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71. 发明公开

EP2121568A2 PREPARATION OF 3-AMINO-3-(CYCLOBUTYLMETHYL)-2-(HYDROXY)-PROPIONAMIDE HYDROCHLORIDE 审中-公开
标题翻译：制备3-氨基-3-（环丁基甲基）-2-（羟基）丙酰胺盐酸盐
公开(公告)号：EP2121568A2
公开(公告)日：2009-11-25
申请号：EP07867791.1
申请日：2007-12-17
申请人： Schering Corporation
发明人： PARK, Jeonghan , VATER, Eugene, J. , DONG, Shuan , IWAMA, Tetsuo , RAGHAVAN, Ramani, R. , LEE, Hong-Chang , WONG, George, S. K.
IPC分类号： C07C205/02 , C07C205/03 , C07C237/14 , C07C205/15 , C07C205/51 , C07C229/22 , C07C231/14 , C07C229/28 , C07C231/02
CPC分类号： C07C1/26 , C07C17/10 , C07C2529/40 , C07C9/00 , C07C19/075
摘要： Disclosed is a process for preparing 3-(amino)-3-cyclobutylmethyl-2-hydroxy-propionamide hydrochloride, an intermediate useful in the preparation of the HCV protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide.

72. 发明授权

EP1735330B1 PROGESTERONE RECEPTOR MODULATORS 有权
标题翻译：孕激素受体调节剂
公开(公告)号：EP1735330B1
公开(公告)日：2007-11-28
申请号：EP05733590.3
申请日：2005-03-18
申请人： N.V. Organon
发明人： HAMERSMA, Johannes Antonius Maria , REWINKEL, Johannes Bernardus Maria
IPC分类号： C07J43/00 , C07J53/00 , A61K31/58 , A61P15/18
CPC分类号： C07J43/003 , C07J5/00 , C07J43/00 , C07J53/001
摘要： The subject invention provides a compound according to Formula I, wherein Formula (1) is O, NOH, NO(1-4C)alkyl, NO(1-4C)acyl; Al-A5 are C, substituted with RI, or N, provided that at least one and not more than three of Al-A5 are N; or one or two of Al, A2 and A5 are N, and the others are C, substituted with Rl, and A3 and A4 together represent a fused benzo ring or a fused five- or six-membered nitrogen-containing aromatic ring, both optionally substituted with one or more halogen and/or (1-4C)alkyl; RI is H, halogen, (1 -4C)alkyl, (1 -4C)alkoxy; R2 is H, (1-4C)alkyl or (1-6C)alkenyl, both optionally substituted with an (6-10)aryl group, which is optionally substituted with one or more halogen and/or (1-4C)alkyl; and R3 is H or (1-4C)alkyl, optionally substituted with one or more halogen atoms; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl; or R2 together with R3 forms a 3-, 4-, 5- or 6-membered carbocyclic ring; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl); or R2 is H or (1-4C)alkyl; and R3 together with R4 forms a 5-, 6- or 7-membered saturated or unsaturated carbocyclic ring; R5 is H or (1-4C)alkyl; or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.

73. 发明公开

EP1511495A1 PROGESTAGENIC DOSAGE UNITS 审中-公开
标题翻译：含孕激素剂量单位
公开(公告)号：EP1511495A1
公开(公告)日：2005-03-09
申请号：EP03735714.2
申请日：2003-05-22
申请人： Akzo Nobel N.V.
发明人： DE HAAN, PieterN.V. Organon
IPC分类号： A61K31/565
CPC分类号： A61K31/565 , A61K9/2018 , A61K9/205 , A61K9/2866
摘要： The subject invention concerns a method of producing pharmaceutical dosage units for oral administration comprising a progestagenic compound which perorally exerts progestagenic activity equivalent to that of the progestagen desogestrel.

