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1. 发明申请

US20090156601A1 PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的吡嗪衍生物
公开(公告)号：US20090156601A1
公开(公告)日：2009-06-18
申请号：US12089874
申请日：2006-10-10
申请人： Edward McDonald , Jonathan M. Large , Adrian J. Folkes , Stephen J. Shuttleworth , Nan Chi Wan
发明人： Edward McDonald , Jonathan M. Large , Adrian J. Folkes , Stephen J. Shuttleworth , Nan Chi Wan
IPC分类号： A61K31/5377 , C07D413/14 , A61P29/00
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： The invention provides compounds which are pyrimidines of formula (I): wherein —XR3 is bonded at ring position 2 and —YR4 is bonded at ring position 5 or 6; R1 and R2 form, together with the N atom to which they are attached, a morphorine ring which is unsubstituted or substituted; X is a direct bond; R3 is selected from (i) a group of the following formula (1): wherein B is a phenyl ring which is unsubstituted or substituted and Z is selected from —OR, CH2OR and —NRS(O) mR, wherein each R is independently selected from H, C1-C6 alkyl, C3-C10 cycloalkyl and a 5- to 12-membered aryl or heteroaryl group, the group being unsubstituted or substituted, and m is 2; and (ii) an indazole group which is unsubstituted or substituted; and Y is selected from —O—(CH2)n—, —NH—(CH2)n, —NHC(O)—(CH2)n— and —C(O)NH—(CH2)n— wherein n is 0 or an integer of 1 to 3, and R4 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted and a group —NR5R6 wherein R5 and R6, which are the same or different, are each independently selected from H, C1-C6 alkyl which is unsubstituted or substituted, C3-C10 cycloalkyl which is unsubstituted or substituted, —C(O)R, —C(O)N(R)2 and —S(O)mR wherein R and m are as defined above, or R5 and R6 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6- or 7-membered N-containing heterocyclic group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof. These compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供了式（I）的嘧啶的化合物：其中-XR3在环位置2键合，-YR4键合在环位置5或6; R1和R2与它们所连接的N原子一起形成未取代或取代的吗啉环; X是直接的债券; R3选自（i）下式（1）的基团：其中B是未取代或取代的苯基环，Z选自-OR，CH 2 OR和-NRS（O）m R，其中每个R独立地为选自H，C 1 -C 6烷基，C 3 -C 10环烷基和5至12元芳基或杂芳基，该基团是未取代或取代的，m为2; 和（ii）未取代或取代的吲唑基; 并且Y选自-O-（CH 2）n - ， - NH - （CH 2）n，-NHC（O） - （CH 2）n - 和-C（O）NH-（CH 2）或1〜3的整数，R 4选自未取代或取代的不饱和5〜12元碳环或杂环基和-NR 5 R 6基，其中R 5和R 6相同或不同，各自独立地为未取代或未取代的C 1 -C 6环烷基，-C（O）R 1 -C（O）N（R）2和-S（O）m R，其中R 和m如上所定义，或者R 5和R 6与它们所连接的氮原子一起形成未取代或取代的饱和的5-，6-或7-元含氮杂环基; 及其药学上可接受的盐。这些化合物是PI3K的抑制剂，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍等相关的异常细胞生长，功能或行为引起的疾病和障碍，神经障碍。

2. 发明授权

US07696204B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US07696204B2
公开(公告)日：2010-04-13
申请号：US12089677
申请日：2006-10-11
申请人： Edward McDonald , Jonathan M Large , Stephen J Shuttleworth
发明人： Edward McDonald , Jonathan M Large , Stephen J Shuttleworth
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Pyrimidines of formula (I): wherein R1 to R4, X and Y are defined in the specification are inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的嘧啶：其中R1至R4，X和Y在本说明书中定义为P13K的抑制剂，因此可用于治疗与P13激酶例如癌症相关的异常细胞生长，功能或行为引起的疾病和病症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

