2009 年2 月 日(05.02.2009)
Contents
1. C _ sec t e rt2. PCT TSA 210 1 2 2007 448 Pcr Jp2008 001 986 c s X 0888 03 S JP 60 42367 A E 1 DU PONT DE NEMOURS amp co 1985 03 06 amp EP 133244 A2 amp EP 133244 Bl amp JP 5 19549 B2 JP 01 110673 A AMERICAN CYANAMID CO 1989 04 27 amp EP 305952 A1 amp US 4847381 A amp EP 305952 B1 amp JP 2760379 B2 WO 2001 24785 A2 INST MOLECULAR amp CELL BIOLOGY 2001 S736 amp EP 1237546 A2 amp JP 2003 510352 A amp US 6841561 B1 WO 2002 36568 Al ASTRAZENECA AB 2002 05
3. pH p DTA
4. ER mg 000mg 1 2 ChemBridge 3 fuo ochem 4 WO 2009 016812 20 PCT JP2008 001986 J Ow Chem 1953 18 910 915 0033
5. I SA J Pp 100 891s 4 3 pCcr rsA 2 io 2 A FUJISAWA PHARM CO LTD 1 2 PCT JP2008 001986 C07D215 52 2006 01 i A61K31 47 2006 01 i A61P7 06 2006 01 i REGISTRY STN 1 4 1 4 1996 01 16 amp US 5643938 A 2004 06 24 Al HE lt
6. p 2 4 WO 2009 016812 15 PCT JP2008 001986 001
7. C oZ FIDE 6 4 3 s ec t e rt a 3 8 lt 5 8 3 8 5 8
8. C 2 6 2 5 ESCH 2 4 2 SA es 2 2 2 3 4 3 2 3 9 2 3 4
9. E k WO 2009 016812 19 PCT JP2008 001986 0029 008 9 0051 0052
10. SO C _ C _ R 3 C _ R 3 C 6
11. C 6 lt 4 lt 3 s ec t ert neo 6 4 6 0 WO 2009 016812 10 PCT JP2008 001986 C 4
12. ENS U AU CNS 6 HAM BEA E LT AB AM Bier KUTA
13. 2 4 R R1 R R 1 1 og 2 4 2 4 2 4
14. PO pPOC PO 7 PO lt 2 3 WO 2009 016812 2 PCT JP2008 001986 000 0004 58
15. PO PO PO PO lt PO PO hypoxia inducible factor HI F 2 HIF F HIF o DP O 2 HIF
16. IF c HI P hypoxia responsible clement HR 7 PO 4 PO 2 HIF p 4 IF PO lt V GF V EGF 5 6 WO 2009 016812 3 PCT JP2008 001986 0005
17. mM 7 V GF HIF PO PO 5 3 IF HR PO IF G ATA 2 NFz PO 8 9 HIF PO 5 IF P O PO GE
18. N N 4 t ert N N WO 2009 016812 18 PCT JP2008 001986 027 008 PO PO D 2 4
19. 57 Abstract Disclosed is a pharmaceutical agent which can enhance the production of EPO and is useful for the prevention and or treatment of anemia Specifically disclosed are an EPO production enhancer comprising a 2 phenylquinoline 4 carboxylic acid derivative represented by the general formula 1 wherein R R2 R3 R4 R R6 R7 R8 R and RO D independently represent a hydrogen atom a halogen atom a C alkyl group which may have 1 to 3 substituents a C cycloalkyl group which may have 1 to 3 substituents or a C alkoxy group which may have 1 to 3 substituents and R represents a hydrogen atom or a Cg alkyl group which may have 1 to 3 substituents a salt of the derivative or a solvate of the derivative or the salt and a prophylactic and or therapeutic agent for a disease whose condition can be ameliorated by enhancing the production of EPO particularly anemia 57 EPO AH 1 R1 R2 R3 R4 R5 R6 R R8 R9 R 1 3 C _ 1 3 OBRE ESL N
20. D R2 R 3 C _ C _ lt D R3 R WO 2009 016812 13 PCT JP2008 001986 0019 R R7 RHs Rs R o 3 C _ 3 WC lt D R1 3 C 3 C _ 2 4
21. WO 2009 016812 11 PCT JP2008 001986
22. DEY 3 P CT 6 4 2 3 SM 1 3 OME RRS 4 5 cc 0 EE MICKA E 03 88 2 HS c 0 ES Ez 48 zt PE BH OK HIB A
23. R R2 R3 R4 R5 2 3 C _ 3 C 3 C _ 3 4 RcO 3 C _ 3 C R2 R3 R R R R3 R R 3 C _ 3 C 3 C _ 3 amp C _ 3 SNA R C _