74. 发明公开

EP1507867A2 PROCESS FOR FERMENTATION OF PHYTOSTEROLS TO ANDROSTADIENEDIONE 有权
标题翻译：植物甾醇androstadienedione的程序进行发酵
公开(公告)号：EP1507867A2
公开(公告)日：2005-02-23
申请号：EP03734636.8
申请日：2003-02-03
申请人： Akzo Nobel N.V.
发明人： KUTNEY, James, P. , HERRINGTON, Edward, J. , SPASSOV, Grigor
IPC分类号： C12P33/16
CPC分类号： C12R1/77 , C12P33/00
摘要： A process of fermenting a phytosterol composition to produce androstenedione (androst-4-ene-3,17-dione) and subsequently androstadienedione (and rosta-1,4-diene,3,17-dione) comprises propagating a microbial culture of the genus Mycobacterium in a first nutrient medium, placing the microbial culture and the phytosterol composition in a bioreactor for a sufficient time to transform the composition substantially to androstenedione (the 'AD solution'), propagating a fungal culture of the genus Fusarium in a second nutrient medium, and then injecting one or more of 1) Fusarium sp, or 2) the fungal culture medium into the bioreactor for a sufficient time to transform the AD solution to androstadienedione.

75. 发明公开

EP1481251A2 ESTROGEN RECEPTOR INTERACTION WITH A TRANSCRIPTION FACTOR 审中-公开
标题翻译：与转录因子雌激素受体的相互作用
公开(公告)号：EP1481251A2
公开(公告)日：2004-12-01
申请号：EP03714927.5
申请日：2003-02-21
申请人： Akzo Nobel N.V.
发明人： BOERSMA, Christine J. C. , VAN GOOL, Alain J.
IPC分类号： G01N33/74 , C12Q1/68 , C12N15/62 , A61K31/00 , G01N33/68
CPC分类号： G01N33/6893 , G01N33/743
摘要： The invention provides a method to measure a direct interaction between an estrogen receptor and a transactivation protein in an in vitro system by providing for a detection parameter proportionally related to the degree of the interaction, whereby the transactivation protein is c-Rel. In an embodiment of the invention a yeast two-hybrid assay for the measurement is provided. Also is provided a method to influence the direct interaction between an estrogen receptor (ER) and c-Rel in a system, by addition to the system of a compound, which influences the direct interaction between an estrogen receptor (ER) and c-Rel.

76. 发明公开

EP1478613A2 SUBSTITUTED 10-ARYL-11H-BENZO[B]FLUORENES AND 7-ARYL-5,6-DIHYDRO-BENZ[A]ANTHRACENES FOR SELECTIVE EFFECTS ON ESTROGEN RECEPTORS 有权转让
标题翻译：替代品10-ARYL-11H-BENZO [B] FLUORENEFÜRSELEKTIVE EFFEKTE AUF ESTROGEN-RECEPTOREN
公开(公告)号：EP1478613A2
公开(公告)日：2004-11-24
申请号：EP03706624.8
申请日：2003-02-14
申请人： Akzo Nobel N.V.
发明人： LOOZEN, Hubert Jan Jozef,N.V. Organon , WAGENER, Markus,N.V. Organon , VEENEMAN, Gerrit Herman,N.V. Organon , ZWART, Eduard Willem,N.V. Organon
IPC分类号： C07C39/17 , C07C39/42 , C07C43/23 , C07C323/18 , C07D295/08 , A61K31/05 , A61P5/30
CPC分类号： C07D239/42 , C07C39/17 , C07C43/225 , C07C43/23 , C07C49/753 , C07C217/58 , C07C323/18 , C07C2603/40 , C07C2603/42 , C07D211/70 , C07D277/62 , C07D295/088 , C07D317/54
摘要： This invention provides a compound, or its possible salt, having the formula, wherein: Re and 'Re are OH, optionally independently etherified or esterified; Z is -CH2CH2- or -C(R4,R5)- , wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3 , or (1C-4C)alkyl; R2 and R3 are independently H, halogen, -CF3, -OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo (1C-8C)alkyl, -O(CH2)mX, wherein X is halogen or phenyl and m = 2-4; -O(CH2)mNRaRb , -S(CH2)mNRaRb or -(CH2)mNRaRb, wherein m = 2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, -CF3, -OCF3, -CN, -NO2, -OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo (1C-8C) alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, -CF3, -OCF3, -CN, -NO2, hydroxy, hydroxy(1C-4C)alkyl, (1C-8C)alkoxy, aryloxy, (1C-8C)alkylthio, carboxyl, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo (1C-8C) alkyl.
摘要翻译：本发明提供具有下式的化合物或其可能的盐，其中：R e和R e是OH，任选地独立地醚化或酯化; Z是-CH 2 CH 2 - 或-C（R 4，R 5） - ，其中R R 4和R 5独立地为H，（1C-2C）烷基或一起形成螺（3C-5C）环烷基; R 1是H，卤素，CF 3或（1C-4C）烷基; R 2和R 3独立地是H，卤素，-CF 3，-OCF 3，（1C- 8C）烷基，羟基，（1C-8C）烷氧基，芳氧基，芳基（1C-8C）烷基，卤代（1C-8C）烷基，-O（CH 2 CH 2） SUB X，其中X是卤素或苯基，m = 2-4; -O（CH 2）2 - ， - （CH 2 CH 2）n - 或 - （CH 2 2）m - 或 - - - - - （CH 2）其中m = 2-4，并且其中R a，R b，R b各自独立地是（1C -8C）烷基，（2C-8C）烯基，（2C-8C）炔基或芳基，其中烷基，烯基和芳基可任选被卤素取代，-CF 3，-OCF

