JP2008539235A5 - - Google Patents
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- JP2008539235A5 JP2008539235A5 JP2008508931A JP2008508931A JP2008539235A5 JP 2008539235 A5 JP2008539235 A5 JP 2008539235A5 JP 2008508931 A JP2008508931 A JP 2008508931A JP 2008508931 A JP2008508931 A JP 2008508931A JP 2008539235 A5 JP2008539235 A5 JP 2008539235A5
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- -1 xanthyl (Xan) Chemical group 0.000 claims 16
- 125000006239 protecting group Chemical group 0.000 claims 14
- 125000003275 alpha amino acid group Chemical group 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 239000000556 agonist Substances 0.000 claims 3
- 150000001408 amides Chemical class 0.000 claims 3
- WTKQMHWYSBWUBE-UHFFFAOYSA-N (3-nitropyridin-2-yl) thiohypochlorite Chemical group [O-][N+](=O)C1=CC=CN=C1SCl WTKQMHWYSBWUBE-UHFFFAOYSA-N 0.000 claims 2
- 125000004217 4-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])* 0.000 claims 2
- 208000010353 Central Nervous System Vasculitis Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 206010063837 Reperfusion injury Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- WSNDAYQNZRJGMJ-UHFFFAOYSA-N 2,2,2-trifluoroethanone Chemical compound FC(F)(F)[C]=O WSNDAYQNZRJGMJ-UHFFFAOYSA-N 0.000 claims 1
- 125000006181 4-methyl benzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])C([H])([H])* 0.000 claims 1
- HTPXFGUCAUTOEL-UHFFFAOYSA-N 9H-fluorene-1-carboxylic acid Chemical compound C1C2=CC=CC=C2C2=C1C(C(=O)O)=CC=C2 HTPXFGUCAUTOEL-UHFFFAOYSA-N 0.000 claims 1
- DNVJGJUGFFYUPT-UHFFFAOYSA-N 9H-fluorene-9-carboxylic acid Chemical group C1=CC=C2C(C(=O)O)C3=CC=CC=C3C2=C1 DNVJGJUGFFYUPT-UHFFFAOYSA-N 0.000 claims 1
- 102000015219 ATP Binding Cassette Transporter 1 Human genes 0.000 claims 1
- 108010064466 ATP Binding Cassette Transporter 1 Proteins 0.000 claims 1
- 206010003284 Arthropathy Diseases 0.000 claims 1
- 208000006673 Asthma Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000001590 Congenital Abnormality Diseases 0.000 claims 1
- 206010011401 Crohn's disease Diseases 0.000 claims 1
- 102100012353 DPP4 Human genes 0.000 claims 1
- 101700039720 DPP4 Proteins 0.000 claims 1
- 206010061619 Deformity Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 1
- KKGQTZUTZRNORY-UHFFFAOYSA-N Fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims 1
- IRXSLJNXXZKURP-UHFFFAOYSA-N Fluorenylmethyloxycarbonyl chloride Chemical compound C1=CC=C2C(COC(=O)Cl)C3=CC=CC=C3C2=C1 IRXSLJNXXZKURP-UHFFFAOYSA-N 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000009883 Joint Disease Diseases 0.000 claims 1
- 208000002780 Macular Degeneration Diseases 0.000 claims 1
- 208000003393 Mammary Paget's Disease Diseases 0.000 claims 1
- 208000010191 Osteitis Deformans Diseases 0.000 claims 1
- 206010061536 Parkinson's disease Diseases 0.000 claims 1
- 206010034636 Peripheral vascular disease Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010040767 Sjogren's syndrome Diseases 0.000 claims 1
