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11. 发明申请

US20150099752A9 PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS 有权
标题翻译：吡咯烷酮衍生物作为PI3K抑制剂
公开(公告)号：US20150099752A9
公开(公告)日：2015-04-09
申请号：US14114541
申请日：2012-04-26
申请人： Francisco Javier Bernal Anchuela , Marta Carrascal Riera , Juan Francisco Caturla Javaloyes , Jordi Gracia Ferrer , Victor Giulio Matassa , Emma Terricabras Belart , Joan Tal Tavul Moll , Montserat Eraa Sola
发明人： Francisco Javier Bernal Anchuela , Marta Carrascal Riera , Juan Francisco Caturla Javaloyes , Jordi Gracia Ferrer , Victor Giulio Matassa , Emma Terricabras Belart , Joan Tal Tavul Moll , Montserat Eraa Sola
IPC分类号： C07D487/04 , A61K45/06 , A61K31/53
CPC分类号： C07D487/04 , A61K31/53 , A61K45/06 , C07D473/34
摘要： New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
摘要翻译：公开了具有式（I）化学结构的新的吡咯并三酮衍生物; 以及它们的制备方法，包含它们的药物组合物及其在治疗中作为磷酸肌醇3-激酶（PI3K）的抑制剂的用途。

12. 发明申请

US20080275086A1 Dpp-Iv Inhibitors 审中-公开
标题翻译： Dpp-Iv抑制剂
公开(公告)号：US20080275086A1
公开(公告)日：2008-11-06
申请号：US11886389
申请日：2006-02-20
申请人： Paul John Edwards , Silvia Cerezo-Galvez , Meritxell Lopez-Canet , Victor Giulio Matassa , Claudia Rosenbaum , Christian Rummey , Sonja Nordhoff
发明人： Paul John Edwards , Silvia Cerezo-Galvez , Meritxell Lopez-Canet , Victor Giulio Matassa , Claudia Rosenbaum , Christian Rummey , Sonja Nordhoff
IPC分类号： A61K31/4525 , A61P3/04 , C07D207/12 , A61K31/40 , A61K31/445 , A61K31/4439 , C07D401/08 , C07D211/06 , C07D421/02
CPC分类号： C07D207/08 , C07D205/04 , C07D207/06 , C07D207/09 , C07D207/14 , C07D207/48 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/58 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D413/04 , C07D413/14
摘要： The invention relates to compounds of formula (I) wherein Z, R1-7, X and n have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.
摘要翻译：本发明涉及其中Z，R 1-7，X和n具有如在说明书和权利要求中引用的含义的式（I）化合物。所述化合物可用作DPP-IV抑制剂。本发明还涉及这种化合物的制备以及其作为药物的生产和使用。

13. 发明授权

US07410996B2 3-aryloxy/thio-2,3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake 失效
公开(公告)号：US07410996B2
公开(公告)日：2008-08-12
申请号：US10533328
申请日：2003-10-24
申请人： Serge Louis Boulet , Sandra Ann Filla , Peter Thaddeus Gallagher , Kevin John Hudziak , Anette Margareta Johansson , Rushad E. Karanjawala , John Joseph Masters , Victor Giulio Matassa , Brian Michael Mathes , Richard Edmund Rathmell , Maria Ann Whatton , Chad Nolan Wolfe
发明人： Serge Louis Boulet , Sandra Ann Filla , Peter Thaddeus Gallagher , Kevin John Hudziak , Anette Margareta Johansson , Rushad E. Karanjawala , John Joseph Masters , Victor Giulio Matassa , Brian Michael Mathes , Richard Edmund Rathmell , Maria Ann Whatton , Chad Nolan Wolfe
IPC分类号： A61K31/381 , C07D333/64
CPC分类号： C07D275/04 , C07C217/16 , C07C217/30 , C07C217/48 , C07C323/32 , C07D307/86 , C07D333/54 , C07D333/62 , C07D475/04
摘要： There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof with the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is —S—.

14. 发明授权

US5849746A Substituted 1,4-piperazine-heteroaryl derivatives as 5-HT.sub.1D receptor agonists 失效
标题翻译：取代的1,4-哌嗪 - 杂芳基衍生物作为5-HT1D受体激动剂
公开(公告)号：US5849746A
公开(公告)日：1998-12-15
申请号：US894302
申请日：1997-07-22
申请人： Mark Stuart Chambers , Angus Murray MacLeod , Victor Giulio Matassa
发明人： Mark Stuart Chambers , Angus Murray MacLeod , Victor Giulio Matassa
IPC分类号： A61K31/495 , A61P9/00 , A61P25/04 , A61P43/00 , C07D403/14 , C07D413/14
CPC分类号： C07D403/14
摘要： A class of 1,4-disubstituted piperazine derivatives, further substituted on one of the carbon atoms of the piperazine ring, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
摘要翻译： PCT No.PCT / GB96 / 00179 Sec。 371日期1997年7月22日 102（e）日期1997年7月22日PCT提交1996年1月29日PCT公布。出版物WO96 / 23785 日期1996年8月8日一类在哌嗪环的一个碳原子上进一步取代的1,4-二取代哌嗪衍生物是5-HT1样受体的选择性激动剂，是人5-HT1Dα的有效激动剂受体亚型，而相对于5-HT1Dβ亚型，对5-HT1Dα受体亚型具有至少10倍的选择性亲和力; 因此，它们可用于治疗和/或预防临床症状，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起更少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

