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1. 发明申请

US20140154725A1 INSECT-BASED EX VIVO MODEL FOR TESTING BLOOD-BRAIN BARRIER PENETRATION AND METHOD FOR EXPOSING INSECT BRAIN TO NANOPARTICLES 有权
标题翻译：用于测试血脑屏障穿刺的基于INSECT的VIVO模型和将脑膜暴露于纳米颗粒的方法
公开(公告)号：US20140154725A1
公开(公告)日：2014-06-05
申请号：US13881566
申请日：2011-09-30
申请人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
发明人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
IPC分类号： G01N33/50
CPC分类号： G01N33/5058 , G01N33/5085
摘要： There is provided an ex-vivo insect screening model to accurately determine blood-brain barrier penetration of different nanoparticles in order to improve the compound screening procedures/processes in the early drug discovery process. This object offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.
摘要翻译：提供了一种离体昆虫筛选模型，以准确地确定不同纳米颗粒的血脑屏障穿透，以改善早期药物发现过程中的复合筛选程序/过程。与现有技术相比，该目标提供了许多优点，因为昆虫模型是决策过程中比现有体外模型更可靠的工具，并且将加速药物筛选过程并减少后期磨耗率。此外，它将减少在药物发现阶段牺牲的哺乳动物的数量。

2. 发明授权

US09097706B2 Insect-based ex vivo model for testing blood-brain barrier penetration and method for exposing insect brain to chemical compounds 有权
标题翻译：用于测试血脑屏障渗透的基于昆虫的离体模型和将昆虫脑暴露于化合物的方法
公开(公告)号：US09097706B2
公开(公告)日：2015-08-04
申请号：US13387088
申请日：2010-08-10
申请人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
发明人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
IPC分类号： C12Q1/00 , G01N33/50
CPC分类号： G01N33/5085
摘要： There is provided an ex-vivo insect screening model to accurately determine blood-brain barrier penetration of different chemical compounds in order to improve the compound screening procedures/processes in the early drug discovery process. This object offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.
摘要翻译：提供了一种离体昆虫筛选模型，以准确确定不同化合物的血脑屏障渗透，以改善早期药物发现过程中的复合筛选程序/过程。与现有技术相比，该目标提供了许多优点，因为昆虫模型是决策过程中比现有体外模型更可靠的工具，并且将加速药物筛选过程并减少后期磨耗率。此外，它将减少在药物发现阶段牺牲的哺乳动物的数量。

3. 发明申请

US20120122144A1 METHODS EMPLOYING INSECT MODELS FOR DETERMINING INTESTINAL ABSORPTION OF CHEMICAL COMPOUNDS 有权
标题翻译：用于确定化学化合物的吸收吸收的方法
公开(公告)号：US20120122144A1
公开(公告)日：2012-05-17
申请号：US13387083
申请日：2010-08-10
申请人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
发明人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
IPC分类号： C12Q1/02 , A01K67/00
CPC分类号： G01N33/5085
摘要： There is provided insect screening models to determine gastrointestinal absorption of different chemical compounds in vertebrates, and in particular humans, in order to improve the compound screening procedures/processes in the early drug discovery process. This offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.
摘要翻译：为了改善早期药物发现过程中的化合物筛选程序/过程，提供了用于确定脊椎动物，特别是人类中不同化合物的胃肠道吸收的昆虫筛选模型。与现有技术相比，昆虫模型是决策过程的可靠工具，而不仅仅是现有的体外模型，因此与现有技术相比具有很多优势，并且将加速药物筛选过程并降低后期的磨耗率。此外，它将减少在药物发现阶段牺牲的哺乳动物的数量。

4. 发明申请

US20110171682A1 SCREENING METHODS EMPLOYING INSECTS WITH BLOOD BRAIN BARRIER 有权
标题翻译：使用血液脑屏障的筛选方法
公开(公告)号：US20110171682A1
公开(公告)日：2011-07-14
申请号：US13060619
申请日：2009-09-16
申请人： Peter Aadal Nielsen , Gunnar Andersson
发明人： Peter Aadal Nielsen , Gunnar Andersson
IPC分类号： C12Q1/24 , C12Q1/02
CPC分类号： G01N33/5085
摘要： There is provided insect models that are aimed to reflect vertebrate blood-brain barrier (BBB) penetration. Investigation of BBB penetration is extremely important in drug discovery; successful CNS drugs have to cross the BBB, while BBB penetration may cause unwanted side effects for peripheral acting drugs. Specifically, the present invention relates to the use of insects in screening for substances with a biological effect on the brain or central nervous system and/or effect on a disease or disorder of the brain or central nervous system. It further relates to use of such insects in screening for substances that have a desired biological activity and which do not cross the blood brain barrier.
摘要翻译：提供旨在反映脊椎动物血脑屏障（BBB）渗透的昆虫模型。 BBB穿透的调查在药物发现中是非常重要的; 成功的CNS药物必须穿过BBB，而BBB渗透可能会对外周作用药物造成不良副作用。具体地，本发明涉及昆虫在对脑或中枢神经系统具有生物学作用的物质的筛选和/或对脑或中枢神经系统疾病或病症的影响中的应用。它进一步涉及这种昆虫在筛选具有所需生物学活性并且不会穿过血脑屏障的物质的用途。

