| EP2308861 - MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS [Right-click to bookmark this link] | |||
| Former [2011/15] | Macrocyclic compounds useful as pharmaceuticals | ||
| [2015/20] | Status | No opposition filed within time limit Status updated on 05.01.2018 Database last updated on 19.03.2026 | |
| Former | The patent has been granted Status updated on 27.01.2017 | Most recent event Tooltip | 06.03.2020 | Lapse of the patent in a contracting state New state(s): TR | published on 08.04.2020 [2020/15] | Applicant(s) | For all designated states Eisai R&D Management Co., Ltd. 6-10, Koishikawa 4-chome, Bunkyo-ku Tokyo 112-8088 / JP | [2011/15] | Inventor(s) | 01 /
Boivin, Roch 11 Oakland Road Lawrence, MA 01843 / US | 02 /
Chiba, Kenichi 5-20-401, Oomachi Tsuchiura-shi, Ibaraki / JP | 03 /
Muramoto, Kenzo 4-2-19 Ninomiya, Tsukuba-shi Ibaraki 305-0051 / JP | 04 /
Shirota, Hiroshi 15 Greybirch Circle Belmont, MA 02478 / US | 05 /
Du, Hong 7 Chandler Road Andover Massachusetts 01810 / US | 06 /
Eguchi, Yoshihito 233-38, Toyoshiki Kashiwa-shi, Chiba / JP | 07 /
Fujita, Masanori 128-3-6, Hitachinonishi Ushiku-shi, Ibaraki / JP | 08 /
Gusovsky, Fabian 28 Algonquin Avenue Andover, MA 01810 / US | 09 /
Goto, Masaki 1141-21, Naka Tsuchiura-shi, Ibaraki / JP | 10 /
Harmange, Jean-Christophe 57 William Street Andover, MA 01810 / US | 11 /
Inoue, Atsushi 2-10-15 Matsuhiro Tsukuba-shi / JP | 12 /
Jiang, Yimin 16 Devonshire Lane Londonderry, NH 03053 / US | 13 /
Kawada, Megumi 4-9 Kamiya 2-chome Ushiku-shi, Ibaraki / JP | 14 /
Kawai, Takatoshi 2-11-33, Higashi Tsukuba-shi, Ibaraki / JP | 15 /
Kawakami, Yoshiyuki 3-6-2 Tokodai, Tsukuba-shi Ibaraki / JP | 16 /
KIMURA, Akifumi 7-2, Inarimae Tsukuba-shi, Ibaraki / JP | 17 /
Kotake, Makoto 144-3-515, Abiko Abiko-shi, Chiba / JP | 18 /
Kuboi, Yoshikazu 670-22 Shimohirooka Tsukuba-shi, Ibaraki / JP | 19 /
Lemelin, Charles-André C-38 Scotty Hollow Drive North Chelmsford, MA 01863 / US | 20 /
Li, Xiang-Yi 329 High Plain Road Andover, MA 01810 / US | 21 /
Matsushima, Tomohiro 10-2, Tagu 2-chome Ushiku-shi, Ibaraki / JP | 22 /
Mizui, Yoshiharu 5-74, Ninomiya 4-Chome Tsukuba-shi, Ibaraki / JP | 23 /
Sakurai, Hideki 2-2-34 Ninomiya Tsukuba-shi, Ibaraki 305-0051 / JP | 24 /
Chow, Jesse 16 Stirling Avenue Hooksett, NH 03106 / US | 25 /
Shen, Yong-Chun 21 Villa Roma Drive Tewksbury, MA 01876 / US | 26 /
Spyvee, Mark 75 Laura Lane Hampstead, NH 03841 / US | 27 /
Tanaka, Isao 2-5-16, Ninomiya Tsukuba-shi, Ibaraki / JP | 28 /
Wang, John (Yuan) 344 River Road Andover, MA 01810 / US | 29 /
Yamamoto, Satoshi 3-9-7, Misono Moriya-shi, Ibaraki / JP | 30 /
Yoneda, Naoki 1-15-4-201 Azuma Tsukuba-shi, Ibaraki / JP | [2011/24] |
| Former [2011/15] | 01 /
Boivin, Roch 11 Oakland Road Lawrence, MA 01843 / US | ||
| 02 /
Chiba, Kenichi 5-20-401, Oomachi Tsuchiura-shi, Ibaraki / JP | |||
| 03 /
Muramoto, Kenzo 4-2-19 Ninomiya, Tsukuba-shi Ibaraki 305-0051 / JP | |||
| 04 /
Shirota, Hiroshi 15 Greybirch Circle Belmont, MA 02478 / US | |||
| 05 /
Du, Hong 43 Upland Street North Andover, MA 01845 / US | |||
| 06 /
Eguchi, Yoshihito 233-38, Toyoshiki Kashiwa-shi, Chiba / JP | |||
