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1. 发明申请

WO2003064428A1 FURANO- AND THIENOPYRIMIDINES AS NEUROKINASE INHIBITORS 审中-公开
标题翻译：作为神经营养因子抑制剂的呋喃丙酮和三烯丙基嘧啶
公开(公告)号：WO2003064428A1
公开(公告)日：2003-08-07
申请号：PCT/DK2003/000054
申请日：2003-01-28
申请人： H. LUNDBECK A/S , ROTTLÄNDER, Mario , GRAVEN, SAMMS, Anette , FELDING, Jakob , PEDERSEN, Jan, Torleif , ANDERSEN, Kim , MOLTZEN, Ejner, Knud , LANGGÅRD, KRISTENSEN, Jesper , BALLE, Thomas
发明人： ROTTLÄNDER, Mario , GRAVEN, SAMMS, Anette , FELDING, Jakob , PEDERSEN, Jan, Torleif , ANDERSEN, Kim , MOLTZEN, Ejner, Knud , LANGGÅRD, KRISTENSEN, Jesper , BALLE, Thomas
IPC分类号： C07D495/04
CPC分类号： C07D491/04 , C07D495/04
摘要： The invention provides in one embodiment the use of a compound represented by the general formula I wherein the variable groups are as defined in the claims or a pharmaceutically acceptable acid addition salt thereof for the preparation of a medicament for the treatment of Parkinson's Disease, dementia such as age related dementia, HIV-1 associated dementia, AIDS dementia complex, HIV encephalopathy and senile dementia of the Alzheimer's type and memory disorders, cerebral ischemias and spinal cord ischemias, ischemias following stroke or traumatic injuries of the brain or the spinal cord, Huntington Chorea, multiple sclerosis, glaucoma, promotion of survival of transplanted cells, ALS/Motor neuron Disease, neuronal trauma or age related macular degeneration. The patent provides in another embodiment for novel compounds of general formula I. The patent provides in yet another embodiment for a pharmaceutical composition comprising a compound of general formula I. The compounds of the invention are neurokinase inhibitors.
摘要翻译：本发明在一个实施方案中提供了由通式I表示的化合物的用途，其中可变基团如权利要求中所定义，或其药学上可接受的酸加成盐用于制备用于治疗帕金森病，痴呆的痴呆作为年龄相关性痴呆，HIV-1相关性痴呆，艾滋病痴呆综合征，艾滋病毒性脑病和老年痴呆症的老年痴呆症和记忆障碍，脑缺血和脊髓缺血，脑缺血或脑或脊髓创伤后的缺血，亨廷顿 Chorea，多发性硬化，青光眼，促进移植细胞存活，ALS /运动神经元疾病，神经元损伤或年龄相关性黄斑变性。该专利在另一个实施方案中提供了通式I的新化合物。该专利在另一个实施方案中提供了包含通式I化合物的药物组合物。本发明化合物是神经激酶抑制剂。

2. 发明申请

WO0149678A9 SUBSTITUTED PHENYL-PIPERAZINE DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译：取代的苯基哌嗪衍生物，其制备和使用
公开(公告)号：WO0149678A9
公开(公告)日：2002-10-10
申请号：PCT/DK0000721
申请日：2000-12-20
申请人： LUNDBECK & CO AS H , RUHLAND THOMAS , KROG-JENSEN CHRISTIAN , ROTTLAENDER MARIO , MIKKELSEN GITTE , ANDERSEN KIM , MOLTZEN EJNER KNUD
发明人： RUHLAND THOMAS , KROG-JENSEN CHRISTIAN , ROTTLAENDER MARIO , MIKKELSEN GITTE , ANDERSEN KIM , MOLTZEN EJNER KNUD
IPC分类号： A61K31/496 , A61K31/5377 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P43/00 , C07D209/14 , C07D405/12 , C07D471/04 , C07D403/02 , C07D403/14 , C07D405/14 , C07D413/14
CPC分类号： C07D405/12 , C07D209/14 , C07D471/04
摘要： The present invention provides compounds of formula (I): wherein R -R , X, Y, Z, n and m are defined in the application.The compounds of the invention have affinity for the 5-HT1A receptor.
摘要翻译：本发明提供了式（I）化合物：其中R 1 -R 8，X，Y，Z，n和m定义在本申请中。本发明化合物对5-HT1A受体具有亲和力。

