公开(公告)号：EP1198454B1

公开(公告)日：2006-03-08

申请号：EP00956343.8

申请日：2000-07-28

申请人： SANDOZ AG

发明人： ASCHER, Gerd ,  BERNER, Heinz ,  HILDEBRANDT, Johannes

IPC分类号： C07D211/60 ,  C07D207/16 ,  C07C323/52 ,  C07D207/34 ,  C07D213/81 ,  C07D213/82 ,  C07D209/42 ,  A61K31/445 ,  A61K31/40 ,  A61K31/21 ,  C07D211/54 ,  C07B59/00

CPC分类号： C07D249/10 ,  C07B59/002 ,  C07B2200/05 ,  C07C323/52 ,  C07C2603/80 ,  C07D207/16 ,  C07D207/34 ,  C07D209/42 ,  C07D211/54 ,  C07D211/56 ,  C07D211/60 ,  C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D233/24 ,  C07D233/64

摘要： A compound of formula (I) wherein R2 is arylene or heterocyclene; or R and R2 together with the nitrogen atom to which they are attached form non-aromatic heterocyclene; and the other residues have various meanings, useful as pharmaceuticals, e.g. antimicrobials.

摘要翻译： 下式的化合物其中R 2是亚芳基或杂环烯，其它残基具有各种含义，可用作药物，例如， 抗菌剂。

公开(公告)号：EP1626958A1

公开(公告)日：2006-02-22

申请号：EP04759769.5

申请日：2004-04-14

申请人： ELI LILLY AND COMPANY

发明人： BLANCO-PILLADO, Maria-Jesus ,  BENESH, Dana, Rae ,  FILLA, Sandra, Ann ,  HUDZIAK, Kevin, John ,  MATHES, Brian, Michael ,  KOHLMAN, Daniel, Timothy ,  YING, Bai-Ping ,  ZHANG, Deyi ,  XU, Yao-Chang

IPC分类号： C07D211/44 ,  C07D211/54 ,  C07D401/12 ,  C07D409/12 ,  A61K31/445 ,  A61P25/06

CPC分类号： C07D401/12 ,  C07D211/44 ,  C07D211/46 ,  C07D211/54 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14

摘要： The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HTIF receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.

公开(公告)号：EP1567495A2

公开(公告)日：2005-08-31

申请号：EP03783254.0

申请日：2003-11-08

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  MASSACHUSETTS INSTITUTE OF TECHNOLOGY

发明人： MAHMOOD, Ashfaq ,  CHENG, Zheng ,  JONES, Alun, G. ,  DAVISON, Alan

IPC分类号： C07D211/56 ,  C07D211/54 ,  C07D211/52 ,  C07D211/32 ,  C07D211/18 ,  C07C211/13 ,  A01N33/02 ,  A01N33/24 ,  A01N37/18 ,  A01N43/40

CPC分类号： C07C323/41 ,  A61K51/0455 ,  A61K51/0478 ,  C07C323/25 ,  C07D211/14 ,  C07D211/52 ,  C07D211/58 ,  C07F13/005

摘要： The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates the methods of imaging tissues, organs or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.

公开(公告)号：EP1534678A1

公开(公告)日：2005-06-01

申请号：EP03771076.1

申请日：2003-07-23

申请人： Sandoz AG

发明人： BERNER, Heinz ,  KERBER, Gabriele

IPC分类号： C07D211/54 ,  C07D211/56 ,  C07D211/58 ,  C07D401/06 ,  A61K31/445 ,  A61K31/45 ,  A61P31/04

CPC分类号： A61K31/445 ,  A61K31/45 ,  C07D207/12 ,  C07D211/20 ,  C07D211/54 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/72 ,  C07D223/06 ,  C07D493/04

摘要： Compounds of formula (I), wherein R1 and R1' are hydrogen or deuterium, R2, R3 and R4 are hydrogen or deuterium, R5 is the residue of an amino acid, X is S or N-ALK, formula (II), is piperidinyl or tetrahydropyridinyl, ALK is (C1-4)alkyl, and R6 is hydrogen, hydroxy or (C2-12)acyloxy, and their use as antimicrobials.

