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1. 发明申请

WO2009152868A1 6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW MAO INHIBITORS AND IMIDAZOLINE RECEPTOR LIGANDS 审中-公开
标题翻译： 6-1H-咪唑 - 喹唑啉和喹啉衍生物，新的MAO抑制剂和咪唑啉受体配体
公开(公告)号：WO2009152868A1
公开(公告)日：2009-12-23
申请号：PCT/EP2008/057908
申请日：2008-06-20
申请人： ROTTAPHARM S.P.A. , GIORDANI, Antonio , LANZA, Marco , CASELLI, Gianfranco , MANDELLI, Stefano , ZANZOLA, Simona , MAKOVEC, Francesco , ROVATI, Lucio, Claudio
发明人： GIORDANI, Antonio , LANZA, Marco , CASELLI, Gianfranco , MANDELLI, Stefano , ZANZOLA, Simona , MAKOVEC, Francesco , ROVATI, Lucio, Claudio
IPC分类号： A61K31/4178 , A61K31/517 , C07D213/00 , A61K31/485
CPC分类号： A61K31/517 , A61K31/4178 , A61K31/485 , C07D401/04 , C07D403/04 , C07D405/14 , A61K2300/00
摘要： The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2-heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical compositions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently selected from -CH group or a nitrogen atom (-N), W is independently selected from an aryl group, an heteroaryl group, or a benzocondensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzothiophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [l,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). R 1 is independently selected from hydrogen (-H), C 1 -C 4 alkyl, hydroxymethyl (-CH 2 OH), aminomethyl (-CH 2 NH 2 ), alkylaminomethyl [CH 2 NH(R 2 )], or di-alkylaminomethyl [CH 2 N(R 2 ) 2 ], trifiuoromethyl (-CF 3 ). Compounds of formula (I) elicited a pharmacological profile suitable for the clinical treatment of depression and related disorders, Parkinson disease, drug abuse, and morphine tolerance and dependence.
摘要翻译：本发明涉及6-（1H-咪唑-1-基）-2-芳基和2-杂芳基喹唑啉和喹啉衍生物，式（I）化合物，其药学上可接受的盐和溶剂化物以及相应的药物组合物，其作用作为单胺氧化酶（MAO）抑制剂和咪唑啉受体配体：其中：X独立地选自-CH基或氮原子（-N），W独立地选自芳基，杂芳基或苯并稠合的杂芳基，例如作为1,3-苯并间二氧杂环戊烯，苯并呋喃，2,3-二氢苯并呋喃，苯并噻吩，2,3-二氢苯并噻吩，吲哚，2,3-二氢吲哚，苯并咪唑，苯并恶唑，苯并噻唑，2H-3,4-二氢苯并吡喃，[1,4] 苯并二恶英，2,3-二氢 - [1,4] - 苯并二恶英（1,4-苯并二恶烷）。 R1独立地选自氢（-H），C1-C4烷基，羟甲基（-CH2OH），氨基甲基（-CH2NH2），烷基氨基甲基[CH2NH（R2）]或二烷基氨基甲基[CH2N（R2） CF3）。式（I）化合物引发适于临床治疗抑郁症和相关疾病，帕金森病，药物滥用和吗啡耐受性和依赖性的药理学特征。

2. 发明申请

WO2008014815A1 AMIDINE DERIVATIVES OF 2-HETEROARYL-QUINAZOLINES AND QUINOLINES; POTENT ANALGESICS AND ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译： 2-异喹啉和喹啉的氨基衍生物; POTENT ANALGESICS和抗炎药物
公开(公告)号：WO2008014815A1
公开(公告)日：2008-02-07
申请号：PCT/EP2006/064841
申请日：2006-07-31
申请人： ROTTAPHARM S.p.A. , GIORDANI, Antonio , MANDELLI, Stefano , ZANZOLA, Simona , TARCHINO, Francesca , CASELLI, Gianfranco , FIORENTINO, Teresa Simonetta , MAZZARI, Silvio , MAKOVEC, Francesco , ROVATI, Lucio Claudio
发明人： GIORDANI, Antonio , MANDELLI, Stefano , ZANZOLA, Simona , TARCHINO, Francesca , CASELLI, Gianfranco , FIORENTINO, Teresa Simonetta , MAZZARI, Silvio , MAKOVEC, Francesco , ROVATI, Lucio Claudio
IPC分类号： C07D405/04 , A61K31/517 , A61P29/00
CPC分类号： C07D405/04
摘要： The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation, to their pharmaceutical compositions and to the use of these compounds, salts and solvates thereof, along with the corresponding pharmaceutical compositions, for the treatment of pain and inflammatory disorders. Compounds of this invention are extremely potent analgesics, suitable for the treatment of both inflammatory and neuropathic pain. Particularly for the treatment of neuropathic pain the compounds of the invention have been proved largely superior to the standards currently in the clinical use. These compounds are not acting through inhibition of COX or NOS enzymes but are effective in inhibiting inflammatory cytokine production induced by inflammatory stimuli.
摘要翻译：本发明涉及通式（I）的2-杂芳基 - 喹唑啉和喹啉的新型脒衍生物，其制备方法，其药物组合物以及这些化合物，其盐和溶剂合物的用途以及相应的药物组合物，用于治疗疼痛和炎症性疾病。本发明的化合物是非常有效的止痛剂，适用于治疗炎性和神经性疼痛。特别是对于神经性疼痛的治疗，本发明的化合物已被证明在很大程度上优于目前在临床应用中的标准。这些化合物不是通过抑制COX或NOS酶而起作用，而是有效抑制由炎症刺激引起的炎性细胞因子产生。

