公开(公告)号：EP2527328A1

公开(公告)日：2012-11-28

申请号：EP12181441.2

申请日：2009-03-31

Applicant: Abbott GmbH & Co. KG ,  Abbott Laboratories, Inc.

Inventor： Amberg, Wilhelm ,  Ochse, Michael ,  Lange, Udo ,  Braje, Wilfried ,  Behl, Berthold ,  Hornberger, Wilfried ,  Mezler, Mario ,  Hutchins, Charles W.

IPC: C07D217/18 ,  C07D401/06 ,  C07D401/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04 ,  C07D513/04 ,  A61K31/472 ,  A61P25/28

CPC classification number: C07D217/18 ,  C07D401/04 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I)

or a physiologically tolerated salt thereof.
The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.

Abstract translation: 本发明涉及式（I）的四氢异喹啉或其生理上耐受的盐。 本发明涉及包含这种四氢异喹啉的药物组合物以及用于治疗目的的这种四氢异喹啉的用途。 四氢异喹啉是GlyT1抑制剂。

公开(公告)号：EP1306373B1

公开(公告)日：2007-05-16

申请号：EP01953336.3

申请日：2001-07-30

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： OGAWA, Mikio, Minase Res.Inst.,Ono Pharm.Co,Ltd. ,  TAKAOKA, Y., Minase Res. Inst.Ono Pharm.Co,Ltd. ,  OHHATA, Akira, Minase Res. Inst., Ono Pharm.Co,Ltd

IPC: C07D217/16 ,  C07D405/06 ,  C07D409/06 ,  C07D221/20 ,  C07D491/107 ,  C07D471/10 ,  C07D401/06 ,  C07D413/06 ,  C07D417/06 ,  C07D405/04 ,  C07D401/04 ,  C07D217/18 ,  C07D491/10 ,  C07D471/04 ,  C07D265/16 ,  C07D495/04 ,  A61K31/435 ,  A61K31/495

CPC classification number: C07D221/20 ,  A61K31/472 ,  A61K31/4725 ,  C07D217/16 ,  C07D217/18 ,  C07D265/14 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04

Abstract: 3,4-Dihydroisoquinoline derivative compounds represented by the following general formula (I) (wherein each symbol has the meaning as specified in the description) or nontoxic salts thereof. Because of having a CB2 receptor agonist activity, the compounds represented by the general formula (I) are useful in preventing and/or treating various diseases, for example, asthma, nasal allergy, atopic dermatitis, autoimmune diseases, rheumatish, immnodeficiency, postoperative pain and carcinomatous pain.

公开(公告)号：EP1397350B1

公开(公告)日：2007-02-28

申请号：EP02724438.3

申请日：2002-04-30

Applicant: Kudos Pharmaceuticals Limited ,  Maybridge Limited

Inventor： MARTIN, Niall M. B., Kudos Pharmaceuticals Limited ,  SMITH, Graeme C. M., Kudos Pharmaceuticals Limited ,  WHITE, Charles Richard ,  NEWTON, Roger Frank, Maybridge plc ,  DOUGLAS, Diane Gillian ,  EVERSLEY, Penny Jane ,  WHITTLE, Alan John, Maybridge plc

IPC: C07D217/18 ,  C07D217/20 ,  C07D417/12 ,  C07D417/14 ,  C07D409/12 ,  C07D407/08 ,  C07D403/12 ,  A61K31/47 ,  A61P35/00

CPC classification number: C07D401/12 ,  A61K31/47 ,  A61K31/4725 ,  C07D217/24 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

Abstract: The use of a compound of the formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of PARP, wherein A and B together represent an optionally substituted, fused aromatic ring, the dotted line between the 3 and 4 positions indicates the optional presence of a double bond, at least one of RC1 and RC2 is independently represented by -L-RL, and if one of RC1 and RC2 is not represented by -L-RL, then that group is H, where L is of formula: -(CH2)¿n1¿-Q¿n2?-(CH2)n3-wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and each Q (if n2 is greater than 1) is selected from O, S, NR3, C(=O), or -CR1R2-, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, -(CH2)n3- (if present) and part of RL, and where R3 is selected from H or C1-7 alkyl, and RL is selected from optionally substituted C3-20 heterocyclyl, C5-20 aryl and carbonyl, and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, C5-20 aryl, hydroxy, ether, nitro, amino, thioether, sulfoxide and sulfone.

