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1. 发明公开

EP2343285A3 Peptoid compounds 有权
标题翻译：拟肽连接
公开(公告)号：EP2343285A3
公开(公告)日：2011-08-10
申请号：EP11158209.4
申请日：2002-06-28
申请人： UNIVERSITY OF WOLLONGONG
发明人： Bremner, John , Pyne, Stephen , Keller, Paul , Coghlan, Dan , Garas, Adel , Witchard, Helen , Boyle, Tim , Coates, Jonathan
IPC分类号： C07D245/04 , C07D255/04 , C07D273/08 , C07D273/02 , C07D487/02 , C07D209/18 , C07D209/88 , C07C233/31 , C07K5/06 , C07K5/08 , C07K5/10 , A61K38/12 , A61K38/06 , A61P31/04 , C07D209/86 , C07D487/04 , C07C229/36 , C07C233/47 , C07C237/22 , C07C251/24
CPC分类号： C07C229/36 , A61K38/00 , C07C233/47 , C07C237/22 , C07C251/24 , C07C279/14 , C07D209/86 , C07D245/04 , C07D255/04 , C07D273/02 , C07D487/04 , C07K5/06086 , C07K5/06095 , C07K5/0812 , C07K5/1016
摘要： A compound of the formula (I):

wherein
A is an aromatic or heteroaromatic ring system or partially or fully reduced derivatives thereof;
Q is hydrogen, C 1 -C 12 straight chain, branched or cyclic alkyl substituted with one or more hydroxy groups, or a mono- or di-saccharide moiety;
Z is -CR 10 R 11 -, -NR 12 -, -C(O)O-, -C(O)NR 12 - or -O-, where R 10 and R 11 are independently selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 6 -C 10 aryl, C 1 -C 6 alkoxy and -N(R 13 ) 2 and where each R 13 is independently selected from hydrogen and C 1 -C 6 alkyl, and where R 12 is selected from hydrogen and C 1 -C 6 alkyl; R 1 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -NR(R 13 ) 2 and -N(R 12 )-COR 14 ; where R 12 and R 13 are as defined above, and where R 14 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy and -NR 12 ;
R 2 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -N(R 13 ) 2 and -N(R 12 )-COCHR 2a R 2b ; where R 2a and R 2b are selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -N(R 13 ) 2 and -N(R 12 )-COR 14 ; where R 12 , R 13 and R 14 are as defined above;
R 3 , R 4 and R 5 are independently selected from hydrogen, C 1 -C 6 alkyl and α side chains of α-amino acids or their enantiomers or their derivatives;
R 6 is -CO 2 R 15 , -CONHR 16 , -CONHOR 16 , -CONHNHR 16 , -SO 2 N(R 16 ) 2 , -SO 2 R 17 or -P(O)(OR 18 )(OR 18 ) where each R 15 , R 16 , R 17 and R 18 is independently selected from hydrogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 6 -C 10 aryl and C 7 -C 10 arylalkyl;
B is an α-amino acid residue, a β-amino acid residue or an α,α-disubstituted amino acid residue, such residue forming amide linkages with the adjacent molecules;
W is -O- or CR 10 R 11 where R 10 and R 11 are as defined above;
Y is an optionally substituted amino group, a moiety containing an optionally substituted amino group or a salt thereof:
------ is a single or double bond;
R 7 and R 8a are hydrogen or are absent if ------ is a double bond; and
R 8b and R 9 are hydrogen, and X is selected from (CR 10 R 11 ) u , -(CR 10 R 11 ) u -CH=CH-, -NR 12 (CR 10 R 11 ) u -, -(CR 10 R 11 ) u NR 12 -, -O(CR 10 R 11 ) u -, -(CR 10 R 11 ) u O- or -O(CR 10 R 11 )CH=CH- where R 10 , R 11 and R 12 are as defined above; or
R 8b and R 9 together form a covalent bond between X and the carbon to which R 8b is attached, and X is selected from (CR 10 R 11 ) x , -NR 12 (CR 10 R 11 ) x -, -(CR 10 R 11 ) x NR 12 -, -O(CR 10 R 11 ) x - or -(CR 10 R 11 ) x O-, where R 10 , R 11 and R 12 are as defined above;
n, m, r and t are independently selected from 0 or 1;
s is an integer selected from 0 to 3;
p is an integer selected from 0 to 6, provided that when W is -O-, p is at least 1; and u, x and q are independently selected from 0 to 4;
and salts and pharmaceutically acceptable derivatives thereof.
The compound of formula (I) are useful in the treatment of bacterial infections.