摘要翻译： 其中R 1和R 1'是氢或氘，R 2，R 3和R 4是氢或氘，R 5是氨基酸的残基，X是S或N-ALK，式（II）是 哌啶基或四氢吡啶基，ALK是（C1-4）烷基，R6是氢，羟基或（C2-12）酰氧基，以及它们作为抗菌剂的用途。

公开(公告)号：EP1076053A4

公开(公告)日：2004-11-10

申请号：EP99917160

申请日：1999-04-26

申请人： KUMIAI CHEMICAL INDUSTRY CO ,  IHARA CHEMICAL IND CO

发明人： TORIYABE KEIJI ,  TAKEFUJI NOBUO ,  ITOU MINORU ,  HIRADE TETSUYA ,  NISHIYAMA KIYOTOSHI ,  ASAHIDA MITSUHARU ,  MAEDA YASUNOBU ,  WADA NOBUHIDE ,  FUJISAWA TOYOKAZU ,  YANO HIROYUKI ,  KOMATSU MASAAKI ,  TADA OSAMU

IPC分类号： A01N41/10 ,  A01N43/08 ,  A01N43/10 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/76 ,  A01N43/78 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/445 ,  A61K31/495 ,  A61K31/498 ,  A61K31/50 ,  A61K31/513 ,  A61K31/53 ,  C07C309/00 ,  C07C317/14 ,  C07C317/22 ,  C07C317/32 ,  C07C323/09 ,  C07C323/18 ,  C07C323/31 ,  C07D211/54 ,  C07D213/52 ,  C07D213/57 ,  C07D213/64 ,  C07D231/12 ,  C07D249/08 ,  C07D253/00 ,  C07D263/32 ,  C07D277/26 ,  C07D307/56 ,  C07D333/24 ,  C07D333/28

CPC分类号： C07D213/12 ,  A01N31/08 ,  A01N31/14 ,  A01N33/10 ,  A01N37/08 ,  A01N37/34 ,  A01N41/10 ,  A01N43/08 ,  A01N43/10 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/76 ,  A01N43/78 ,  A01N47/18 ,  C07C317/32 ,  C07C317/48 ,  C07C323/18 ,  C07C323/20 ,  C07C323/36 ,  C07C323/63 ,  C07D213/32 ,  C07D213/48 ,  C07D213/57 ,  C07D213/64 ,  C07D239/36 ,  C07D239/38 ,  C07D239/40 ,  C07D249/08 ,  C07D333/24

摘要： 3-Arylphenyl sulfide derivatives represented by general formula (I) and insecticides and miticides containing these derivatives as the active ingredient, wherein R represents C2-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, etc.; B0 to B2 and B3 represent each hydrogen, halogeno, cyano, C1-4 haloalkyl, etc.; n is 0, 1 or 2; and Ar represents a phenyl, thiophene or pyrazole ring, etc.

公开(公告)号：EP1278728B1

公开(公告)日：2004-08-25

申请号：EP01940321.1

申请日：2001-04-11

申请人： F. HOFFMANN-LA ROCHE AG

发明人： ALANINE, Alexander ,  BUETTELMANN, Bernd ,  HEITZ NEIDHART, Marie-Paule ,  JAESCHKE, Georg ,  PINARD, Emmanuel ,  WYLER, Rene

IPC分类号： C07D207/12 ,  C07D211/54 ,  C07D231/56 ,  C07D263/58 ,  C07D209/34 ,  C07D205/04 ,  A61K31/40 ,  A61K31/44 ,  A61K31/395 ,  A61P25/28

