公开(公告)号：EP1660428A1

公开(公告)日：2006-05-31

申请号：EP04779442.5

申请日：2004-08-17

Applicant: ELI LILLY AND COMPANY

Inventor： GONZALEZ VALCARCEL, Isabel, Cristina ,  MANTLO, Nathan, Bryan ,  SHI, Qing ,  WANG, Minmin ,  WINNEROSKI, Leonard, Larry, Junior ,  XU, Yanping ,  YORK, Jeremy, Schulenburg

IPC: C07C59/68 ,  A61K31/095 ,  A61K31/185 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D213/30 ,  A61K31/095 ,  A61K31/185 ,  A61K45/06 ,  C07B2200/07 ,  C07C59/68 ,  C07C59/72 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C07C61/39 ,  C07C62/34 ,  C07C251/48 ,  C07C317/22 ,  C07C323/20 ,  C07C323/52 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/69 ,  C07D239/26 ,  C07D261/20 ,  C07D263/32 ,  C07D277/24 ,  C07D307/79 ,  A61K2300/00

Abstract: The present invention is directed to a compound of formula I, or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，溶剂合物，水合物或立体异构体，其可用于治疗或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，例如综合征X，II型 糖尿病，高血糖症，高脂血症，肥胖，凝血病，高血压，动脉硬化以及与综合征X和心血管疾病相关的其它疾病。

公开(公告)号：EP1581471A1

公开(公告)日：2005-10-05

申请号：EP02808276.6

申请日：2002-12-20

Applicant: Dabur Research Foundation

Inventor： GURJAR, M., K.,National Chemical Laboratory ,  WAKHARKAR, R., D.,National Chemical Laboratory ,  BORATE, H.B.R.,National Chemical Laboratory ,  DESIRAJU, Gautam, R.,School of Chemistry ,  NANGIA, Ashwini,School of Chemistry ,  SARKHEL, Sanjay,School of Chemistry ,  SAIRAM, K.V.V.M.,School of Chemistry ,  YADAV, J.S.,Indian Inst. of Chemical Technology ,  CHANDRASEKHAR, S.,Indian Inst. of Chemical Techn. ,  BURMAN, Anand, C.,Dabur Research Foundation ,  MUKHERJEE, Rama,Dabur Research Foundation ,  JAGGI, Manu,Dabur Research Foundation ,  SINGH, Anu, T.,Dabur Research Foundation ,  KAPOOR, Kamal, K.,Dabur Research Foundation

IPC: C07C49/753 ,  C07C59/90 ,  C07C205/45 ,  C07C45/50 ,  C07C45/68 ,  C07C45/30 ,  C07C45/67 ,  A61K31/122 ,  A61P35/00 ,  C07C251/44 ,  C07C251/66 ,  C07C235/16 ,  C07C69/63 ,  C07C69/013

CPC classification number: C07C251/44 ,  C07C49/747 ,  C07C49/753 ,  C07C59/90 ,  C07C69/013 ,  C07C205/45 ,  C07C225/22 ,  C07C233/33 ,  C07C251/66 ,  C07C2601/10

Abstract: The invention relates to the use of derivatives of cyclopentenone for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of derivatives of cyclopentenone for the inhibition and/or prevention of cancer of the colon, pancreas, larynx, ovary, duodenum, kidney, oral cavity, prostate, lung, endothelial cells and leukemias.

公开(公告)号：EP1565422A1

公开(公告)日：2005-08-24

申请号：EP03781741.8

申请日：2003-11-20

Applicant: ELI LILLY AND COMPANY

Inventor： BUNEL, Emilio, Enrique ,  GAJEWSKI, Robert, Peter ,  JONES, Charles, David ,  LU, Jianliang ,  MA, Tianwei ,  NAGPAL, Sunil ,  YEE, Ying, Kwong

IPC: C07C59/90 ,  C07C62/24 ,  C07C69/78 ,  C07C235/34 ,  C07C311/50 ,  C07C317/28 ,  C07D257/06 ,  C07D277/34 ,  A61K31/12 ,  A61K31/165 ,  A61K31/18 ,  A61K31/19 ,  A61K31/192 ,  A61K31/235 ,  A61K31/41 ,  A61K31/426

CPC classification number: C07D207/27 ,  C07C59/48 ,  C07C59/64 ,  C07C59/66 ,  C07C59/90 ,  C07C65/24 ,  C07C65/34 ,  C07C65/40 ,  C07C69/732 ,  C07C69/734 ,  C07C69/738 ,  C07C69/76 ,  C07C69/94 ,  C07C235/34 ,  C07C235/42 ,  C07C311/51 ,  C07C317/28 ,  C07D207/26 ,  C07D233/78 ,  C07D257/04 ,  C07D257/06 ,  C07D261/12 ,  C07D271/113 ,  C07D277/34 ,  C07D295/185

Abstract: The present invention relates to novel, non-secosteroidal, diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1a,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.