2. 发明授权

EP1289968B1 COMPOSES UREES CYCLIQUES ET LEUR PROCEDE DE PREPARATION 有权
标题翻译：环脲化合物和工艺及其
公开(公告)号：EP1289968B1
公开(公告)日：2008-02-20
申请号：EP01945420.6
申请日：2001-06-13
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , Immupharma (France) SA
发明人： RODRIGUEZ, Marc , GUICHARD, Gilles , PLAUE, Serge , SEMETEY, Vincent , SCHAFFNER, Arnaud-Pierre , BRIAND, Jean-Paul
IPC分类号： C07D255/02 , C07D487/04 , C07D255/04 , C07D259/00 , C07D487/14 , C07D243/04 , C07D239/10
CPC分类号： C07D239/10 , C07D243/04 , C07D255/02 , C07D255/04 , C07D259/00 , C07D487/04 , C07D487/14 , Y02P20/55
摘要： The invention concerns a method for preparing cyclic urea compounds from at least an activated carbamic acid derivative containing an unprotected primary or secondary amine function, comprising a cyclization step which consists in a reaction between the primary or secondary amine function and the carbamic acid function of said carbamic acid derivative(s).

3. 发明公开

EP1640368A2 Composés urées cycliques et leur procédé de préparation 审中-公开
标题翻译： ZYKLISCHE HARNSTOFFVERBINDUNGEN UND VERFAHREN ZU DEREN HERSTELLUNG
公开(公告)号：EP1640368A2
公开(公告)日：2006-03-29
申请号：EP05015015.0
申请日：2001-06-13
申请人： The Centre National de la Recherche Scientifique , NEOMPS
发明人： Guichard, Gilles , Plaue, Serge , Semetey, Vincent , Schaffner, Arnaud-Pierre , Briand, Jean-Paul , Rodriguez, Marc
IPC分类号： C07D255/02 , C07D487/04 , C07D255/04 , C07D259/00 , C07D487/14 , C07D243/04 , C07D239/10 , C07D255/00 , C07D209/00
CPC分类号： C07D239/10 , C07D243/04 , C07D255/02 , C07D255/04 , C07D259/00 , C07D487/04 , C07D487/14 , Y02P20/55
摘要： La présente invention a pour objet un procédé de préparation de composés urées cycliques à partir d'au moins un dérivé activé d'acide carbamique contenant une fonction amine primaire ou secondaire non protégée, comprenant une étape de cyclisation par réaction entre la fonction amine primaire ou secondaire et la fonction acide carbamique dudit ou desdits dérivés d'acide carbamique.
摘要翻译：来自活性氨基甲酸衍生物（II）的环状脲化合物（I）的制备是新的。含有未被保护的伯或仲胺官能团的活性氨基甲酸衍生物（II）的环状脲化合物（I）的制备涉及选择性地脱保护含有受保护的伯或仲胺官能团的活性氨基甲酸衍生物（III）通过保护基团的裂解或转化，并通过氨基和氨基甲酸的功能之间的反应环化（II）。一些化合物（I）是新的。还包括以下独立权利要求：（1）具有至少7个（优选7-50个，特别是7-20个）含有至少一个酰胺官能团和至少一个酰胺官能团的环的新的环状脲化合物（I'）尿素功能，这些功能中的每一个与最接近的酰胺或脲官能团分开至少1C（优选1-4℃）; 和（2）式（I“）或（I”“）的新的环状三脲和四脲化合物。 Q 1 -Q 16H或天然或非天然氨基酸的任选受保护的侧链; 条件是排除以下化合物（除非另有说明，Q 1〜Q 16为H）：（I“; Q 3-Q 5，Q 7 -Q 9，Q 11 = Me），（I”; Q 3 ，Q 5，Q 7，Q 9，Q 11 = Me），（I“'; Q 2，Q 6，Q 10，Q 14 = Me）和（I”'; Q 2，Q 4，Q 6，Q 8，Q 10，Q 12，Q 14，Q 16 = Me）。活性：病毒抗HIV。作用机制：HIV蛋白酶抑制剂; 因子Xa抑制剂。