公开(公告)号：EP1300464A4

公开(公告)日：2006-02-01

申请号：EP01947898

申请日：2001-07-06

Applicant: EISAI CO LTD

Inventor： TSUKAHARA KAPPEI ,  HATA KATSURA ,  SAGANE KOJI ,  NAKAMOTO KAZUTAKA ,  TSUCHIYA MAMIKO ,  WATANABE NAOAKI ,  OBA FUMINORI ,  TSUKADA ITARU ,  UEDA NORIHIRO ,  TANAKA KEIGO ,  KAI JUNKO

IPC: A61K31/00 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/44 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/5377 ,  A61K38/00 ,  A61P31/10 ,  C07D213/68 ,  C07D217/18 ,  C07D217/20 ,  C07D491/048 ,  C07D491/056 ,  C07K14/37 ,  C07K14/38 ,  C07K14/39 ,  C07K14/395 ,  C07K14/40 ,  C12N15/09 ,  A61K39/395 ,  A61K45/00 ,  C07K16/14 ,  C12N15/31 ,  G01N33/15 ,  G01N33/50

CPC classification number: C07K14/40 ,  A61K31/00 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/44 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/5377 ,  A61K38/00 ,  C07D213/68 ,  C07D217/18 ,  C07D217/20 ,  C07K14/37 ,  C07K14/38 ,  C07K14/39 ,  C07K14/395 ,  C07K2319/02 ,  G01N2500/00 ,  Y10S435/911

Abstract: A reporter system reflecting the transport process of GPI anchor protein to cell wall is constructed and a compound inhibiting this process is found out. Further, a gene imparting tolerance to the above compound is identified and a method of screening a compound inhibiting the activity of the protein encoded by this gene is developed. Thus, it is clarified by the novel compound that antifungal agents depending on a novel mechanism, wherein the transport process of GPI anchor protein to cell wall is inhibited, are available.

公开(公告)号：EP1611104A1

公开(公告)日：2006-01-04

申请号：EP04722563.6

申请日：2004-03-23

Applicant: Actelion Pharmaceuticals Ltd.

Inventor： AISSAOUI, Hamed ,  CLOZEL, Martine ,  WELLER, Thomas ,  KOBERSTEIN, Ralf ,  SIFFERLEN, Thierry ,  FISCHLI, Walter

IPC: C07D217/02 ,  C07D217/18 ,  C07D217/20 ,  C07D405/06 ,  C07D217/04 ,  C07D217/16 ,  A61P3/04 ,  A61P25/20 ,  A61K31/472

CPC classification number: C07D217/02 ,  C07D217/04 ,  C07D217/16 ,  C07D217/18 ,  C07D217/20 ,  C07D405/06

Abstract: The invention relates to novel acetamide derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.

Abstract translation: 本发明涉及式（I）的新型乙酰胺衍生物及其在制备药物组合物中作为活性成分的用途。 本发明还涉及相关方面，包括制备这些化合物的方法，含有一种或多种这些化合物的药物组合物，特别是它们作为食欲素受体拮抗剂的用途。

