JP2010509195A5 - - Google Patents
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- Publication number
- JP2010509195A5 JP2010509195A5 JP2009534984A JP2009534984A JP2010509195A5 JP 2010509195 A5 JP2010509195 A5 JP 2010509195A5 JP 2009534984 A JP2009534984 A JP 2009534984A JP 2009534984 A JP2009534984 A JP 2009534984A JP 2010509195 A5 JP2010509195 A5 JP 2010509195A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- cyclo
- alkyl
- residue
- och
- 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
- KZOWNALBTMILAP-JBMRGDGGSA-N ancitabine hydrochloride Chemical compound Cl.N=C1C=CN2[C@@H]3O[C@H](CO)[C@@H](O)[C@@H]3OC2=N1 KZOWNALBTMILAP-JBMRGDGGSA-N 0.000 claims 30
- 108090000765 processed proteins & peptides Proteins 0.000 claims 27
- 125000003277 amino group Chemical group 0.000 claims 22
- 239000000816 peptidomimetic Substances 0.000 claims 21
- 235000001014 amino acid Nutrition 0.000 claims 19
- 150000001413 amino acids Chemical class 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 17
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 17
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 16
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 10
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 10
- 235000013922 glutamic acid Nutrition 0.000 claims 10
- 239000004220 glutamic acid Substances 0.000 claims 10
- 125000004974 2-butenyl group Chemical group C(C=CC)* 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 210000004899 c-terminal region Anatomy 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 7
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 7
- 125000004917 3-methyl-2-butyl group Chemical group CC(C(C)*)C 0.000 claims 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 6
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 claims 6
- 125000006239 protecting group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000000524 functional group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 4
- 125000004920 4-methyl-2-pentyl group Chemical group CC(CC(C)*)C 0.000 claims 3
- 108060008539 Transglutaminase Proteins 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 102000003601 transglutaminase Human genes 0.000 claims 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- 108010016626 Dipeptides Proteins 0.000 claims 2
- 229930194542 Keto Natural products 0.000 claims 2
- 102000007079 Peptide Fragments Human genes 0.000 claims 2
- 108010033276 Peptide Fragments Proteins 0.000 claims 2
- 150000001721 carbon Chemical group 0.000 claims 2
- WKQDFBKYIAEZEP-UHFFFAOYSA-N dimethyl 2-[(4-nitrophenyl)methylidene]propanedioate Chemical compound COC(=O)C(C(=O)OC)=CC1=CC=C([N+]([O-])=O)C=C1 WKQDFBKYIAEZEP-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- KWIUHFFTVRNATP-UHFFFAOYSA-N glycine betaine Chemical group C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 102000004196 processed proteins & peptides Human genes 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 241000222122 Candida albicans Species 0.000 claims 1
- 206010007134 Candida infections Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 150000001336 alkenes Chemical class 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000003984 candidiasis Diseases 0.000 claims 1
- 125000006358 carbonyl ethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([*:1])=O 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- AGMKVZDPATUSMS-UHFFFAOYSA-N ethyl pent-2-enoate Chemical compound CCOC(=O)C=CCC AGMKVZDPATUSMS-UHFFFAOYSA-N 0.000 claims 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 230000009759 skin aging Effects 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102006052755A DE102006052755A1 (de) | 2006-11-08 | 2006-11-08 | Michaelsysteme als Transglutaminaseinhibitoren |
| DE102006052755.0 | 2006-11-08 | ||
| US87424606P | 2006-12-12 | 2006-12-12 | |
| US60/874,246 | 2006-12-12 | ||
| PCT/DE2007/002014 WO2008055488A1 (de) | 2006-11-08 | 2007-11-08 | Michaelsysteme als transglutaminaseinhibitoren |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010509195A JP2010509195A (ja) | 2010-03-25 |
| JP2010509195A5 true JP2010509195A5 (https=) | 2010-12-24 |
| JP5528113B2 JP5528113B2 (ja) | 2014-06-25 |
Family
ID=39277495
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009534984A Active JP5528113B2 (ja) | 2006-11-08 | 2007-11-08 | トランスグルタミナーゼ阻害剤としてのマイケル・システム |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8471063B2 (https=) |