4. 发明公开

EP0792880A4 OSTEOPOROSIS REMEDY AND TRIAZEPINE COMPOUND 失效
标题翻译：骨质疏松症药物-AND TRIAZEPINVERBINDUNG
公开(公告)号：EP0792880A4
公开(公告)日：1998-03-25
申请号：EP95938016
申请日：1995-11-15
申请人： JAPAN TOBACCO INC
发明人： NAKAMURA TAKESHI , KOGA YOSHIHISA , SHINDO MASANORI
IPC分类号： C07D255/04 , C07D401/06 , C07D487/04 , C07D495/04 , C07D495/14 , A61K31/55 , C07D409/12
CPC分类号： C07D401/06 , C07D255/04 , C07D487/04 , C07D495/04 , C07D495/14
摘要： An osteoporosis remedy containing a triazepine compound represented by general formula (I) or a salt thereof as the active ingredient; novel triazepine compounds; and intermediate compounds for producing the same, wherein: R1 represents aryl or heteroaryl; R2 represents hydrogen, hydroxy, halogeno or lower alkyl; R4 represents hydrogen or halogeno, or R?2 and R4¿ together with the carbon atom to which they are bonded from carbonyl; R3 represents hydrogen, lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, -X-Y (wherein X represents -(CH¿2?)m-, -CO-, -COCH2-, -NH-, -NHCH2-, -CH2NH-, -CH2NHCO-, -OCH2-, -(CH2)nO- or -CH2S; and Y represents halogeno, cycloalkyl, aryl or heteroaryl), etc.; and A represents a benzene or thiophene ring. The compound has such an excellent effect of inhibiting bone resorption that it is useful as an osteoporosis remedy.

5. 发明授权

EP0102580B1 Substituted 1,3,4-benzotriazepines, a method of preparing the same and theire use as medicaments 有权
标题翻译：取代1,3,4-苯并噻唑类，其制备方法及其作为药物使用
公开(公告)号：EP0102580B1
公开(公告)日：1986-04-09
申请号：EP83108291.2
申请日：1983-08-23
申请人： HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED
发明人： Martin, Lawrence Leo , Setescak, Linda Louise
IPC分类号： C07D255/04 , A61K31/55
CPC分类号： C07C243/00 , C07D255/04

6. 发明公开

EP3089966A1 NEW SUBSTITUTED BIPHENYL ANALOGUES AS DUAL INHIBITORS OF AROMATASE AND SULFATASE 有权转让
标题翻译： NEUETITUIERTE BIPHENYLANALOGA ALS DUALE INHIBITOREN VON AROMATASE UND SULFATASE
公开(公告)号：EP3089966A1
公开(公告)日：2016-11-09
申请号：EP13900631.6
申请日：2013-12-31
申请人： Beaufour Ipsen Tianjin Pharmaceutical Co., Ltd
发明人： AUVIN, Serge , LAVERGNE, Olivier , CHAO, Qi , CHEN, Yufeng
IPC分类号： C07D249/18 , C07D247/02 , C07D255/04 , A61K31/395 , A61P35/00
摘要： These compounds acting as aromatase and sulfatase inhibitors, they are particularly useful for treating pathological conditions or diseases in which aromatase and sulfatase are involved. Moreover, the present invention provides processes for the preparation of these compounds. The invention also relates to pharmaceutical compositions containing said products and their use for the preparation of a medicament, in particular for the treatment of diseases characterized by aromatase and sulfatase activity such as hormone-dependent cancers.
摘要翻译：这些化合物作为芳香酶和硫酸酯酶抑制剂，特别适用于治疗涉及芳香酶和硫酸酯酶的病理状况或疾病。此外，本发明提供了制备这些化合物的方法。本发明还涉及含有所述产品的药物组合物及其用于制备药物的用途，特别是用于治疗以芳香酶和硫酸酯酶活性为特征的疾病如激素依赖性癌症。

7. 发明公开

EP2195303A4 3-SUBSTITUTED 1,2,3-TRIAZIN-4-ONE'S AND 3-SUBSTITUTED 1,3-PYRIMIDINONE'S FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 审中-公开
标题翻译： 3-取代的1,2,3-三嗪-4-酮和3-取代的1,3- PYRIMIDIONE用于增加谷氨酸能突触REACTIONS
公开(公告)号：EP2195303A4
公开(公告)日：2011-07-20
申请号：EP08831417
申请日：2008-09-19
申请人： CORTEX PHARMA INC
发明人： MUELLER RUDOLF , STREET LESLIE J , RACHWAL STANISLAW , ALISALA KASHINATHAM
IPC分类号： C07D255/04 , C07D239/88
CPC分类号： C07D487/04