| 07 /
Fujita, Masanori 128-3-6, Hitachinonishi Ushiku-shi, Ibaraki / JP | |||
| 08 /
Gusovsky, Fabian 28 Algonquin Avenue Andover, MA 01810 / US | |||
| 09 /
Goto, Masaki 1141-21, Naka Tsuchiura-shi, Ibaraki / JP | |||
| 10 /
Harmange, Jean-Christophe 57 William Street Andover, MA 01810 / US | |||
| 11 /
Inoue, Atsushi 2-10-15 Matsuhiro Tsukuba-shi / JP | |||
| 12 /
Jiang, Yimin 16 Devonshire Lane Londonderry, NH 03053 / US | |||
| 13 /
Kawada, Megumi 4-9 Kamiya 2-chome Ushiku-shi, Ibaraki / JP | |||
| 14 /
Kawai, Takatoshi 2-11-33, Higashi Tsukuba-shi, Ibaraki / JP | |||
| 15 /
Kawakami, Yoshiyuki 3-6-2 Tokodai, Tsukuba-shi Ibaraki / JP | |||
| 16 /
KIMURA, Akifumi 7-2, Inarimae Tsukuba-shi, Ibaraki / JP | |||
| 17 /
Kotake, Makoto 144-3-515, Abiko Abiko-shi, Chiba / JP | |||
| 18 /
Kuboi, Yoshikazu 670-22 Shimohirooka Tsukuba-shi, Ibaraki / JP | |||
| 19 /
Lemelin, Charles-André C-38 Scotty Hollow Drive North Chelmsford, MA 01863 / US | |||
| 20 /
Li, Xiang-Yi 329 High Plain Road Andover, MA 01810 / US | |||
| 21 /
Matsushima, Tomohiro 10-2, Tagu 2-chome Ushiku-shi, Ibaraki / JP | |||
| 22 /
Mizui, Yoshiharu 5-74, Ninomiya 4-Chome Tsukuba-shi, Ibaraki / JP | |||
| 23 /
Sakurai, Hideki 2-2-34 Ninomiya Tsukuba-shi, Ibaraki 305-0051 / JP | |||
| 24 /
Chow, Jesse 16 Stirling Avenue Hooksett, NH 03106 / US | |||
| 25 /
Shen, Yong-Chun 21 Villa Roma Drive Tewksbury, MA 01876 / US | |||
| 26 /
Spyvee, Mark 75 Laura Lane Hampstead, NH 03841 / US | |||
| 27 /
Tanaka, Isao 2-5-16, Ninomiya Tsukuba-shi, Ibaraki / JP | |||
| 28 /
Wang, John (Yuan) 344 River Road Andover, MA 01810 / US | |||
| 29 /
Yamamoto, Satoshi 3-9-7, Misono Moriya-shi, Ibaraki / JP | |||
| 30 /
Yoneda, Naoki 1-15-4-201 Azuma Tsukuba-shi, Ibaraki / JP | Representative(s) | Harris, Jennifer Lucy, et al Kilburn & Strode LLP Lacon London 84 Theobalds Road London WC1X 8NL / GB | [N/P] |
| Former [2011/15] | Harris, Jennifer Lucy, et al Kilburn & Strode LLP 20 Red Lion Street London WC1R 4PJ / GB | Application number, filing date | 10075633.7 | 07.03.2003 | [2011/15] | Priority number, date | US20020362883P | 08.03.2002 Original published format: US 362883 P | US20020380711P | 14.05.2002 Original published format: US 380711 P | [2011/15] | Filing language | EN | Procedural language | EN | Publication | Type: | A1 Application with search report | No.: | EP2308861 | Date: | 13.04.2011 | Language: | EN | [2011/15] | Type: | B1 Patent specification | No.: | EP2308861 | Date: | 01.03.2017 | Language: | EN | [2017/09] | Search report(s) | (Supplementary) European search report - dispatched on: | EP | 24.02.2011 | Classification | IPC: | C07D313/00, A61K31/335, A61P29/00, C07D225/06, C07D407/12, C07D491/04, C07D267/00, C07D493/04, A61K31/36, A61K31/395, A61P11/06, A61P17/06, A61P17/16, A61P19/04, A61P35/00, A61P37/06 | [2011/15] | CPC: |
C07D405/12 (EP,US);
C07D313/00 (EP,CN,KR,US);
A61K31/335 (EP,US);
A61K31/36 (EP,US);
A61K31/395 (EP,CN,US);
A61P1/00 (EP);
A61P1/04 (EP);
A61P1/16 (EP);
A61P11/00 (EP);
A61P11/02 (EP);
A61P11/06 (EP);
A61P11/08 (EP);
A61P13/02 (EP);
A61P17/00 (EP);
A61P17/02 (EP);
A61P17/04 (EP);