24. 000 009p Eryth opoietin PO PO 65 PO CRF 2 5 AIDS 6 KK PO PO
25. C _ R 2 R3 R R 3 C 3 C _ 2 4 R R7 Rs Re R r3 C _ 3 C _ C _ WO 2009 016812 14 PCT JP2008 001986 C _ D 2 4 R 3 C _ lt C _
26. 2 HVT CC Jn WO 2009 016812 12 PCT JP2008 001986 0017 0018 C _ SO C _
27. 0 00 6 4 0 2 096 pO R228 PO WO 2009 016812 21 PCT JP2008 001986 0036 2 4 PO P WO 2009 016812 22 PCT JP2008 001986 1 D 163 1 Xm R1 R2 R R R R R7 R R ROR 3 C 3
28. He pG2 Minimum Assen tial Medium M M YAY 24 x T 0O DMEM DM S O 3uM OM 4 0 0u 496 CO 48 PO JI SA Bnzyme Linked ImmunoS Orbent Assay ISA ZPO IISA PO 0 096 pPO 2 004 2 EPO 1 04M 1 6 7 206 a BR WwW bv 005 3 M 0gM
29. C R KART Xii C _ 2 4 P 2 4 PO D 2 4 WO 2009 016812 7 PCT JP2008 001986 0011 2 4
30. 4 PO 7 2 4 PO 7 2 4 WO 2009 016812 8 PCT JP2008 001986 0012 0013 2 4 PO
31. 002 1 2 4 4 2 4 4 2 3 4 4 2 3 4 4 2 4 4 093 2 5 ChemBridge 3 Tu Orochem 4 C Of Chem 1953 18 91 915 2 4 0094 WO 2009 016812 16 PCT JP2008 001986 1652 R R3 Re O RS Q 2 R d R 1 10 H 5 05 R R R
32. 6 29 Aichi JP 74 iH A fe 485 SAEKL Norio T 1030027 RRB 2 15 8 75 TO OD ASHIKAWA Masanori JP JP T 1890022 81 2 17 43 AE AG AL AM AO AT AU AZ BA BB BG Tokyo JP TAGASHIRA BH BR BW BY BZ CA CH CN CO CR CU CZ DE Junya JP JP T 1890022 DK DM DO DZ EC EE EG ES FI GB GD GE GH 2 17 4 3 GM GT HN HR HU ID IL IN IS JP KE KG KM Tokyo JP 48 3 3 KOKETSU Akiyasu JP JP T KN KP KR KZ LA LC LK LR LS LT LU LY MA 1890022 2 17 43 MD ME MG MK MN MW MX MY MZ NA NG NI Tokyo JP NO NZ OM PG PH PL PT RO RS RU sC SD SE 7 54 Title PROPHYLACTIC AND OR THERAPEUTIC AGENT FOR ANEMIA COMPRISING 2 PHENYLQUINOLINE 4 CARBOXYLIC ACID DERIVATIVE AS ACTIVE INGREDIENT 54 2 4
33. PO r 2 4 2 4 D 2 4 PO PO 2 4 2
34. C 3 C R11 3 C _ 2 4 PO 2 2 4 3 P 164 WO 2009 016812 23 PCT JP2008 001986 Xm RI R2 R R R R R7 R8 R9 RUR lS 3 C o ZILELE 3 C 3 C _ R11 3 C _ od 2
35. C 3 C _ R 11 3 C _ o J 2 4 PO PO 7 PO 6 ERNATIONAL S EARCH RE International application No PCT JP2008 001986 A CLASSIFICATION OF SUBJECT MATTER CO7D215 52 2006 01 i A6IK3 1 4 7 2006 01 i A61P7 0 6 2006 01 i According to International Patent Classification IPC or to both national classification and IPC B FIELDS SEARCHED Minimum documentation searched classification system followed by classification symbols C07D215 52 A61K31 47 A61P7 06 Documentation searched other than minimum documentation to the extent that such documents are included in the fields searched Jitsuyo Shinan Koho 1922 1996 Jitsuyo Shinan Toroku Koho 1996 2008 Kokai Jitsuyo Shinan Koho 1971 2008 Toroku Jitsuyo Shinan Koho 1994 2008 Electro
36. C _ C _ C _ 4 C C 5 0 C s C _ C _ C s C _ C _ RES C _ C g C Ce a 7 UV B C2 FIL C _ 5 0 C _ C C _ C _ WO 2009 016812 9 PCT JP2008 001986 0014 0015 C _ C _
37. c 1 3 C s R 1 3 C e 2 4 EPO EPO EL CRM 9 16 12 A1 II RVKIRR RR TRXVIICIIKRIAR RL KY ODO D N TIR IGARI RH WO 2009 016812 A1 lU QA OD URINE NN SG SK SL SM ST SV SY TJ TM TN TR TT TZ CH CY CZ DE DK EE ES FI FR GB GR HR HU UA UG US UZ VC VN ZA ZM ZW IE IS IT LT LU LV MC MT m No PL PT RO SE SI SK TR OAPI BF BJ CF CG CI CM GA GN GQ 84 GW ML MR NE SN TD TG 8E ARIPO BW GH GM KE LS MW MZ NA SD SL SZ TZ UG ZM ZW X 2 Z Y AM AZ BY KG KZ MD RU T TM 3 H y i AT BE BG WO 2009 016812 PCT JP2008 001986 H 2 4
