JP2009530277A5 - - Google Patents
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- Publication number
- JP2009530277A5 JP2009530277A5 JP2009500411A JP2009500411A JP2009530277A5 JP 2009530277 A5 JP2009530277 A5 JP 2009530277A5 JP 2009500411 A JP2009500411 A JP 2009500411A JP 2009500411 A JP2009500411 A JP 2009500411A JP 2009530277 A5 JP2009530277 A5 JP 2009530277A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- splice variant
- ghrelin splice
- isolated
- gly
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 51
- 102100033367 Appetite-regulating hormone Human genes 0.000 claims 37
- GNKDKYIHGQKHHM-RJKLHVOGSA-N ghrelin Chemical compound C([C@H](NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)CN)COC(=O)CCCCCCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C1=CC=CC=C1 GNKDKYIHGQKHHM-RJKLHVOGSA-N 0.000 claims 36
- 101800001586 Ghrelin Proteins 0.000 claims 35
- 150000001413 amino acids Chemical class 0.000 claims 10
- 125000002252 acyl group Chemical group 0.000 claims 5
- 125000001165 hydrophobic group Chemical group 0.000 claims 5
- 125000006239 protecting group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 101710111255 Appetite-regulating hormone Proteins 0.000 claims 2
- 102100039256 Growth hormone secretagogue receptor type 1 Human genes 0.000 claims 2
- 101710202385 Growth hormone secretagogue receptor type 1 Proteins 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 230000036528 appetite Effects 0.000 claims 2
- 235000019789 appetite Nutrition 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 230000005714 functional activity Effects 0.000 claims 2
- 239000003324 growth hormone secretagogue Substances 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 230000004584 weight gain Effects 0.000 claims 2
- 235000019786 weight gain Nutrition 0.000 claims 2
- -1 γ-maleimido-butyryloxysuccinimide ester Chemical class 0.000 claims 2
- QZGLLONPRSPJNS-UHFFFAOYSA-N 1-(3-benzoyl-2,5-dioxopyrrolidin-3-yl)pyrrole-2,5-dione Chemical compound C1C(=O)NC(=O)C1(N1C(C=CC1=O)=O)C(=O)C1=CC=CC=C1 QZGLLONPRSPJNS-UHFFFAOYSA-N 0.000 claims 1
- GVJXGCIPWAVXJP-UHFFFAOYSA-N 2,5-dioxo-1-oxoniopyrrolidine-3-sulfonate Chemical compound ON1C(=O)CC(S(O)(=O)=O)C1=O GVJXGCIPWAVXJP-UHFFFAOYSA-N 0.000 claims 1
- MDNSLPICAWKNAG-UHFFFAOYSA-N 2-(2,5-dioxopyrrol-1-yl)propanoic acid Chemical compound OC(=O)C(C)N1C(=O)C=CC1=O MDNSLPICAWKNAG-UHFFFAOYSA-N 0.000 claims 1
- JLLYLQLDYORLBB-UHFFFAOYSA-N 5-bromo-n-methylthiophene-2-sulfonamide Chemical compound CNS(=O)(=O)C1=CC=C(Br)S1 JLLYLQLDYORLBB-UHFFFAOYSA-N 0.000 claims 1
- 102000003916 Arrestin Human genes 0.000 claims 1
- 108090000328 Arrestin Proteins 0.000 claims 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 1
- 229920002307 Dextran Polymers 0.000 claims 1
- 102000000393 Ghrelin Receptors Human genes 0.000 claims 1
- 108010016122 Ghrelin Receptors Proteins 0.000 claims 1
- JLXVRFDTDUGQEE-YFKPBYRVSA-N Gly-Arg Chemical group NCC(=O)N[C@H](C(O)=O)CCCN=C(N)N JLXVRFDTDUGQEE-YFKPBYRVSA-N 0.000 claims 1
- FUESBOMYALLFNI-VKHMYHEASA-N Gly-Asn Chemical group NCC(=O)N[C@H](C(O)=O)CC(N)=O FUESBOMYALLFNI-VKHMYHEASA-N 0.000 claims 1
- SCCPDJAQCXWPTF-VKHMYHEASA-N Gly-Asp Chemical group NCC(=O)N[C@H](C(O)=O)CC(O)=O SCCPDJAQCXWPTF-VKHMYHEASA-N 0.000 claims 1
