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41. 发明授权

EP1169298B1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药剂师VERBINDUNGEN
公开(公告)号：EP1169298B1
公开(公告)日：2006-01-04
申请号：EP00926870.7
申请日：2000-04-11
申请人： NICOX S.A.
发明人： DEL SOLDATO, Piero
IPC分类号： C07C219/06 , C07C219/22 , C07C219/24 , C07D219/10 , C07D233/64 , C07D277/06 , C07D277/14 , C07D309/30 , C07D401/12 , C07D405/14 , C07D417/06 , C07D473/18 , C07D495/04 , C07D499/68 , C07F9/38 , C07H15/252 , C07K5/02 , A61K31/21
CPC分类号： C07H15/252 , C07C219/06 , C07C219/22 , C07C219/24 , C07C271/28 , C07C2601/14 , C07F9/3873 , C07K5/0222
摘要： Compounds or their salts having general formulas (I) and (II) wherein: s = is an integer equal to 1 or 2, preferably s = 2; b0 = 0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.
摘要翻译：具有通式（I）和（II）的化合物或其盐，其中：s =等于1或2，优选s = 2的整数; b0 = 0或1; A是药物的基团，并且是为了满足说明书中报道的药理学试验，C和C 1是两个二价基团。基团B和B 1的前体是满足说明书中报道的药理学试验。

42. 发明公开

EP1575495A2 COMPOUNDS AND METHODS 审中-公开
标题翻译： VERBINDUNGEN UND VERFAHREN
公开(公告)号：EP1575495A2
公开(公告)日：2005-09-21
申请号：EP03745638.1
申请日：2003-03-26
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： THOMPSON, Scott, K. , FRAZEE, James, S. , KALLANDER, Lara, S. , MA, Chun , MARINO, Joseph, P. , NEEB, Michael, J. , BHAT, Ajita , MCATEE, John, Jeffrey , STAVENGER, Robert, A.
IPC分类号： A61K6/00
CPC分类号： C07C311/29 , C07C217/18 , C07C217/20 , C07C217/22 , C07C217/36 , C07C219/22 , C07C229/34 , C07C233/25 , C07C271/28 , C07C275/34 , C07C291/02 , C07C309/73 , C07C311/08 , C07C311/09 , C07C311/21 , C07C323/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D211/34 , C07D211/60 , C07D213/38 , C07D213/64 , C07D213/74 , C07D231/14 , C07D233/64 , C07D239/42 , C07D249/08 , C07D257/04 , C07D295/096 , C07D295/125 , C07D295/185 , C07D307/66 , C07D307/68 , C07D317/58 , C07D317/68 , C07D319/18 , C07D333/20
摘要： Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.
摘要翻译：公开了具有下式的化合物：其药学上可接受的盐或溶剂合物和含有该化合物的药物组合物，其中结构变量如本文所定义。本发明的化合物，盐和溶剂化物可用作LXR激动剂。

43. 发明公开

EP0807111A1 COMPOSES HETEROCYCLIQUES SUBSTITUES, PROCEDE POUR LEUR PREPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT 失效
标题翻译：取代的杂环化合物，PROCESS FOR THEIR AND YOU药物组合物含
公开(公告)号：EP0807111A1
公开(公告)日：1997-11-19
申请号：EP96902305.0
申请日：1996-01-30
申请人： SANOFI
发明人： EMONDS-ALT, Xavier , GROSSRIETHER, Isabelle , GUEULE, Patrick , PROIETTO, Vincenzo , VAN BROECK, Didier
IPC分类号： C07D263 , C07D265 , C07D309 , C07D405 , A61K31 , A61P1 , A61P7 , A61P9 , A61P11 , A61P13 , A61P17 , A61P19 , A61P25 , A61P27 , A61P29 , A61P35 , A61P37 , A61P43 , C07C215 , C07C219 , C07C233 , C07C255 , C07C271 , C07D401 , C07D413 , C07D417 , C07D453
CPC分类号： C07D453/02 , C07C215/28 , C07C215/30 , C07C219/22 , C07C233/18 , C07C255/36 , C07C255/42 , C07C255/43 , C07C271/22 , C07D263/38 , C07D265/32 , C07D309/12 , C07D401/06 , C07D413/06 , C07D413/14 , C07D417/14 , Y02P20/55
摘要： Compounds of formula (I), wherein A is a bivalent radical selected from: A1)-O-CO-, A2)-CH2-O-CO-, A3)-O-CH2-CO-, A4)-O-CH2-CH2-, A5-N(R1)-CO-, A6)-N(R1)-CO-CO-, A7)-N(R1)-CH2-CH2-, A8)-O-CH2-, where R1 is hydrogen or C1-4alkyl, and Am is a heterocyclic nitrogen ring, are provided for use as neurokinin receptor antagonists.