38. 5 3 2 C 2 6 2 5 2 4 2 3 AE 2 4 5 0016 AFORE 4 2 5 0 lt 5 6 5 0O
39. 4 4 PO 3 5 D 5 P RI R2 R3 R R R R7 R8 R9 ROR Z 3 C _ 3 C 3 C _ R11 3 C o J 2 4 P O 6 T WO 2009 016812 24 PCT JP2008 001986 1 xr R R2 R3 R R R R7 R R9 ROR OU F 3 C 3
40. 2 00C OC 00C 0 5 7 p 7 5 4 0 S8 3 DCC 3 3 MaRa WSC T P
41. Y 1 I amp J IT FX A BE 03 3581 1101 3492 200 7 4 B PCT JP200 8 001986 1 2 42585 28338 PCT 17 Q a 1 HE 5 7 DE 5 7 PCT17 2 a G Pcr 39 1 GV 2 J
42. 3 KUC 4 2 4 p II O C 2 0 0 C 5
43. r 2 4 PO m A I DS PO 3 C _ 3 C 3 C _ C e
44. 10 amp EP 1339689 A1 amp US 2004 053964 A1 amp JP 2004 513117 A amp us 6906193 B2 scr SA 2 10 2 2007 4 A
45. 2008 26 08 08 Name and mailing address ofthe ISA Japanese Patent Office Facsimile No Form PCT ISA 210 second sheet April 2007 I DU PONT DE the last paragraph 644762 644762 DIDA 2006 040986 A1 ral F NI EMOURS amp CO 133244 L See patent family annex later document published after the international filing date or ptomty date and not in conflict with the application but cited to understand the p7nciple or theory underlying the invention document of particular relevance the claimed invention cannot be considered novel or cannot be considered to involve an inventive step when the document istaken alone document of particular relevance the claimed invention cannot be considered to involve an inventive step when the document is combined with one or more other such documents such combination being obvious to a person skilled in the art document member of the same patent family Date of mailing ofthe international search report 09 September 2008 09 09 08 A thonzed officer Telephone No INTERNATIONAL SEARCH REPORT International application No PCT JP2008 001986 C Continuation DOCUMENTS CONSIDERED TO BE RELEVANT C Continuation DOCUMENTS CONSIDERED TO BE RELEVANT DOCUMENTS CONSIDERED TO BE RELEVANT Citation of document with indication where appropriate of the relevant passages Relevant to claim No JP 01 110673 A MERICAN CYAN
46. 0006 4 PCT JP2008 001986 P 2 4 lt 1 2 006 37763 2 WO2 003 53997 3 WO2 005 6965NYVILYL 4 WO2 007 3857 5 WO 997 42953 60 WO2002 36568 7 8 9 10 11 12 13 14 1 1985 2 18 1987 3 Med 111 4 I 33 262 5 110 108 11 6 WO2 00 24785 062 48669 59 2 2 6 09228538 2 229 6G 6 3 3428 O673 WO 995 32948 6 0 42367 Lin F K et al Proc Natl Acad Sci USA 82 7580 7584 Bschbach OW Egrie gC Downing MR et al
47. 1811 1813 20M 20 RBS Blood 108 1830 1834 206 PO WO 2009 016812 6 PCT JP2008 001986 0008 0009 001 0 PO H epG2 PO D 461 1 st R1 Rz Re R R R R7 He Re R 3 C 3 0BRMEBERLTEAWUC 3
48. 2 3 Pfitzinger lt HAM Buu Hoi J Org Chem 1953 18 12 9 Jones Quinolines Part 1 r 977 Wiley 97 207 WO 2009 016812 17 PCT JP2008 001986 0026 O 00C 2 24 2 4 2 4 0