3. 发明申请

WO2008014822A1 6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW POTENT ANALGESICS AND ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译： 6-1H-IMIDAZO-喹唑啉和喹啉衍生物，新的药物和抗炎药物
公开(公告)号：WO2008014822A1
公开(公告)日：2008-02-07
申请号：PCT/EP2006/065013
申请日：2006-08-03
申请人： ROTTAPHARM S.p.A. , GIORDANI, Antonio , MANDELLI, Stefano , VERPILIO, Ilario , ZANZOLA, Simona , TARCHINO, Francesca , CASELLI, Gianfranco , PIEPOLI, Tiziana , MAZZARI, Silvio , MAKOVEC, Francesco , ROVATI, Lucio Claudio
发明人： GIORDANI, Antonio , MANDELLI, Stefano , VERPILIO, Ilario , ZANZOLA, Simona , TARCHINO, Francesca , CASELLI, Gianfranco , PIEPOLI, Tiziana , MAZZARI, Silvio , MAKOVEC, Francesco , ROVATI, Lucio Claudio
IPC分类号： C07D401/04 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , A61K31/4709 , A61K31/517 , A61P29/00
CPC分类号： C07D413/14 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/14
摘要： The present invention is directed to novel 6-lH-imidazo-2- aryl and 2-heteroaryl quinazoline and quinoline of Formula (I), corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases.
摘要翻译：本发明涉及式（I）的新颖的6-1H-咪唑-2-基和2-杂芳基喹唑啉和喹啉，其相应的盐和溶剂合物，涉及其制备方法和该化合物及其相应的用于治疗疼痛和炎症相关疾病的药物组合物。除了具有显着的抗炎特性之外，本发明的化合物已经被证明在炎性和神经性疼痛的药理学治疗中都是非常有效的。它们在干扰COX-2和炎性细胞因子表达和产生方面的有效性，也将它们作为有趣的化合物，也用于治疗癌症以及多种炎性疾病。

4. 发明申请

WO2009109230A1 2-ARYL AND 2 -HETEROARYL 4H-1-BENZOPYRAN-4-ONE-6-AMIDINO DERIVATIVES FOR THE TREATMENT OF ARTHRITIS, CANCER AND RELATED PAIN 审中-公开
标题翻译：用于治疗ARTHRITIS，CANCER和相关疼痛的2-ARYL和2-HOTEROARYL 4H-1-苯并噻吩-4-酮-6-氨基吡啶衍生物
公开(公告)号：WO2009109230A1
公开(公告)日：2009-09-11
申请号：PCT/EP2008/052739
申请日：2008-03-06
申请人： ROTTAPHARM S.P.A. , GIORDANI, Antonio , VERPILIO, Ilario , PUCCI, Sabrina , ARTUSI, Roberto , CASELLI, Gianfranco , LANZA, Marco , MENNUNI, Laura , MAKOVEC, Francesco , ROVATI, Lucio, Claudio
发明人： GIORDANI, Antonio , VERPILIO, Ilario , PUCCI, Sabrina , ARTUSI, Roberto , CASELLI, Gianfranco , LANZA, Marco , MENNUNI, Laura , MAKOVEC, Francesco , ROVATI, Lucio, Claudio
IPC分类号： C07D311/30 , C07D401/04 , C07D405/10 , C07D407/04 , A61K31/352 , A61K31/4178 , A61K31/44 , A61P19/02 , A61P25/04 , A61P35/00
CPC分类号： C07D311/30 , C07D401/04 , C07D405/10 , C07D407/04
摘要： 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives of formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.
摘要翻译：式（I）的2-芳基和2-杂芳基4h-1-苯并吡喃-4-酮-6-脒基衍生物可用作治疗关节炎，癌症和相关疼痛的药理学。