3. 发明申请

WO1995012591A1 PHENYLINDOLE COMPOUNDS 审中-公开
标题翻译：苯乙烯化合物
公开(公告)号：WO1995012591A1
公开(公告)日：1995-05-11
申请号：PCT/DK1994000407
申请日：1994-10-28
申请人： H. LUNDBECK A/S , PERREGAARD, Jens, Kristian , MOLTZEN, Ejner, Knud , ANDERSEN, Kim , PEDERSEN, Henrik , BOGESO, Klaus, Peter , PERNET, Andre , BOPP, Barbara , MULFORD, Darcy , SAKAMOTO, Kiyoshi
发明人： H. LUNDBECK A/S
IPC分类号： C07D401/14
CPC分类号： C07D401/14
摘要： Phenylindole compound having general formula (I), wherein R -R are independently hydrogen, deuterium, halogen, alkyl, aryl, hydroxy, alkoxy, aryloxy, alkylthio and arylthio; or R and R and/or R and R constitute an oxo or thioxo group; or R and R and/or R and R , respectively, are joined together to form a 3-8 membered spiro ring; are non-cataleptogenic 5-HT2 receptor antagonists in vivo and show in a model indicative of antipsychotic effect. Thus the compounds may be useful in the treatment of psychosis, depression, negative symptoms of schizophrenia, hypertension or extrapyramidal side effects induced by antipsychotic drugs.
摘要翻译：具有通式（I）的苯基吲哚化合物，其中R 1 -R 4独立地是氢，氘，卤素，烷基，芳基，羟基，烷氧基，芳氧基，烷硫基和芳硫基; 或R 1和R 2和/或R 3和R 4构成氧代或硫代基团; 或R 1和R 2和/或R 3和R 4分别连接在一起形成3-8元螺环; 在体内是非催产素的5-HT2受体拮抗剂，并在表现抗精神病作用的模型中显示。因此，这些化合物可用于治疗由精神抑制药物引起的精神病，抑郁症，精神分裂症的阴性症状，高血压或锥体束外副作用。

4. 发明申请

WO2003029232A1 PHENYL-PIPERAZINE DERIVATIVES AS SEROTONIN REUPTAKE INHIBITORS 审中-公开
标题翻译：作为丝氨酸还原抑制剂的苯基哌嗪衍生物
公开(公告)号：WO2003029232A1
公开(公告)日：2003-04-10
申请号：PCT/DK2002/000659
申请日：2002-10-02
申请人： H. LUNDBECK A/S , RUHLAND, Thomas , SMITH, Garrick, Paul , BANG-ANDERSEN, Benny , PÜSCHL, Ask , MOLTZEN, Ejner, Knud , ANDERSEN, Kim
发明人： RUHLAND, Thomas , SMITH, Garrick, Paul , BANG-ANDERSEN, Benny , PÜSCHL, Ask , MOLTZEN, Ejner, Knud , ANDERSEN, Kim
IPC分类号： C07D295/096
CPC分类号： C07D295/145 , C07D211/20 , C07D211/70 , C07D243/08 , C07D295/033 , C07D295/096
摘要： The invention provides compounds represented by the general formula I Iwherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
摘要翻译：本发明提供由通式I I表示的化合物，其中取代基在本申请中定义。这些化合物可用于治疗情感障碍，包括抑郁症，焦虑症，包括一般焦虑症，惊恐障碍和强迫症。

5. 发明申请

WO2002102387A1 TREATMENT OF NEUROPATHIC PAIN 审中-公开
标题翻译：治疗神经痛PAIN
公开(公告)号：WO2002102387A1
公开(公告)日：2002-12-27
申请号：PCT/DK2002/000407
申请日：2002-06-18
申请人： H. LUNDBECK A/S , SANCHEZ, Connie , MOLTZEN, Ejner, Knud
发明人： SANCHEZ, Connie , MOLTZEN, Ejner, Knud
IPC分类号： A61K31/537
CPC分类号： A61K31/537 , A61K31/547
摘要： The present invention relates the use of a spiro-piperidine compounds for the preparation of a medicament useful for the treatment of neuropathic pain.
摘要翻译：本发明涉及螺哌啶化合物在制备用于治疗神经性疼痛的药物中的用途。

6. 发明申请

WO01049678A1 SUBSTITUTED PHENYL-PIPERAZINE DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译：取代的苯基哌嗪衍生物，其制备和使用
公开(公告)号：WO01049678A1
公开(公告)日：2001-07-12
申请号：PCT/DK2000/000721
申请日：2000-12-20
申请人： H. LUNDBECK A/S , RUHLAND, Thomas , KROG-JENSEN, Christian , ROTTLÄNDER, Mario , MIKKELSEN, Gitte , ANDERSEN, Kim , MOLTZEN, Ejner, Knud
发明人： RUHLAND, Thomas , KROG-JENSEN, Christian , ROTTLÄNDER, Mario , MIKKELSEN, Gitte , ANDERSEN, Kim , MOLTZEN, Ejner, Knud
IPC分类号： C07D403/02
CPC分类号： C07D405/12 , C07D209/14 , C07D471/04
摘要： The present invention provides compounds of formula (I): wherein R 1 -R 8 , X, Y, Z, n and m are defined in the application.The compounds of the invention have affinity for the 5-HT 1A receptor.
摘要翻译：本发明提供了式（I）化合物：其中R 1 -R 8，X，Y，Z，n和m定义在本申请中。本发明化合物对5-HT1A受体具有亲和力。