3. 发明申请

US20090042884A1 Pharmaceutical Compounds 失效
标题翻译：药物化合物
公开(公告)号：US20090042884A1
公开(公告)日：2009-02-12
申请号：US12089677
申请日：2006-10-11
申请人： Edward McDonald , Jonathan M. Large , Stephen J. Shuttleworth
发明人： Edward McDonald , Jonathan M. Large , Stephen J. Shuttleworth
IPC分类号： C07D413/04 , A61K31/5377 , C07D413/14 , A61P35/00 , A61P31/12 , A61P9/00 , A61P29/00 , A61P37/00 , A61P3/00
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Pyrimidines of formula (I): wherein R1 to R4, X and Y are defined in the specification are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的嘧啶：其中R1至R4，X和Y在本说明书中定义为PI3K的抑制剂，因此可用于治疗与PI3激酶例如癌症相关的异常细胞生长，功能或行为引起的疾病和障碍，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

4. 发明申请

US20110190297A1 PYRIDINE AND PYRIMIDINE BASED COMPOUNDS AS WNT SIGNALING PATHWAY INHIBITORS FOR THE TREATMENT OF CANCER 失效
标题翻译：作为Wnt信号途径抑制剂治疗癌症的吡啶和吡啶基化合物
公开(公告)号：US20110190297A1
公开(公告)日：2011-08-04
申请号：US13122555
申请日：2009-10-06
申请人： Edward McDonald , Julian Blagg , Mark Pichowicz , Simon Ross Crumpler
发明人： Edward McDonald , Julian Blagg , Mark Pichowicz , Simon Ross Crumpler
IPC分类号： A61K31/5377 , A61P35/00 , C07D401/04 , A61K31/4545 , C07D413/14 , A61K31/496 , A61K31/4439 , A61K31/506 , C07D401/14 , C07D471/10 , A61K31/438
CPC分类号： C07D471/10 , C07D213/74 , C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
摘要翻译：本发明涉及基于吡啶和嘧啶的化合物，包含这些化合物的药物组合物及其作为用于治疗和/或预防癌症的治疗剂的潜在用途。

5. 发明授权

US07612201B2 Pyrazole compounds 失效
标题翻译：吡唑化合物
公开(公告)号：US07612201B2
公开(公告)日：2009-11-03
申请号：US10536899
申请日：2003-12-18
申请人： Mandy Christine Beswick , Martin James Drysdale , Brian William Dymock , Edward McDonald
发明人： Mandy Christine Beswick , Martin James Drysdale , Brian William Dymock , Edward McDonald
IPC分类号： C07D231/38 , C07D401/04 , C07D403/04 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D231/38 , A61K31/415 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers. In the formulae, Ar is an aryl, aryl(C1-C6 alkyl), aryl(C1-C6 alkyl), heteroaryl, heteroarylaryl(C1-C6 alkyl), or heteroarylaryl(C1-C6 alkyl) group, any of which being optionally substituted in the aryl or heteroaryl part thereof; R1, is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and ring A is a non aromatic carbocyclic or heterocyclic ring wherein (i) a ring carbon is optionally substituted, and/or (ii) a ring nitrogen is optionally substituted by a group of formula -(Alk1)p (Cyc)n-(Alk3)m-(Z)r (Alk2)s Q where Alk1, Alk2 and Alk3 are optionally substituted C1-C3 alkyl, Cyc is an optionally substituted carbocyclic or heterocyclic radical; m, n, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —S02-, —C(═O)O—, —OC(═O)—, —NW—, —C(═O)NRA-, —NRAC(═O)—, —SO2NRA—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical.
摘要翻译：式（IA）或（IB）化合物或其盐，N-氧化物，水合物或溶剂合物是HSP90的抑制剂，并且在治疗对HSP90抑制作用的疾病如癌症的治疗中具有价值。在式中，Ar是芳基，（C 1 -C 6烷基），芳基（C 1 -C 6烷基），杂芳基，杂芳基芳基（C 1 -C 6烷基）或杂芳基芳基（C 1 -C 6烷基）在其芳基或杂芳基部分取代; R1是氢或任选取代的C 1 -C 6烷基; R 2是氢，任选取代的环烷基，环烯基，C 1 -C 6烷基，C 1 -C 6烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团; 环A是非芳族碳环或杂环，其中（i）环碳任选被取代，和/或（ii）环氮任选地被式 - （Alk1）p（Cyc）n-（ Alk3）m-（Z）r（Alk2）sQ其中Alk1，Alk2和Alk3是任选取代的C 1 -C 3烷基，Cyc是任选取代的碳环或杂环基; m，n，p，r和s独立地为0或1，Z为-O - ， - S - ， - （CO） - ， - SO2-，-C - ，-NW-， - C（ - O）NRA - ， - NRAC（-O） - ， - SO2NRA-或-NRASO2-，其中RA是氢或C1-C6烷基，Q是氢或任选取代的碳环或杂环基。

