  C07D401/06 ,  C07K5/02

CPC classification number: C07K5/06026 ,  C07D401/06 ,  C07K5/0202

Abstract: Crystalline forms of anamorelin which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.

公开(公告)号：US20170183419A1

公开(公告)日：2017-06-29

申请号：US15371738

申请日：2016-12-07

Applicant: ImmunoGen, Inc.

Inventor： Wei Li ,  Nathan Elliott Fishkin ,  Robert Yongxin Zhao ,  Michael Louis Miller ,  Ravi V.J. Chari

IPC: C07K16/28 ,  A61K38/07 ,  C07K16/46 ,  C07D487/04 ,  C07K19/00 ,  C07K5/02 ,  A61K31/5517 ,  A61K45/06

CPC classification number: C07K16/2896 ,  A61K31/5517 ,  A61K38/07 ,  A61K45/06 ,  A61K47/60 ,  A61K47/6835 ,  A61K47/6849 ,  A61K47/6863 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  C07K5/0202 ,  C07K5/1008 ,  C07K16/2803 ,  C07K16/46 ,  C07K19/00

Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

公开(公告)号：US20170158734A1

公开(公告)日：2017-06-08

申请号：US15325998

申请日：2015-07-14

Applicant: CENTRAX INTERNATIONAL, INC.

Inventor： Jinfu YANG ,  Jian James CEN ,  Xiaoqing Michelle FAN

IPC: C07K5/065

CPC classification number: C07K5/06078 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0806 ,  C07K5/0821

Abstract: The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein have improved proteasome potency and selectivity, and increased aqueous solubility, and are useful in treating various conditions or diseases associated with proteasomes.

公开(公告)号：US20170157264A1

公开(公告)日：2017-06-08

申请号：US15293579

申请日：2016-10-14

Applicant: ImmunoGen, Inc.

Inventor： Ravi V.J. Chari ,  Robert Yongxin Zhao ,  Yelena Kovtun ,  Rajeeva Singh ,  Wayne C. Widdison

IPC: A61K39/00 ,  C07K16/28 ,  C07K5/083

CPC classification number: C07K16/28 ,  A61K31/5365 ,  A61K47/65 ,  A61K47/6809 ,  A61K47/6849 ,  C07D207/46 ,  C07K5/0202 ,  C07K5/06026 ,  C07K5/0806 ,  C07K5/0819 ,  Y02A50/423 ,  Y02A50/491

Abstract: Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.

公开(公告)号：US09669102B2

公开(公告)日：2017-06-06

申请号：US14843520

申请日：2015-09-02

Applicant: ImmunoGen, Inc.

Inventor： Ravi V. J. Chari ,  Michael Louis Miller ,  Manami Shizuka

IPC: C07D487/04 ,  A61K47/48 ,  C07K16/28 ,  C07D519/00 ,  C07K5/093 ,  C07K5/113 ,  C07K5/02 ,  A61K39/00

CPC classification number: A61K47/64 ,  A61K2039/505 ,  C07D487/04 ,  C07D519/00 ,  C07K5/0202 ,  C07K5/0819 ,  C07K5/1021 ,  C07K16/28 ,  C07K16/2863 ,  C07K16/2866 ,  C07K2317/24 ,  C07K2317/92

Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

公开(公告)号：US09642889B2

公开(公告)日：2017-05-09

申请号：US14719242

申请日：2015-05-21

Applicant: Selcia Limited ,  Gilead Sciences, Inc.

Inventor： Caroline Aciro ,  Jean Yves Chiva ,  David Kenneth Dean ,  Adrian John Highton ,  Petr Jansa ,  Andrew John Keats ,  Linos Lazarides ,  Richard Mackman ,  Karine G. Poullennec ,  Adam James Schrier ,  Dustin Scott Siegel ,  Victoria Alexandra Steadman ,  Greg Watt

IPC: A61K38/21 ,  A61K38/12 ,  C07D487/08 ,  C07D498/08 ,  C07D498/18 ,  C07D498/22 ,  A61K39/29 ,  A61K45/06 ,  C07K5/02 ,  A61K39/05 ,  A61K38/15 ,  A61K38/00

CPC classification number: C07K5/0202 ,  A61K38/00 ,  A61K38/12 ,  A61K38/15 ,  A61K39/05 ,  A61K39/29 ,  A61K45/06 ,  C07D487/08 ,  C07D498/08 ,  C07D498/18 ,  C07D498/22 ,  C07K5/02 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/391 ,  Y02A50/393 ,  Y02A50/395

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.

公开(公告)号：US20170080391A1

公开(公告)日：2017-03-23

申请号：US15124575

申请日：2015-03-19

Applicant: E.W. - Hydrophilic Processes Ltd.

Inventor： Avital Ehre

IPC: B01D69/10 ,  B01D61/02 ,  C02F1/44 ,  B01D71/56 ,  B01D71/64 ,  C07K5/02 ,  B01D71/16

CPC classification number: B01D69/105 ,  B01D61/025 ,  B01D69/10 ,  B01D69/125 ,  B01D71/16 ,  B01D71/56 ,  B01D71/64 ,  C02F1/44 ,  C02F1/441 ,  C07K5/0202

Abstract: A reverse-osmosis membrane filter comprising: a porous support layer; a porous skin layer, and at least one water binding composition predominantly bound between the skin layer and the support layer.