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1. 发明授权

US09029392B2 Quinoline derivatives as kinase inhibitors 有权
标题翻译：喹啉衍生物作为激酶抑制剂
公开(公告)号：US09029392B2
公开(公告)日：2015-05-12
申请号：US13821294
申请日：2011-09-02
申请人： Andrew Harry Parton , Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Daniel James Ford , Richard Jeremy Franklin , Judi Charlotte Neuss , Joanna Rachel Quincey , Jackalyn Hinkins
发明人： Andrew Harry Parton , Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Daniel James Ford , Richard Jeremy Franklin , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Quincey
IPC分类号： A61K31/4709 , C07D215/12 , C07D471/04 , A61K31/519
CPC分类号： C07D471/04 , A61K31/519
摘要： Disclosed are a series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. The compounds are of general formula (I):
摘要翻译：公开了一系列包含氟化乙基侧链的喹啉和喹喔啉衍生物，其是PI3激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病。该化合物具有通式（I）：

2. 发明申请

US20130296338A1 Quinoline and Quinoxaline Derivatives as Kinase Inhibitors 有权
标题翻译：喹啉和喹喔啉衍生物作为激酶抑制剂
公开(公告)号：US20130296338A1
公开(公告)日：2013-11-07
申请号：US13821294
申请日：2011-09-02
申请人： Andrew Harry Parton , Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Daniel James Ford , Richard Jeremy Franklin , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Quincey
发明人： Andrew Harry Parton , Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Daniel James Ford , Richard Jeremy Franklin , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Quincey
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/519
摘要： A series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译：包含氟化乙基侧链的一系列喹啉和喹喔啉衍生物是P13激酶的选择性抑制剂，因此在医学中是有益的，例如在治疗炎症，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害感受性或伤害性感受器眼科病情。

3. 发明授权

US07323464B2 Pyridine and pyrimidine derivatives 失效
标题翻译：吡啶和嘧啶衍生物
公开(公告)号：US07323464B2
公开(公告)日：2008-01-29
申请号：US10495885
申请日：2002-11-20
申请人： Jeremy Martin Davis , Barry John Langham , Manisha Naik , Daniel Christopher Brookings , Rachel Jane Cubbon , Richard Jeremy Franklin
发明人： Jeremy Martin Davis , Barry John Langham , Manisha Naik , Daniel Christopher Brookings , Rachel Jane Cubbon , Richard Jeremy Franklin
IPC分类号： C07D403/04 , A61K31/506
CPC分类号： C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14
摘要： Compounds of formula (1) are described in which Ra and Rb is each independently a hydrogen atom or a group Rc, or Ra and Rb together form an oxo (═O) or thio (═S) group; X is a N atom or an optionally substituted CH group: Y is a —O— or —S— atom or —SO— or —SO2— group or an optionally substituted —CH2— or —NH— group with the proviso that when Ra and Rb together form an oxo (═O) or thio (═S) group Y is an optionally substituted —CH2— or —NH-group; L1 is a covalent bond or a linker atom or group; p is zero or the integer 1; Alk1 is an optionally substituted C1-10aliphatic or C1-10heteroaliphatic chain; n is zero the integer 1, 2 or 3 with the proviso that when n is zero Y is an optionally substituted —CH2— group; Ar is an optionally substituted C6-12aromatic or C1-9heteroaromatic group; m is zero or the integer 1, 2 or 3; q is zero or the integer 1 or 2; R1, Rc and Rd are hydrogen atoms or the substituents described in the patent specification; and the salts, solvates, hydrates and N-oxides thereof. The compounds are potent and selective inhibitors of p38 kinase and are useful in the treatment of immune or inflammatory disorders.
摘要翻译：描述式（1）的化合物，其中R a和R b各自独立地为氢原子或基团R c，或R （-O）或硫代（-S）基团一起形成一个或多个， X是N原子或任选取代的CH基团：Y是-O-或-S-原子或-SO-或-SO 2 - 基团或任选取代的-CH 2 或-NH-基团，条件是当R a a和R b一起形成氧代（-O）或硫代（-S）基团Y 是任选取代的-CH 2 - 或-NH-基团; L 1是共价键或连接子原子或基团; p为零或整数1; Alk 1是任选取代的C 1-10 1-10脂族或C 1-10 1-10杂脂肪族链; n为整数1,2或3，条件是当n为零时，Y为任选取代的-CH 2 - 基团; Ar是任选取代的C 6-12芳族或C 1-19杂芳族基团; m为零或整数1,2或3; q为零或整数1或2; R 1，R 2和R d是氢原子或专利说明书中所述的取代基; 及其盐，溶剂合物，水合物和N-氧化物。这些化合物是p38激酶的有效和选择性抑制剂，可用于治疗免疫或炎症性疾病。