44. 发明授权

EP0446798B1 1-alkyl-, 1-alkenyl- and 1-alkynylaryl-2-amino-1, 3-propanediols and related compounds, a process and intermediates for their preparation and their use as medicaments 有权
标题翻译： 1-烷基，1-链烯基 - 和1-炔基-2-氨基-1,3-丙二醇以及它们的制备和它们作为药物的用途相关的化合物，方法和中间体。
公开(公告)号：EP0446798B1
公开(公告)日：1994-11-23
申请号：EP91103556.6
申请日：1991-03-08
申请人： HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED
发明人： Tegeler, John Joseph , Rauckman, Barbara Seavey , Hamer, Russell Richard Lee , Freed, Brian Scott
IPC分类号： C07D213/28 , C07D213/38 , C07D213/40 , C07D213/61 , C07D333/20 , C07D333/22 , C07D333/24 , C07D213/48 , C07D213/55 , C07D213/56 , C07D261/08
CPC分类号： C07D213/40 , C07C45/68 , C07C47/542 , C07C215/36 , C07C219/22 , C07C233/18 , C07D213/38 , C07D213/48 , C07D213/61 , C07D213/80 , C07D261/08 , C07D333/20 , C07D333/22 , C07D333/24 , C07D405/04 , C07D409/04

45. 发明公开

KR1020110103834A 2-아미노-2-페닐-알칸올 유도체, 이의 제조 및 이것을 함유하는 약학 조성물 无效
标题翻译： 2-氨基-2-苯基 - 烷基醇衍生物，其制备和含有它们的药物组合物
公开(公告)号：KR1020110103834A
公开(公告)日：2011-09-21
申请号：KR1020107016877
申请日：2009-01-30
申请人： 오록셀 , 알렉시 드니
发明人： 알렉시드니 , 빠쇼장 , 디니크리스또프
IPC分类号： C07C219/22 , C07C217/48 , A61K31/24 , A61P29/00
CPC分类号： C07C271/16 , A61K9/2054 , C07C219/22 , C07C271/22 , C07C271/48 , C07C333/04 , C07D213/80 , C07D213/82 , C07D317/40
摘要： 본 발명은 R형 또는 S형의 하기 화학식 (I)의 2-아미노-2-페닐-알칸올 에스테르 유도체 또는 이들의 혼합물 및 존재할 경우 이들의 약학적으로 허용 가능한 염에 관한 것이다:

상기 식 중,
R
1 은 H, 직쇄형 또는 분지쇄형 1∼4C 알킬, OH, 알콕시, 알킬티오, 아실옥시, NH
2 , 알킬아미노, 디알킬아미노, 알킬카르바모일옥시, 알콕시카르보닐아미노, 우레이도 또는 알킬우레이도로 치환된 직쇄형 또는 분지쇄형 2∼4C 알킬이고,
R
2 는 CO-R 라디칼(여기서, R은 H, 알킬, 아릴, 헤테로시클릴, 벤질 또는 헤테로시클릴메틸임)이거나, 또는
R
2 는 -CO-YR
4 라디칼[여기서, Y는 -O-, -S-, -NH-, -Nalk-(여기서, alk는 직쇄형 또는 분지쇄형 (1∼4C) 알킬이고, R
4 는 알킬, 아릴, 아랄킬 또는 헤테로시클릴알킬 (하나 이상의 할로겐 원자 또는 OH 라디칼로 치환될 수 있음), 직쇄형 또는 분지쇄형 (1∼4C) 알킬, 알콕시, 알킬티오, 아실아미노알킬티오, 알콕시카르보닐 또는 아실아미노 (1∼4C) 직쇄형 또는 분지쇄형 또는 옥소이거나, 또는 R
5 COO-(여기서, R
5 는 벤질옥시카르보닐아미노, 아실아미노 또는 아미노산 잔기로 임의로 치환된 알킬이거나 헤테로시클릴 라디칼임)로 치환될 수 있음]이거나, 또는
R
2 는 OH, 알콕시, 알킬티오, 아실옥시, NH
2 , 알킬아미노, 디알킬아미노로 치환된 (2∼4C) 알킬로서, 이것은 이들이 결합된 질소 원자와 함께 임의로 5 또는 6원 복소환을 형성할 수 있고, 상기 복소환은 임의로 다른 헤테로원자(O 또는 N)를 함유하거나 알킬카르바모일옥시, 알콕시카르보닐아미노, 우레이도 또는 알킬우레이도로 치환되며, 상기 치환된 직쇄형 또는 분지쇄형 알킬 라디칼은 >NR
2 및 치환기 사이에 적어도 2C를 포함하며,
R
3 는 직쇄형 또는 분지쇄형 (1∼ 4C) 알킬이고,
구체적으로 달리 언급하지 않는 한, 알킬 또는 아실은 직쇄형 또는 분지쇄형 (1∼7C)이다.

