公开(公告)号：EP3205639A4

公开(公告)日：2018-03-21

申请号：EP15848889

申请日：2015-09-30

Applicant: KYUSHU UNIV NATIONAL UNIV CORPORATION

Inventor： TORIKAI KOHEI

IPC: C07C43/174 ,  C07B41/02 ,  C07B51/00 ,  C07C15/14 ,  C07C22/04 ,  C07C41/16 ,  C07C43/164 ,  C07C309/63 ,  C07D209/04 ,  C07D215/02 ,  C07D333/72

CPC classification number: C07B41/02 ,  C07B51/00 ,  C07C15/14 ,  C07C22/04 ,  C07C41/16 ,  C07C43/164 ,  C07C43/174 ,  C07C309/63 ,  C07D209/04 ,  C07D215/02 ,  C07D333/72 ,  Y02P20/55

Abstract: A novel agent for introducing a protecting group for a hydroxy group and/or a mercapto group that can be introduced and removed under mild conditions is provided. The agent for introducing a protecting group for a hydroxy group and/or mercapto group of a substrate compound having the hydroxy group and/or mercapto group is represented by the following formula (I), wherein A represents a ring structure having 1 to 5 rings in which two carbon atoms of an adjacent benzene ring are included, the ring structure comprises a substituted or unsubstituted five-membered ring or six-membered ring and optionally include a heterocycle; each of R 1 , R 2 , R 3 , and R 4 is independently a hydrogen atom or a linear or branched alkyl group having 1 to 5 carbon atoms; and X is a halogen atom or OSO 2 R 5 (R 5 = an aryl group or an alkyl group) .

公开(公告)号：EP2847166A4

公开(公告)日：2016-01-06

申请号：EP13786971

申请日：2013-04-29

Applicant: BASF SE

Inventor： DÖTZ FLORIAN ,  WEITZ THOMAS ,  JIAO CHONGJUN ,  NOGUCHI HIROYOSHI ,  SWEEMENG ANG ,  ZHOU MI ,  IORI DOI ,  MISHRA ASHOK KUMAR

IPC: H01L51/30 ,  C07D333/50 ,  C07D495/02 ,  H01L51/05

CPC classification number: H01L51/0074 ,  C07D209/86 ,  C07D307/78 ,  C07D307/87 ,  C07D333/52 ,  C07D333/72 ,  C07D495/04 ,  H01L51/0508 ,  H01L51/0545 ,  H01L51/0558 ,  H01L51/42 ,  H01L51/5012 ,  Y02E10/549

公开(公告)号：EP2934133A1

公开(公告)日：2015-10-28

申请号：EP13815504.9

申请日：2013-12-20

Applicant: Novartis Tiergesundheit AG

Inventor： DUPONT, Emilie ,  GAUVRY, Noëlle ,  NANCHEN, Steve ,  OGAWA, Chikako ,  TAHTAOUI, Chouaib

IPC: A01N37/18 ,  A01N43/04 ,  A01N43/08 ,  A01N43/10 ,  A01N43/40

CPC classification number: A01N37/34 ,  A01N37/18 ,  A01N37/30 ,  A01N43/08 ,  A01N43/10 ,  A01N43/16 ,  A01N43/20 ,  A01N43/36 ,  A01N43/40 ,  A01N43/42 ,  A01N43/44 ,  A01N43/80 ,  A01N47/16 ,  C07C233/65 ,  C07C233/66 ,  C07C233/69 ,  C07C237/22 ,  C07C255/29 ,  C07C255/46 ,  C07C255/48 ,  C07C327/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2602/50 ,  C07D205/04 ,  C07D207/273 ,  C07D213/40 ,  C07D213/75 ,  C07D215/48 ,  C07D261/04 ,  C07D295/192 ,  C07D305/06 ,  C07D305/08 ,  C07D307/52 ,  C07D307/79 ,  C07D309/14 ,  C07D331/04 ,  C07D333/38 ,  C07D333/72 ,  C07D409/12

Abstract: The present invention relates to new compounds of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.

Abstract translation: 本发明涉及新的式（I）化合物，其中变量具有如权利要求中所示的含义; 以游离形式和盐形式; 和任选的其对映体和几何异构体。 式（I）化合物可用于控制脊椎动物内和寄生虫上的寄生虫，特别是外寄生虫。

公开(公告)号：EP2399893A2

公开(公告)日：2011-12-28

申请号：EP11177567.2

申请日：2005-12-21

Applicant: Ambrx, Inc.