4. 发明授权

US08242116B2 Fused thiazole derivatives as kinase inhibitors 有权
标题翻译：融合噻唑衍生物作为激酶抑制剂
公开(公告)号：US08242116B2
公开(公告)日：2012-08-14
申请号：US12306151
申请日：2007-06-26
申请人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crépy , Anne Marie Foley , Richard Jeremy Franklin , Alan Findlay Haughan , Helen Tracey Horsley , William Mark Jones , Bénédicte Irma Léonce Frédérique Lallemand , Stephen Robert Mack , Trevor Morgan , Patrick Marie Ghislain Pasau , David Jonathan Phillips , Verity Margaret Sabin , George Martin Buckley , Kerry Jenkins , Benjamin Garfield Perry
发明人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crépy , Anne Marie Foley , Richard Jeremy Franklin , Alan Findlay Haughan , Helen Tracey Horsley , William Mark Jones , Bénédicte Irma Léonce Frédérique Lallemand , Stephen Robert Mack , Trevor Morgan , Patrick Marie Ghislain Pasau , David Jonathan Phillips , Verity Margaret Sabin , George Martin Buckley , Kerry Jenkins , Benjamin Garfield Perry
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： C07D495/04 , C07D513/04 , C07D513/12 , C07D519/00
摘要： A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译：一系列6,7-二氢[1,3]噻唑并[5,4-c]吡啶-4（5H） - 酮衍生物及其类似物，其在2-位被任选取代的吗啉-4- 作为PI3激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎性，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害性感受性或眼科疾病中。

5. 发明申请

US20100137302A1 Fused Thiazole Derivatives as Kinase Inhibitors 有权
标题翻译：稠合噻唑衍生物作为激酶抑制剂
公开(公告)号：US20100137302A1
公开(公告)日：2010-06-03
申请号：US12306151
申请日：2007-06-26
申请人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crepy , Anne Marie Foley , Richard Jeremy Franklin , Alan Findlay Haughan , Helen Tracey Horsley , William Mark Jones , Benedicte Irma Leonce Frederique Lallemand , Stephen Robert Mack , Trevor Morgan , Patrick Marie Ghislain Pasau , David Jonathan Phillips , Verity Margaret Sabin , George Martin Buckley , Kerry Jenkins , Benjamin Garfield Perry
发明人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crepy , Anne Marie Foley , Richard Jeremy Franklin , Alan Findlay Haughan , Helen Tracey Horsley , William Mark Jones , Benedicte Irma Leonce Frederique Lallemand , Stephen Robert Mack , Trevor Morgan , Patrick Marie Ghislain Pasau , David Jonathan Phillips , Verity Margaret Sabin , George Martin Buckley , Kerry Jenkins , Benjamin Garfield Perry
IPC分类号： A61K31/5377 , C07D513/04 , A61P35/04
CPC分类号： C07D495/04 , C07D513/04 , C07D513/12 , C07D519/00
摘要： A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译：一系列6,7-二氢[1,3]噻唑并[5,4-c]吡啶-4（5H） - 酮衍生物及其类似物，其在2-位被任选取代的吗啉-4- 作为PI3激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎性，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害性感受性或眼科疾病中。

6. 发明申请

US20080261951A1 Condensed azepines as vasopressin agonists 审中-公开
标题翻译：浓缩吖庚因作为血管加压素激动剂
公开(公告)号：US20080261951A1
公开(公告)日：2008-10-23
申请号：US12213651
申请日：2008-06-23
申请人： Doreen Mary Ashworth , Gary Robert William Pitt , Peter Hudson , Christopher Martyn Yea , Richard Jeremy Franklin
发明人： Doreen Mary Ashworth , Gary Robert William Pitt , Peter Hudson , Christopher Martyn Yea , Richard Jeremy Franklin
IPC分类号： C07D403/12 , C07D495/04 , C07D471/04 , C07D487/04 , C07D498/04 , A61K31/55 , A61K31/551 , A61K31/553 , A61P13/00
CPC分类号： C07D403/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)S—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.
摘要翻译：本发明提供了根据通式（1）的新化合物，其中A是双环或三环吖庚因衍生物，V 1和V 2均为H，OMe或F，或 V 1和V 2之一是Br，Cl，F，OH，OMe，OBn，OPh，O-酰基，N 3， NH 2，NHBn或NH-酰基，另一个是H，或V 1和V 2一起是-O，-O（CH O-或-S（CH 2 CH 2）S - ; O 1或O 2是O或S; X 1和X 2均为H或一起为-O或-S; Y是OR 5或NR 6 R 7; R 1，R 2，R 3和R 4独立地选自H，低级烷基，低级烷氧基，F，Cl和Br; R 5选自H和低级烷基; R 6和R 7独立地选自H和低级烷基，或者一起是 - （CH 2）n - ; n = 3,4,5,6; p是2或3.化合物是加压素V2受体的激动剂，可用作抗利尿剂和促凝剂。本发明还包括掺入这些加压素激动剂的药物组合物，该组合物特别可用于治疗中枢性尿崩症，夜间遗尿和夜尿症。