公开(公告)号：EP1226104A4

公开(公告)日：2005-05-04

申请号：EP00979142

申请日：2000-11-06

Applicant: EMISPHERE TECH INC

Inventor： LEONE-BAY ANDREA ,  KRAFT KELLY ,  MOYE-SHERMAN DESTARDI ,  GSCHNEIDNER DAVID ,  BOYD MARIA A P ,  LIU PUCHUN ,  TANG PINGWAH ,  LIAO JUN ,  SMART JOHN E ,  FREEMAN JOHN J JR

IPC: A61K9/08 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/352 ,  A61K31/727 ,  A61K38/00 ,  A61K38/21 ,  A61K38/23 ,  A61K38/27 ,  A61K38/28 ,  A61K45/00 ,  A61K47/12 ,  A61K47/18 ,  A61P3/10 ,  A61P5/10 ,  A61P5/14 ,  A61P5/48 ,  A61P7/02 ,  A61P19/08 ,  A61P19/10 ,  A61P31/04 ,  A61P37/08 ,  A61P43/00 ,  C07C59/66 ,  C07C59/68 ,  C07C59/90 ,  C07C59/92 ,  C07C65/21 ,  C07C65/24 ,  C07C65/40 ,  C07C205/37 ,  C07C217/84 ,  C07C229/18 ,  C07C229/56 ,  C07C233/25 ,  C07C235/46 ,  C07C235/48 ,  C07C237/30 ,  C07C62/32

CPC classification number: C07C65/24 ,  C07C59/68 ,  C07C59/90 ,  C07C59/92 ,  C07C65/40 ,  C07C229/18 ,  C07C229/56 ,  C07C237/30

公开(公告)号：EP1509188A2

公开(公告)日：2005-03-02

申请号：EP01998301.4

申请日：2001-11-28

Applicant: KARO BIO AB ,  Abbot Laboratories

Inventor： PELCMAN, Benjamin ,  GUSTAFSSON, Annika ,  KYM, Philip, R.

IPC: A61K6/00

CPC classification number: C07D213/30 ,  C07C59/90 ,  C07C69/76 ,  C07C205/35 ,  C07C323/12 ,  C07D277/24 ,  C07D295/088 ,  C07D317/62

Abstract: This invention relates to novel compounds of formula I that are liver selective glucocorticoid receptor antagonists, methods of preparing the compounds and methods for the use of the compounds in the regulation of metabolism and lowering of blood glucose levels.

公开(公告)号：EP1454893A1

公开(公告)日：2004-09-08

申请号：EP04012220.2

申请日：1997-07-14

Applicant: The Regents of the University of California

Inventor： McMorris, Trevor C. ,  Kelner, Michael J.

IPC: C07C49/737 ,  C07C49/755 ,  C07H15/18 ,  C07C69/007 ,  C07C323/22 ,  C07C323/52 ,  C07C39/225 ,  C07F7/18 ,  C07C49/757 ,  C07C205/45 ,  A61K31/12 ,  A61K31/215 ,  A61K31/10

CPC classification number: C07D317/72 ,  C07C35/37 ,  C07C39/17 ,  C07C49/737 ,  C07C49/755 ,  C07C49/757 ,  C07C59/90 ,  C07C69/007 ,  C07C69/96 ,  C07C205/45 ,  C07C323/22 ,  C07C323/52 ,  C07C323/58 ,  C07C2601/14 ,  C07C2603/94 ,  C07D233/54 ,  C07D319/08 ,  C07F7/1856 ,  C07H15/18

Abstract: The present invention provides illudin analogs of general formula (I) where R 1 is (CH 2 ) n -X-Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C 1 - C 8 )alkyl, (C 6 -C 10 )aryl, (C 6 -C 10 )aryl(C 1 -C 4 )alkyl or cyclo(C 3 -C 6 ) alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R 2 is absent; or R 1 and R 2 together comprise a 5-7-membered cyclic ring; R 3 is (C 1 -C 4 )alkyl or H; R 4 is H, SCH 2 CO 2 (C 1 -C 4 )alkyl, O-(C 5 -C 12 )aryl or -S-(C 5 -C 12 )aryl; R 5 is H, OH or absent; R 6 is (C 1 -C 4 )alkyl or absent; R 7 is OH or OSi((C 1 -C 4 )alkyl) 3 ; or R 6 and R 7 together are ethylenedioxy; R 8 is optionally substituted (C 1 -C 4 )alkyl, and the bonds represented by ---- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).