49. 2 f 19 43 10 2009 2 5 H 05 02 2009 WO 2009 016812 A1 51 NISHIYAMA Tatsuaki JP JP T 1890022 C07D 215 52 2006 01 A6IP 7 06 2006 01 17 4 3 467 31 47 2006 01 Tokyo JP amp GODA Satoshi JP JP E T 1890022 2 17 438 21 E PCT JP2008 001986 QD HIM KS Tokyo UP WX ER 22 2008 7 23 25 07 2008 YAMABI Masaki JP JP T 1890022 25 EE 2 17 43 Sa Tokyo JP DOI Takeshi JP JP T Q6 1890022 2 17 43 30 Tokyo JP 2007 196778 2007 7 27 27 07 2007 JP ISHIWATA Hiroyuki JP JP T 1890022 71 lt vostro MR EL KOWA COMPANY LTD JP JP 74608625 PA okyo JP
50. 2 0 PO PO 2 4 5 N 6 7 8 lt 9 0 2 CNS NK3 3 4 WO 2009 016812
51. NEM 316 73 Pschbach OW Abdulhadi MH Browne X et al Ann Intern 992 989 Bsrie IL Aschbach W McGuire T Adamson JW Kidney mt 988 Lim VS Degowin RL Zavala D et al Ann ntern Med 4 989 Danna RP Rudnick SA Abels RI Garnick MB Erythropo iet WO 2009 016812 5 PCT JP2008 001986 0007 in in Glinical Applications An International Perspective New York M arcel Dekker 1990 p301 324 7 Sakanaka et al Proc Nat1Acad Sci USA 95 4635 4640 1 998 8 Celik et al Proc Nat IAcad Sci USA 99 2258 2263 200 9 Brines et al Proc Nat1Acad Sci USA 97 10526 10531 2 000 10 Calapai et al EUr J Pharmacol 401 349 356 2000 11 Siren et al Proc Nat1Acad Sci USA 98 4044 404 200 1 12 Spivack gu and Hogans BB Blood 73 90 1989 13 McMahon G et al Blood 76 1718 990 14 Wolfgang Jelkman Internal Medicine 43 649 659 2004 15 Maxwell PH et al Proc Nat lAcad Sci USA 94 15 8104 9 1997 16 Cancer Res 61 15 Fang J et al 5731 5 2001 17 Danna RP Rudnick SA Abels RI Garnick MB Erythropo ie tin in Clinical Applicati ons An International Perspective New York Marcel Dekker 1990 p3 01 324 18 magawa S et al Blood 89 1430 1439 1997 19 ra erlaK et al ASB J 16
52. AMID CO 1 4 27 April 1989 hee 04 89 Claims amp EP 305952 A amp US 4847381 A amp EP 305952 B amp JP 2760379 B2 WO 2001 24785 A2 INST MOLECULAR amp CELL BIOLOGY 12 April 2001 12 04 01 Claims amp EP 1237546 A2 amp JP 2003 510352 A amp US 6841561 Bl WO 2002 36568 Al ASTRAZENE B 10 May 2002 10 05 02 Claims amp EP 1339689 Al amp US 2004 053964 amp JP 2004 513117 A amp US 6906193 B2 Form PCT ISA 210 continuation of second sheet April 2007 INTERNATIONAL SEARCH REPORT International application No PCT JP2008 001986 Box No II Observations where certain claims were found unsearchable Continuation of item 2 of first sheet This international search report has not been established in respect of certain claims under Article 17 2 a for the following reasons l Claims Nos 5 7 because they relate to subject matter not required to be searched by this Authority namely Claims 5 to 7 pertain to a method for treatment of a human body by therapy and thus relate to a subject matter which this International Searching Authority is not required under the provisions of PCT Article 17 2 a i and PCT Rule 39 1 iv to search 2 C Claims Nos because they relate to parts of the international application that do not comply with the prescribed requirements to such an extent that no meaningful international search can be carried ou
