公开(公告)号：US06586441B2

公开(公告)日：2003-07-01

申请号：US09788956

申请日：2001-02-20

申请人： Edilio Maurizio Borroni ,  Gerda Huber-Trottmann ,  Gavin John Kilpatrick ,  Roger David Norcross

发明人： Edilio Maurizio Borroni ,  Gerda Huber-Trottmann ,  Gavin John Kilpatrick ,  Roger David Norcross

IPC分类号： A61K31505

CPC分类号： C07D239/42 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  C07D213/85 ,  C07D231/12 ,  C07D233/56 ,  C07D239/47 ,  C07D239/48 ,  C07D239/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D495/04

摘要： The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.

摘要翻译： 本发明涉及含有至少一个氮原子的环状杂芳族化合物及其在制备用于治疗与腺苷受体调节剂诸如阿尔茨海默氏病，帕金森病，神经保护，精神分裂症，焦虑症等相关的疾病的药物中的用途， 疼痛，呼吸困难，抑郁症，哮喘，过敏反应，缺氧，局部缺血，癫痫发作，物质滥用，镇静作用，并且它们可能作为肌肉松弛剂，抗精神病药，抗癫痫药，抗惊厥药和心脏保护剂起作用。

公开(公告)号：US06355653B1

公开(公告)日：2002-03-12

申请号：US09645127

申请日：2000-08-24

申请人： Gerda Huber Trottmann ,  Walter Hunkeler ,  Roland Jakob-Roetne ,  Gavin John Kilpatrick ,  Matthias Heinrich Nettekoven ,  Claus Riemer

发明人： Gerda Huber Trottmann ,  Walter Hunkeler ,  Roland Jakob-Roetne ,  Gavin John Kilpatrick ,  Matthias Heinrich Nettekoven ,  Claus Riemer

IPC分类号： A61K314439

CPC分类号： C07D471/04

摘要： The invention relates to compounds of formula wherein R1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, —(CH2)nOH, halogen or lower alkoxy, and wherein the heteroaryl groups may be optionally linked to the pyrazole ring via an alkylene or alkenyl group, or is phenyl, optionally substituted by one or two substituents being lower alkyl, hydroxy-lower alkyl, halogen, hydroxy or lower alkoxy or is —O(CH2)n,phenyl, benzofuryl, indolyl or benzothiophenyl, or is —S-lower alkyl; R2 and R4 are independently from each other hydrogen, cyano or —S(O)2-phenyl; R3 is hydrogen, halogen or is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, —(CH2)n-aryl, hydroxy, halogen, lower alkoxy, morpholinyl, amino, lower alkylamino or —C(O)NR′2, and wherein R′ is lower alkyl or hydrogen, or is phenyl, optionally substituted by one or two substituents being halogen, lower alkyl, lower alkoxy, amino, di-lower alkyl amino, CF3, —OCF3, —NHC(O)lower alkyl, cyano, —C(O)-lower alkyl, —C(O)O-lower alkyl, —S-lower alkyl, —S(O)2NH-phenyl, —S(O)2-methylpiperazinyl; or is —NR′R″, wherein R′ and R″ are independently from each other hydrogen, —(CH2)nphenyl, which phenyl ring is optionally substituted by halogen or lower alkoxy, —CH(lower alkyl)-phenyl, indan-1-yl, 1,2,3,4-tetrahydro-naphthalen, or cycloalkyl; or is —O-phenyl, which phenyl ring is optionally substituted by halogen, lower alkyl or lower alkoxy, —O-tetrahydronaphthalenyl or —O—CH2-6-methyl-pyridin-2-yl; or is -benzo[1,3]dioxolyl, -1H-indol-5-yl, naphthyl, benzofuran-2-yl, 1,3,4,9-tetrahydro-b-carbolin-2-yl, piperidin-1-yl, pyrrolidin-1-yl, piperazin-4-yl-methyl or morpholinyl; R5 is —NR2, wherein R may be the same or different and is hydrogen, lower alkyl, phenyl, benzyl, —CO-lower alkyl, —CO-lower alkoxy, -lower alkenyl, —CO(CH2)n-phenyl or —COO(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by CF3, lower alkoxy, halogen or lower alkyl, —CO(CH2)3-NHCO-lower alkoxy, —(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by lower alkoxy, CF3 or halogen, or is 4,5-dihydro-1H-imidazol-2-yl-benzoic acid, 1,4,5,6-tetrahydro-pyrimidin-2-yl-benzoic acid or 4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-yl-benzoic acid; n is 0-4 and their pharmaceutically acceptable salts