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1. 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。

2. 发明申请

WO2013127913A1 4,4-DIFLUORO-PIPERIDINE-COMPOUNDS 审中-公开
标题翻译： 4,4-二氟 - 哌啶化合物
公开(公告)号：WO2013127913A1
公开(公告)日：2013-09-06
申请号：PCT/EP2013/054017
申请日：2013-02-28
申请人： ROTTAPHARM S.P.A.
发明人： STASI, Luigi Piero , ROVATI, Lucio , ARTUSI, Roberto , BOVINO, Clara , COLACE, Fabrizio , MANDELLI, Stefano
IPC分类号： C07D401/12 , C07D401/14 , C07D417/14 , A61K31/4523 , A61P25/00
CPC分类号： C07D401/14 , C07D401/12 , C07D417/14
摘要： The invention, in a first aspect relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered aromatic ring, or a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, or a 6-membered benzocondensed heteroaromatic ring containing N as heteroatom, optionally each of said rings being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, cyano, trifluoromethyl, dimethylamino, or phenyl which optionally is substituted with one or more halogen atoms, or a 5- or 6-membered heterocycle containing from one to three nitrogen atoms; X is O or N; P is pyridyl, pyrimidyl, pyrazyl, or pyridazyl, each being optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, and cyano, and use thereof as pharmaceuticals.
摘要翻译：本发明在第一方面涉及式（I）化合物或其药学上可接受的盐，其中R是6元芳族环，或含有1至3个选自S的杂原子的5或6元杂芳族环，O和N，或含有N作为杂原子的6元苯并稠杂杂芳环，任选地，所述环中的每一个被一个或两个选自（C 1 -C 3）烷基，（C 3 -C 5）环烷氧基，（C 1 -C 3）烷基羰基，氰基，三氟甲基，二甲基氨基或任选被一个或多个卤素原子取代的苯基，或含有1至3个氮原子的5或6元杂环; X是O或N; P是吡啶基，嘧啶基，吡嗪基或哒嗪基，各自任选被一个或多个选自（C 1 -C 3）烷基，卤素，三氟甲基和氰基的取代基取代，并且作为药物使用。

3. 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。

4. 发明申请

WO2006100204A1 BENZAMIDINE DERIVATIVES FOR TREATMENT AND PREVENTION OF CANCER THERAPY INDUCED MUCOSITIS 审中-公开
标题翻译：用于治疗和预防癌症治疗诱导的脑膜瘤的苯扎明衍生物
公开(公告)号：WO2006100204A1
公开(公告)日：2006-09-28
申请号：PCT/EP2006/060789
申请日：2006-03-16
申请人： ROTTAPHARM S.p.A. , LETARI, Ornella , D'AMATO, Massimo Maria , ZANZOLA, Simona , ARTUSI, Roberto , ROVATI, Lucio Claudio , CASELLI, Gianfranco , GIORDANI, Antonio
发明人： LETARI, Ornella , D'AMATO, Massimo Maria , ZANZOLA, Simona , ARTUSI, Roberto , ROVATI, Lucio Claudio , CASELLI, Gianfranco , GIORDANI, Antonio
IPC分类号： A61K31/17 , A61P1/04
CPC分类号： A61K31/17
摘要： Mucositis is the result of a complex process of interactive biologic phenomena that take place in both the epitelium and the submucosa, often leading to severe pain and increased risk of dangerous systemic infections. Mucositis is often a side effect during chemotherapy and radiation therapy. The benzamidine derivatives herein described are particularly effective for treating and preventing mucositis since they are acting simultaneously at the several phases that characterize this disease.
摘要翻译：粘膜炎是由上皮和粘膜下层发生的交互式生物现象的复杂过程的结果，常常导致严重的疼痛和增加的危险全身感染的风险。在化学疗法和放射治疗中，粘膜炎往往是副作用的。本文所述的苄脒衍生物对于治疗和预防粘膜炎是特别有效的，因为它们在表征该疾病的几个阶段同时作用。