6. 发明申请

US20090247507A1 Enzyme Inhibitors 有权
标题翻译：酶抑制剂
公开(公告)号：US20090247507A1
公开(公告)日：2009-10-01
申请号：US12158339
申请日：2006-12-21
申请人： Vassilios Bavetsias , Edward McDonald , Spyridon Linardopoulos
发明人： Vassilios Bavetsias , Edward McDonald , Spyridon Linardopoulos
IPC分类号： A61K31/551 , C07D471/04 , A61P37/02 , A61P35/00 , C12N9/99 , A61K31/4545 , A61K31/5377 , A61K31/496
CPC分类号： C07D471/04
摘要： Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2—N—, —CH2—CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2—, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; Alk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, —CN, —CF3, —OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z&It;1> is —S—, —S(O)—, —S(O)2—, —O—, —SO2NH—, —NHSO2—, NHC(═O)NH, —NH(C═S)NH—, Or —N(R4)—wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and Alk&It;1> and Alk&It;2> are, independently, optionally substituted divalent C1-C3 alkylene radicals; and m, n and p are independently 0 or 1. Data supplied from the esp@cenet datatbase—Worldwide d77
摘要翻译：式（I）化合物是极光激酶抑制剂：其中X是-N-，-CH 2 -N，-CH 2 -CH-或-CH-; R1是式（IA）的基团，其中Z是-CH 2 - ， - NH - ， - O - ， - S（O）-S - ， - S（O）2或具有3价的二价单环碳环或杂环基 -7环原子; Alk是任选取代的二价C 1 -C 6亚烷基; A是氢或任选取代的具有5-7个环原子的单环碳环或杂环; r，s和t独立地为0或1，条件是当A为氢时，r和s中的至少一个为1; R2是卤素，-CN，-CF3，-OCH3或环丙基; 并且R 3是式（IB）的基团，其中Q是氢或具有5或6个环原子的任选取代的苯基或单环杂环; （O） - ， - S（O）2 - ， - O - ， - SO 2 NH-，-NHSO 2 - ，NHC（-O）NH，-NH（CS）NH- 或-N（R4） - 其中R4是氢，C1-C3烷基，环烷基或苄基; 和Alk＆It; 1>和Alk＆It; 2>独立地是任选取代的二价C1-C3亚烷基; m，n和p独立为0或1.从esp @ cenet datatbase-Worldwide d77提供的数据

7. 发明申请

US20060235058A1 Substituted 5-membered ring compounds and their use 失效
标题翻译：取代的5元环化合物及其用途
公开(公告)号：US20060235058A1
公开(公告)日：2006-10-19
申请号：US10561969
申请日：2004-06-24
申请人： Kwai Cheung , Brian Dymock , Edward McDonald , Martin Drysdale
发明人： Kwai Cheung , Brian Dymock , Edward McDonald , Martin Drysdale
IPC分类号： A61K31/4196 , A61K31/4192 , C07D249/04 , C07D249/08 , A61K31/41
CPC分类号： A61K31/4196 , A61K31/4192 , A61K31/427 , A61K31/433
摘要： Compound of a compound of formula (1) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for example 1,2,3-triazolyl or a 1,2,4-triazolyl or a tetrazolyl ring; and R1 R2 R3 are as defined in the specification are inhibitors of HSP90 and therefore of use in the treatment of, for example, cancers, viral disease, inflammatory diseases such as rheumatoid arthritis, asthma, multiple sclerosis, Type I diabetes, lupus, psoriasis and inflammatory bowel disease; cystic fibrosis angiogenesis-related disease such as diabetic retinopathy, haemangiomas, and endometriosis; or for protection of normal cells against chemotherapy-induced toxicity; or diseases where failure to undergo apoptosis is an underlying factor, or protection from hypoxia-ischemic injury due to elevation of Hsp70 in the heart and brain; scrapie /CJD, Huntingdon's and Alzheimer's disease.
摘要翻译：式（1）化合物或其盐，N-氧化物，水合物或溶剂化物的化合物在制备抑制HSP90活性的组合物中的用途：其中环A是具有5个或更多个碳原子的芳族或非芳族碳环或杂环环原子，例如1,2,3-三唑基或1,2,4-三唑基或四唑基环; 和R 1 R 2 R 3 R 3如本说明书中所定义的是HSP90的抑制剂，因此用于治疗，例如，癌症，病毒性疾病，炎性疾病如类风湿性关节炎，哮喘，多发性硬化，I型糖尿病，狼疮，牛皮癣和炎症性肠病; 囊性纤维化血管生成相关疾病如糖尿病性视网膜病变，血管瘤和子宫内膜异位症; 或用于保护正常细胞免受化疗诱导的毒性; 或未能进行细胞凋亡的疾病是潜在的因素，或由于心脏和脑中Hsp70的升高而保护缺氧缺血性损伤; 瘙痒病/ CJD，亨廷顿氏症和阿尔茨海默病。