CPC分类号： C07D263/58 ,  C07D205/04 ,  C07D207/12 ,  C07D209/34 ,  C07D211/54 ,  C07D231/56

公开(公告)号：EP1278728A1

公开(公告)日：2003-01-29

申请号：EP01940321.1

申请日：2001-04-11

申请人： F. HOFFMANN-LA ROCHE AG

发明人： ALANINE, Alexander ,  BUETTELMANN, Bernd ,  HEITZ NEIDHART, Marie-Paule ,  JAESCHKE, Georg ,  PINARD, Emmanuel ,  WYLER, Rene

IPC分类号： C07D207/12 ,  C07D211/54 ,  C07D231/56 ,  C07D263/58 ,  C07D209/34 ,  C07D205/04 ,  A61K31/40 ,  A61K31/44 ,  A61K31/395 ,  A61P25/28

CPC分类号： C07D263/58 ,  C07D205/04 ,  C07D207/12 ,  C07D209/34 ,  C07D211/54 ,  C07D231/56

摘要： The invention relates to compounds of formula (I) wherein Ar1 is pyridyl or phenyl, substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group (a) wherein Z1 is a five membered heterocyclic ring, which contains one or two heteroatoms, selected from N or O; R1 is hydrogen, hydroxy or an oxo group; Ar2 is pyridyl or phenyl, optionally substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group (b) wherein Z2 is a five or six membered ring, which optionally contains one or two heteroatoms, selected from N or O; and Q is -S-, -S(O)- or -S(O)¿2?-; X is a bond, -CH(OH)- or -(CH2)n-; A is a bond or -(CHR)m-; R is hydrogen, halogen or hydroxy, independently from each other if m is 2 or 3; Y is -(CR2)m-, -O-, -C=C-, -C C-, piperidin-1-yl, pyrrolidin-1yl or C4-C6-cycloalkyl, which rings are optionally substituted by hydroxy; B is a bond, -O- or -(CHR)m; n is 1 or 2; and m is 1 to 3 and pharmaceutically acceptable acid addition salts thereof with the exception of compounds, wherein A and B are simultaneously a bond and Y is -CHR-. The compounds may be used in the treatment of neurodegenerative diseases.

公开(公告)号：EP0983258A4

公开(公告)日：2001-01-17

申请号：EP98908964

申请日：1998-03-04

申请人： MONSANTO CO

发明人： BARTA THOMAS E ,  BECKER DANIEL P ,  VILLAMIL CLARA I ,  FRESKOS JOHN N ,  MISCHKE BRENT V ,  MULLINS PATRICK B ,  HEINTZ ROBERT M ,  GETMAN DANIEL P ,  MCDONALD JOSEPH J

IPC分类号： C07D211/62 ,  A61K31/16 ,  A61K31/165 ,  A61K31/166 ,  A61K31/17 ,  A61K31/18 ,  A61K31/198 ,  A61K31/27 ,  A61K31/341 ,  A61K31/351 ,  A61K31/36 ,  A61K31/381 ,  A61K31/382 ,  A61K31/40 ,  A61K31/401 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/4465 ,  A61K31/451 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/472 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/54 ,  A61K45/00 ,  A61P1/04 ,  A61P1/14 ,  A61P7/02 ,  A61P7/04 ,  A61P7/08 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P19/08 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07C317/22 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C317/50 ,  C07C323/65 ,  C07D207/16 ,  C07D207/404 ,  C07D211/10 ,  C07D211/46 ,  C07D211/52 ,  C07D211/60 ,  C07D211/64 ,  C07D211/96 ,  C07D213/30 ,  C07D213/32 ,  C07D213/34 ,  C07D213/38 ,  C07D213/63 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/71 ,  C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D217/02 ,  C07D217/26 ,  C07D233/60 ,  C07D233/84 ,  C07D233/90 ,  C07D235/08 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D241/12 ,  C07D249/12 ,  C07D263/32 ,  C07D263/46 ,  C07D263/54 ,  C07D263/56 ,  C07D263/58 ,  C07D277/20 ,  C07D277/26 ,  C07D277/36 ,  C07D277/56 ,  C07D277/62 ,  C07D277/66 ,  C07D277/70 ,  C07D277/74 ,  C07D277/76 ,  C07D295/08 ,  C07D295/14 ,  C07D295/15 ,  C07D307/56 ,  C07D307/68 ,  C07D309/08 ,  C07D317/62 ,  C07D317/64 ,  C07D333/18 ,  C07D333/36 ,  C07D333/38 ,  C07D333/40 ,  C07D333/54 ,  C07D335/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D491/056 ,  C07D491/113 ,  C07D493/10 ,  A61K31/35 ,  C07D211/54 ,  C07D407/12