15. 发明授权

US07417064B2 3-aryloxy/thio-3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake 失效
公开(公告)号：US07417064B2
公开(公告)日：2008-08-26
申请号：US10532657
申请日：2003-10-24
申请人： Serge Louis Boulet , Sandra Ann Filla , Peter Thaddeus Gallagher , Kevin John Hudziak , Anette Margareta Johansson , Rushad E. Karanjawala , John Joseph Masters , Victor Giulio Matassa , Brian Michael Mathes , Richard Edmund Rathmell , Maria Ann Whatton , Chad Nolan Wolfe
发明人： Serge Louis Boulet , Sandra Ann Filla , Peter Thaddeus Gallagher , Kevin John Hudziak , Anette Margareta Johansson , Rushad E. Karanjawala , John Joseph Masters , Victor Giulio Matassa , Brian Michael Mathes , Richard Edmund Rathmell , Maria Ann Whatton , Chad Nolan Wolfe
IPC分类号： A61K31/381 , C07D333/64
CPC分类号： C07C217/20 , C07C217/34 , C07D333/54
摘要： There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl.

16. 发明申请

US20080176838A1 Dpp-IV Inhibitors 审中-公开
标题翻译： Dpp-IV抑制剂
公开(公告)号：US20080176838A1
公开(公告)日：2008-07-24
申请号：US11570098
申请日：2005-06-08
申请人： Paul John Edwards , Silvia Cerezo-Galvez , Achim Feurer , Oliver Hill , Meinolf Thiemann , Victor Giulio Matassa , Sonja Nordhoff , Meritxell Lopez-Canet
发明人： Paul John Edwards , Silvia Cerezo-Galvez , Achim Feurer , Oliver Hill , Meinolf Thiemann , Victor Giulio Matassa , Sonja Nordhoff , Meritxell Lopez-Canet
IPC分类号： C07D279/12 , C07D211/06 , A61K31/535 , A61K31/445 , A61K31/497
CPC分类号： C07D217/26 , C07D207/08 , C07D207/09 , C07D207/16 , C07D217/14 , C07D217/16 , C07D241/04
摘要： The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament for the treatment of type 2 diabetes mellitus, obesity and lipid disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1-9，Z，n，X，A和R b具有本说明书中引用的含义，索赔。所述化合物可用作DPP-IV抑制剂。本发明还涉及这些化合物的制备以及其作为用于治疗2型糖尿病，肥胖症和脂质疾病的药物的生产和用途。

17. 发明授权

US07119073B2 Peptides and their use as inhibitors of hepatitis C virus ns3 protease 失效
标题翻译：肽及其作为丙型肝炎病毒ns3蛋白酶抑制剂的用途
公开(公告)号：US07119073B2
公开(公告)日：2006-10-10
申请号：US10473443
申请日：2002-03-26
申请人： Stefania Colarusso , Cristina Gardelli , Benjamin Gerlach , Steven Harper , Uwe Koch , Victor Giulio Matassa , Ester Muraglia , Frank Narjes , Jesus Maria Ontoria Ontoria , Alessia Petrocchi , Simona Ponzi , Ian Stansfield , Vicenzo Summa
发明人： Stefania Colarusso , Cristina Gardelli , Benjamin Gerlach , Steven Harper , Uwe Koch , Victor Giulio Matassa , Ester Muraglia , Frank Narjes , Jesus Maria Ontoria Ontoria , Alessia Petrocchi , Simona Ponzi , Ian Stansfield , Vicenzo Summa
IPC分类号： A61K38/06 , A61K38/07 , C07K5/08 , C07K5/10 , C07K7/04 , A61K38/00 , C07K2/00
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/021 , C07K5/0819 , C07K5/0827 , C07K5/1021 , C07K5/1027 , C07K7/02
摘要： Compounds of formula (I), and pharmaceutically acceptable salts and esters thereof: (I); wherein Q, R2, X, Y and Z are as defined herein; are inhibitors of the hepatitis C virus (HCV) NS3 protease
摘要翻译：式（I）化合物及其药学上可接受的盐和酯：（I）; 其中Q，R2，X，Y和Z如本文所定义; 是丙型肝炎病毒（HCV）NS3蛋白酶的抑制剂