- 206010064996 Ulcerative keratitis Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 201000008804 arthropathy Diseases 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 1
- 201000007717 corneal ulcer Diseases 0.000 claims 1
- 201000004624 dermatitis Diseases 0.000 claims 1
- 231100000406 dermatitis Toxicity 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229960005167 everolimus Drugs 0.000 claims 1
- 229940121360 farnesoid X receptor (FXR) agonists Drugs 0.000 claims 1
- 229960000556 fingolimod Drugs 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 230000000302 ischemic Effects 0.000 claims 1
- 230000000116 mitigating Effects 0.000 claims 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 200000000008 restenosis Diseases 0.000 claims 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 claims 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 201000006704 ulcerative colitis Diseases 0.000 claims 1
Claims (12)
- 再狭窄、気腫、ページェット病、ヴェーゲナー肉芽腫症、中枢神経系脈管炎(CNSV)、シェーグレン症候群、角膜潰瘍、潰瘍性大腸炎、再潅流障害、虚血性再潅流障害、ガン、変形性関節症、炎症性腸疾患、アレルギー性鼻炎、悪液質、クローン病、皮膚炎、喘息、勃起機能障害、および黄斑変性からなる群より選択される状態についての哺乳動物における1つ以上の症状を緩和するための組成物であって、
表2、3、4、5、6、7、8、9、10、11、15、16または18に列挙されるペプチドのアミノ酸配列またはレトロアミノ酸配列を含む「D」ペプチドまたは「L」ペプチド
を含む、組成物。 - パーキンソン病および末梢血管疾患からなる群より選択される状態についての哺乳動物における1つ以上の症状を緩和するための組成物であって、
表2、3、4、5、6、7、8、9、10、11または18に列挙されるペプチドのアミノ酸配列またはレトロアミノ酸配列を含む「D」ペプチドまたは「L」ペプチド
を含む、組成物。 - 請求項1〜2のうちのいずれか1項に記載の組成物であって、前記ペプチドは、アミノ酸配列DWFKAFYDKVAEKFKEAF(配列番号5)またはFAEKFKEAVKDYFAKFWD(配列番号104)を含む、組成物。
- 前記ペプチドはさらに、そのアミノ末端またはカルボキシル末端に結合させられた保護基を含む、請求項1〜3のうちのいずれか1項に記載の組成物。
- 前記ペプチドはさらに、そのアミノ酸末端に結合させられた第1の保護基と、そのカルボキシル末端に結合させられた第2の保護基とを含む、請求項1〜3のうちのいずれか1項に記載の組成物。
- 前記第1の保護基および第2の保護基が、アセチル、アミド、および3個から20個の炭素のアルキル基、Fmoc、Tboc、9−フルオレンアセチル基、1−フルオレンカルボン酸基、9−フルオレンカルボン酸基、9−フルオレノン−1−カルボン酸基、ベンジルオキシカルボニル、キサンチル(Xan)、トリチル(Trt)、4−メチルトリチル(Mtt)、4−メトキシトリチル(Mmt)、4−メトキシ−2,3,6−トリメチル−ベンゼンスルホニル(Mtr)、メシチレン−2−スルホニル(Mts)、4,4−ジメトキシベンズヒドリル(Mbh)、トシル(Tos)、2,2,5,7,8−ペンタメチルクロマン−6−スルホニル(Pmc)、4−メチルベンジル、(MeBzl)、4−メトキシベンジル(MeOBzl)、ベンジルオキシ(BzlO)、ベンジル(Bzl)、ベンゾイル(Bz)、3−ニトロ−2−ピリジンスルフェニル(Npys)、1−(4,4−ジメチル−2,6−ジアキソシクロヘキシリデン)エチル(Dde)、2,6−ジクロロベンジル(2,6−DiCl−Bzl)、2−クロロベンジルオキシカルボニル(2−Cl−Z)、2−ブロモベンジルオキシカルボニル(2−Br−Z)、ベンジルオキシメチル(Bom)、t−ブトキシカルボニル(Boc)、シクロヘキシルオキシ(cHxO)、t−ブトキシメチル(Bum)、t−ブトキシ(tBuO)、t−ブチル(tBu)、アセチル(Ac)、およびトリフルオロアセチル(TFA)からなる群より独立して選択される、請求項5に記載の組成物。
- 前記ペプチドは、そのアミノ末端に結合させられた保護基を含み、該アミノ末端保護基が、アセチル、プロペオニル、および3個から20個の炭素のアルキルからなる群より選択される保護基である、請求項1〜6のうちのいずれか1項に記載のペプチド。
- 前記ペプチドは、そのカルボキシル末端に結合させられた保護基を含み、該カルボキシル末端保護基がアミドである、請求項7に記載のペプチド。
- 前記ペプチドが、
そのアミノ末端に結合させられた第1の保護基であって、アセチル、プロペオニル、および3個から20個の炭素のアルキルからなる群より選択される、保護基;および
そのカルボキシル末端に結合させられた第2の保護基であって、アミドである、保護基
を含む、請求項7に記載のペプチド。 - 前記ペプチドが薬理学的に許容される賦形剤と混合されている、請求項1〜9のうちのいずれか1項に記載の組成物。
- 表2、3、4、5、6、7、8、9、10、11、15、16または18に列挙されるペプチドのアミノ酸配列またはレトロアミノ酸配列を含む「D」ペプチドまたは「L」ペプチドと、
CETP阻害剤、FTY720、Certican、DPP4阻害剤、LXRアゴニスト、FXRアゴニスト、ABCA1アゴニスト、CB−1アゴニスト、およびPKC阻害剤からなる群より選択される薬剤と、
