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52. 发明授权

EP2086956B1 INHIBITORS OF IKK- BETA SERINE-THREONINE PROTEIN KINASE 有权
标题翻译： IKK BETA SERINTHREONINPROTEINKINASE抑制剂的
公开(公告)号：EP2086956B1
公开(公告)日：2011-09-14
申请号：EP07824361.5
申请日：2007-10-29
申请人： Chroma Therapeutics Limited
发明人： MOFFAT, David, Festus, Charles , DAVIES, Stephen, John , CHARLTON, Michael, Hugh , HIRST, Simon, Christopher , ONIONS, Stuart, Thomas , WILLIAMS, Jonathon, Gareth
IPC分类号： C07D333/38 , A61K31/381
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases wherein R7 is hydrogen or optionally substituted (C1C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1-(CH2)z-, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or -(C=O)R3, -(C=O)OR3, Or -(C=O)NR3 wherein R3 is hydrogen.or optionally substituted (C1-C6)alkyl; Y1 is a bond, -(C=O)-, -S(O2)-, -C(=O)O-, -OC(=O)-, -(C=O)NR3-, -NR3(C=O)-, -S(O2)NR3-, -NR3S(O2)-, or -NR3(C=O)NR4-, wherein R3 and R4 are independently hydrogen or optionally substituted (CrC6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and AIk2 are as defined in the claims.

53. 发明公开

EP2324006A2 ANTI-CANCER DRUGS AND USES RELATING THERETO FOR METASTATIC MALIGNANT MELANOMA AND OTHER CANCERS 有权
标题翻译：抗癌药和与之有关的使用针对转移性恶性黑色素瘤和其他癌症
公开(公告)号：EP2324006A2
公开(公告)日：2011-05-25
申请号：EP09760623.0
申请日：2009-09-14
申请人： Kasina Laila Innova Pharmaceuticals Private Ltd.
发明人： KASINA, Sudhakar , GOKARAJU, Rama, Raju , GOLAKOTI, Trimurtulu , SOMEPALLI, Venkateswarlu , KRISHANU, Sengupta , BHUPATHIRAJU, Kiran , GOKARAJU, Ganga, Raju
IPC分类号： C07D333/38 , C07D333/40 , C07D495/04 , A61K31/381 , A61P35/00
CPC分类号： C07D333/38 , C07D333/40 , C07D495/04
摘要： The present invention discloses triazene analogs of the general formula (I) and formula (II), their tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts thereof for the metastatic malignant melanoma and other cancers including but not limited to lymphomas, sarcomas, carcinomas, and gliomas. The invention further discloses a process for the preparation of the above said triazene analogs of formula (I) and formula (II), and their pharmaceutically acceptable compositions.

54. 发明授权

EP1373210B1 HETEROCYCLIC DIAMIDE INVERTEBRATE PEST CONTROL AGENTS 有权
标题翻译：杂环二酰胺进行战斗脊椎动物害虫
公开(公告)号：EP1373210B1
公开(公告)日：2011-05-18
申请号：EP02723322.0
申请日：2002-02-28
申请人： E.I. DU PONT DE NEMOURS AND COMPANY
发明人： ANNIS, Gary, David , FINKELSTEIN, Bruce, Lawrence
IPC分类号： C07D213/82 , C07D231/40 , C07D333/38 , C07D403/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D401/12 , C07D213/81 , C07D413/12
CPC分类号： C07D213/82 , A01N43/10 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/80 , C07D231/40 , C07D333/38 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
摘要： This invention provides compounds of Formula (I), N-oxides and suitable salts thereof, wherein A and B are independently O or S; each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5; K is, together with the two contiguous linking carbon atoms, a 5- or 6-membered heteroaromatic ring optionally substituted with 1 to 3 R?4; and R1 R2, R3, R4, R5¿ and n are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula (I), an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein). This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula (I), an N-oxide thereof or a suitable salt of the compound and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents.

55. 发明公开

EP2297128A1 INHIBITORS OF IKK- SERINE-THREONINE PROTEIN KINASE 有权
标题翻译： IKK-丝氨酸 - 苏氨酸蛋白激酶的抑制剂
公开(公告)号：EP2297128A1
公开(公告)日：2011-03-23
申请号：EP08737089.6
申请日：2008-04-23
申请人： Chroma Therapeutics Ltd.
发明人： MOFFAT, David, Festus, Charles , DAVIES, Stephen, John , CHARLTON, Michael, Hugh , HIRST, Simon, Christopher , ONIONS, Stuart, Thomas , WILLIAMS, Jonathon, Gareth
IPC分类号： C07D333/38 , A61K31/381 , A61P25/28 , A61P37/00
CPC分类号： C07D333/38
摘要： Cyclopentyl (2S,4
E )-2-amino-5-{3-[4-carbamoyl-5 (carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl (2S,4
E )-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl (2S,4
E )-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl
O -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl
O -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienylJphenyl}-L-homoserinate; Cyclopentyl
N -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and
tert -Butyl
N -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.
摘要翻译：（2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5-（氨基甲酰氨基）-2-噻吩基]苯基}戊-4-烯酸环戊酯; 5- {3- [4-氨基甲酰基-5-（氨基甲酰氨基）-2-噻吩基]苯基} -L-正缬氨酸环戊酯; （2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基] -5-甲基苯基}戊-4-烯酸环戊酯; （2S，4E）-2-氨基-5- {5- [4-氨基甲酰基-5-（氨基甲酰氨基）-2-噻吩基] -2-甲基苯基}戊-4-烯酸环戊酯; O- [3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸酯; O- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸环戊酯; N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸环戊酯; 和N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸叔丁酯通过细胞内羧酸酯酶水解成相应的羧酸，并用于抑制IKKβ活性。