公开(公告)号：EP1373212A4

公开(公告)日：2004-06-23

申请号：EP01964673

申请日：2001-03-29

Applicant: MOLECULAR DESIGN INT

Inventor： FELLER DENNIS R ,  MILLER DUANE D

IPC: C07D217/18 ,  C07D217/20 ,  C07D217/02 ,  A61K31/47

CPC classification number: C07D217/18 ,  C07D217/20

Abstract: Compounds which are highly potent and highly specific β3-Adrenoreceptor agonists are provided. The compounds are formulated into pharmaceutical preparations and administered for stimulating, regulating and modulating metabolism of fats in adipose tissues in animals, particularly humans and other mammals. The compounds of the invention have the structure (A). R1 and R2 are each independently members selected from the group consisting of H, OH, C1, NO2, CH3SO2NH, NH2, CH3O and weak acids of the structure R7-NH, where R7 is an acyl group, wherein at least one of R1 and R2 is OH. It is generally preferred that R2 be OH; R3, R4 and R5 are variously and independently members selected from I, Br, C1, F, OCH3, CH3, alkyl, alkylaryl, aminoalkyl, thioalkyl, and O-alkyl. Preferably, R4 and R5 are each a halogen, the same or different; R6 is an acid moiety which forms an acid salt with the NH group. R6 is desirably HC1 or (COOH)2. While the racemic mixtures are active, selective, and bioavailable, we have found that the isolated isomers are ordinarily of more particular interest. The S(-) isomers are preferred, as they will be found to have the highest selectivity and the highest bioavailability. The R(+) isomers are also of interest, as the R-isomers are in some cases easier to isolate. The compounds are formulated into pharmaceutical carriers to serve as highly selective, effective and safe β3-Adrenoreceptor agonists to provide long term weight control. In humans, the compositions are administered to control body fat levels, and to maintain acceptable body fat levels over time. In domesticated animals, the compositions are administered to attain desirably low fat content in carcass meats intended for human consumption.

Abstract translation: 提供了高度有效和高度特异性β3-肾上腺素受体激动剂的化合物。 将这些化合物配制成药物制剂并施用用于刺激，调节和调节动物特别是人和其他哺乳动物脂肪组织中脂肪的代谢。 本发明的化合物具有结构（A）。 R 1和R 2各自独立地选自H，OH，Cl，NO 2，CH 3 SO 2 NH，NH 2，CH 3 O和结构R 7 -NH的弱酸，其中R 7为酰基，其中R 1和R 2中的至少一个 R2是OH。 一般优选R2为OH; R 3，R 4和R 5各自独立地选自I，Br，C 1，F，OCH 3，CH 3，烷基，烷基芳基，氨基烷基，硫代烷基和O-烷基。 优选地，R4和R5各自是相同或不同的卤素; R6是与NH基团形成酸式盐的酸性部分。 R6优选为HCl或（COOH）2。 尽管外消旋混合物具有活性，选择性和生物可利用性，但我们发现分离的异构体通常更具特殊意义。 S（ - ）异构体是优选的，因为它们将被发现具有最高的选择性和最高的生物利用度。 R（+）异构体也是有意义的，因为R-异构体在某些情况下更容易分离。 将这些化合物配制成药物载体，作为高度选择性，有效和安全的β3-肾上腺素受体激动剂，以提供长期的体重控制。 在人体中，施用组合物以控制体内脂肪水平，并随时间维持可接受的体脂肪水平。 在家养动物中，施用组合物以达到预期供人食用的屠体肉中理想的低脂肪含量。

公开(公告)号：EP1397350A1

公开(公告)日：2004-03-17

申请号：EP02724438.3

申请日：2002-04-30

Applicant: Kudos Pharmaceuticals Limited ,  Maybridge Limited

Inventor： MARTIN, Niall M. B.,Kudos Pharmaceuticals Limited ,  SMITH, Graeme C. M.,Kudos Pharmaceuticals Limited ,  WHITE, Charles Richard ,  NEWTON, Roger Frank,Maybridge plc ,  DOUGLAS, Diane Gillian ,  EVERSLEY, Penny Jane ,  WHITTLE, Alan John,Maybridge plc

IPC: C07D217/18 ,  C07D217/20 ,  C07D417/12 ,  C07D417/14 ,  C07D409/12 ,  C07D407/08 ,  C07D403/12 ,  A61K31/47 ,  A61P35/00

CPC classification number: C07D401/12 ,  A61K31/47 ,  A61K31/4725 ,  C07D217/24 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

Abstract: The use of a compound of the formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of PARP, wherein A and B together represent an optionally substituted, fused aromatic ring, the dotted line between the 3 and 4 positions indicates the optional presence of a double bond, at least one of RC1 and RC2 is independently represented by -L-RL, and if one of RC1 and RC2 is not represented by -L-RL, then that group is H, where L is of formula: -(CH2)¿n1¿-Q¿n2?-(CH2)n3-wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and each Q (if n2 is greater than 1) is selected from O, S, NR3, C(=O), or -CR1R2-, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, -(CH2)n3- (if present) and part of RL, and where R3 is selected from H or C1-7 alkyl, and RL is selected from optionally substituted C3-20 heterocyclyl, C5-20 aryl and carbonyl, and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, C5-20 aryl, hydroxy, ether, nitro, amino, thioether, sulfoxide and sulfone.