18. 发明授权

US5919783A Indoline and azaindoline derivatives as 5-HT.sub.1D alpha receptor agonists 失效
标题翻译：二氢吲哚和唑啉衍生物作为5-HT1Dα受体激动剂
公开(公告)号：US5919783A
公开(公告)日：1999-07-06
申请号：US776626
申请日：1997-01-21
申请人： Mark Stuart Chambers , Victor Giulio Matassa , Leslie Joseph Street
发明人： Mark Stuart Chambers , Victor Giulio Matassa , Leslie Joseph Street
IPC分类号： C07D521/00 , A61K31/495 , C07D403/14 , C07D471/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole, and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1-4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1-6 carbon atoms; T represents nitrogen or CH; R.sup.1 represents aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, either of which groups may be optionally substituted; and R.sup.2 represents hydrogen or C.sub.1-6 alkyl are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists. ##STR1##
摘要翻译： PCT No.PCT / GB95 / 01756 Sec。 371日期1997年1月21日 102（e）1997年1月21日PCT PCT 1995年7月24日PCT公布。出版物WO96 / 04269 日期：2002年2月15日式（I）化合物或其盐或前体药物，其中Z表示选自呋喃，噻吩，吡咯，恶唑，噻唑，异恶唑，异噻唑，咪唑，吡唑等的任选取代的五元杂芳族环，恶二唑，噻二唑，三唑和四唑; E表示化学键或含有1-4个碳原子的直链或支链亚烷基链; Q表示含有1-6个碳原子的直链或支链亚烷基链; T表示氮或CH; R1表示芳基（C1-6）烷基或杂芳基（C1-6）烷基，其中任一个可以任选被取代; 并且R 2表示氢或C 1-6烷基是5-HT1样受体的选择性激动剂，其是人5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

19. 发明授权

US08178679B2 Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the β2 adrenergic receptors 失效
标题翻译： 4-（2-氨基-1-羟乙基）苯酚的衍生物作为二肾上腺素能受体的激动剂
公开(公告)号：US08178679B2
公开(公告)日：2012-05-15
申请号：US12745195
申请日：2008-11-10
申请人： Victor Giulio Matassa , Carlos Puig Duran , Maria Prat Quiñones , Laia Sole Feu , Oriol Llera Soldevila
发明人： Victor Giulio Matassa , Carlos Puig Duran , Maria Prat Quiñones , Laia Sole Feu , Oriol Llera Soldevila
IPC分类号： C07D215/26 , C07C233/43 , C07C215/34
CPC分类号： C07D215/26 , C07C217/60 , C07C233/43 , C07C2603/74
摘要： The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 adrenergic receptor.
摘要翻译：本公开涉及式（I）的4-（2-氨基-1-羟乙基）苯酚衍生物以及包含它们的药物组合物，以及它们在治疗中作为β肾上腺素能受体激动剂的用途。

20. 发明申请

US20110311485A1 1,2,4-OXADIAZOLE DERIVATIVES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： 1,2,4-OXADIAZOLE DERIVATIVES AND THEUR THERAPEUTIC USE
公开(公告)号：US20110311485A1
公开(公告)日：2011-12-22
申请号：US13142104
申请日：2009-12-15
申请人： Victor Giulio Matassa , Nuria Aguilar Izquierdo , Marta Mir Cepeda , Marta Carrascal Riera , Silvia Fonquerna Pou , Aranzazu Cardus Figueras , Julio Cesar Castro Palomino Laria , Montserrat Erra Sola
发明人： Victor Giulio Matassa , Nuria Aguilar Izquierdo , Marta Mir Cepeda , Marta Carrascal Riera , Silvia Fonquerna Pou , Aranzazu Cardus Figueras , Julio Cesar Castro Palomino Laria , Montserrat Erra Sola
IPC分类号： A61K31/4245 , C07D413/14 , C07D417/04 , A61K31/4439 , A61K31/496 , A61K31/454 , A61K31/5377 , A61K31/437 , A61K31/444 , A61K31/433 , A61P37/00 , A61P29/00 , A61P37/06 , A61P35/00 , A61P7/00 , A61P25/00 , A61P31/12 , A61P31/00 , A61P19/04 , A61P11/06 , A61P17/06 , A61P19/02 , A61P1/00 , A61K38/21 , A61K39/395 , A61K31/573 , C07D413/04
CPC分类号： C07D413/04 , C07D413/14 , C07D471/04
摘要： The present disclosure relates to 1, 2, 4 oxadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.
摘要翻译：本公开涉及式（I）的1,2,4-恶二唑衍生物以及包含它们的药物组合物，以及它们在作为S1P1受体的激动剂的治疗中的用途。

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