Inventor： Miao, Zhenwei ,  Liu, Junjie ,  Norman, Thea ,  Driver, Russell

IPC: C07C22/00 ,  C07C227/00 ,  C07C2/00 ,  A61K38/00 ,  C07C251/28 ,  C07D307/83 ,  C07D307/88 ,  C07D307/89 ,  C07D317/22 ,  C07D317/26 ,  C07D317/28 ,  C07D317/30 ,  C07D333/72 ,  C07C229/36 ,  C07C237/32 ,  C07C251/54 ,  C07C251/60 ,  C07C251/86 ,  C07C323/63 ,  C07D209/38

CPC classification number: C07C225/10 ,  A61K31/198 ,  A61K38/17 ,  A61K47/08 ,  A61K47/10 ,  A61K47/34 ,  A61K47/60 ,  C07C229/36 ,  C07C237/32 ,  C07C251/28 ,  C07C251/54 ,  C07C251/60 ,  C07C251/86 ,  C07C323/63 ,  C07C2601/08 ,  C07D209/38 ,  C07D209/46 ,  C07D307/83 ,  C07D307/88 ,  C07D307/89 ,  C07D317/22 ,  C07D317/26 ,  C07D317/28 ,  C07D317/30 ,  C07D333/72 ,  C07K14/61 ,  C12P21/02 ,  G01N33/5008 ,  G01N33/68 ,  G01N33/6848 ,  G01N2500/00 ,  Y02A50/473 ,  Y02P20/55

Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oximine, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

公开(公告)号：EP1735276B1

公开(公告)日：2011-02-16

申请号：EP05715124.3

申请日：2005-03-23

Applicant: LEO PHARMA A/S

Inventor： HANSEN, Erik, Torngaard ,  SABROE, Thomas, Peter ,  CALVERLEY, Martin, John ,  PEDERSEN, Henrik ,  DEUSSEN, Heinz-Josef, Wilhelm

IPC: C07C401/00

CPC classification number: C07C401/00 ,  C07C2601/02 ,  C07D333/72

Abstract: The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.

公开(公告)号：EP1530470A1

公开(公告)日：2005-05-18

申请号：EP03765254.2

申请日：2003-07-16

Applicant: ELI LILLY AND COMPANY

Inventor： DALLY, Robert, Dean ,  DODGE, Jeffrey, Alan ,  FRANK, Scott, Alan ,  JONES, Scott, Alan ,  SHEPHERD, Timothy, Alan ,  WALLACE, Owen, Brendan ,  FONG, Kin, Chiu ,  HUMMEL, Conrad, Wilson ,  LEWIS, Geroge, Sal

IPC: A61K31/4453 ,  A61P5/32 ,  C07D295/08 ,  C07D333/56 ,  C07D333/72 ,  C07D295/12 ,  C07D333/64

CPC classification number: C07D295/088 ,  C07D295/13 ,  C07D333/56 ,  C07D333/64 ,  C07D333/72 ,  C07D409/02

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.

公开(公告)号：EP0986545B1

公开(公告)日：2004-12-29

申请号：EP98928338.7

申请日：1998-06-02

Applicant: SCHERING AKTIENGESELLSCHAFT

Inventor： LEHMANN, Manfred ,  SCHÖLLKOPF, Klaus ,  STREHLKE, Peter ,  HEINRICH, Nikolaus ,  FRITZEMEIER, Karl-Heinrich ,  MUHN, Hans-Peter ,  KRATTENMACHER, Rolf

IPC: C07D249/18 ,  A61K31/41 ,  C07D271/12 ,  C07D285/10 ,  C07C235/26 ,  A61K31/16 ,  C07D307/88 ,  A61K31/365 ,  C07D333/72 ,  A61K31/38 ,  C07D311/76 ,  C07D265/02 ,  A61K31/535 ,  C07D237/32 ,  A61K31/50

CPC classification number: C07D285/10 ,  C07C225/22 ,  C07C235/38 ,  C07C235/84 ,  C07C255/57 ,  C07C2602/08 ,  C07D237/32 ,  C07D249/18 ,  C07D265/02 ,  C07D271/08 ,  C07D307/88 ,  C07D307/94 ,  C07D311/76 ,  C07D333/72 ,  C07D409/12

Abstract: The invention relates to non-steroidal gestagens of general formula (I), wherein R?1 and R2¿ are the same or different and stand for a hydrogen atom, a C¿1?-C5 alkyl group or a halogen atom, or together with the C atom of the chain stand for a ring with 3-7 units, R?3¿ means a C¿1?-C5 alkyl group or a partially or fully fluorinated C1-C5 alkyl group, A stands for an optionally substituted mono or bi-cyclic aromatic ring, an ester group -COOR?4¿, an alkenyl group -CR5=CR6R7, an alkinyl group -C CR5 or for a partially or fully fluorinated C¿1?-C5 alkyl group, B means a carbonyl group or a CH2 group and Ar is a ring system selected from the group of general partial formulae (2-11). When B represents a CH2 group in general formula (I), Ar additionally means a phenyl radical of partial general formula (12). The novel compounds display a very strong affinity to the gestagen receptor. They can be used on their own or in combination with oestrogen's in contraceptive preparations. They can also be used in the treatment of endometriosis. They can be used with oestrogen's in preparations for the treatment of gynaecological disorders. They can also be used to treat pre-menstrual complaints and in substitution therapy. Their androgen activity enables them to be used for male fertility control, male HRT and to treat andrological syndromes.