7. 发明申请

WO1995033729A1 SEROTONIN 5-HT1A AND DOPAMIN D2 RECEPTOR LIGANDS 审中-公开
标题翻译： SEROTONIN 5-HT1A和DOPAMIN D2受体配体
公开(公告)号：WO1995033729A1
公开(公告)日：1995-12-14
申请号：PCT/DK1995000229
申请日：1995-06-08
申请人： H. LUNDBECK A/S , PERREGAARD, Jens, Kristian , MOLTZEN, Ejner, Knud
发明人： H. LUNDBECK A/S
IPC分类号： C07D233/32
CPC分类号： C07D401/06 , C07D233/32 , C07D233/36
摘要： The present invention relates to a novel series of 4-phenylpiperazines, 4-phenyl-piperidines and 4-phenyl-1,2,3,6-tetrahydropyridines compound of general formula (I) wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene; R is a C3-10 alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R - R are optional substituents; R and R are hydrogen, alkyl or together form an ethylene or propylene bridge; W is O or S; V is O, S, CR R , or NR wherein R , R , and R are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R and R constitute a 3-7 membered spiroring; Z is -(CH2)m-, m being 2 or 3 or Z is -CH=CH-; X is N, C or CH; show effects on central serotonin 5-HT1A and dopamine D2 receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders in particular psychosis.
摘要翻译：本发明涉及一种新的一系列4-苯基哌嗪，4-苯基 - 哌啶和4-苯基-1,2,3,6-四氢吡啶类化合物，其中A是亚烷基，亚烯基，亚炔基和C3 -7亚环烷基; R 1是C 3-10烷基，烯基或炔基，环烷（烯）基，环烷基（烯）基 - 烷（烯/炔）基，三氟甲基磺酰基或烷基磺酰基，R 2 -R 5 >是任选的取代基; R 9和R 10是氢，烷基或一起形成乙烯或丙烯桥; W为O或S; V是O，S，CR 6 R 7或NR 8，其中R 6，R 7和R 8是氢或烷基，烯基，环烷基，环烷基烷基，任选取代的芳基烷基或芳基，或R 6和R 7构成3-7元的激发; Z是 - （CH 2）m - ，m是2或3或Z是-CH = CH-; X为N，C或CH; 显示对中枢5-羟色胺5-HT1A和多巴胺D2受体的影响。因此，这些新化合物可用于治疗某些精神病和神经系统疾病，特别是精神病。

8. 发明申请

WO2003002556A1 NOVEL HETEROARYL DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译：新型异构体衍生物，其制备和使用
公开(公告)号：WO2003002556A1
公开(公告)日：2003-01-09
申请号：PCT/DK2002/000435
申请日：2002-06-27
申请人： H. LUNDBECK A/S , ROTTLÄNDER, Mario , MOLTZEN, Ejner, Knud , MIKKELSEN, Ivan , RUHLAND, Thomas , ANDERSEN, Kim , KROG-JENSEN, Christian
发明人： ROTTLÄNDER, Mario , MOLTZEN, Ejner, Knud , MIKKELSEN, Ivan , RUHLAND, Thomas , ANDERSEN, Kim , KROG-JENSEN, Christian
IPC分类号： C07D405/12
CPC分类号： C07D401/12 , C07D405/12 , C07D409/14 , C07D413/12
摘要： A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disorders, and neurological disorders such as psychosis.
摘要翻译：具有式（I）的杂芳基衍生物。本发明的化合物被认为可用于治疗诸如一般性焦虑障碍，恐慌症，强迫症，抑郁症，社交恐惧症和进食障碍以及诸如精神病之类的神经障碍的实质性疾病。

9. 发明申请

WO2003002552A1 NOVEL INDOLE DERIVATIVES 审中-公开
标题翻译：新的印度衍生物
公开(公告)号：WO2003002552A1
公开(公告)日：2003-01-09
申请号：PCT/DK2002/000436
申请日：2002-06-27
申请人： H. LUNDBECK A/S , ROTTLÄNDER, Mario , MOLTZEN, Ejner, Knud , MIKKELSEN, Ivan , RUHLAND, Thomas , ANDERSEN, Kim , KROG-JENSEN, Christian
发明人： ROTTLÄNDER, Mario , MOLTZEN, Ejner, Knud , MIKKELSEN, Ivan , RUHLAND, Thomas , ANDERSEN, Kim , KROG-JENSEN, Christian
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D403/12 , C07D409/14
摘要： A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disorders, and neurological disorders such as psychosis.
摘要翻译：具有式（I）的杂芳基衍生物。认为本发明的化合物可用于治疗情绪障碍，例如一般性焦虑障碍，恐慌症，强迫症，抑郁症，社交恐惧症和进食障碍以及神经障碍如精神病。

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