56. 发明公开

EP2288600A1 SUBSTITUTED ARYLCYCLOPENTENES AS PROSTAGLANDIN EP2 AGONISTS 审中-公开
标题翻译：取代ARYLCYCLOPENTENE前列腺素EP2受体激动剂
公开(公告)号：EP2288600A1
公开(公告)日：2011-03-02
申请号：EP09734769.4
申请日：2009-04-22
申请人： Allergan, Inc.
发明人： DONDE, Yariv , NGUYEN, Jeremiah, H.
IPC分类号： C07D333/38 , A61K31/381 , A61P27/06 , A61P17/14
CPC分类号： C07D333/38 , Y10S514/88
摘要： Compounds comprising formula (I) or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, and B are as described. Methods, compositions, and medicaments for the treatment of glaucoma, ocula hypertension and inflammatory bowel disease, and for the stimulation of hair growth are also disclosed.

57. 发明公开

EP2285797A1 SUBSTITUTED THIOPHENECARBOXAMIDES AS IKK-BETA SERINE-, THREONINE-PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：取代噻吩羧AS IKK-BETA-SERIN-，苏氨酸蛋白激酶抑制剂
公开(公告)号：EP2285797A1
公开(公告)日：2011-02-23
申请号：EP09733957.6
申请日：2009-04-23
申请人： Chroma Therapeutics Ltd.
发明人： MOFFAT, David, Festus, Charles , DAVIES, Stephen, John
IPC分类号： C07D333/38 , A61K31/381
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are IKK inhibitors useful in the treatment of autoimmune and inflammatory diseases: wherein R
7 is hydrogen or optionally substituted (C
1 -C
6 )alkyl; A is an optionally substituted aryl or heteroaryl of 5-13 ring atoms; Z is a radical of formula R
1 C( R
2 )(R
3 )NH-Y-L
1 -X1-(CH
2 )
z - wherein R
1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R
2 and R
3 independently represent the side chain of a natural or non-natural alpha amino acid but neither of R
2 and R
3 is hydrogen, or R
2 and R
3 taken together with the carbon atom to which they are attached form a C
3 -C
7 cycloalkyl ring, and z, Y, L
1 and X
1 are as defined in the claims.

58. 发明授权

EP1421074B1 NOVEL COMPOUNDS 有权
公开(公告)号：EP1421074B1
公开(公告)日：2010-09-29
申请号：EP02751935.4
申请日：2002-07-19
申请人： AstraZeneca AB
发明人： FAULL, Alan , JOHNSTONE, Craig , MORLEY, Andrew , POYSER, Jeffrey Philip
IPC分类号： C07D333/38 , C07D409/02 , A61K31/381 , A61K31/435 , A61K31/495
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D333/38 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08 , C07D491/08
摘要： The invention relates to thiophene carboxamides of formula (I). wherein A, R?1, R2, R3¿, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

59. 发明授权

EP1735275B1 ARYL SULFONES AND USES RELATED THERETO 有权
标题翻译：芳基砜及有关的用途
公开(公告)号：EP1735275B1
公开(公告)日：2010-08-18
申请号：EP05778401.9
申请日：2005-04-14
申请人： Amgen Inc.
发明人： FAN, Pingchen , GOTO, Hiroyuki , HE, Xiao , KAKUTANI, Makoto , LABELLE, Marc , MCMINN, Dustin, L. , POWERS, Jay, P. , REW, Yosup , SUN, Daqing , YAN, Xuelei
IPC分类号： C07C317/22 , C07C317/14 , C07C317/44 , C07D215/36 , C07D233/54 , C07D295/10 , C07D277/36 , C07D277/54 , C07D277/56 , C07D333/34 , C07D333/38 , C07D417/04 , A61K31/10 , A61P3/04 , A61P3/10
CPC分类号： C07C317/44 , C07C317/14 , C07C317/22 , C07C2601/02 , C07D215/36 , C07D233/54 , C07D277/36 , C07D277/54 , C07D277/56 , C07D295/096 , C07D295/112 , C07D417/04
摘要： Aryl sulfone compounds of formula (I) and (II) are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders.

60. 发明公开

EP2189443A4 TRICYCLIC AMIDE COMPOUND 有权
标题翻译： TRICYCLISCHE AMIDVERBINDUNG
公开(公告)号：EP2189443A4
公开(公告)日：2010-08-04
申请号：EP08792457
申请日：2008-08-14
申请人： RES FOUND ITSUU LAB
发明人： AMANO YOHEI , NOGUCHI MASAYUKI , SHUDO KOICHI
IPC分类号： C07C233/65 , A61K31/381 , A61K31/44 , A61K31/455 , A61P35/00 , A61P43/00 , C07C233/81 , C07C311/21 , C07D213/79 , C07D213/81 , C07D213/82 , C07D333/38 , C07D333/40
CPC分类号： C07C233/81 , C07C233/65 , C07C311/21 , C07C2603/28 , C07C2603/34 , C07D213/79 , C07D213/81 , C07D213/82 , C07D333/38 , C07D333/40

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