77. 发明公开

EP1307471A1 16ALPHA-METHYL OR ETHYL SUBSTITUTED ESTROGENS 有权
标题翻译： 16alpha甲基或乙基取代的雌激素
公开(公告)号：EP1307471A1
公开(公告)日：2003-05-07
申请号：EP01960546.8
申请日：2001-07-23
申请人： Akzo Nobel N.V.
发明人： MESTRES, Jordi , LOOZEN, Hubert, Jan, Jozef , VEENEMAN, Gerrit, Herman
IPC分类号： C07J1/00 , A61K31/565 , A61P5/30 , C07J51/00 , C07J71/00
CPC分类号： C07J1/0096 , C07J51/00 , C07J71/001
摘要： The invention makes a 16α-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a Δ5-10 double bond; R1 is (C¿1?-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R?2¿ is (C¿1?-C4)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R?3¿ is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor α selective treatment.

79. 发明授权

EP2560645B1 CONJUGATES OF CC-1065 ANALOGS AND BIFUNCTIONAL LINKERS 有权转让
标题翻译： CC-1065类似物和双功能连接的缀合物
公开(公告)号：EP2560645B1
公开(公告)日：2016-07-13
申请号：EP11720340.6
申请日：2011-04-21
申请人： Syntarga B.V.
发明人： BEUSKER, Patrick, Henry , COUMANS, Rudy, Gerardus, Elisabeth , ELGERSMA, Ronald, Christiaan , MENGE, Wiro, Michaël, Petrus, Bernardus , JOOSTEN, Johannes, Albertus, Frederikus , SPIJKER, Henri, Johannes , DE GROOT, Franciscus, Marinus, Hendrikus
IPC分类号： A61K31/437 , A61P35/00 , A61K47/48 , C07D471/04
CPC分类号： A61K47/64 , A61K31/437 , A61K38/385 , A61K39/44 , A61K47/545 , A61K47/60 , A61K47/643 , A61K47/646 , A61K47/65 , A61K47/6803 , A61K47/6851 , C07D471/04
摘要： This invention relates to novel conjugates of the DNA-alkylating agent CC-1065. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The conjugates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the conjugates of this invention may be used to treat a tumor.

80. 发明公开

EP2791170A1 COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY DISEASES 审中-公开
标题翻译：化合物和方法治疗炎性疾病
公开(公告)号：EP2791170A1
公开(公告)日：2014-10-22
申请号：EP12812562.2
申请日：2012-12-14
申请人： Synthon Biopharmaceuticals B.V.
发明人： ARIAANS, Gerardus Joseph Andreas , DALEN van, Frans , NOLAN, DeclanThomas
IPC分类号： C07K16/24 , A61P17/06 , A61P1/00 , A61P19/02
CPC分类号： C07K16/241 , A61K9/0053 , A61K39/00 , A61K2039/505 , A61K2039/54 , C07K16/244 , C07K2317/13 , C07K2317/24 , C07K2317/41 , C07K2317/565 , C07K2317/76 , C12N15/8258
摘要： A monoclonal secretory IgA antibody, which binds to and neutralizes human p40 (the p40 subunit of IL-12 and IL-23). The secretory antibody is useful in treating a variety of inflammatory conditions in humans.
摘要翻译：分泌型IgA抗体可通过表达在稳定转化的浮萍制成。

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