CN1354662A - 奥桑唐特在用于治疗心情疾病的药物制剂中的应用 - Google Patents

奥桑唐特在用于治疗心情疾病的药物制剂中的应用 Download PDF

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Publication number
CN1354662A
CN1354662A CN00806091A CN00806091A CN1354662A CN 1354662 A CN1354662 A CN 1354662A CN 00806091 A CN00806091 A CN 00806091A CN 00806091 A CN00806091 A CN 00806091A CN 1354662 A CN1354662 A CN 1354662A
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treatment
osanetant
application
depression
milligrams
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CN00806091A
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X·埃蒙兹-阿尔特
P·索布里
R·斯坦伯格
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Sanofi Aventis France
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Sanofi Synthelabo SA
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

本发明涉及奥桑唐特及其药学可接受盐在制备治疗心情障碍,特别是抑郁症有效的药物中的应用。

Description

奥桑唐特在用于治疗心情疾病的药物制剂中的应用
本发明的目的是奥桑唐特(Osanetant)的新应用。
奥桑唐特是下式(R)-(+)-N-[(3-(1-苯甲酰基-3-(3，4-二氯苯基)哌啶-3-基)丙基)-4-苯基哌啶-4-基]-N-甲基乙酰胺的国际通用名(D.C.I.)：
在欧洲专利申请EP 673 928中已描述这种化合物及其药学可接受的盐。
这些化合物描述作为人类NK3受体选择性拮抗剂在治疗与多巴胺能的和去甲肾上腺素能系统的机能障碍相关的疾病是有效的。
现在已发现，奥桑唐特及其药学可接受的盐在治疗心情失调，特别是治疗抑郁症是有效的。关于抑郁症，尤其应当理解是严重抑郁症、轻微抑郁症、心理沮丧症、与焦虑相关的抑郁症以及与双相性精神障碍(troubles bipolaires)相关的抑郁症。
曾研究过奥桑唐特对18-65岁病人的严重抑郁症的效果。这些病人服用奥桑唐特(200毫克/天)约6个星期。
抑郁症状的改善可使用Hamilton标准记分大大降低来进行度量(J.Neurol.Neurosurg.Psychiat.，1960，23，56-62)以及通过临床医生收集的视觉印象和病人的总体视觉印象进行判断。
因此，本发明的目的是使用奥桑唐特及其药学可接受的盐在制备治疗心情障碍，特别是抑郁症有效的药物中的应用。
根据欧洲专利申请EP 673 928制备奥桑唐特及其药学可接受的盐，同样地，根据这同一专利申请的说明书可以制备药物组合物。
以口服、舌下含服、皮下、肌肉内、静脉内、经皮的、局部或直肠方式使用本发明的药物组合物，动物或人可以使用呈单一用药形式或与通常的药物载体混合形式的单一的或与其他活性成分配合的活性成分。合适的单一用药形式包括口服形式，如片剂、胶囊、粉剂、颗粒剂和口服液或悬液，舌下含服形式和经口腔用药形式、气雾剂、植入物、皮下、经皮、肌肉内、静脉内、鼻内的用药形式和直肠用药形式。
本发明化合物的每天用量是0.05-5毫克/千克，有利地是1-2.5毫克/千克，优选地是2-2.5毫克/千克，可一次或多次使用。这些化合物一般配制成每剂量单位含有2.5-500毫克，有利地是50-250毫克，优选地是100-250毫克活性组分的剂量单位，根据需要，可分一次、二次或多次使用。尽管这些剂量是一般情况的实例，但其中包括特定的情况，其中更高或更低的剂量是合适的这样的剂量也属于本发明。根据通常的实际情况，每个病人的合适剂量应由医生根据给药方式，所述病人的年龄、体重和反应情况进行确定。
根据本发明，口服形式是优选的。
本发明的化合物可以与其他活性成分配合使用，特别是另一种抗抑郁剂，如锂盐，三环抗抑郁剂、单胺氧化酶抑制剂或血清素再捕获(再摄取)抑制剂。
本发明还涉及一种给病人服用适当剂量的奥桑唐特或其药学可接受盐治疗心情障碍的方法，更具体地涉及治疗抑郁症的方法。
实施例1：250毫克奥桑唐特胶囊
奥桑唐特                            250毫克
一水合乳糖(200目)                   40.80毫克
玉米淀粉                            40.80毫克
聚乙烯吡咯烷酮(povidone)K-30        8.40毫克
纯化水*                            90.00毫克
硬脂酸镁                            3.40毫克
对于O形不透明白色胶囊，填充到       343.4毫克
*在湿制粒之后蒸发至干。
实施例2：100毫克奥桑唐特胶囊
奥桑唐特                            100毫克
一水合乳糖(200目)                   115.80毫克玉米淀粉                            115.80毫克聚乙烯吡咯烷酮(povidone)K-30        8.40毫克纯化水*                            90.00毫克硬脂酸镁                            3.40毫克对于O形不透明白色胶囊，填充到       343.4毫克*在湿制粒之后蒸发至干。

Claims (7)