5. 发明申请

WO2005105789A2 NOVEL PYRROLE DERIVATIVES WITH ANGIOTENSIN II ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有血管紧张素II拮抗剂活性的新型吡咯烷酮衍生物
公开(公告)号：WO2005105789A2
公开(公告)日：2005-11-10
申请号：PCT/EP2005/051911
申请日：2005-04-27
申请人： ROTTAPHARM S.p.A. , MAKOVEC, Francesco , ARTUSI, Roberto , GIORDANI, Antonio , ZANZOLA, Simona , ROVATI, Lucio Claudio
发明人： MAKOVEC, Francesco , ARTUSI, Roberto , GIORDANI, Antonio , ZANZOLA, Simona , ROVATI, Lucio Claudio
IPC分类号： C07D403/10
CPC分类号： C07D403/10
摘要： Compounds which may be represented by the general formula (I) shown below and in which: R 1 is a group independently selected from among: CHO, -COOH, -CH 2 OH R 2 is hydrogen or a linear or branched C 1 -C 6 alkyl group R 3 is hydrogen or a halogen group selected from among Cl and Br R 4 is a linear or branched C 3 -C 5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT 1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.
摘要翻译：可以由下述通式（I）表示的化合物，其中：R 1是独立地选自：CHO，-COOH，-CH 2 OH的基团R 2是氢或直链或支链C 1 -C 6烷基R 3是氢或选自Cl和Br R4中的卤素基团是直链或支链C 3 -C 5烷基及其药学上可接受的盐，例如钠盐或钾盐。该化合物显示出有效和选择性的所有拮抗剂活性，并且可用于治疗其中AT1受体的全部或过度表达的合成升高可能起主要病理作用的任何障碍，如在动脉高血压，充血性心功能不全，血小板与其相关的聚集和紊乱，例如心肌和脑梗死，肾缺血，静脉和动脉血栓形成，外周血管病变，肺动脉高压，糖尿病，糖尿病性神经病，青光眼和糖尿病性视网膜病变。

6. 发明申请

WO2009040331A3 AMIDINE, THIOUREA AND GUANIDINE DERIVATIVES OF 2-AMINOBENZOTHIAZOLES AND AMINOBENZOTHIAZINES FOR THEIR USE AS PHARMACOLOGICAL AGENTS FOR THE TREATMENT OF NEURODEGENERATIVE PATHOLOGIES 审中-公开
公开(公告)号：WO2009040331A3
公开(公告)日：2009-04-02
申请号：PCT/EP2008/062636
申请日：2008-09-22
申请人： ROTTAPHARM S.P.A. , ANZINI, Maurizio , GIORDANI, Antonio , MAKOVEC, Francesco , CAPPELLI, Andrea , VOMERO, Salvatore , CASELLI, Gianfranco , ROVATI, Lucio Claudio
发明人： ANZINI, Maurizio , GIORDANI, Antonio , MAKOVEC, Francesco , CAPPELLI, Andrea , VOMERO, Salvatore , CASELLI, Gianfranco , ROVATI, Lucio Claudio
IPC分类号： C07D277/82 , C07D279/16
摘要： The present invention relates to novel amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,l-4H-benzothiazines and 3- amino-l,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: Formula (I): and the use of said products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.

7. 发明申请

WO2008014821A1 3-SUBSTITUTED-1,5-DIARLY-2-ALKYL-PYRROLES HIGHLY SELECTIVE AND ORALLY EFFECTIVE COX-2 INHIBITORS 审中-公开
标题翻译： 3-取代的-1,5-二-2-甲基-2-吡咯烷酮高选择性和有效的COX-2抑制剂
公开(公告)号：WO2008014821A1
公开(公告)日：2008-02-07
申请号：PCT/EP2006/065011
申请日：2006-08-03
申请人： ROTTAPHARM S.P.A. , CAPPELLI, Andrea , ANZINI, Maurizio , BIAVA, Mariangela , MAKOVEC, Francesco , GIORDANI, Antonio , CASELLI, Gianfranco , ROVATI, Lucio Claudio
发明人： CAPPELLI, Andrea , ANZINI, Maurizio , BIAVA, Mariangela , MAKOVEC, Francesco , GIORDANI, Antonio , CASELLI, Gianfranco , ROVATI, Lucio Claudio
IPC分类号： C07D207/337 , A61K31/402 , A61P29/00
CPC分类号： C07D207/333 , C07D207/337
摘要： This invention relates to 3-substituted-l, 5-diaryl-2-alkyl- pyrroles of Formula (I), pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and - 5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsul- phonyl-phenyl or with 4-aminosulphonly-phenyl groups.
摘要翻译：本发明涉及式（I）的3-取代-1,5-二芳基-2-烷基吡咯，含有它们的药物组合物及其用于药理学治疗疼痛和COX-2过激活相关疾病的用途。本发明的化合物是具有吡咯环位置-3的新型吡咯衍生物，几种各种官能化的非脂肪族侧链，其赋予化合物相关COX-2效力和选择性以及显着的口服功效。位置-1和-5的苯环被不同地取代，但特别感兴趣的化合物是在位置-5与4-甲基磺酰基 - 苯基或与4-氨基磺酰基苯基取代的那些。