8. 发明授权

US06906067B2 N-heterocyclic inhibitors of TNF-α expression 有权
公开(公告)号：US06906067B2
公开(公告)日：2005-06-14
申请号：US09891750
申请日：2001-06-26
申请人： Kevin Joseph Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn David Erickson , Jeffrey John Letourneau , Edward McDonald , Katerina Leftheris , Stephen T. Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John J. Baldwin , Alaric J. Dyckman
发明人： Kevin Joseph Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn David Erickson , Jeffrey John Letourneau , Edward McDonald , Katerina Leftheris , Stephen T. Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John J. Baldwin , Alaric J. Dyckman
IPC分类号： A61K31/40 , A61K31/551 , C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D521/00 , C07D251/40 , A61K31/53 , A61P35/00 , C07D251/48
CPC分类号： C07D251/52 , C07D231/12 , C07D233/56 , C07D249/08 , C07D251/48 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.

9. 发明授权

US4898968A Cyclopropane derivatives 失效
标题翻译：环丙烷衍生物
公开(公告)号：US4898968A
公开(公告)日：1990-02-06
申请号：US188850
申请日：1988-05-02
申请人： Edward McDonald , Roger Salmon
发明人： Edward McDonald , Roger Salmon
IPC分类号： A01N53/00 , C07D239/26 , C07D239/30 , C07D401/12
CPC分类号： C07D239/26 , A01N53/00 , C07D239/30 , C07D401/12
摘要： Compounds of the formula ##STR1## wherein R.sup.2 represents an .alpha.-branched alkyl group containing from 3 to 6 carbon atoms, and R represents either (a) hydroxy, halo or alkoxy of up to six carbon atoms, or (b) the group --OR.sup.1 where R.sup.1 is the residue of an alcohol of formula R.sup.1 OH which forms an insecticidal ester with chrysanthemic acid, permethrin acid or cyhalothrin acid. Methods for using these compounds to combat insect and acarine pests, as well as novel intermediates, are also disclosed.
摘要翻译：其中R 2表示含有3至6个碳原子的α-支链烷基，R表示（a）至多6个碳原子的羟基，卤素或烷氧基，或（b）基团 - OR1，其中R1是式为R1OH的醇的残基，其与菊酸，氯菊酯酸或三氟氯氰酸形成杀虫剂。还公开了使用这些化合物来防治昆虫和螨类害虫以及新型中间体的方法。

10. 发明授权

US08846696B2 Purine derivatives 有权
标题翻译：嘌呤衍生物
公开(公告)号：US08846696B2
公开(公告)日：2014-09-30
申请号：US12489663
申请日：2009-06-23
申请人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： A61K31/52 , C07D473/16
CPC分类号： C07D473/16 , A61K31/52 , Y02A50/411
摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链的C 1 -C 6烷基或芳基，并且其中R 3和R 4中的至少一个不是H; R5是支链或非支链C 1 -C 5烷基或C 1 -C 6环烷基，其各自可以任选被一个或多个OH基取代; R6，R7，R8和R9各自独立地为H，卤素，NO2，OH，OMe，CN，NH2，COOH，CONH2或SO2NH2。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中风，脱发，中枢神经系统疾病，神经变性疾病或糖尿病中的用途。

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