公开(公告)号：US20100273773A1

公开(公告)日：2010-10-28

申请号：US12746092

申请日：2008-12-04

Applicant: Henricus Jacobus Maria Gijsen ,  Marc Hubert Mercken

Inventor： Henricus Jacobus Maria Gijsen ,  Marc Hubert Mercken

IPC: A61K31/553 ,  C07D223/20 ,  C07D267/20 ,  C07D403/10 ,  A61K31/55 ,  A61P29/00

CPC classification number: C07D267/20 ,  C07D223/20

Abstract: The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.

Abstract translation: 本发明涉及具有TRPA1受体激动性的式（I）的新型三环化合物，包含这些化合物的药物组合物，用于制备这些化合物的化学方法及其作为药理学工具的用途，或作为刺激性丧失能力的治疗或治疗疾病 与动物，特别是人类中TRPA1受体的调节有关。

公开(公告)号：US20100074901A1

公开(公告)日：2010-03-25

申请号：US12251518

申请日：2008-10-15

Applicant: Marc Hubert Mercken ,  Jacqueline M. Benson ,  Sun-Yung S. Jung ,  Haiyan Jiang ,  Gopalan Raghunathan ,  Lionella Borozdina-Birch

Inventor： Marc Hubert Mercken ,  Jacqueline M. Benson ,  Sun-Yung S. Jung ,  Haiyan Jiang ,  Gopalan Raghunathan ,  Lionella Borozdina-Birch

IPC: A61K39/395 ,  G01N33/567 ,  C12P21/06 ,  C12N5/00 ,  C12N5/02 ,  C12N1/00 ,  C07K16/18 ,  C07H21/04 ,  C12P21/00

CPC classification number: C07K16/18 ,  A61K2039/505 ,  C07K2317/21 ,  C07K2317/56 ,  C07K2317/565

Abstract: The present invention relates to at least one novel human anti-amyloid antibody, including isolated nucleic acids that encode at least one anti-amyloid antibody, amyloid, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.

Abstract translation: 本发明涉及至少一种新的人抗淀粉样蛋白抗体，包括编码至少一种抗淀粉样蛋白抗体，淀粉样蛋白，载体，宿主细胞，转基因动物或植物的分离的核酸及其制备和使用方法，包括 治疗组合物，方法和装置。

公开(公告)号：US09329189B2

公开(公告)日：2016-05-03

申请号：US10528928

申请日：2003-09-09

Applicant: Marc Hubert Mercken ,  Marc Maria Pierre Vandermeeren

Inventor： Marc Hubert Mercken ,  Marc Maria Pierre Vandermeeren

IPC: A61K39/395 ,  A61K39/00 ,  C07K16/00 ,  C12P21/08 ,  G01N33/68 ,  C07K16/18

CPC classification number: G01N33/6896 ,  C07K16/18 ,  C07K2317/34 ,  G01N2333/4709 ,  G01N2800/2821 ,  G01N2800/52

Abstract: This invention relates to antibodies, including specified portions or variants, specific for at least the human Amyloid-beta 11 N-terminal site, i.e. Aβ11-x peptides. It further provides methods of making and using said antibodies, including therapeutic formulations, administration and devices.

Abstract translation: 本发明涉及针对至少人淀粉样蛋白-β11N-末端位点即A和B-11肽的特异性的抗体，包括特定的部分或变体。 其进一步提供制备和使用所述抗体的方法，包括治疗剂型，给药方式和装置。

公开(公告)号：US08461145B2

公开(公告)日：2013-06-11

申请号：US12746092

申请日：2008-12-04

Applicant: Henricus Jacobus Maria Gijsen ,  Marc Hubert Mercken

Inventor： Henricus Jacobus Maria Gijsen ,  Marc Hubert Mercken

IPC: A61K31/55 ,  A61K31/553 ,  C07D233/20 ,  C07D267/20 ,  A61P25/00

CPC classification number: C07D267/20 ,  C07D223/20

Abstract: The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.

Abstract translation: 本发明涉及具有TRPA1受体激动性的式（I）的新型三环化合物，包含这些化合物的药物组合物，用于制备这些化合物的化学方法及其作为药理学工具的用途，或作为刺激性丧失能力的治疗或治疗疾病 与动物，特别是人类中TRPA1受体的调节有关。

公开(公告)号：US20140154715A1

公开(公告)日：2014-06-05

申请号：US14233068

申请日：2012-07-06

Applicant: Marc Hubert Mercken ,  Marianne Borgers ,  Marc, Maria, Pierre, Pelagie Vandermeeren ,  Bianca Julia J Van Broeck

Inventor： Marc Hubert Mercken ,  Marianne Borgers ,  Marc, Maria, Pierre, Pelagie Vandermeeren ,  Bianca Julia J Van Broeck

IPC: G01N33/577 ,  C07K16/18

CPC classification number: G01N33/577 ,  C07K16/18

Abstract: The present invention provides monoclonal antibodies which specifically recognize the shorter Aβ peptides obtained after cleavage of the APP protein mediated by γ-secretase, i.e. the Aβ-peptide fragments Aβ1-37, Aβ3-37, Aβ3p-37, Aβ1-37 and Aβ11p-37, and other like fragments ending at the 37th amino acid of APP, hereinafter also referred to as the Aβx-37 peptides. It further provides hybridoma cells producing the monoclonal antibodies as well as methods for producing the antibodies and the hybridoma cells; and an immunoassay for an Aβx-37 peptide by a competitive method or a sandwich method using the antibody of the present invention; and methods for measuring the level of Aβx-37 peptides in a sample, such as a biological sample.