A61P17/06 (EP);
A61P17/16 (EP);
A61P19/00 (EP);
A61P19/02 (EP);
A61P19/04 (EP);
A61P19/10 (EP);
A61P21/04 (EP);
A61P25/00 (EP);
A61P25/02 (EP);
A61P25/08 (EP);
A61P25/28 (EP);
A61P27/02 (EP);
A61P29/00 (EP);
A61P3/10 (EP);
A61P31/04 (EP);
A61P31/18 (EP);
A61P33/06 (EP);
A61P35/00 (EP);
A61P35/02 (EP);
A61P37/00 (EP);
A61P37/02 (EP);
A61P37/06 (EP);
A61P37/08 (EP);
A61P43/00 (EP);
A61P7/00 (EP);
A61P7/04 (EP);
A61P9/00 (EP);
A61P9/10 (EP);
C07D231/12 (EP,US);
C07D233/56 (EP,US);
C07D249/08 (EP,US);
C07D401/12 (EP,US);
C07D407/12 (KR);
C07D491/04 (EP,US);
C07D491/044 (EP,US);
| Designated contracting states | AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LI, LU, MC, NL, PT, RO, SE, SI, SK, TR [2017/09] |
| Former [2011/15] | AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LI, LU, MC, NL, PT, RO, SE, SI, SK, TR | Extension states | AL | 10.10.2011 | LT | 10.10.2011 | LV | 10.10.2011 | MK | 10.10.2011 | Title | German: | MACROCYCLISCHE VERBINDUNGEN VERWENDBAR ALS ARZNEITMITTELN | [2015/19] | English: | MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS | [2015/20] | French: | COMPOSES MACROCYCLIQUES UTILES EN TANT QU'AGENTS PHARMACEUTIQUES | [2015/19] |
| Former [2011/15] | Macrocyclische verbindungen verwendbar als Arzneitmitteln | ||
| Former [2011/15] | Macrocyclic compounds useful as pharmaceuticals | ||
| Former [2011/15] | Composés macrocycliques utiles en tant qu'agents pharmaceutiques | Examination procedure | 10.10.2011 | Examination requested [2011/46] | 27.01.2012 | Amendment by applicant (claims and/or description) | 02.11.2012 | Despatch of a communication from the examining division (Time limit: M06) | 28.08.2013 | Reply to a communication from the examining division | 13.03.2015 | Cancellation of oral proceeding that was planned for 17.03.2015 | 17.03.2015 | Date of oral proceedings (cancelled) | 15.04.2015 | Communication of intention to grant the patent | 14.08.2015 | Disapproval of the communication of intention to grant the patent by the applicant or resumption of examination proceedings by the EPO | 04.09.2015 | Communication of intention to grant the patent | 12.04.2016 | Despatch of communication that the application is deemed to be withdrawn, reason: fee for grant / fee for printing not paid in time | 21.06.2016 | Fee for grant paid | 21.06.2016 | Fee for publishing/printing paid | 21.06.2016 | Receipt of the translation of the claim(s) | Parent application(s) Tooltip | EP03721353.5 / EP1507773 | Divisional application(s) | The date of the Examining Division's first communication in respect of the earliest application for which a communication has been issued (EP20030721353) is 21.09.2005 | Opposition(s) | 04.12.2017 | No opposition filed within time limit [2018/06] | Request for further processing for: | The application is deemed to be withdrawn due to failure to fulfill actions required for granting the patent | 21.06.2016 | Request for further processing filed | 21.06.2016 | Full payment received (date of receipt of payment) Request granted | 01.07.2016 | Decision despatched | The application is deemed to be withdrawn due to failure to reply to the