7. 发明授权

US08338592B2 Fused thiazole derivatives as kinase inhibitors 有权
标题翻译：融合噻唑衍生物作为激酶抑制剂
公开(公告)号：US08338592B2
公开(公告)日：2012-12-25
申请号：US12666481
申请日：2008-06-24
申请人： Rikki Peter Alexander , Karen Viviane Lucile Crépy , Anne Marie Foley , Richard Jeremy Franklin
发明人： Rikki Peter Alexander , Karen Viviane Lucile Crépy , Anne Marie Foley , Richard Jeremy Franklin
IPC分类号： C07D413/14 , A61K31/535
CPC分类号： C07D495/04 , C07D513/04 , C07D513/12 , C07D519/00
摘要： A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译：一系列在二位被取代的吗啉-4-基部分取代的6,7-二氢[1,3]噻唑并[5,4-c]吡啶-4（5H） - 酮衍生物是因此PI3激酶的选择性抑制剂在医学中是有益的，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病中。

8. 发明申请

US20110003785A1 Fused Thiazole Derivatives As Kinase Inhibitors 有权
标题翻译：稠合噻唑衍生物作为激酶抑制剂
公开(公告)号：US20110003785A1
公开(公告)日：2011-01-06
申请号：US12666481
申请日：2008-06-24
申请人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crepy , Anne Marie Foley , Richard Jeremy Franklin
发明人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crepy , Anne Marie Foley , Richard Jeremy Franklin
IPC分类号： A61K31/397 , C07D413/14 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P9/00 , A61P3/00
CPC分类号： C07D495/04 , C07D513/04 , C07D513/12 , C07D519/00
摘要： A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译：一系列在二位被取代的吗啉-4-基部分取代的6,7-二氢[1,3]噻唑并[5,4-c]吡啶-4（5H） - 酮衍生物是因此PI3激酶的选择性抑制剂在医学中是有益的，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病中。

9. 发明授权

US07560454B2 Condensed azepines as vasopressin agonists 有权
标题翻译：浓缩吖庚因作为血管加压素激动剂
公开(公告)号：US07560454B2
公开(公告)日：2009-07-14
申请号：US11370861
申请日：2006-03-09
申请人： Doreen Mary Ashworth , Gary Robert William Pitt , Peter Hudson , Christopher Martyn Yea , Richard Jeremy Franklin
发明人： Doreen Mary Ashworth , Gary Robert William Pitt , Peter Hudson , Christopher Martyn Yea , Richard Jeremy Franklin
IPC分类号： A61P13/00 , A61K31/55 , C07D403/12 , C07D495/04 , C07D471/04 , C07D487/04 , C07D498/04
CPC分类号： C07D403/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.
摘要翻译：本发明提供根据通式（1）的新化合物，其中A为双环或三环吖庚因衍生物，V1和V2均为H，OMe或F，或V1和V2中的一个为Br，Cl，F，OH，OMe， OBn，OPh，O-酰基，N3，NH2，NHBn或NH-酰基，另一个为H，或V 1和V 2一起为-O，-O（CH 2）p O-或-S（CH 2）p -S-; W1是O或S; X1和X2均为H，或一起为-O或-S; Y为OR5或NR6R7; R 1，R 2，R 3和R 4独立地选自H，低级烷基，低级烷氧基，F，Cl和Br; R5选自H和低级烷基; R6和R7独立地选自H和低级烷基，或一起是 - （CH 2）n - ; n = 3,4,5,6; p是2或3.化合物是加压素V2受体的激动剂，可用作抗利尿剂和促凝剂。本发明还包括掺入这些加压素激动剂的药物组合物，该组合物特别可用于治疗中枢性尿崩症，夜间遗尿和夜尿症。

10. 发明授权

US07074781B2 Condensed azepines as vasopressin agonists 有权
标题翻译：浓缩吖庚因作为血管加压素激动剂
公开(公告)号：US07074781B2
公开(公告)日：2006-07-11
申请号：US10130749
申请日：2001-01-04
申请人： Doreen Mary Ashworth , Gary Robert William Pitt , Peter Hudson , Christopher Martyn Yea , Richard Jeremy Franklin
发明人： Doreen Mary Ashworth , Gary Robert William Pitt , Peter Hudson , Christopher Martyn Yea , Richard Jeremy Franklin
IPC分类号： A61P13/00 , A61K31/55 , C07D403/12 , C07D471/04 , C07D495/04
CPC分类号： C07D403/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.
摘要翻译：本发明提供了根据通式（1）的新化合物，其中A是双环或三环吖庚因衍生物，V 1和V 2均为H，OMe或F，或 V 1和V 2之一是Br，Cl，F，OH，OMe，OBn，OPh，O-酰基，N 3， NH 2，NHBn或NH-酰基，另一个是H，或V 1和V 2一起是-O，-O（CH O - 或-S（CH 2）n -S-; -S-（CH 2）n - O 1或O 2是O或S; X 1和X 2均为H或一起为-O或-S; Y是OR 5或NR 6 R 7; R 1，R 2，R 3和R 4独立地选自H，低级烷基，低级烷氧基，F，Cl和Br; R 5选自H和低级烷基; R 6和R 7独立地选自H和低级烷基，或者一起是 - （CH 2）n - ; n = 3,4,5,6; 并且p是2或3.化合物是加压素V2受体的激动剂，并且可用作抗利尿剂和促凝剂。本发明还包括掺入这些加压素激动剂的药物组合物，该组合物特别可用于治疗中枢性尿崩症，夜间遗尿和夜尿症。

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