- MFBYPDKTAJXHNI-VKHMYHEASA-N Gly-Cys Chemical group [NH3+]CC(=O)N[C@@H](CS)C([O-])=O MFBYPDKTAJXHNI-VKHMYHEASA-N 0.000 claims 1
- PNMUAGGSDZXTHX-BYPYZUCNSA-N Gly-Gln Chemical group NCC(=O)N[C@H](C(O)=O)CCC(N)=O PNMUAGGSDZXTHX-BYPYZUCNSA-N 0.000 claims 1
- IEFJWDNGDZAYNZ-BYPYZUCNSA-N Gly-Glu Chemical group NCC(=O)N[C@H](C(O)=O)CCC(O)=O IEFJWDNGDZAYNZ-BYPYZUCNSA-N 0.000 claims 1
- YIWFXZNIBQBFHR-LURJTMIESA-N Gly-His Chemical group [NH3+]CC(=O)N[C@H](C([O-])=O)CC1=CN=CN1 YIWFXZNIBQBFHR-LURJTMIESA-N 0.000 claims 1
- IKAIKUBBJHFNBZ-LURJTMIESA-N Gly-Lys Chemical group NCCCC[C@@H](C(O)=O)NC(=O)CN IKAIKUBBJHFNBZ-LURJTMIESA-N 0.000 claims 1
- BCCRXDTUTZHDEU-VKHMYHEASA-N Gly-Ser Chemical group NCC(=O)N[C@@H](CO)C(O)=O BCCRXDTUTZHDEU-VKHMYHEASA-N 0.000 claims 1
- OLIFSFOFKGKIRH-WUJLRWPWSA-N Gly-Thr Chemical group C[C@@H](O)[C@@H](C(O)=O)NC(=O)CN OLIFSFOFKGKIRH-WUJLRWPWSA-N 0.000 claims 1
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical group NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 1
- 101000979342 Homo sapiens Nuclear factor NF-kappa-B p105 subunit Proteins 0.000 claims 1
- 108091054455 MAP kinase family Proteins 0.000 claims 1
- 102000043136 MAP kinase family Human genes 0.000 claims 1
- NQTADLQHYWFPDB-UHFFFAOYSA-N N-Hydroxysuccinimide Chemical compound ON1C(=O)CCC1=O NQTADLQHYWFPDB-UHFFFAOYSA-N 0.000 claims 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 1
- 108010002311 N-glycylglutamic acid Chemical group 0.000 claims 1
- 102100023050 Nuclear factor NF-kappa-B p105 subunit Human genes 0.000 claims 1
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
- INAPMGSXUVUWAF-GCVPSNMTSA-N [(2r,3s,5r,6r)-2,3,4,5,6-pentahydroxycyclohexyl] dihydrogen phosphate Chemical compound OC1[C@H](O)[C@@H](O)C(OP(O)(O)=O)[C@H](O)[C@@H]1O INAPMGSXUVUWAF-GCVPSNMTSA-N 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 150000007942 carboxylates Chemical class 0.000 claims 1
- 238000010494 dissociation reaction Methods 0.000 claims 1
- 230000005593 dissociations Effects 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003995 emulsifying agent Substances 0.000 claims 1
- 125000005313 fatty acid group Chemical group 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 125000000267 glycino group Chemical group [H]N([*])C([H])([H])C(=O)O[H] 0.000 claims 1
- 108010089804 glycyl-threonine Chemical group 0.000 claims 1
- 108010010147 glycylglutamine Chemical group 0.000 claims 1
- 108010020688 glycylhistidine Chemical group 0.000 claims 1
- 108010015792 glycyllysine Chemical group 0.000 claims 1
- 230000002779 inactivation Effects 0.000 claims 1
- 230000031852 maintenance of location in cell Effects 0.000 claims 1
- MGJXBDMLVWIYOQ-UHFFFAOYSA-N methylazanide Chemical compound [NH-]C MGJXBDMLVWIYOQ-UHFFFAOYSA-N 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 239000006174 pH buffer Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920001515 polyalkylene glycol Polymers 0.000 claims 1
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
- 229940068984 polyvinyl alcohol Drugs 0.000 claims 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000027425 release of sequestered calcium ion into cytosol Effects 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
- 230000005945 translocation Effects 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 239000000080 wetting agent Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78186006P | 2006-03-13 | 2006-03-13 | |