8. 发明申请

WO2007014872A1 COMBINATION OF ITRIGLUMIDE AND PROTON PUMP INHIBITORS IN THE TREATMENT OF GASTROINTESTINAL AND RELATED DISORDERS 审中-公开
标题翻译：烟碱与原液泵抑制剂联合治疗胃肠病和相关疾病
公开(公告)号：WO2007014872A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064567
申请日：2006-07-24
申请人： ROTTAPHARM S.p.A. , ROVATI, Lucio, Claudio , CASELLI, Gianfranco , D'AMATO, Massimo, Maria , GIORDANI, Antonio , MAKOVEC, Francesco
发明人： ROVATI, Lucio, Claudio , CASELLI, Gianfranco , D'AMATO, Massimo, Maria , GIORDANI, Antonio , MAKOVEC, Francesco
IPC分类号： A61P1/04 , A61K45/06 , A61K31/438 , A61K31/4439
CPC分类号： A61K45/06 , A61K31/438 , A61K31/4439 , A61K2300/00
摘要： The invention relates to the combination of the cholecystokinin-2 (CCK-2) receptor antagonist Itriglumide and proton pump inhibitors (PPIs) for the treatment of patients suffering from gastrointestinal and related disorders.
摘要翻译：本发明涉及胆囊收缩素-2（CCK-2）受体拮抗剂伊立格精和质子泵抑制剂（PPI）的组合，用于治疗患有胃肠道和相关疾病的患者。

9. 发明申请

WO2007039869A2 USE OF NEBOGLAMINE IN THE TREATMENT OF TOXICODEPENDENCY 审中-公开
标题翻译： NEBOGLAMINE在治疗毒性反应中的应用
公开(公告)号：WO2007039869A2
公开(公告)日：2007-04-12
申请号：PCT/IB2006/053603
申请日：2006-10-03
申请人： ROTTAPHARM S.p.A. , MAKOVEC, Francesco , CASELLI, Gianfranco , ROVATI, Lucio Claudio , GIORDANI, Antonio
发明人： MAKOVEC, Francesco , CASELLI, Gianfranco , ROVATI, Lucio Claudio , GIORDANI, Antonio
IPC分类号： A61K31/16 , A61P25/30 , A61P25/32 , A61P25/36
CPC分类号： A61K31/16
摘要： Use of neboglamine, (S)-4-amino-N (4, 4-dimethyl-cyclohexyl) glutamic acid (CR 2249) (CAS Registry Number 163000-63-3) , the racemic mixture thereof or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the treatment of toxicodependency induced by drugs such as CNS sedatives such as opiates, barbiturates, benzodiazepines, alcohol, stimulants such as amphetamines and cocaine, and hallucinogens such as LSD, mescalin, cannabis (marijuana) or fencyclidine.
摘要翻译：（S）-4-氨基-N-（4,4-二甲基 - 环己基）谷氨酸（CR2249）（CAS注册号163000-63-3），外消旋混合物其药物可接受的盐在制备用于治疗由药物例如CNS镇静剂如阿片制剂，巴比妥酸盐，苯并二氮杂，酒精，兴奋剂如安非他明和可卡因以及致幻剂如LSD诱导的药物毒性的药物中的用途，mescalin，大麻（大麻）或fencyclidine。

10. 发明申请

WO2008014814A1 COMBINATION ANDOLAST/GLUCOCORTICOIDS 审中-公开
标题翻译：组合和/ / GLUCOCORTICOIDS
公开(公告)号：WO2008014814A1
公开(公告)日：2008-02-07
申请号：PCT/EP2006/064840
申请日：2006-07-31
申请人： ROTTAPHARM S.p.A. , MAKOVEC, Francesco , D'AMATO, Massimo Maria , GIORDANI, Antonio , ROVATI, Lucio Claudio
发明人： MAKOVEC, Francesco , D'AMATO, Massimo Maria , GIORDANI, Antonio , ROVATI, Lucio Claudio
IPC分类号： A61K31/41 , A61K31/57 , A61K31/573 , A61K31/58 , A61P11/00
CPC分类号： A61K31/41 , A61K31/57 , A61K31/573 , A61K31/58 , A61K2300/00
摘要： The invention relates to the combination of Andolast, a calcium-activated potassium channel opener and glucocorticoids for the treatment of patients suffering for airway diseases. Pharmaceutical compositions comprising Andoalst and glucocorticoids are also disclosed.
摘要翻译：本发明涉及用于治疗患有气道疾病的患者的钙激活钾通道开放剂和糖皮质激素的组合。还公开了包含Andoalst和糖皮质激素的药物组合物。

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