examination report | 28.08.2013 | Request for further processing filed | 28.08.2013 | Full payment received (date of receipt of payment) Request granted | 09.09.2013 | Decision despatched | The application is deemed to be withdrawn due to failure to reply to the Extended European Search Report/Written Opinion of the International Searching Authority/International Preliminary Examination Report/Supplementary international search report/Supplementary European search report | 27.01.2012 | Request for further processing filed | 27.01.2012 | Full payment received (date of receipt of payment) Request granted | 10.02.2012 | Decision despatched | Fees paid | Renewal fee | 18.01.2011 | Renewal fee patent year 03 | 18.01.2011 | Renewal fee patent year 04 | 18.01.2011 | Renewal fee patent year 05 | 18.01.2011 | Renewal fee patent year 06 | 18.01.2011 | Renewal fee patent year 07 | 18.01.2011 | Renewal fee patent year 08 | 29.03.2011 | Renewal fee patent year 09 | 26.03.2012 | Renewal fee patent year 10 | 27.03.2013 | Renewal fee patent year 11 | 27.03.2014 | Renewal fee patent year 12 | 27.03.2015 | Renewal fee patent year 13 | 31.03.2016 | Renewal fee patent year 14 |
| Opt-out from the exclusive Tooltip competence of the Unified Patent Court | See the Register of the Unified Patent Court for opt-out data | ||
| Responsibility for the accuracy, completeness or quality of the data displayed under the link provided lies entirely with the Unified Patent Court. | Lapses during opposition Tooltip | HU | 07.03.2003 | AT | 01.03.2017 | CY | 01.03.2017 | CZ | 01.03.2017 | DK | 01.03.2017 | EE | 01.03.2017 | ES | 01.03.2017 | FI | 01.03.2017 | IT | 01.03.2017 | MC | 01.03.2017 | RO | 01.03.2017 | SI | 01.03.2017 | SK | 01.03.2017 | TR | 01.03.2017 | IE | 07.03.2017 | LU | 07.03.2017 | BE | 31.03.2017 | BG | 01.06.2017 | GR | 02.06.2017 | PT | 03.07.2017 | [2020/15] |
| Former [2019/46] | HU | 07.03.2003 | |
| AT | 01.03.2017 | ||
| CY | 01.03.2017 | ||
| CZ | 01.03.2017 | ||
| DK | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| MC | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SI | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| IE | 07.03.2017 | ||
| LU | 07.03.2017 | ||
| BE | 31.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| PT | 03.07.2017 | ||
| Former [2019/31] | HU | 07.03.2003 | |
| AT | 01.03.2017 | ||
| CZ | 01.03.2017 | ||
| DK | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| MC | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SI | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| IE | 07.03.2017 | ||
| LU | 07.03.2017 | ||
| BE | 31.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| PT | 03.07.2017 | ||
| Former [2018/24] | AT | 01.03.2017 | |
| CZ | 01.03.2017 | ||
| DK | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| MC | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SI | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| IE | 07.03.2017 | ||
| LU | 07.03.2017 | ||
| BE | 31.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| PT | 03.07.2017 | ||
| Former [2018/13] | AT | 01.03.2017 | |
| CZ | 01.03.2017 | ||