CPC分类号： C07D213/30 ,  C07C317/22 ,  C07C317/44 ,  C07C323/65 ,  C07D207/16 ,  C07D211/62 ,  C07D213/82 ,  C07D295/15

摘要： An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as is a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metall protease activity.

公开(公告)号：EP1060162A1

公开(公告)日：2000-12-20

申请号：EP98962423.4

申请日：1998-12-08

申请人： Boehringer Ingelheim Pharma KG

发明人： MAIER, Roland ,  MÜLLER, Peter ,  SCHILCHER, Gebhard ,  ADELGOSS, Gebhard ,  HURNAUS, Rudolf ,  MARK, Michael ,  EISELE, Bernhard

IPC分类号： C07D211/54 ,  C07D211/32 ,  C07D211/26 ,  C07D211/70 ,  A61K31/445

CPC分类号： C07D211/26 ,  A23K20/132 ,  A23K50/75 ,  C07D211/54

摘要： The present invention relates to urethanes derived from azacycloalkanes in addition to thio and dithio analogues of general formula (I), wherein m= 0 or 1, n=1or 2, A is a single bond, a straight-chain or branched C1-8 alkylene group, a C2-8 alkenylene or C2-8 alkylene group, whereby an unsaturated group is not directly bonded to radical Y; X and Y is an oxygen or sulphur atom, R?1 and R2¿ are a straight-chain or branched C¿1-6? alkyl group, a C1-4 alkenyl group or a C1-4 alkinyl group, whereby a multiple bond is isolated from the nitrogen-carbon bond, or R?1 and R2 ¿together with the nitrogen atom represent a 5-7 membered saturated heterocyclic ring, whereby one methylene group isolated from the nitrogen atom can be replaced by an oxygen or sulphur atom or by an -NH or -N (alkyl) group, R3-R6 can be identical or different and represent hydrogen atoms or alkyl groups, R7 is a C¿3-7? cycloalkyl group, optionally a phenyl or naphtyl group substituted by two halogen atoms, an alkyl, alkoxy, trifluoromethyl or cyano group or a hydrogen atom, provided that A does not represent a single bond, E is an oxygen or sulphur atom, a methylene, carbonyl or sulfinyl group and R?8¿ represents a hydrogen atom or E represents the -C(R9R10)- group, wherein R10 and adjacent group R8 represent a carbon-carbon bond. The invention also relates to enantiomers, diastereomers and salts thereof, especially physiologically acceptable acid additive salts with valuable properties such as exhibiting an inhibiting effect on cholesterol biosynthesis, in addition to medicaments containing said compounds, the use thereof and a method for the production thereof.

公开(公告)号：EP0743939B1

公开(公告)日：2000-05-10

申请号：EP95907110.1

申请日：1995-02-06

申请人： MERCK SHARP & DOHME LTD.

发明人： BAKER, Raymond ,  MACLEOD, Angus, Murray ,  SEWARD, Eileen, Mary ,  SWAIN, Christopher, John

IPC分类号： C07D211/42 ,  C07D211/54 ,  C07D401/06 ,  A61K31/445

CPC分类号： C07D401/06 ,  C07D211/42 ,  C07D211/54