8. 发明公开

EP2195303A2 3-SUBSTITUTED 1,2,3-TRIAZIN-4-ONE'S AND 3-SUBSTITUTED 1,3-PYRIMIDINONE'S FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 审中-公开
标题翻译： 3-取代的1,2,3-三嗪-4-酮和3-取代的1,3- PYRIMIDIONE用于增加谷氨酸能突触REACTIONS
公开(公告)号：EP2195303A2
公开(公告)日：2010-06-16
申请号：EP08831417.4
申请日：2008-09-19
申请人： CORTEX PHARMACEUTICALS, INC.
发明人： MUELLER, Rudolf , STREET, Leslie, J. , RACHWAL, Stanislaw , ALISALA, Kashinatham
IPC分类号： C07D255/04 , C07D239/88
CPC分类号： C07D487/04
摘要： This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke- induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

9. 发明授权

EP1091942B1 POTASSIUM CHANNEL BLOCKING AGENTS 有权
标题翻译：钾通道阻断剂
公开(公告)号：EP1091942B1
公开(公告)日：2005-03-30
申请号：EP99931019.6
申请日：1999-07-01
申请人： NEUROSEARCH A/S
发明人： TEUBER, Lene , OLESEN, S ren-Peter , STR B K, Dorte , JENSEN, Bo, Skaaning , PETERS, Dan
IPC分类号： C07D235/30 , C07D417/04 , C07D403/10 , C07D417/12 , C07D219/08 , C07D255/04 , C07D239/42 , C07D487/18 , C07D235/20 , C07D279/18 , A61K31/415 , A61K31/425 , A61K31/435 , A61K31/395 , A61K31/505 , A61K31/155
CPC分类号： C07D235/24 , C07C279/18 , C07D219/08 , C07D235/20 , C07D235/30 , C07D239/42 , C07D255/04 , C07D403/10 , C07D417/04 , C07D417/12

10. 发明公开

EP0792880A1 OSTEOPOROSIS REMEDY AND TRIAZEPINE COMPOUND 失效
标题翻译： OSTEOPOROSIS-MEDIKAMENT UND TRIAZEPINVERBINDUNG
公开(公告)号：EP0792880A1
公开(公告)日：1997-09-03
申请号：EP95938016.3
申请日：1995-11-15
申请人： Japan Tobacco Inc.
发明人： NAKAMURA, Takeshi, Central Phar. Res. Ins. of , KOGA, Yoshihisa, Central Phar. Res. Ins. of Japan , SHINDO, Masanori, Central Phar. Res. Ins. of Japan
IPC分类号： C07D487/04 , C07D495/14 , C07D495/04 , C07D255/04 , C07D401/06 , C07D409/12 , A61K31/55
CPC分类号： C07D401/06 , C07D255/04 , C07D487/04 , C07D495/04 , C07D495/14
摘要： Therapeutic agents for osteoporosis comprising, as an active ingredient, a triazepine compound of the formula [I]
wherein R 1 is aryl or heteroaryl; R 2 is hydrogen atom, hydroxy, halogen atom or lower alkyl; R 4 is hydrogen atom or halogen atom, or R 2 and R 4 form carbonyl combinedly together with the carbon atom to which they bond; R 3 is hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, -X-Y wherein X is -(CH 2 ) m -, -CO-, -COCH 2 -, -NH-, -NHCH 2 -, -CH 2 NH-, -CH 2 NHCO-, -OCH 2 -, -(CH 2 ) n O- or -CH 2 S- and Y is halogen atom, cycloalkyl, aryl or heteroaryl; and A is benzene ring or thiophene ring, or a salt thereof, novel triazepine compounds, and intermediate triazepine compounds for producing these triazepine compounds. The triazepine compounds of the formula [I] have superior bone resorption-inhibitory action and are useful as therapeutic agents for osteoporosis.
摘要翻译：用于骨质疏松症的治疗剂包括作为活性成分的下式的三氮化合物其中R 1为芳基或杂芳基; R 2是氢原子，羟基，卤素原子或低级烷基; R 4是氢原子或卤素原子，或者R 2和R 4与它们键合的碳原子一起形成羰基; R 3是氢原子，低级烷基，低级烷氧基，环烷基，芳基，杂芳基，-XY，其中X是 - （CH 2）m - ， - CO - ， - COCH 2 - ， - NH - ， - NHCH 2 - ， - CH 2 NH - ， - CH 2 NHCO - ， - OCH 2 - ， - （CH 2）n O-或-CH 2 S-，Y是卤素原子，环烷基，芳基或杂芳基; A是苯环或噻吩环，或其盐，新的三氮化合物和用于制备这些三氮化合物的中间体三氮化合物。式ÄIÜ的三氮化合物具有优异的骨吸收抑制作用，可用作骨质疏松症的治疗剂。

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