| DK | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| MC | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SI | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| IE | 07.03.2017 | ||
| LU | 07.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| PT | 03.07.2017 | ||
| Former [2018/10] | AT | 01.03.2017 | |
| CZ | 01.03.2017 | ||
| DK | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| MC | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| LU | 07.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| PT | 03.07.2017 | ||
| Former [2018/09] | AT | 01.03.2017 | |
| CZ | 01.03.2017 | ||
| DK | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| MC | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| PT | 03.07.2017 | ||
| Former [2018/06] | AT | 01.03.2017 | |
| CZ | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| MC | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| PT | 03.07.2017 | ||
| Former [2017/51] | AT | 01.03.2017 | |
| CZ | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| PT | 03.07.2017 | ||
| Former [2017/49] | AT | 01.03.2017 | |
| CZ | 01.03.2017 | ||
| EE | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| IT | 01.03.2017 | ||
| RO | 01.03.2017 | ||
| SK | 01.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| Former [2017/48] | AT | 01.03.2017 | |
| CZ | 01.03.2017 | ||
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | ||
| Former [2017/42] | AT | 01.03.2017 | |
| ES | 01.03.2017 | ||
| FI | 01.03.2017 | ||
| BG | 01.06.2017 | ||
| GR | 02.06.2017 | Documents cited: | Search | [ID] EP0606044 (SANDOZ LTD et al.) | [ID] WO9613259 (COR THERAPEUTICS INC et al.) | [ID] WO0038674 (NOVATION PHARMACEUTICALS INC et al.) | [IP] WO0248136 (CHUGAI PHARMACEUTICAL CO LTD et al.) | [I] AGAMUSTA T. ET AL.: "Revised Structure and Stereochemistry of Hypothemycin", CHEM. PHARM. BULL., vol. 41, no. 2, 1993, pages 373 - 375, XP001152923 | [I] TAKEHANA K. ET AL.: "A Radicicol-Related Macrocyclic Nonanketide Compound, Antibiotic LL-Z1640-2, Inhibits the JNK/p38 Pathways in Signal-Specific Manner", BIOCHEM. BIOPHYS. RES. COMM., vol. 257, 1999, pages 19 - 23, XP002244484 DOI: http://dx.doi.org/10.1006/bbrc.1999.0401 | by applicant | GB323845 | EP0606044 | WO0038674 | JPH0840893 | WO9613259 | US5728726 | US5674892 | US5795910 | US5837224 | US6517889 | US6273913 | US6258121 | US6251136 | US6248127 | US6231600 | US6203551 | US6153252 | US6071305 | US5891507 | US5837313 | US2001027340 | US6515016 | US4768523 | US4776337 | US5041126 | US5052998 | US5064435 | US5089606 | US5147370 | US5176626 | US5213580 | US5328471 | US2002106339 | US4336243 | US4615699 | US4751087 | MCGAHREN ET AL., J ORG. CHEM., vol. 43, 1978, pages 2339 | THOMAS SORRELL: "Organic Chemistry", 1999, UNIVERSITY SCIENCE BOOKS | . GREENE, T.W. AND WUTS, P.G.,: "Protective Groups in Organic Synthesis,3rd ed.", 1999, JOHN WILEY & SONS | S.M. BERGE ET AL., J. PHARMACEUTICAL SCIENCES, vol. 66, 1977, pages 1 - 19 | T. HIGUCHI; V. STELLA: "Pro-drugs as Novel Delivery Systems", A.C.S. SYMPOSIUM SERIES, vol. 14 | EDWARD B. ROCHE,: "Bioreversible Carriers in Drug Design", 1987, AMERICAN PHARMACEUTICAL