Abstract translation: 本发明涉及通式（I）的非甾体孕激素，其中R 1和R 2相同或不同，代表氢原子，C1-C5烷基或卤素原子，或一起 链的C原子代表具有3-7个单元的环，R 3表示C 1 -C 5烷基或部分或全部氟化的C 1 -C 5烷基，A代表任选取代的单或双 - 环状芳环，酯基-COOR 4，烯基-CR 5 = CR 6 R 7，炔基-CCR 5或部分或全部氟化的C 1 -C 5烷基 基团，B表示羰基或CH2基团，Ar是选自通式（2-11）的环系。 当B表示通式（I）中的CH 2基时，Ar另外表示部分通式（12）的苯基。 新颖的化合物对孕激素受体表现出非常强的亲和力。 它们可以自己使用，也可以与雌激素在避孕药物中配合使用。 它们也可用于治疗子宫内膜异位症。 它们可用于治疗妇科疾病的制剂中的雌激素。 它们也可以用于治疗月经前的投诉和替代治疗。 他们的雄激素活性使他们能够用于男性生育控制，男性HRT和治疗组织学综合征。

公开(公告)号：EP0570041B1

公开(公告)日：1999-11-10

申请号：EP93201148.9

申请日：1993-04-21

Applicant: AGFA-GEVAERT N.V.

Inventor： Van Rompuy, Ludo ,  Dewanckele, Jean-Marie

IPC: G03F7/07 ,  G03C8/06 ,  G03C1/09 ,  G03C1/485

CPC classification number: G03C1/09 ,  C07C323/16 ,  C07C323/22 ,  C07C327/28 ,  C07D333/72 ,  C07D333/74 ,  G03C1/485 ,  G03C8/06 ,  G03C2001/03517 ,  G03C2001/03564 ,  G03C2007/3032 ,  G03C2200/38 ,  G03F7/07

公开(公告)号：EP0528209B1

公开(公告)日：1999-11-10

申请号：EP92112775.9

申请日：1992-07-27

Applicant: F. HOFFMANN-LA ROCHE AG

Inventor： Manchand, Percy Sarwood ,  Yiannikouros, George Petros

IPC: C07F7/18 ,  C07C401/00

CPC classification number: C07J9/00 ,  C07C401/00 ,  C07D333/72 ,  C07F7/1856 ,  C07F7/1892 ,  C07J51/00

公开(公告)号：EP0794950A1

公开(公告)日：1997-09-17

申请号：EP95941681.0

申请日：1995-12-01

Applicant: AgrEvo UK Limited

Inventor： RIORDAN, Peter, Dominic ,  WEST, Peter, John ,  BODDY, Ian, Kenneth

IPC: A01N43 ,  A01N55 ,  C07D207 ,  C07D231 ,  C07D233 ,  C07D235 ,  C07D249 ,  C07D261 ,  C07D275 ,  C07D277 ,  C07D285 ,  C07D307 ,  C07D333 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D487 ,  C07D495 ,  C07F7

CPC classification number: C07D231/38 ,  A01N43/06 ,  A01N43/36 ,  A01N43/50 ,  A01N43/52 ,  A01N43/54 ,  A01N43/56 ,  A01N43/647 ,  A01N43/653 ,  A01N43/74 ,  A01N43/80 ,  A01N43/90 ,  A01N55/00 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D231/22 ,  C07D233/90 ,  C07D235/24 ,  C07D249/06 ,  C07D249/10 ,  C07D261/18 ,  C07D275/03 ,  C07D277/56 ,  C07D285/06 ,  C07D307/68 ,  C07D307/73 ,  C07D307/84 ,  C07D333/38 ,  C07D333/44 ,  C07D333/68 ,  C07D333/72 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D487/04 ,  C07D495/04 ,  C07F7/0812

Abstract: Compounds of formula (I), wherein A is a 5-membered optionally substituted, heteroaryl group comprising at least one hetero atom selected from nitrogen, sulfur and oxygen, which is optionally substituted by one or more of the group R2; R1 is alkyl, cycloakyl, cycloalkenyl, alkenyl, alkynyl, or amino (each of which is optionally substituted), Y1-X-, halogen, cyano, nitro, acyl, acyloxy, optionally substituted heterocyclyl or optionally substituted phenyl; or two adjacent groups together with the carbon atoms to which they are attached can form an optionally substituted benzo ring; R2 has the same meaning as R1 or two adjacent groups together with the carbon atoms to which they are attached can form an optionally substituted heterocyclic ring; Y is alkyl, cycloalkyl, cycloalkenyl, alkenyl or alkynyl, each of which is optionally substituted, hydrogen or acyl; Y1 has the same meaning as Y or is optionally substituted phenyl or optionally substituted heterocyclyl; Z is C(=X?1)-X2-R3¿, cyano, nitro, amino, acyl, optionally substituted heterocyclyl, -C(R?5)=N-OR6¿ or -C(R?5)=N-NR6R7; R3¿ is alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl, phenyl or heterocyclyl, each of which is optionally substituted, hydrogen or an inorganic or organic cationic group; X?1 and X2¿, which may be the same or different, are O or S; R?5, R6 and R7¿ which may be the same or different, are alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl, phenyl or heterocyclyl, each of which is optionally substituted or hydrogen or R?6 and R7¿ together with the atom(s) to which they are attached can form a ring; and n is 0 to 4, have fungicidal activity.