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31. 发明授权

EP1592684B1 MALONAMIDE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS 有权
标题翻译： MALONAMIDDERIVATE伽马分泌酶
公开(公告)号：EP1592684B1
公开(公告)日：2008-07-30
申请号：EP04705404.4
申请日：2004-01-27
申请人： F. Hoffmann-La Roche AG
发明人： GALLEY, Guido , GOERGLER, Annick , JACOBSEN, Helmut , KITAS, Eric, Argirios , PETERS, Jens-Uwe
IPC分类号： C07D401/06 , C07D217/06 , C07D403/06 , C07D471/08 , C07D401/04 , C07D471/04 , C07D471/06 , C07D209/44 , C07D209/18 , C07D223/18 , C07D401/12 , C07D405/12 , C07D409/12 , C07C237/12 , C07C237/14
CPC分类号： C07C237/22 , C07C233/47 , C07C323/41 , C07C2601/14 , C07D209/18 , C07D209/44 , C07D215/227 , C07D217/06 , C07D223/18 , C07D243/12 , C07D243/14 , C07D243/24 , C07D265/30 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/06
摘要： The invention relates to malonamide derivatives of formula (IA) or (IB) and to pharmaceutically suitable acid addition salts thereof. The compounds are Ϝ-secretase inhibitors and the related compounds may be useful in the treatment of Alzheimer's disease.

32. 发明公开

EP1711470A1 MALONAMIDE DERIVATIVES BLOCKING THE ACTIVTIY OF GAMMA-SECRETASE 有权
标题翻译：阻断γ-分泌酶活性的氨基乙酰衍生物
公开(公告)号：EP1711470A1
公开(公告)日：2006-10-18
申请号：EP04764665.8
申请日：2004-08-31
申请人： F. HOFFMANN-LA ROCHE AG
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
IPC分类号： C07D223/18 , C07D223/16 , C07D243/14 , C07D313/14 , A61K31/5513 , A61K31/55
CPC分类号： C07D223/16 , A61K31/335 , A61K31/55 , A61K31/5513 , C07D223/20 , C07D243/24 , C07D273/00 , C07D313/14
摘要： The invention relates to malonamide derivatives of formula (I), wherein: R1 is one of the following groups (Formulae a), b), c), d)); R2 is lower alkyl, lower alkinyl, -(CH2)n-O-lower alkyl, -(CH2)n-S-lower alkyl, -(CH2)n-CN, -(CR'R')n-CF3, -(CR'R')n-CHF2, -(CR'R')n-CH2F, -(CH2)n-C(O)O-lower alkyl, -(CH2)n-halogen, or is -(CH2)n-cycloalkyl, optionally substituted by one or more substituents, selected from the group consisting of phenyl, halogen or CF3; R',R' are independently from n and from each other hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R3, R4 are independently from each other hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; R5 is hydrogen, lower alkyl, -(CH2)n-CF3 or -(CH2)n-cycloalkyl; R6 is hydrogen or halogen; R7 is hydrogen or lower alkyl; R8 is hydrogen, lower alkyl, lower alkinyl, -(CH2)n-CF3,-(CH2)n-cycloalkyl or -(CH2)n-phenyl, optionally substituted by halogen; R9 is hydrogen, lower alkyl, -C(O)H, -C(O)-lower alkyl, -C(O)-CF3,-C(O)-CH2F,-C(O)-CHF2,-C(O)-cycloalkyl,-C(O)-(CH2)n-O-lower alkyl,-C(O)O-(CH2)n-cycloalkyl, -C(O)-phenyl, optionally substituted by one or more substituents selected from the group consisting of halogen or -C(O)O-lower alkyl, or is -S(O)2-lower alkyl, -S(O)2-CF3,-(CH2)n-cycloalkyl or is -(CH2)n-phenyl, optionally substituted by halogen; n is 0, 1, 2, 3 or 4; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixture thereof. These compounds may be used for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及式（I）的丙二酰胺衍生物，其中：R 1为以下基团之一（式a），b），c），d））; （CH 2）n -S-低级烷基， - （CH 2）n -CN， - （CR'R'）n -CF 3， - （CR'R （CR'R'）n -CH 2 F， - （CH 2）n C（O）O-低级烷基， - （CH 2）n - 卤素或 - （CH 2）n - 由一个或多个选自苯基，卤素或CF 3的取代基取代; R'，R'独立地为n并且彼此独立地为氢，低级烷基，低级烷氧基，卤素或羟基; R3，R4彼此独立地为氢，低级烷基，低级烷氧基，苯基或卤素; R5是氢，低级烷基， - （CH2）n-CF3或 - （CH2）n-环烷基; R6是氢或卤素; R7是氢或低级烷基; R8为氢，低级烷基，低级炔基， - （CH2）n-CF3， - （CH2）n-环烷基或 - （CH2）n-苯基，任选被卤素取代; （O） - 低级烷基，-C（O）-CF 3，-C（O）-CH 2 F，-C（O）-CHF 2，-C（O） O） - 环烷基，-C（O） - （CH 2）n O-低级烷基，-C（O）O-（CH 2）n - 环烷基，-C（O） - 苯基，任选被一个或多个选自（O）O-低级烷基，或为-S（O）2 - 低级烷基，-S（O）2 -CF 3， - （CH 2）n - 环烷基或 - （CH 2）任选被卤素取代的N-苯基; n是0,1,2,3或4; 并涉及药学上合适的酸加成盐，旋光纯对映体，外消旋体或其非对映体混合物。这些化合物可以用于治疗阿尔茨海默氏病。