を含む、組成物。 - 請求項11に記載の組成物であって、前記ペプチドは、アミノ酸配列DWFKAFYDKVAEKFKEAF(配列番号5)またはFAEKFKEAVKDYFAKFWD(配列番号104)を含む、組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US67643105P | 2005-04-29 | 2005-04-29 | |
US69749505P | 2005-07-07 | 2005-07-07 | |
PCT/US2006/014839 WO2006118805A2 (en) | 2005-04-29 | 2006-04-18 | Peptides and peptide mimetics to treat pathologies characterized by an inflammatory response |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2008539235A JP2008539235A (ja) | 2008-11-13 |
JP2008539235A5 true JP2008539235A5 (ja) | 2009-06-04 |
Family
ID=37308461
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2008508931A Pending JP2008539235A (ja) | 2005-04-29 | 2006-04-18 | 炎症反応によって特徴付けられる病状を処置するためのペプチドおよびペプチド模倣物 |
Country Status (17)
Country | Link |
---|---|
US (1) | US20100227825A1 (ja) |
EP (3) | EP2269623A1 (ja) |
JP (1) | JP2008539235A (ja) |
KR (1) | KR20080007491A (ja) |
AU (1) | AU2006242651B2 (ja) |
BR (1) | BRPI0610983A2 (ja) |
CA (1) | CA2607483A1 (ja) |
EA (2) | EA200900786A1 (ja) |
EC (1) | ECSP077829A (ja) |
IL (1) | IL186959A0 (ja) |
MA (1) | MA29488B1 (ja) |
MX (1) | MX2007013430A (ja) |
NO (1) | NO20076022L (ja) |
NZ (2) | NZ580954A (ja) |
SG (1) | SG173373A1 (ja) |
TN (1) | TNSN07396A1 (ja) |
WO (1) | WO2006118805A2 (ja) |
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-
2006
- 2006-04-18 EP EP10177858A patent/EP2269623A1/en not_active Withdrawn
- 2006-04-18 NZ NZ580954A patent/NZ580954A/en unknown
- 2006-04-18 NZ NZ563187A patent/NZ563187A/en unknown
- 2006-04-18 EP EP11155927.4A patent/EP2368561B1/en active Active
- 2006-04-18 EA EA200900786A patent/EA200900786A1/ru unknown
- 2006-04-18 EP EP06750791A patent/EP1890715A4/en not_active Withdrawn
- 2006-04-18 BR BRPI0610983-7A patent/BRPI0610983A2/pt not_active Application Discontinuation
- 2006-04-18 JP JP2008508931A patent/JP2008539235A/ja active Pending
- 2006-04-18 WO PCT/US2006/014839 patent/WO2006118805A2/en active Application Filing
- 2006-04-18 KR KR1020077027948A patent/KR20080007491A/ko not_active Application Discontinuation
- 2006-04-18 AU AU2006242651A patent/AU2006242651B2/en not_active Ceased
- 2006-04-18 CA CA002607483A patent/CA2607483A1/en not_active Abandoned
- 2006-04-18 MX MX2007013430A patent/MX2007013430A/es active IP Right Grant
- 2006-04-18 SG SG2011051224A patent/SG173373A1/en unknown
- 2006-04-18 EA EA200702392A patent/EA012440B1/ru not_active IP Right Cessation
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2007
- 2007-10-24 TN TNP2007000396A patent/TNSN07396A1/en unknown
- 2007-10-26 EC EC2007007829A patent/ECSP077829A/es unknown
- 2007-10-28 IL IL186959A patent/IL186959A0/en unknown
- 2007-11-22 NO NO20076022A patent/NO20076022L/no not_active Application Discontinuation
- 2007-11-27 MA MA30425A patent/MA29488B1/fr unknown
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2010
- 2010-03-10 US US12/721,366 patent/US20100227825A1/en not_active Abandoned
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