1、奥桑唐特及其药学可接受盐用于在制备治疗心情障碍的药物中的应用。
2、根据权利要求1所述的在治疗抑郁症中的应用。
3、根据权利要求2所述的在治疗严重抑郁症中的应用。
4、根据权利要求2所述的在治疗心理沮丧症中的应用。
5、根据权利要求2所述的在治疗轻微抑郁症中的应用。
6、根据权利要求2所述的在治疗与焦虑相关的抑郁症中的应用。
7、根据权利要求2所述的在治疗与双相性精神障碍相关的抑郁症中的应用。
CN00806091A 1999-04-13 2000-04-11 奥桑唐特在用于治疗心情疾病的药物制剂中的应用 Pending CN1354662A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR9904699A FR2792199B3 (fr) 1999-04-13 1999-04-13 Utilisation de l'osanetant pour la preparation de medicaments utiles dans le traitement des troubles de l'humeur
FR99/04699 1999-04-13

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CN1354662A true CN1354662A (zh) 2002-06-19

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US (1) US6420388B1 (zh)
EP (1) EP1175215A2 (zh)
JP (1) JP2002541190A (zh)
KR (1) KR20010105418A (zh)
CN (1) CN1354662A (zh)
AR (1) AR023452A1 (zh)
AU (1) AU3971600A (zh)
BG (1) BG105984A (zh)
BR (1) BR0009704A (zh)
CA (1) CA2369638A1 (zh)
CZ (1) CZ20013645A3 (zh)
EE (1) EE200100527A (zh)
FR (1) FR2792199B3 (zh)
HR (1) HRP20010741A2 (zh)
HU (1) HUP0200655A3 (zh)
ID (1) ID30458A (zh)
IS (1) IS6098A (zh)
MX (1) MXPA01010340A (zh)
NO (1) NO20014953L (zh)
PE (1) PE20010032A1 (zh)
PL (1) PL351554A1 (zh)
SK (1) SK14552001A3 (zh)
TR (1) TR200102930T2 (zh)
WO (1) WO2000061125A2 (zh)
ZA (1) ZA200108289B (zh)

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AU7552401A (en) * 2000-06-12 2001-12-24 Univ Rochester Method of treating symptoms of hormonal variation, including hot flashes, using tachykinin receptor antagonist
PL1711530T3 (pl) * 2003-12-22 2010-01-29 Glaxo Group Ltd Immunoglobuliny neutralizujące Nogo-A do leczenia chorób neurologicznych
WO2005094801A1 (en) * 2004-03-25 2005-10-13 Smithkline Beecham Corporation Use of an nk3 antagonist for the treatment of bipolar disorders
WO2006098488A1 (ja) * 2005-03-15 2006-09-21 Sumitomo Chemical Company, Limited 気分障害による疾患症状を改善させる方法
JP2006320201A (ja) * 2005-05-17 2006-11-30 Sumitomo Chemical Co Ltd 気分障害又は関連障害による疾患症状を改善させる方法
GB0525662D0 (en) 2005-12-16 2006-01-25 Glaxo Group Ltd Immunoglobulins
EP3915560A1 (en) 2014-06-25 2021-12-01 Emory University Methods of managing conditioned fear with neurokinin receptor antagonists

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2719311B1 (fr) 1994-03-18 1998-06-26 Sanofi Sa Composés antagonistes sélectifs du récepteur NK3 humain et leur utilisation comme médicaments et outils de diagnostic.
FR2729954B1 (fr) 1995-01-30 1997-08-01 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
FR2738819B1 (fr) 1995-09-14 1997-12-05 Sanofi Sa Nouveaux composes antagonistes selectifs du recepteur nk3 humain, procede pour leur obtention et compositions pharmaceutiques les contenant
WO1998011090A2 (en) * 1996-09-16 1998-03-19 Warner-Lambert Company 3-alkyl-3-phenyl-piperidines

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BR0009704A (pt) 2002-01-08
CA2369638A1 (en) 2000-10-19
PE20010032A1 (es) 2001-04-11
ID30458A (id) 2001-12-06
FR2792199A1 (fr) 2000-10-20
KR20010105418A (ko) 2001-11-28
AU3971600A (en) 2000-11-14
AR023452A1 (es) 2002-09-04
HUP0200655A2 (hu) 2002-07-29
WO2000061125A3 (fr) 2001-04-19
WO2000061125A2 (fr) 2000-10-19
CZ20013645A3 (cs) 2002-01-16
ZA200108289B (en) 2002-12-24
FR2792199B3 (fr) 2001-05-18
NO20014953D0 (no) 2001-10-11
SK14552001A3 (sk) 2002-02-05
EE200100527A (et) 2002-12-16
BG105984A (bg) 2002-04-30
EP1175215A2 (fr) 2002-01-30
MXPA01010340A (es) 2002-05-06
PL351554A1 (en) 2003-05-05
HUP0200655A3 (en) 2002-11-28
US6420388B1 (en) 2002-07-16
NO20014953L (no) 2001-12-11
JP2002541190A (ja) 2002-12-03
IS6098A (is) 2001-09-28
HRP20010741A2 (en) 2002-10-31
TR200102930T2 (tr) 2002-04-22

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