33. 发明公开

EP1323711A4 NOVEL PHENYLALANINE DERIVATIVES 有权
标题翻译：新的苯丙氨酸衍生物
公开(公告)号：EP1323711A4
公开(公告)日：2004-03-31
申请号：EP01970268
申请日：2001-09-28
申请人： AJINOMOTO KK
发明人： SUZUKI NOBUYASU , YOSHIMURA TOSHIHIKO , IZAWA HIROYUKI , SAGI KAZUYUKI , MAKINO SHINGO , NAKANISHI EIJI , MURATA MASAHIRO , TSUJI TAKASHI
IPC分类号： A61K31/395 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/435 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/438 , A61K31/4412 , A61K31/45 , A61K31/472 , A61K31/48 , A61K31/4985 , A61K31/55 , A61P1/00 , A61P3/10 , A61P7/06 , A61P9/00 , A61P11/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D207/38 , C07D207/44 , C07D207/452 , C07D209/46 , C07D209/48 , C07D209/52 , C07D209/66 , C07D209/76 , C07D211/88 , C07D217/24 , C07D217/26 , C07D221/14 , C07D221/20 , C07D223/10 , C07D223/18 , C07D403/12 , C07D471/04 , C07D487/04 , C07D495/04 , A61K31/41
CPC分类号： C07D207/452 , A61K31/395 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/435 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/438 , A61K31/4412 , A61K31/45 , A61K31/472 , A61K31/48 , A61K31/4985 , A61K31/55 , C07D207/38 , C07D209/46 , C07D209/48 , C07D209/52 , C07D209/66 , C07D209/76 , C07D211/88 , C07D217/24 , C07D217/26 , C07D221/14 , C07D221/20 , C07D223/10 , C07D223/18 , C07D403/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof which have an effect of inhibiting α4 integrin and, therefore, are useful as remedies or preventives for inflammatory diseases wherein the α4 integrin-dependent adhesion process participates in the pathological conditions, for example, rheumatoid arthritis, inflammatory intestinal diseases, systemic lupus erythematosus, multiple sclerosis, Sjoegren's disease, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arteriosclerosis, restenosis, tumor proliferation, tumor metastasis and rejection in transplantation.

34. 发明公开

EP1313426A4 SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF A-BETA PROTEIN PRODUCTION 审中-公开
标题翻译：琥珀酰胺基苯并二氮杂-α-ALS抑制剂A-β蛋白制备
公开(公告)号：EP1313426A4
公开(公告)日：2003-05-28
申请号：EP99964322
申请日：1999-12-23
申请人： BRISTOL MYERS SQUIBB PHARMA CO
发明人： OLSON RICHARD E
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/00 , A61P25/28 , A61P43/00 , C07D223/16 , C07D223/18 , C07D243/12 , C07D243/14 , C07D243/24 , C07D401/04 , A61K6/00
CPC分类号： C07D223/16 , C07D243/12 , C07D243/14 , C07D243/24 , C07D401/04
摘要： This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Abeta-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to beta-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译：本发明涉及具有式（I）的新型内酰胺及其药物组合物及其使用方法。这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地说，抑制Aβ-肽的产生，从而起到防止淀粉样蛋白神经沉积形成的作用。更具体地说，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合症。