5. 发明授权

US09513279B2 Insect-based ex vivo model for testing blood-brain barrier penetration and method for exposing insect brain to nanoparticles 有权
标题翻译：用于测试血脑屏障渗透的基于昆虫的离体模型和将昆虫脑暴露于纳米颗粒的方法
公开(公告)号：US09513279B2
公开(公告)日：2016-12-06
申请号：US13881566
申请日：2011-09-30
申请人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
发明人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
IPC分类号： G01N33/50
CPC分类号： G01N33/5058 , G01N33/5085
摘要： There is provided an ex-vivo insect screening model to accurately determine blood-brain barrier penetration of different nanoparticles in order to improve the compound screening procedures/processes in the early drug discovery process. This object offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.
摘要翻译：提供了一种离体昆虫筛选模型，以准确地确定不同纳米颗粒的血脑屏障穿透，以改进早期药物发现过程中的复合筛选程序/过程。与现有技术相比，该目标提供了许多优点，因为昆虫模型是决策过程中比现有体外模型更可靠的工具，并且将加速药物筛选过程并减少后期磨耗率。此外，它将减少在药物发现阶段牺牲的哺乳动物的数量。

6. 发明授权

US09194864B2 Screening methods employing insects with blood brain barrier 有权
标题翻译：使用具有血脑屏障的昆虫的筛选方法
公开(公告)号：US09194864B2
公开(公告)日：2015-11-24
申请号：US13060619
申请日：2009-09-16
申请人： Peter Aadal Nielsen , Gunnar Andersson
发明人： Peter Aadal Nielsen , Gunnar Andersson
IPC分类号： G01N33/50
CPC分类号： G01N33/5085
摘要： There is provided insect models that are aimed to reflect vertebrate blood-brain barrier (BBB) penetration. Investigation of BBB penetration is extremely important in drug discovery; successful CNS drugs have to cross the BBB, while BBB penetration may cause unwanted side effects for peripheral acting drugs. Specifically, the present invention relates to the use of insects in screening for substances with a biological effect on the brain or central nervous system and/or effect on a disease or disorder of the brain or central nervous system. It further relates to use of such insects in screening for substances that have a desired biological activity and which do not cross the blood brain barrier.
摘要翻译：提供旨在反映脊椎动物血脑屏障（BBB）渗透的昆虫模型。 BBB穿透的调查在药物发现中是非常重要的; 成功的CNS药物必须穿过BBB，而BBB渗透可能会对外周作用药物造成不良副作用。具体地，本发明涉及昆虫在对脑或中枢神经系统具有生物学作用的物质的筛选和/或对脑或中枢神经系统疾病或病症的影响中的应用。它进一步涉及这种昆虫在筛选具有所需生物学活性并且不会穿过血脑屏障的物质的用途。

7. 发明授权

US09176118B2 Methods employing insect models for determining intestinal absorption of chemical compounds 有权
标题翻译：采用昆虫模型测定化学化合物肠道吸收的方法
公开(公告)号：US09176118B2
公开(公告)日：2015-11-03
申请号：US13387083
申请日：2010-08-10
申请人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
发明人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
IPC分类号： C12Q1/00 , G01N33/50
CPC分类号： G01N33/5085
摘要： There is provided insect screening models to determine gastrointestinal absorption of different chemical compounds in vertebrates, and in particular humans, in order to improve the compound screening procedures/processes in the early drug discovery process. This offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.
摘要翻译：为了改善早期药物发现过程中的化合物筛选程序/过程，提供了用于确定脊椎动物，特别是人类中不同化合物的胃肠道吸收的昆虫筛选模型。与现有技术相比，昆虫模型是决策过程的可靠工具，而不仅仅是现有的体外模型，因此与现有技术相比具有很多优势，并且将加速药物筛选过程并降低后期的磨耗率。此外，它将减少在药物发现阶段牺牲的哺乳动物的数量。

