公开(公告)号：JP2011207891A

公开(公告)日：2011-10-20

申请号：JP2011108474

申请日：2011-05-13

Applicant: Endacea Inc ,  エンダセア, インコーポレイテッド

Inventor： WILSON CONSTANCE N ,  PARTRIDGE JOHN J

IPC: C07D473/04 ,  A61K20060101 ,  A61K31/522 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P13/12 ,  A61P25/00 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P31/12 ,  A61P31/14 ,  A61P31/18 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D473/02 ,  C07D473/06

CPC classification number: C07D473/04 ,  C07D473/06

Abstract: PROBLEM TO BE SOLVED: To provide a compound usable as an Aadenosine receptor antagonist.SOLUTION: There is provided a compound represented by formula (I), wherein, Ris a 1-8C linear or branched chain alkyl group optionally and selectively substituted with one or more of OR, NRRand a halogen group; Ris H, a 1-8C alkyl group or the like; and Ris a 1-8C linear chain, an alkylene group, an alkenyl group or the like.

Abstract translation: 要解决的问题：提供可用作阿丹诺星受体拮抗剂的化合物。溶液：提供由式（I）表示的化合物，其中R 1为1-8C直链或支链烷基，任选和选择性地被一个或多个 更多的OR，​​NRR和卤素基团; Ris H，1-8C烷基等; Ris为1-8C直链，亚烷基，烯基等。

公开(公告)号：CA2528385C

公开(公告)日：2011-03-15

申请号：CA2528385

申请日：2004-06-04

Applicant: ENDACEA INC

Inventor： WILSON CONSTANCE N ,  PARTRIDGE JOHN J

IPC: C07D473/04 ,  A61K20060101 ,  A61K31/522 ,  A61P9/04 ,  A61P11/00 ,  A61P11/06 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P31/18 ,  A61P37/06 ,  A61P37/08 ,  C07D473/02 ,  C07D473/06

Abstract: R3 is Alk14ArR16, wherein Alk14 is C1-8 straight or branched alkylene or alkenylene, Ar is a 5- or 6-member aromatic ring containing 0 to 4 heteroatoms selected from N, O, and S, or is a bicyclic 9- or 11-member aromatic ring containing 0 to 6 heteroatoms selected from N, O, and S; R4 is --((CH2)r-Phenyl-R20 wherein r is 1 to 20, R20 is SO3H, PO3H2, halogen, OR13c, COOR13d, NO2, NR21R22, and other choices. The compound optionally has one or more radioactive or non-radioactive label moieties wherein the label moieties are optionally connected to the compound through one or more spacer moiety. The present invention also provides for their use as therapeutic agents and diagnostic agents.

公开(公告)号：US20230346883A1

公开(公告)日：2023-11-02

申请号：US17734574

申请日：2022-05-02

Applicant: Endacea, Inc.

Inventor： Constance N. Wilson

IPC: A61K38/17 ,  A61K39/395 ,  A61K9/51 ,  A61P35/00 ,  A61K45/06 ,  A61K38/21 ,  C12N15/85

CPC classification number: A61K38/177 ,  A61K39/39558 ,  A61K9/5123 ,  A61P35/00 ,  A61K45/06 ,  A61K38/217 ,  C12N15/85 ,  C12N2800/107

Abstract: Novel mutant A1 adenosine receptor cDNA sequences and plasmids. Novel mutant A1 adenosine receptor cDNA sequences and plasmids which can improve immune cells ability to kill cancer cells.

公开(公告)号：US20150283143A1

公开(公告)日：2015-10-08

申请号：US14440395

申请日：2011-01-25

Applicant: ENDACEA, INC.

Inventor： Constance Neely Wilson

IPC: A61K31/522 ,  A61K45/06

CPC classification number: A61K31/522 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06

Abstract: The present invention relates to methods for treating and preventing renal impairment by administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist alone or in combination with at least one additional therapeutic agent. The invention further encompasses pharmaceutical compositions comprising an A1 adenosine receptor antagonist alone or with, at least, one additional therapeutic agent in a pharmaceutically acceptable carrier. The pharmaceutical compositions of the invention find use in methods for treating and preventing renal impairment.

Abstract translation: 本发明涉及通过向受试者施用治疗有效量的单独的或与至少一种另外的治疗剂组合的A1腺苷受体拮抗剂来治疗和预防肾损伤的方法。 本发明还包括药物组合物，其单独或与药学上可接受的载体中的至少一种另外的治疗剂单独包含A1腺苷受体拮抗剂。 本发明的药物组合物可用于治疗和预防肾损伤的方法。

公开(公告)号：CA2810725A1

公开(公告)日：2012-03-22

申请号：CA2810725

申请日：2011-09-15

Applicant: ENDACEA INC

Inventor： WILSON CONSTANCE NEELY

IPC: G01N33/68 ,  G01N33/52 ,  G01N33/533 ,  G01N33/92

Abstract: The present invention relates to the methods of use for measurement of lipopolysaccharide (LPS) and methods of use for diagnosis of sepsis and LPS-related conditions. Specifically the present invention relates to a time resolved fluorescence (TRF) based assay for the measurement of LPS and methods of use for the measurement of LPS to diagnose sepsis, Gram-negative bacterial infections, and LPS-related conditions.