5. 发明公开

EP1704860A1 Benzamidine derivatives for treatment and prevention of mucositis 有权
标题翻译：苯甲脒衍生物zur Behandlung und Vorbeugung von Mucositis
公开(公告)号：EP1704860A1
公开(公告)日：2006-09-27
申请号：EP05102423.0
申请日：2005-03-24
申请人： ROTTAPHARM S.P.A.
发明人： LETARI, Ornella , D'AMATO, Massimo Maria , ZANZOLA, Simona , ARTUSI, Roberto , ROVATI, Lucio Claudio , CASELLI, Gianfranco , GIORDANI, Antonio
IPC分类号： A61K31/17 , A61P1/04
CPC分类号： A61K31/17
摘要： Mucositis is the result of a complex process of interactive biologic phenomena that take place in both the epitelium and the submucosa, often leading to severe pain and increased risk of dangerous systemic infections. Mucositis is often a side effect during chemotherapy and radiation therapy. The benzamidine derivatives herein decribed are particularly effective for treating and preventing mucositis since they are acting simultaneously at the several phases that characterize this disease.
摘要翻译：粘膜炎是由上皮层和粘膜下层发生的复杂生物学现象的复杂过程的结果，常常导致严重的疼痛和增加的危险的全身感染的风险。在化学疗法和放射治疗中，粘膜炎往往是副作用。本文描述的苯甲脒衍生物对于治疗和预防粘膜炎是特别有效的，因为它们在表征该疾病的几个阶段同时作用。

6. 发明授权

EP1753746B8 NOVEL PYRROLE DERIVATIVES WITH ANGIOTENSIN II ANTAGONIST ACTIVITY 有权
标题翻译：血管紧张素Ⅱ拮抗剂活性的新吡咯
公开(公告)号：EP1753746B8
公开(公告)日：2012-02-15
申请号：EP05747406.6
申请日：2005-04-27
申请人： ROTTAPHARM S.P.A.
发明人： MAKOVEC, Francesco , ARTUSI, Roberto , GIORDANI, Antonio , ZANZOLA, Simona , ROVATI, Lucio Claudio
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10

7. 发明授权

EP1753746B1 NOVEL PYRROLE DERIVATIVES WITH ANGIOTENSIN II ANTAGONIST ACTIVITY 有权
标题翻译：血管紧张素Ⅱ拮抗剂活性的新吡咯
公开(公告)号：EP1753746B1
公开(公告)日：2011-07-27
申请号：EP05747406.6
申请日：2005-04-27
申请人： ROTTAPHARM S.P.A.
发明人： MAKOVEC, Francesco , ARTUSI, Roberto , GIORDANI, Antonio , ZANZOLA, Simona , ROVATI, Lucio Claudio
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, -COOH, -CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 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 AT1 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.

8. 发明授权

EP1704860B1 Benzamidine derivatives for treatment and prevention of mucositis 有权
标题翻译：用于治疗和预防粘膜炎的苯甲脒衍生物
公开(公告)号：EP1704860B1
公开(公告)日：2010-10-27
申请号：EP05102423.0
申请日：2005-03-24
申请人： ROTTAPHARM S.P.A.
发明人： LETARI, Ornella , D'AMATO, Massimo Maria , ZANZOLA, Simona , ARTUSI, Roberto , ROVATI, Lucio Claudio , CASELLI, Gianfranco , GIORDANI, Antonio
IPC分类号： A61K31/17 , A61P1/04
CPC分类号： A61K31/17

9. 发明授权

EP2268628B1 2-ARYL AND 2 -HETEROARYL 4H-1-BENZOPYRAN-4-ONE-6-AMIDINO DERIVATIVES FOR THE TREATMENT OF ARTHRITIS, CANCER AND RELATED PAIN 有权
标题翻译： 2-芳基和2-杂芳基 - 4H-1-苯并吡喃-4-酮-6-脒用于治疗关节炎，癌症以及与相关的疼痛CONNECTION
公开(公告)号：EP2268628B1
公开(公告)日：2012-05-16
申请号：EP08717486.8
申请日：2008-03-06
申请人： Rottapharm S.p.A.
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.

10. 发明公开

EP2268628A1 2-ARYL AND 2 -HETEROARYL 4H-1-BENZOPYRAN-4-ONE-6-AMIDINO DERIVATIVES FOR THE TREATMENT OF ARTHRITIS, CANCER AND RELATED PAIN 有权
标题翻译： 2-芳基和2-杂芳基 - 4H-1-苯并吡喃-4-酮-6-脒用于治疗关节炎，癌症以及与相关的疼痛CONNECTION
公开(公告)号：EP2268628A1
公开(公告)日：2011-01-05
申请号：EP08717486.8
申请日：2008-03-06
申请人： Rottapharm S.p.A.
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.

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