35. 发明公开

EP1268434A1 CYCLIC LACTAMS AS INHIBITORS OF A-BETA PROTEIN PRODUCTION 审中-公开
标题翻译： ZYKLISCHE LACTAME ALS A-BETA PROTEINPRODUKTIONSINHIBITOREN
公开(公告)号：EP1268434A1
公开(公告)日：2003-01-02
申请号：EP01926583.4
申请日：2001-04-03
申请人： Bristol-Myers Squibb Pharma Company
发明人： YANG, Michael, G. , LIU, Hong
IPC分类号： C07D223/18 , C07D243/24 , C07D407/12 , C07D243/14 , C07K5/06 , A61K38/00 , A61K31/55 , A61K31/5513 , A61P25/28
CPC分类号： C07D407/12 , A61K38/00 , C07D223/18 , C07D243/14 , C07D243/24 , C07K5/06078
摘要： This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

36. 发明公开

EP1230220A1 BETA-AMINOACID COMPOUNDS USEFUL FOR INHIBITING BETA-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS 审中-公开
标题翻译： BETA-氨基酸化合物FORβ淀粉样肽和/或它的合成来抑制释放
公开(公告)号：EP1230220A1
公开(公告)日：2002-08-14
申请号：EP00978213.7
申请日：2000-10-26
申请人： ELI LILLY AND COMPANY
发明人： AUDIA, James, Edmund , PORTER, Warren, Jaye , SCOTT, William, Leonard , STACK, Douglas, Richard , THOMPSON, Richard, Craig
IPC分类号： C07D223/18 , C07D223/16 , C07D243/12 , C07D243/24 , C07D267/14 , C07D281/10 , C07D487/04 , A61K31/5513 , A61K31/5517 , A61K31/551 , A61K31/554 , A61P25/28
CPC分类号： C07D409/12 , C07D223/18
摘要： The present invention relates β-aminoacid containing compounds of formula (I) which inhibit β-amyloid peptide release and/or its synthesis and are useful in treating Alzheimer's disease and cognition enhancement.

37. 发明公开

EP1042298A1 POLYCYCLIC ALPHA-AMINO-EPSILON-CAPROLACTAMS AND RELATED COMPOUNDS 审中-公开
标题翻译：多环芳烃α-氨基的EPSILON己内酰胺和相关化合物
公开(公告)号：EP1042298A1
公开(公告)日：2000-10-11
申请号：EP98956198.0
申请日：1998-10-29
申请人： Elan Pharmaceuticals, Inc. , ELI LILLY AND COMPANY
发明人： AUDIA, James, E. , MABRY, Thomas, E. , NISSEN, Jeffrey, S. , MCDANIEL, Stacey L.
IPC分类号： C07D223/18 , C07D471/06 , C07D471/04 , C07D471/08 , A61K31/55
CPC分类号： C07D471/04 , C07D223/18 , C07D471/06 , C07D471/08
摘要： Disclosed are polycyclic α-amino-⊂-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of β-amyloid peptide release and/or its synthesis.

38. 发明公开

EP0640592A1 N-acylated tricyclic azaheterorings useful as vasopressin antagonists 失效
标题翻译： N-Acylierte trizyklische azaheteroringe verwendbar als Vasopressin-Antagonisten。
公开(公告)号：EP0640592A1
公开(公告)日：1995-03-01
申请号：EP94111040.5
申请日：1994-07-15
申请人： AMERICAN CYANAMID COMPANY
发明人： Albright, Jay D. , Reich, Marvin F. , Sum, Fuk-Wah , Xuemei Du
IPC分类号： C07D221/12 , C07D225/08 , C07D223/18 , C07D267/16 , C07D281/16 , C07D281/18 , C07D243/38 , C07D245/04 , A61K31/55 , A61K31/435 , C07D498/04 , C07D487/04 , C07D495/04 , C07D513/04 , C07D471/04
CPC分类号： C07D401/12 , C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/16 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Tricyclic compounds of the general Formula I:

as defined herein which exhibit antagonist activity at V₁ and/or V₂ receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
摘要翻译：在V1和/或V2受体上表现出拮抗活性并显示体内血管加压素拮抗剂活性的通式I：的三环化合物，其用于治疗特征在于肾脏过度吸收水的疾病的方法，以及制备此类化合物的方法。