ASSOCIATION AND PERGAMON PRESS | E. W. MARTIN: "Remington's Pharmaceutical Sciences, Sixteenth Edition,", 1980, MACK PUBLISHING CO. | "Defense and Disease", J CLIN. INVESTIG., vol. 107, 2001, pages 7 | "Angiogenesis: Potentials for Pharmacologic Intervention in the Treatment of Cancer, Cardiovascular Diseases, and Chronic Inflammation", PHARMACOLOGICAL REVIEWS, vol. 52, 2000, pages 237 | "The Merck Manual", 1999, MERCK & CO. | P. ANGEL ET AL.: "Function and regulation of AP-1 subunits in skin physiology and pathology", ONCOGENE, vol. 20, 2001, pages 2413 - 2423 | A. GRANDJEAN-LAQUERRIERE ET AL.: "Relative contribution of NF-kB and AP-1 in the modulation by Curcumin and pyrrolidine dithiocarbamate of the UVB-induced cytokine expression by keratinocytes", CYTOKINE, vol. 18, no. 3, 2002, pages 168 - 177 | "Angiogenesis: Potentials for Pharmacologic Intervention in the Treatment of Cancer, Cardiovascular Diseases, and chronic Inflammation", PHARMACOLOGICAL REVIEWS, vol. 52, 2000, pages 253 | PRESBITERO P. ET AL.: "Drug eluting stents do they make the difference?", MINERVA CARDIOANGIOL, vol. 50, no. 5, 2002, pages 431 - 442 | RUYGROK P.N. ET AL.: "Rapamycin in cardiovascular medicine", INTERN. MED J., vol. 33, no. 3, 2003, pages 103 - 109 | MARX S.O. ET AL.: "Bench to bedside: the development of rapamycin and its application to stent restenosis", CIRCULATION, vol. 104, no. 8, 2001, pages 852 - 855 | GOODMAN; GILMAN'S: "The Pharmacological Basis of Therapeutics", 2001, MCGRAW-HILL PRESS, pages: 155 - 173 | CHEN: "Activation of p38 MAP kinase and ERK are required for ultraviolet-B induced c-fos gene expression in human keratinocytes", ONCOGENE, vol. 18, 1999, pages 7469 - 7476 | LI ET AL.: "Rays and arrays: the transcriptional program in the response of human epidermal keratotinocutes to UVB illumination", THE FASEB JOURNAL, 17 September 2001 (2001-09-17) | "Remington's Pharmaceutical Sciences, 16th Edition", 1980, MACK PUBLISHING COMPANY, pages: 1985 | MAIBACH H. I. AND SMITH H. E.: "Percutaneous Penetration Enhancers", 1995, CRC PRESS, INC. | BUYUKTIMKIN ET AL.: "Transdermal and Topical Drug Delivery Systems", 1997, INTERPHARM PRESS INC., article "Chemical Means of Transdermal Drug Permeation Enhancement" | GHOSH, T. K.; PFISTER, W. R.; YUM, S. I.: "Transdermal and Topical Drug Delivery Systems", INTERPHARM PRESS, INC., pages: 249 - 297 | PETERSON, T. A.; DREYER, S. J., PROCEED. INTERN. SYMP. CONTROL. REL. BIOACT. MATER., vol. 21, pages 477 - 478 | WESTER, R. C.; MAIBACH, H. I.: "Percutaneous Absorption, Mechanism, Methodology, Drug Delivery", 1989, MARCEL DEKKER, INC., article "Regional variation in Percutaneous Absorption", pages: 111 - 119 | "The Merck Manual", 1999 | FIESER; FIESER: "Reagents for Organic Synthesis", vol. 1-17, 1991, JOHN WILEY AND SONS | RODD: "Chemistry of Carbon Compounds", vol. 1-5, 1989, ELSEVIER SCIENCE PUBLISHERS | "Organic Reactions", vol. 1-40, 1991, JOHN WILEY AND SONS | MARCH: "Advanced Organic Chemistry 5th ed.", 2001, JOHN WILEY AND SONS | LAROCK: "Comprehensive Organic Transformations: A Guide to Functional Group Preparations", 1990, VCH PUBLISHERS |