46. 发明公开

KR1020090088442A 아미노알코올 유도체 및 그들의 치료적 용도 无效
标题翻译：氨基醇衍生物及其治疗用途
公开(公告)号：KR1020090088442A
公开(公告)日：2009-08-19
申请号：KR1020097014285
申请日：2007-12-12
申请人： 바이오코피아 리미티드
发明人： 웜슬리,안드레아 , 라스텔라,엘레나
IPC分类号： C07C219/22 , A61K31/222 , A61P19/02 , A61P29/00
CPC分类号： C07D309/08 , C07B2200/07 , C07C219/22
摘要： A compound of formula (1) Including pharmaceutically acceptable salts thereof, wherein: R1 is aryl or heteroaryl optionally substituted with R8; R2 is H or alkyl or CH2 (when forming part of a ring with R3, R4 or R5); R3 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R4 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R5 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R6 is H, alkyl, COH, COOR9, CON(R9)2, COR9, COR10, COR11, P(O)nR9, P(O)nR10S(O)nR10 or S(O)nR9and can be part of a ring with R2, R3, R4 or R5; R7 is H, alkyl, COOR9, COOR11, COR9 or CON(R9)2, and can be part of a ring with R2, R3, R4, R5 or R6; R8 is alkyl, CF3, OR9, OCOR9, CONH2, CN, F, Cl, Br, I, N(R9)2, NO2, NHCHO, NHCONH2, NHSO2R9, CON(R9)2, S(O)nR9, CH2OH Or OCON(R9)2; R9 is H, alkyl or cycloalkyl; R10 is aryl or heteroaryl (optionally substituted with R8) or a four to seven membered ring (which is optionally substituted with R8 and can contain one or more additional heteroatoms selected from the list O, S(O)n and NR9); R11 is alkyl optionally substituted with R8 or R10; and n is O, 1 or 2; provided that when R3, R4 or R5 is CH2OH then R6 is not H, and that when R7 is H and R3, R4 and R5 are alkyl then R6 is not H. is of therapeutic use in the treatment of a condition associated with T-cell proliferation or that is mediated by pro-and/or anti-inflammatory cytokines. ® KIPO & WIPO 2009
摘要翻译：式（1）的化合物包括其药学上可接受的盐，其中：R 1是任选被R 8取代的芳基或杂芳基; R2是H或烷基或CH2（当与R3，R4或R5形成环的一部分时）; R3是H，烷基，CH2OH或CH2OR6，可以是R2的环的一部分; R4是H，烷基，CH2OH或CH2OR6，并且可以是具有R2的环的一部分; R5是H，烷基，CH2OH或CH2OR6，并且可以是具有R2的环的一部分; R6是H，烷基，COH，COOR9，CON（R9）2，COR9，COR10，COR11，P（O）nR9，P（O）nR10S（O）nR10或S（O）nR9， R2，R3，R4或R5; R7是H，烷基，COOR9，COOR11，COR9或CON（R9）2，并且可以是R2，R3，R4，R5或R6的环的一部分; R8是烷基，CF3，OR9，OCOR9，CONH2，CN，F，Cl，Br，I，N（R9）2，NO2，NHCHO，NHCONH2，NHSO2R9，CON（R9）2，S（O）nR9，CH2OH或 OCON（R 9）2; R9为H，烷基或环烷基; R 10是芳基或杂芳基（任选被R 8取代）或4-7元环（其任选被R 8取代并且可以含有一个或多个选自列表O，S（O）n和NR 9的另外的杂原子）; R11是任选被R8或R10取代的烷基; 并且n为O，1或2; 条件是当R 3，R 4或R 5为CH 2 OH时，R 6不为H，当R 7为H且R 3，R 4和R 5为烷基时，R 6不为H.在治疗与T- 细胞增殖或由促炎和/或抗炎细胞因子介导的细胞增殖。 ®KIPO＆WIPO 2009

47. 发明申请

US20170260435A1 Biological Buffers with Wide Buffering Ranges 审中-公开
公开(公告)号：US20170260435A1
公开(公告)日：2017-09-14
申请号：US15606757
申请日：2017-05-26
申请人： Thomas P. Daly
发明人： Thomas P. Daly
IPC分类号： C09K3/00 , C07C215/08 , C07C217/08 , C07C217/48 , C07C219/22 , C07C205/40 , C07D213/74 , C07C309/14 , C07C229/12 , C07C229/22 , C07F9/58 , C07F9/09 , C07F9/38 , C07C217/28 , C07C219/06 , C07D295/088 , C07D295/15 , C07C205/15 , C11D1/66
CPC分类号： C09K3/00 , C07C205/15 , C07C205/40 , C07C215/08 , C07C217/08 , C07C217/28 , C07C217/48 , C07C219/06 , C07C219/22 , C07C229/12 , C07C229/22 , C07C309/14 , C07D213/74 , C07D295/088 , C07D295/15 , C07F9/091 , C07F9/3808 , C07F9/3817 , C07F9/58 , C10L1/10 , C10L1/22 , C10L1/2222 , C10L1/2225 , C10L1/238 , C10L1/2387 , C10L1/2608 , C11D1/66
摘要： Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