Abstract translation: 本发明提供特异性识别较短A和Bgr的单克隆抗体。 在由γ-分泌酶介导的APP蛋白切割后获得的肽，即A＆bgr;肽片段A＆bgr; 1-37，A＆bgr; 3-37，A＆bgr; 3p-37，A＆bgr; 1-37和A＆bgr; 11p-37 ，以及以APP的第37个氨基酸终止的其他类似片段，以下也称为A＆bgr; x-37肽。 其进一步提供产生单克隆抗体的杂交瘤细胞以及产生抗体和杂交瘤细胞的方法; 以及使用本发明的抗体的竞争方法或夹心方法对A＆bgr; x-37肽的免疫测定; 以及用于测量样品（例如生物样品）中A＆bgr x-37肽水平的方法。

公开(公告)号：US07183288B2

公开(公告)日：2007-02-27

申请号：US10493454

申请日：2002-10-29

Applicant: Eddy Jean Edgard Freyne ,  Peter Jacobus Johannes Antonius Buijnsters ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Jean Fernand Armand Lacrampe ,  Herwig Josephus Margareta Janssen, legal representative ,  Paul Peter Maria Janssen, legal representative ,  Graziella Maria Constantina Janssen, legal representative ,  Jasmine Josée Werner Janssen, legal representative ,  Maroussia Godelieve Frank Janssen, legal representative ,  Theodora Joanna Francisca Arts ,  Paulus Joannes Lewi ,  Jan Heeres ,  Marc René de Jonge ,  Lucien Maria Henricus Koymans ,  Frederik Frans Desiré Daeyaert ,  Michael Joseph Kukla ,  Hugo Alfons Gabriel Geerts ,  Rony Maria Nuydens ,  Marc Hubert Mercken ,  Donald William Ludovici

Inventor： Paul Adriaan Jan Janssen, deceased

IPC: A61K31/505 ,  C07D239/42

CPC classification number: C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7; —C(═NH)R21; R4a or R4b each independently represent hydrogen, R8, —Y1—NR9—Y2—NR10R11, —Y1—NR9—Y1—R8, —Y1—NR9R10; provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

公开(公告)号：US08911731B2

公开(公告)日：2014-12-16

申请号：US14233068

申请日：2012-07-06

Applicant: Marc Hubert Mercken ,  Marianne Borgers ,  Marc Maria Pierre Pelagie Vandermeeren ,  Bianca Julia J Van Broeck

Inventor： Marc Hubert Mercken ,  Marianne Borgers ,  Marc Maria Pierre Pelagie Vandermeeren ,  Bianca Julia J Van Broeck

IPC: A61K39/395 ,  C07K14/47 ,  A61K48/00 ,  A61K38/10 ,  C07K16/18 ,  G01N33/577

CPC classification number: G01N33/577 ,  C07K16/18

Abstract: The present invention provides monoclonal antibodies which specifically recognize the shorter Aβ peptides obtained after cleavage of the APP protein mediated by γ-secretase, i.e. the Aβ-peptide fragments Aβ1-37, Aβ3-37, Aβ3p-37, Aβ1-37 and Aβ11p-37, and other like fragments ending at the 37th amino acid of APP, hereinafter also referred to as the Aβx-37 peptides. It further provides hybridoma cells producing the monoclonal antibodies as well as methods for producing the antibodies and the hybridoma cells; and an immunoassay for an Aβx-37 peptide by a competitive method or a sandwich method using the antibody of the present invention; and methods for measuring the level of Aβx-37 peptides in a sample, such as a biological sample.

Abstract translation: 本发明提供特异性识别较短A和Bgr的单克隆抗体。 在由γ-分泌酶介导的APP蛋白切割后获得的肽，即A＆bgr;肽片段A＆bgr; 1-37，A＆bgr; 3-37，A＆bgr; 3p-37，A＆bgr; 1-37和A＆bgr; 11p-37 ，以及以APP的第37个氨基酸终止的其他类似片段，以下也称为A＆bgr; x-37肽。 其进一步提供产生单克隆抗体的杂交瘤细胞以及产生抗体和杂交瘤细胞的方法; 以及使用本发明的抗体的竞争方法或夹心方法对A＆bgr; x-37肽的免疫测定; 以及用于测量样品（例如生物样品）中A＆bgr x-37肽水平的方法。

公开(公告)号：US08383637B2

公开(公告)日：2013-02-26

申请号：US11197669

申请日：2005-08-04

Applicant: Ellen Baxter ,  Francois Paul Bischoff ,  Robert E. Boyd ,  Mirielle Braeken ,  Steve Coats ,  Yifang Huang ,  Alfonzo D. Jordan ,  Chi Luo ,  Marc Hubert Mercken ,  Serge Maria Aloysius Pieters ,  Allen B. Reitz ,  Charles H. Reynolds ,  Tina Morgan Ross ,  Brett A. Tounge ,  Mark J. Schulz ,  Hans Louis Jos De Winter

Inventor： Ellen Baxter ,  Francois Paul Bischoff ,  Robert E. Boyd ,  Mirielle Braeken ,  Steve Coats ,  Yifang Huang ,  Alfonzo D. Jordan ,  Chi Luo ,  Marc Hubert Mercken ,  Serge Maria Aloysius Pieters ,  Allen B. Reitz ,  Charles H. Reynolds ,  Tina Morgan Ross ,  Brett A. Tounge ,  Mark J. Schulz ,  Hans Louis Jos De Winter

IPC: A61K31/517 ,  C07D239/88 ,  C07D239/94 ,  C07D401/06 ,  A61K31/535 ,  C07D265/30

CPC classification number: C07D413/06 ,  C07D239/84 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06

Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE.

Abstract translation: 本发明涉及新的2-氨基-3,4-二氢 - 喹唑啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关病症中的用途。 本发明的化合物是分泌酶的抑制剂，也称为“切割酶”和BACE。