| US60/781,860 | 2006-03-13 | ||
| PCT/US2007/006189 WO2007108990A2 (en) | 2006-03-13 | 2007-03-09 | Use of ghrelin splice variant for treating cachexia and/or anorexia and/or anorexia-cachexia and/or malnutrition and/or lipodystrophy and/or muscle wasting and/or appetite stimulation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009530277A JP2009530277A (ja) | 2009-08-27 |
| JP2009530277A5 true JP2009530277A5 (https=) | 2012-07-19 |
| JP5325092B2 JP5325092B2 (ja) | 2013-10-23 |
Family
ID=38522911
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009500411A Expired - Fee Related JP5325092B2 (ja) | 2006-03-13 | 2007-03-09 | 悪液質および／または食欲不振症および／または食欲不振症−悪液質および／または栄養失調および／または脂肪異栄養症および／または筋肉消耗および／または食欲−刺激を治療するためのグレリンスプライス変異体の使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US7981860B2 (https=) |
| EP (1) | EP1999146B1 (https=) |
| JP (1) | JP5325092B2 (https=) |
| KR (1) | KR101201055B1 (https=) |
| CN (1) | CN101443358B (https=) |
| AU (1) | AU2007227641B2 (https=) |
| BR (1) | BRPI0708895A2 (https=) |
| CA (1) | CA2645844C (https=) |
| NZ (1) | NZ571183A (https=) |
| RU (1) | RU2470940C2 (https=) |
| WO (1) | WO2007108990A2 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7176292B2 (en) * | 2003-09-11 | 2007-02-13 | Dialean, Ltd. | Ghrelin variant protein |
| JP5147827B2 (ja) | 2006-03-28 | 2013-02-20 | リアット・ミンツ | 高コレステロール血症および／または高コレステロールおよび／または高コレステロール関連疾患および／または脂血症および／または脂血症関連疾患および／または冠動脈疾患および／または体重管理および／または糖尿病および／または高血糖の治療のためのグレリンスプライス変種の使用 |
| EP2952522B1 (en) | 2007-01-31 | 2019-10-30 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| AU2008232709C1 (en) | 2007-03-28 | 2015-01-15 | President And Fellows Of Harvard College | Stitched polypeptides |
| KR20170058446A (ko) | 2010-08-13 | 2017-05-26 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| AR088392A1 (es) | 2011-10-18 | 2014-05-28 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| CA2862038C (en) | 2012-02-15 | 2021-05-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| TWI732158B (zh) * | 2012-09-27 | 2021-07-01 | 美商雅瑞塔那醫療公司 | 使用食慾喪失控制化合物之組合物及方法 |
| BR112015009470A2 (pt) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | aminoácidos dissubstituídos e seus métodos de preparação e uso |
| CA2914979C (en) | 2013-07-16 | 2022-12-06 | Liat Mintz | Ghrelin splice variant for treating neuronal damage,neurodegenerative disease, parkinsons disease, alzheimers disease, and/or depression |
| US9119832B2 (en) | 2014-02-05 | 2015-09-01 | The Regents Of The University Of California | Methods of treating mild brain injury |
| EP3182992A4 (en) * | 2014-08-19 | 2018-05-16 | Oxeia Biopharmaceuticals Inc. | Methods of treating mild brain injury |
| WO2016049359A1 (en) | 2014-09-24 | 2016-03-31 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| AU2015322029A1 (en) * | 2014-09-25 | 2017-04-27 | Oxeia Biopharmaceuticals, Inc. | Methods of treating traumatic brain injury |
| US10253067B2 (en) | 2015-03-20 | 2019-04-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| CN105145470A (zh) * | 2015-07-08 | 2015-12-16 | 上海交通大学医学院附属瑞金医院 | 成熟脂肪组织β-catenin敲除的小鼠模型的构建方法 |
| CN105920602B (zh) * | 2016-06-28 | 2021-07-06 | 西安交通大学 | NF-κB p65/HMGCS2调控途径在制备调控酮体合成的药物中的应用 |
| AU2018225163A1 (en) * | 2017-02-22 | 2019-09-19 | Bioincept, Llc | Peptides and methods of treating dystrophy-related disorders using the same |