公开(公告)号：EP1438283A1

公开(公告)日：2004-07-21

申请号：EP02772084.6

申请日：2002-10-15

Applicant: NOVO NORDISK A/S

Inventor： SAUERBERG, Per ,  BURY, Paul, Stanley ,  JEPPESEN, Lone ,  MOGENSEN, John, Patrick

IPC: C07C69/734 ,  C07C59/68 ,  C07C229/36 ,  C07C59/90 ,  A61K31/225 ,  A61K31/194 ,  A61P9/00 ,  A61P3/06 ,  A61P3/10 ,  A61P3/04 ,  C07C69/712 ,  C07C323/21

CPC classification number: C07C323/62 ,  C07C51/09 ,  C07C59/68 ,  C07C59/90 ,  C07C69/712 ,  C07C69/734 ,  C07C229/36 ,  C07C323/20

Abstract: A novel class of dicarboxylic acid derivatives, the use of these compounds as phar-maceutical compositions, pharmaceutical compositions comprising the compounds and meth-ods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Prolifera-tor-Activated Receptors (PPAR).

Abstract translation: 一类新的二羧酸衍生物，这些化合物作为药物组合物的用途，包含这些化合物的药物组合物和使用这些化合物和组合物的处理方法。 本发明化合物可用于治疗和/或预防由过氧化物酶体释放激活受体（PPAR）介导的病症。

公开(公告)号：EP1270737A4

公开(公告)日：2004-06-16

申请号：EP01917587

申请日：2001-03-29

Applicant: SHIONOGI & CO

Inventor： ABE KENJI

IPC: A61K31/19 ,  A61K31/192 ,  A61P31/14 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C12Q1/00 ,  C12Q1/18 ,  C12Q1/48 ,  G01N33/52 ,  G01N33/574 ,  C07C57/26 ,  C07C57/30 ,  C12N9/99 ,  C12Q1/25

CPC classification number: C12Q1/48 ,  A61K31/19 ,  A61K31/192 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C12Q1/00 ,  C12Q1/18 ,  G01N33/52 ,  G01N33/57415

Abstract: By incubating a solution containing an enzyme in the absence of any test substance or the substrate of the enzyme, false positive can be reduced in random screening.

公开(公告)号：EP1370510A2

公开(公告)日：2003-12-17

申请号：EP01944599.8

申请日：2001-06-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： WALKER, Michael, A. ,  JOHNSON, Timothy, D. ,  KIM, Oak, A. ,  ZHANG, Yunhui

IPC: C07C59/90 ,  A61K31/19 ,  A61P31/18

CPC classification number: C07D213/30 ,  C07C59/90 ,  C07C235/28 ,  C07C235/74 ,  C07C237/42 ,  C07C311/51 ,  C07C2601/02 ,  C07D213/38 ,  C07D213/40 ,  C07D307/52 ,  C07D317/34 ,  C07D317/40 ,  C07D317/46 ,  C07D317/58 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12

Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the formula (I), or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug of said compound or of a tautomer thereof, wherein R1 is phenyl, wherein said phenyl is substituted from 1-3 times with R?2, or R1¿ naphthyl, and wherein said naphthyl is optionally substituted from 1-3 times with R2; each R2 is independently selected from halo, C¿1?-C3 alkyl, C1-C2 alkoxy, C1-C3 haloalkyl, and phenyl-(CH2)mOn-; m is 0 or 1; n is 0 or 1; and Z is methylene or -C(O)-, provided that when Z is -C(O)- said substituted phenyl is not ortho-chloro phenyl.

Abstract translation: 本发明涉及式I的化合物R1和Z的HIV整合酶抑制剂如本说明书中所定义。

公开(公告)号：EP1366013A1

公开(公告)日：2003-12-03

申请号：EP02719734.2

申请日：2002-01-28

Applicant: Solchem Italiana S.p.A

Inventor： GUAZZI, Giuseppe

IPC: C07C67/31 ,  C07C69/736

CPC classification number: C07C51/367 ,  C07C67/31 ,  C07C2601/02 ,  C07C59/72 ,  C07C59/90 ,  C07C59/68 ,  C07C69/712

Abstract: A process for the preparation of fibrates of formula (I) in which R1 is a halogen atom, a 2,2-dichloro-cyclopropyl group, a (4-chlorophenyl)-hydroxymethyl group, a 4-cholobenzoyl group or a 2-(4-chlorobenzamido)-ethyl group, and R2 is hydrogen or a C1-C4 alkyl group.

Abstract translation: 制备其中R 1是卤素原子的式I的贝特类的制备方法，2,2-二氯 - 环丙基，（4-氯苯基） - 羟基甲基， 氯苯甲酰基或2-（4-氯苯甲酰氨基） - 乙基，R 2是氢或C 1 -C 4烷基 。