53. nic data base consulted during the international search name of data base and where practicable search terms used BIOSIS STN CAplus STN EMBASE STN MEDLINE STN REGISTRY STN C DOCUMENTS CONSIDERED TO BE RELEVANT Citation of document with indication where appropriate of the relevant passages LTD JP 08 500338 A FUJISAWA PHARM Relevant to claim No 16 January 1996 16 01 96 Claims page 12 amp WO 93 25205 A1 amp US 5643938 A amp JP 3269084 B2 in G In in G I amp amp WO 2004 052859 Al KOWA CO 24 June 2004 24 06 04 Claims amp EP 1568691 A1 amp US JP 60 42367 A 06 March 1985 Claims amp EP 133244 A2 amp JP 5 19549 B2 E 06 03 85 E EP E amp X Further documents are listed in the continuation of Box C Special categories of cited documents document defining the general state of the art which is not considered to be of particular relevance earlier application or patent but published on or after the international filing date document which may throw doubts on priority claim s or which is cited to establish the publication date of another citation or other special reason as specified document referring to an oral disclosure use exhibition or other means document published pror to the international filing date but later than the Po7ty date claimed Date ofthe actual completion ofthe international search 26 August
54. of first sheet 2 April 2007 A IPC IntCl B IPC IntCl C07D215 52 A61K31 47 A61P7 06 co BIOSIS STN CAplus STN EMBASE STN MEDLINE STN C t JP 08 300338 amp wo 93 25205 Al amp EP 644762 amp EP 644762 Bl amp JP 3269084 A B2 wo 2004 052859 Al amp EP 1568691 Al amp US 2006 040986 KOWA CO LTD A A E C lt A L lt
55. t specifically 3 Cla nis Nos because they are dependent claims and are not aged in accordance with the second and third sentences of Rule 6 4 a Box No Ill Observations where unity of invention is lacking Continuation of item 3 of first sheet This International Searching Authority found multiple inventions in this international application as follows As all required additional search fees were timely paid by the applicant this international search report covers all searchable claims As all searchable claims could be searched without effort justifying additional fees this Authority did not invite payment of additional fees As only some of the required additional search fees were timely paid by the applicant this international search report covers only those claims for which fees were paid specifically claims Nos Norequired additional search fees were timely paid by the applicant Consequently this international search report is restricted tothe invention first mentioned in the claims it is covered by claims Nos Remark on Protest Tle additional search fees were accompanied by the applicant s protest and where applicable the payment of a protest fee The additional search fees were accompanied by the applicants protest but the applicable protest fee was not paid within the time limit specified in the invitation No protest accompanied the payment of additional search fees Form PCT ISA 210 contmua on
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