| CN121627804B (zh) * | 2026-02-04 | 2026-04-17 | 湖南中晟全肽生物科技股份有限公司 | 一种促进生长激素释放的多肽及其应用 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4179337A (en) | 1973-07-20 | 1979-12-18 | Davis Frank F | Non-immunogenic polypeptides |
| US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
| US4501728A (en) | 1983-01-06 | 1985-02-26 | Technology Unlimited, Inc. | Masking of liposomes from RES recognition |
| EP0279582A3 (en) | 1987-02-17 | 1989-10-18 | Pharming B.V. | Dna sequences to target proteins to the mammary gland for efficient secretion |
| US5082767A (en) | 1989-02-27 | 1992-01-21 | Hatfield G Wesley | Codon pair utilization |
| EP0470128B2 (en) | 1989-04-19 | 2003-08-13 | Enzon, Inc. | Active carbonates of polyalkylene oxides for modification of polypeptides |
| US5643575A (en) | 1993-10-27 | 1997-07-01 | Enzon, Inc. | Non-antigenic branched polymer conjugates |
| US5932462A (en) | 1995-01-10 | 1999-08-03 | Shearwater Polymers, Inc. | Multiarmed, monofunctional, polymer for coupling to molecules and surfaces |
| US5869046A (en) | 1995-04-14 | 1999-02-09 | Genentech, Inc. | Altered polypeptides with increased half-life |
| US6291653B1 (en) * | 1997-03-24 | 2001-09-18 | Zymogenetics, Inc. | Antibodies to motilin homologs |
| KR100827973B1 (ko) | 1999-07-23 | 2008-05-21 | 겐지 간가와 | 신규 펩티드 |
| US6646110B2 (en) | 2000-01-10 | 2003-11-11 | Maxygen Holdings Ltd. | G-CSF polypeptides and conjugates |
| CA2411667A1 (en) * | 2000-05-30 | 2001-12-06 | Merck & Co. Inc. | Ghrelin analogs |
| US7244701B2 (en) | 2000-06-16 | 2007-07-17 | Zealand Phama A/S | Diuretic peptide conjugate |
| WO2003097083A1 (en) | 2002-05-21 | 2003-11-27 | Daiichi Suntory Pharma Co.,Ltd. | Medicinal compositions containing ghrelin |
| AU2003254119B2 (en) * | 2002-07-23 | 2007-11-29 | Ipsen Pharma S.A.S. | Ghrelin analogs |
| WO2005014032A2 (en) | 2003-08-06 | 2005-02-17 | Gastrotech Pharma A/S | Use of secretagogues like ghrelin in cancer cachexia and for stimulating appetite |
| US20070037751A1 (en) * | 2003-08-06 | 2007-02-15 | Gastrotech Pharma A/S | Uses of secretagogues like ghrelin in cancer cachexia and for stimulating appetite |
| US7176292B2 (en) * | 2003-09-11 | 2007-02-13 | Dialean, Ltd. | Ghrelin variant protein |
| EP1524274B1 (en) * | 2003-10-16 | 2008-03-05 | F. Hoffmann-La Roche Ag | Fluorescently labelled Ghrelin peptides. |
-
2007
- 2007-03-09 BR BRPI0708895-7A patent/BRPI0708895A2/pt not_active IP Right Cessation
- 2007-03-09 US US11/716,137 patent/US7981860B2/en active Active
- 2007-03-09 NZ NZ571183A patent/NZ571183A/en not_active IP Right Cessation
- 2007-03-09 JP JP2009500411A patent/JP5325092B2/ja not_active Expired - Fee Related
- 2007-03-09 EP EP07752859A patent/EP1999146B1/en not_active Not-in-force
- 2007-03-09 AU AU2007227641A patent/AU2007227641B2/en not_active Ceased
- 2007-03-09 KR KR1020087024810A patent/KR101201055B1/ko not_active Expired - Fee Related
- 2007-03-09 CN CN200780017275.4A patent/CN101443358B/zh not_active Expired - Fee Related
- 2007-03-09 CA CA2645844A patent/CA2645844C/en active Active
- 2007-03-09 RU RU2008140303/10A patent/RU2470940C2/ru not_active IP Right Cessation
- 2007-03-09 WO PCT/US2007/006189 patent/WO2007108990A2/en not_active Ceased
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