8. 发明申请

US20120119081A1 INSECT-BASED MODEL FOR PHARMACO-KINETIC STUDIES 审中-公开
标题翻译：基于INSECT的药物动力学研究模型
公开(公告)号：US20120119081A1
公开(公告)日：2012-05-17
申请号：US13387098
申请日：2010-08-10
申请人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
发明人： Peter Aadal Nielsen , Gunnar Andersson , Olga Andersson
IPC分类号： H01J49/26 , G01N33/50
CPC分类号： G01N33/5085
摘要： There is provided a new methodology for initial assessment of compound PK. The invention is generally particular useful for efficient screening of and assessment of PK profiles of newly synthesized compounds in the early phase of drug discovery.
摘要翻译：为化合物PK的初步评估提供了新的方法。本发明通常特别适用于药物发现早期新合成化合物的PK谱的有效筛选和评估。

9. 发明申请

US20100144701A1 Modulators of CB1 Receptors 有权
公开(公告)号：US20100144701A1
公开(公告)日：2010-06-10
申请号：US12518446
申请日：2007-12-17
申请人： Martin Cooper , Jean-Marie Receveur , Thomas Hoegberg , Peter Aadal Nielsen , Jean-Michel Linget , Pia Marina Noeregaard , Anthony Murray , Emelie Bjurling
发明人： Martin Cooper , Jean-Marie Receveur , Thomas Hoegberg , Peter Aadal Nielsen , Jean-Michel Linget , Pia Marina Noeregaard , Anthony Murray , Emelie Bjurling
IPC分类号： A61K31/4155 , C07D403/14 , C07D403/06 , C07D401/06 , C07D401/14 , A61K31/506 , A61K31/454 , A61K31/4725 , A61K31/4545 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P9/00 , A61P25/00 , A61P25/30
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH,or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3, and B1 is —CO—, —O—, —S—, —SO—, —SO2—, —CH2—, —CHCH3—, —CHOH— or —NR7—; or (iii) a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* and —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is as defined in the specification; R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.

10. 发明申请

US20100010061A1 CB1 RECEPTOR MODULATORS 有权
标题翻译： CB1受体调节剂
公开(公告)号：US20100010061A1
公开(公告)日：2010-01-14
申请号：US12519432
申请日：2007-12-17
申请人： Martin Cooper , Jean-Marie Receveur , Thomas Hoegberg , Peter Aadal Nielsen , Jean-Michel Linget , Pia Karina Noeregaard , Anthony Murray , Emelie Bjurling
发明人： Martin Cooper , Jean-Marie Receveur , Thomas Hoegberg , Peter Aadal Nielsen , Jean-Michel Linget , Pia Karina Noeregaard , Anthony Murray , Emelie Bjurling
IPC分类号： C07D231/12 , A61K31/415 , A61K31/41 , C07D257/04 , A61P3/10 , A61P3/06 , A61P9/00 , A61P3/00 , A61P1/16 , A61P25/30 , A61P25/00 , A61P15/00
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 is (i) a bond, or (ii) —(CH2)aB1(CH2)b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is 1, 2 or 3; or (iii) —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* or —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; R2 is a divalent radical of formula -Q1-A4-[Q2]w- wherein Q1, A4 Q2 and w are as defined in the specification; and R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.
摘要翻译：式（I）化合物抑制正常的信号传导活性CB1受体，因此可用于治疗由CB1受体信号传导活性介导的疾病或病症，例如治疗肥胖和超重，预防体重增加，治疗疾病和与肥胖和超重直接或间接相关的病症：其中A1是氢，-COOH或四唑基，A2是氢，-COOH或四唑基，条件是A1和A2之一是-COOH或四唑基; p是0或1，A3是苯基或环烷基，其中任一个任选被R 4和/或R 5取代; q为0或1; R3是氢，C1-C4烷基，环烷基，-CF3或-OR9; R4和R5独立地为-R9，-CN，-F，-Cl，-Br，-OR9，-NR7R8，-NR7COR6，-NR7SO2R6，-COR6，-SR9，-SOR9或-SO2R6; R6是C1-C4烷基，环烷基，-CF3或-NR7R8; R7和R8独立地是氢，C1-C4烷基，-CF3或环烷基; R9是氢，C1-C4烷基，环烷基，完全或部分氟化的C1-C4烷基; R1是（i）键或（ii） - （CH2）aB1（CH2）b-，其中a和b独立地为0,1,2或3，条件是a + b为1,2或3; 或（iii）-C（R 10）（R 11） - *，-C（R 10）（R 11）-O-，-C（R 10）（R 11）（R 11） - *，-CH 2 C（R 10）（R 11）-O- *，-CH 2 -O（R 10）（R 11） - *或-C（R 10）（R 11） O-CH2- *，其中由星号表示的键连接到吡唑环上; R2是式-Q1-A4- [Q2] w-的二价基团，其中Q1，A4 Q2和w如说明书中所定义; 和R 10是氢，R 11是（C 1 -C 3）烷基或-OH; 或R 10和R 11均为（C 1 -C 3）烷基; 或R 10和R 11与它们所连接的碳原子一起形成（C 3 -C 5）环烷基环。

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