48. 发明授权

US09446995B2 Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 有权
标题翻译：以吖啶鎓离子的区域选择性和立体选择性开环为中心的治疗和诊断药物的合成
公开(公告)号：US09446995B2
公开(公告)日：2016-09-20
申请号：US13896524
申请日：2013-05-17
申请人： Hyun-Soon Chong
发明人： Hyun-Soon Chong
IPC分类号： C07C253/14 , C07C209/08 , C07C209/74 , C07C213/00 , C07C209/10 , C07C319/04 , C07C247/10 , C07C327/06 , C07D221/10 , C07B43/00 , C07B43/04 , C07C331/28 , C07C227/18 , C07D255/02 , C07D217/04 , C07D209/16 , C07C209/62 , C07D265/32 , C07D207/404
CPC分类号： C07B43/04 , C07B43/00 , C07B2200/07 , C07C209/08 , C07C209/10 , C07C209/62 , C07C209/74 , C07C213/00 , C07C227/18 , C07C247/10 , C07C253/14 , C07C319/04 , C07C327/06 , C07C331/28 , C07C2102/08 , C07C2602/08 , C07D207/404 , C07D209/16 , C07D217/04 , C07D221/10 , C07D255/02 , C07D265/32 , C07C229/16 , C07C211/27 , C07C229/34 , C07C255/42 , C07C211/29 , C07C215/30 , C07C211/49 , C07C219/22 , C07C323/29
摘要： Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
摘要翻译：通过用于立体选择性和区域选择性合成治疗和诊断化合物的吖啶鎓离子的亲核开环反应的化合物的立体选择性和区域选择性合成。

49. 发明申请

US20160052868A1 Biological buffers with wide buffering ranges 有权
公开(公告)号：US20160052868A1
公开(公告)日：2016-02-25
申请号：US14810106
申请日：2015-07-27
申请人： Thomas P. Daly
发明人： Thomas P. Daly
IPC分类号： C07C229/16 , C07C215/08 , C09K3/00 , C07C217/48 , C07C219/22 , C07C205/40 , C07C205/15 , C07C217/08
CPC分类号： C09K3/00 , C07C205/15 , C07C205/40 , C07C215/08 , C07C217/08 , C07C217/28 , C07C217/48 , C07C219/06 , C07C219/22 , C07C229/12 , C07C229/22 , C07C309/14 , C07D213/74 , C07D295/088 , C07D295/15 , C07F9/091 , C07F9/3808 , C07F9/3817 , C07F9/58 , C11D1/66
摘要： Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

50. 发明申请

US20150175526A2 THE NOVEL REFERENCE MARKERS FOR FESOTERODINE FUMARATE 审中-公开
标题翻译： FESOTERODINE FUMARATE的新参考标记
公开(公告)号：US20150175526A2
公开(公告)日：2015-06-25
申请号：US14370577
申请日：2013-01-08
申请人： Venkatraman Jayaraman , Sundara Kalyana Balaji , Samir Patel , Thakor Indrajit , Viral Parekh , Mahesh Ladani , Chetan Patil , Ronak Patel , Darshan Parmar , Venkatraman Jayaraman , Sundara Kalyana Balaji , Samir Patel , Thakor Indrajit , Viral Parekh , Mahesh Ladani , Chetan Patil , Ronak Patel , Darshan Parmar
发明人： Venkatraman Jayaraman , Sundara Kalyana Balaji , Samir Patel , Thakor Indrajit , Viral Parekh , Mahesh Ladani , Chetan Patil , Ronak Patel , Darshan Parmar
IPC分类号： C07C219/22 , B65D81/26 , A61J1/10 , B65D81/20 , C07C217/48 , C07C213/06
CPC分类号： C07C219/22 , A61J1/10 , A61K31/222 , B65D81/2023 , B65D81/264 , C07C213/06 , C07C213/10 , C07C217/48 , C07C219/28 , G01N33/15
摘要： The present invention relates to the new impurities of Fesoterodine, Fesoterodine symmetric dimer impurity and asymmetric dimer impurity, process for preparing and isolating thereof. The invention also deals with analytical standards and analytical methods used for the control of the production process and final quality of Fesoterodine.
摘要翻译：本发明涉及非索罗定，非索罗定对称二聚体杂质和不对称二聚体杂质的新杂质，其制备和分离方法。本发明还涉及用于控制生产过程和费斯托罗定最终质量的分析标准和分析方法。

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