39. 发明公开

EP0309422A2 New amidino tricycle derivatives 失效
标题翻译：氨基甜菜碱衍生物
公开(公告)号：EP0309422A2
公开(公告)日：1989-03-29
申请号：EP88830374.0
申请日：1988-09-19
申请人： ISTITUTO DE ANGELI S.p.A.
发明人： Turconi, Marco , Donetti, Arturo , Cereda, Enzo , Quintero, Myrna Gil , Schiavi, Giovanni Battista , Micheletti, Rosamaria
IPC分类号： C07D471/04 , C07D223/26 , C07D223/18 , C07D243/38 , C07D495/04 , C07D403/06 , C07D401/06 , C07D451/00 , C07D519/00 , C07D405/06 , C07D403/12
CPC分类号： C07D451/02 , C07D223/20 , C07D223/26 , C07D223/28 , C07D243/38 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D471/04 , C07D495/04
摘要： New pharmacologically active amidino tricycle derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders of the following formula:
wherein
R represents a hydrogen atom or a halogen atom
X represents nitrogen or -CH-group
W represents a -NH-CO-, -CH=CH-, -CH₂-CH₂- group, oxygen or sulfur
R₁ represents a hydrogen atom or a C₁₋₄ alkyl group
n is 0 or 1
Y represents sulfur or a -CH- group
A represents carbon or nitrogen
B represents a -CH- group (provided that A is different from nitrogen), -COO-, -CO-, or -CH₂- group
m is 0 or an integer from 1 to 3
Z represents -NH-, -CO-, -COO- or -CH- group, or it is absent
p is 0 or 1
Het represents piperazinyl, homopiperazinyl, piperidinyl, tropyl or tetrahydropirimidinyl group, each group being optionally substituted by a C₁₋₄ alkyl group or an amino group
q is 0 or 1
R₂ represents a hydrogen atom, a C₁₋₄ alkyl group or an amino group optionally substituted by a linear or branched C₁₋₄ alkyl group or phenyl group
R₃ represents a linear or branched C₁₋₈alkyl group or a hydrogen atom (provided that the bond between Het and the group
is a carbon- carbon bond or A=C and B=CH), or
R₂ and R₃ may join together to form a heterocyclic 5-membered ring, tautomers thereof and acid addition salts of the aforesaid compounds.
The process for the preparation of the compounds of formula (I) as well as pharmaceuticals compositions containing them are also described.
摘要翻译：新的药理活性的脒基三环类衍生物作为毒蕈碱受体阻断剂，可用于治疗胃肠道疾病，具有下式：其中R表示氢原子或卤素原子X表示氮或-CH-基团W表示-NH -CO-，-CH = CH-，-CH 2 -CH 2 - 基，氧或硫R 1表示氢原子或C 1-4烷基n为0或1 Y表示硫或-CH-基团A表示碳或氮B表示-CH-基（A不同于氮），-COO-，-CO-或-CH 2 - 基团m为0或1-3的整数Z表示-NH-，-CO- ，-COO-或-CH-基团，或者不存在p是0或1 Het表示哌嗪基，高哌嗪基，哌啶基，丙基或四氢嘧啶基，每个基团任选被C 1-4烷基或氨基取代q是 0或1 R 2表示氢原子，C 1-4烷基或任选被直链或支链C 1-4烷基杂环取代的氨基或苯基R3表示直链或支链C 1-8烷基或氢原子（条件是Het和基团之间的键为碳 - 碳键或A = C和B = CH），或R2和 R3可以连接在一起形成杂环五元环，其互变异构体和上述化合物的酸加成盐。还描述了制备式（I）化合物的方法以及含有它们的药物组合物。

40. 发明公开

EP0192034A3 Dibenzazepinderivate, deren Herstellung, zu deren Herstellung dienende Ausgangsmaterialien und Verwendung der Dibenzazepinderivate als Schädlingsbekämpfungsmittel 失效
标题翻译：二苯甲酮衍生物，其制备，起始材料的制备和使用作为杀虫剂的二苯甲酮衍生物
公开(公告)号：EP0192034A3
公开(公告)日：1989-02-22
申请号：EP86100288.9
申请日：1986-01-10
申请人： CIBA-GEIGY AG
发明人： Bruderer, Hans, Dr. , Zurflüh, René, Dr.
IPC分类号： C07D223/18 , A01N43/46
CPC分类号： C07D223/18 , A01N47/42
摘要： Die Erfindung betrifft neue heterocyclische Verbindungen der Formel
worin R C 1-12 -Alkyl, C 3-12 -Alkenyl, C 3-12 -Alkinyl oder C 3-8 --Cycloalkyl und X Sauerstoff oder Schwefel bedeuten, und keine der allfälligen Mehrfachbindungen von R in a-Stellung zu X steht, und deren Säureadditionssalze, Verfahren zu deren Herstellung, Schädlingsbekämpfungsmittel, die diese Verbindungen als Wirkstoffe enthalten sowie die Verwendung solcher Verbindungen bzw. Mittel zur Bekämpfung von Schädlingen. Zudem betrifft die Erfindung zur Herstellung solcher Verbindungen dienende Ausgangsmaterialien.

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