公开(公告)号：EP1020445A4

公开(公告)日：2001-06-20

申请号：EP98945593

申请日：1998-10-02

Applicant: EISAI CO LTD

Inventor： UENO KOHSHI ,  SASAKI ATSUSHI ,  KAWANO KOKI ,  OKABE TADASHI ,  KITAZAWA NORITAKA ,  TAKAHASHI KEIKO ,  YAMAMOTO NOBORU ,  SUZUKI YUICHI ,  MATSUNAGA MANABU ,  KUBOTA ATSUHIKO

IPC: C07D217/22 ,  C07D217/24 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04 ,  C07D217/14 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  C07D217/16 ,  C07D217/18 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

CPC classification number: C07D401/04 ,  C07D217/22 ,  C07D217/24 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04

Abstract: Clinically highly useful drugs having an antagonism to serotonin, in particular, central muscle relaxing drugs for treating, ameliorating or preventing spastic paralysis or ameliorating myotonia and comprising fused pyridine derivatives represented by general formula (I), pharmacologically acceptable salts thereof or hydrates of either (I) or (1), wherein the ring A represents a benzene, pyridine, thiophene or furan ring; and B represents (2).

公开(公告)号：EP1069901A4

公开(公告)日：2001-06-13

申请号：EP99917374

申请日：1999-04-08

Applicant: SMITHKLINE BEECHAM CORP ,  NPS PHARMA INC

Inventor： BHATNAGAR PRADIP KUMAR ,  CALLAHAN JAMES FRANCIS ,  DEL MAR ERIC G ,  LAGO MARIA AMPARO

IPC: A61K31/18 ,  A61K31/235 ,  A61K31/275 ,  A61K31/343 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/47 ,  A61K31/472 ,  A61K31/5377 ,  A61P1/02 ,  A61P3/12 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  C07C255/54 ,  C07D213/38 ,  C07D215/12 ,  C07D217/14 ,  C07D307/79 ,  A61K31/535 ,  A01N43/02 ,  A01N43/40 ,  A01N43/42 ,  C07D211/70 ,  C07D211/72 ,  C07D217/12 ,  C07D217/16 ,  C07D217/18 ,  C07D307/02

CPC classification number: C07D307/79 ,  C07C255/54 ,  C07D213/38 ,  C07D215/12 ,  C07D217/14

公开(公告)号：EP0541946A1

公开(公告)日：1993-05-19

申请号：EP92116761.5

申请日：1992-09-30

Applicant: HOECHST AKTIENGESELLSCHAFT

Inventor： Jacobi, Detlef, Dr. ,  Jendralla, Joachim-Heiner, Dr. ,  Kammermeier, Bernhard, Dr.

IPC: C07C269/06 ,  C07C271/20 ,  C07C315/04 ,  C07C317/44 ,  C07D217/18 ,  C07C213/00

CPC classification number: C07C271/20 ,  C07C213/00 ,  C07C269/00 ,  C07C271/22 ,  C07C315/04 ,  C07D217/16 ,  C07D217/18 ,  C07C317/44

Abstract: Es wird ein Verfahren zur Herstellung von optisch reinen symmetrischen Verbindungen der Formel I

beschrieben, worin R¹, R² und R³ in der Beschreibung erläutert sind, unter gleichzeitiger Kontrolle der vier mit * gekennzeichneten Chiralitätszentren.

Abstract translation: 描述了制备式I“IMAGE”的光学纯对称化合物的方法，其中R 1，R 2和R 3在说明书中解释，同时控制四个中心 手势标记*。