公开(公告)号：AT315567T

公开(公告)日：2006-02-15

申请号：AT97947567

申请日：1997-11-19

Applicant: ENDACEA INC

Inventor： NEELY CONSTANCE F

IPC: G01N33/60 ,  A01N1/02 ,  A61K31/522 ,  A61P1/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/06 ,  A61P13/00 ,  A61P15/00 ,  A61P19/02 ,  A61P37/08 ,  C07D473/06 ,  A61K31/52 ,  G01N33/06

Abstract: The invention provides compounds useful as A 1 adenosine receptor antagonists which have the formula: wherein R 1 is selected from C 1 -C 8 alkyl; R 2 is of the formula: wherein n is an integer ranging from 1 to 8; R 5 is H or CH 3 (CH 2 ) p , wherein p is an integer ranging from 1 to 7; and R 6 is H; (CH 2 ) m H; or (CH 2 ) m OH, wherein m is an integer ranging from 1 to 8; R 3 is of the formula: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€• (CH 2 ) q C 6 H 4 €•R 7 wherein q is an integer ranging from 1 to 8; wherein R 7 is selected from H, OH, NH 2, R 9 COOH, wherein R 9 is an alkylene or alkenylene group having 1 to 8 carbon atoms, and (CH 2 ) t OH, wherein t is an integer ranging from 1 to 8; and R 4 is of the formula: wherein R 8 is selected from H, OH, NH 2 , (CH 2 ) f NH 2 wherein f is selected from 0 and an integer ranging from 1 to 8, (CH 2 ) s OH wherein s is an integer ranging from 1 to 8, and R 10 COOH wherein R 10 is an alkyxene or alkenylene group having 1 to 8 carbon atoms; and r is an integer ranging from 1 to 8.

公开(公告)号：CA2444487A1

公开(公告)日：2002-11-28

申请号：CA2444487

申请日：2002-05-17

Applicant: ENDACEA INC

Inventor： WILSON CONSTANCE NEELY

IPC: A61K31/52 ,  A61K31/522 ,  A61K39/395 ,  A61K45/06 ,  A61P31/18 ,  A61P37/02 ,  C07K16/28

Abstract: A1 adenosine receptor antagonists and P2X receptor antagonists are useful in the treatments of disorders of the immune system, which include HIV infectio n, AIDS, and adenosine deaminase deficiency-dependent severe immunodeficiency disease (ADA SCID).

公开(公告)号：AU5269300A

公开(公告)日：2000-12-05

申请号：AU5269300

申请日：2000-05-12

Applicant: ENDACEA INC

Inventor： NEELY CONSTANCE F

IPC: A61K9/127 ,  A61K31/00 ,  A61K31/136 ,  A61K31/522 ,  A61K31/55 ,  A61K31/573 ,  A61K31/704 ,  A61K31/7135 ,  A61K38/06 ,  A61K38/17 ,  A61K38/19 ,  A61K38/21 ,  A61K45/00 ,  A61K45/06 ,  A61K47/44 ,  A61K47/48 ,  A61K48/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C12N15/09 ,  C12Q1/02 ,  G01N33/50 ,  G01N33/566 ,  G01N33/574 ,  G01N33/68

Abstract: Subjects at risk for developing cancer may be identified by obtaining samples of diagnostic cells from the subjects and determining a measure of cytotoxicity of the cells, the measure of cytotoxicity correlating negatively with the risk of developing cancer. The development of cancer may be prevented in subjects determined to be at risk for developing cancer by administering priming and activating agents to the subject, by increasing the expression of A 1 adenosine receptors in cells of the subject, and increasing the affinity of cells of the subject for A 1 adenosine receptor ligands. The preventative and diagnostic methods of the present invention may be carried out with kits and pharmaceutical liposomal formulations.

公开(公告)号：CA2709772A1

公开(公告)日：2009-07-09

申请号：CA2709772

申请日：2008-12-19

Applicant: ENDACEA INC

Inventor： WILSON CONSTANCE N

IPC: C07D473/14 ,  C07D473/02

Abstract: This invention relates to compounds of formula (I), Wherein R1 - R4 are defined in the Specification, their uses in the practice of medicine, their medicinal formulations, their use in medical diagnosis, and their preparation.

公开(公告)号：CA2638448A1

公开(公告)日：2009-02-15

申请号：CA2638448

申请日：2008-07-31

Applicant: ENDACEA INC

Inventor： WILSON CONSTANCE N

IPC: A61K31/522 ,  A61P31/04

Abstract: Methods for treating and preventing tissue injury and sepsis associated with a Yersinia pestis infection, particularly pneumonic plague, are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist alone or in combination with a t least one additional therapeutic agent, including an antibiotic agent. The present methods find use in biodefense as a means of preventing and treating tissue injury a nd sepsis associated with Y. pestis infection, particularly pneumonic plague, in the event of a bioterrorist attack with this deadly bacterium.