| EP (1) | EP2086993B1 (https=) |
| JP (1) | JP5528113B2 (https=) |
| CN (2) | CN101563359A (https=) |
| AU (1) | AU2007317045B2 (https=) |
| CA (1) | CA2662876C (https=) |
| DE (1) | DE102006052755A1 (https=) |
| DK (1) | DK2086993T3 (https=) |
| ES (1) | ES2538262T3 (https=) |
| HK (1) | HK1219745A1 (https=) |
| IL (1) | IL198588A (https=) |
| PL (1) | PL2086993T3 (https=) |
| PT (1) | PT2086993E (https=) |
| RU (1) | RU2501806C2 (https=) |
| SI (1) | SI2086993T1 (https=) |
| WO (1) | WO2008055488A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2249853A4 (en) | 2008-01-30 | 2012-12-26 | Univ Indiana Res & Tech Corp | ESTER BASED PEPTIDE PRODRUGS |
| PE20120332A1 (es) | 2008-12-19 | 2012-04-14 | Univ Indiana Res & Tech Corp | Profarmacos de peptido de la superfamilia de glucagon basado en amida |
| WO2010080605A1 (en) * | 2008-12-19 | 2010-07-15 | Indiana University Research And Technology Corporation | Dipeptide linked medicinal agents |
| EP2322926A1 (en) | 2009-11-11 | 2011-05-18 | Zedira GmbH | Stabilized open form transglutaminase as a diagnostic indicator for autoimmune diseases |
| WO2011057826A1 (en) | 2009-11-11 | 2011-05-19 | Zedira Gmbh | Stabilized open form transglutaminase as a diagnostic indicator for autoimmune diseases |
| US8946197B2 (en) | 2009-11-16 | 2015-02-03 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| JP5604948B2 (ja) * | 2010-04-09 | 2014-10-15 | 独立行政法人科学技術振興機構 | トランスグルタミナーゼによるｉｐ３レセプターの修飾 |
| EP2585102B1 (en) | 2010-06-24 | 2015-05-06 | Indiana University Research and Technology Corporation | Amide-based insulin prodrugs |
| US8889716B2 (en) * | 2011-05-10 | 2014-11-18 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| SG187271A1 (en) * | 2011-07-07 | 2013-02-28 | Agency Science Tech & Res | Anti-amyloidogenic, alpha-helix breaking ultra-small peptide therapeutic |
| PT2794618T (pt) | 2011-12-20 | 2017-01-17 | Sanofi Sa | Isotiazolopiridina-2-carboxamidas e seu uso como produtos farmacêuticos |
| EP2687511A1 (de) * | 2012-07-17 | 2014-01-22 | Zedira GmbH | Pyridinonderivate als Gewebetransglutaminaseinhibitoren |
| US9845292B2 (en) | 2013-09-19 | 2017-12-19 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Selective FKBP51 ligands for treatment of psychiatric disorders |
| EP3342779A1 (en) * | 2016-12-27 | 2018-07-04 | Zedira GmbH | Inhibitors of transglutaminases |
| SE1751041A1 (en) * | 2017-08-30 | 2019-03-01 | Jaywant Phopase | Functionalized polypeptide for hair treatment |
| WO2019201432A1 (en) * | 2018-04-17 | 2019-10-24 | Zedira Gmbh | Inhibitors of blood coagulation factor xiii |
| TWI825144B (zh) | 2018-08-10 | 2023-12-11 | 美商思達利醫藥公司 | 第二型轉麩醯胺酸酶(tg2)抑制劑 |
| CN111171114B (zh) * | 2020-01-17 | 2022-08-12 | 遵义医科大学 | 一种膦酸酯二肽类化合物及其应用 |
| ES2955368T3 (es) * | 2020-04-24 | 2023-11-30 | Dr Falk Pharma Gmbh | Formulación sistémica de un derivado de la piridinona para la enfermedad celíaca |
| EP3900706A1 (en) * | 2020-04-24 | 2021-10-27 | Dr. Falk Pharma Gmbh | Systemic formulation of a pyridinone derivate for coeliac disease |
| SI4192814T1 (sl) * | 2021-06-30 | 2025-02-28 | Zedira Gmbh | Zaviralci transglutaminaz |
| US20240376055A1 (en) * | 2021-06-30 | 2024-11-14 | Zedira Gmbh | Inhibitors of transglutaminases |
| WO2023072368A1 (en) * | 2021-10-25 | 2023-05-04 | Dr. Falk Pharma Gmbh | Oral formulation of a pyridinone derivate and use thereof in prophylaxis and/or treatment of intestinal fibrosis |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GR890100827A (el) | 1988-12-21 | 1991-03-15 | Abbott Lab | Μέ?οδος παραγωγής παραγώγων τετραπεπτιδίων ως ανταγωνιστών CCK. |
| AU2003234634A1 (en) * | 2002-05-14 | 2003-12-02 | Felix Hausch | Drug therapy for celiac sprue |
| US20030236290A1 (en) * | 2002-06-12 | 2003-12-25 | Gabriel Fenteany | Inhibitors of animal cell motility and growth |
| WO2005025620A2 (en) * | 2003-08-13 | 2005-03-24 | Pharmacia Corporation | Combination therapy with inhibitors of inducible nitric oxide synthase and alkylating agents |
| US7320805B2 (en) * | 2003-10-01 | 2008-01-22 | Institut National De La Sante Et De La Recherche Medicale | CB2 receptors blocks accumulation of human hepatic myofibroblasts: a novel artifibrogenic pathway in the liver |
| TW200526552A (en) * | 2003-12-25 | 2005-08-16 | Ishihara Sangyo Kaisha | Haloalkene compounds, process for their production and pesticides containing them |
| BRPI0418245B8 (pt) * | 2004-01-05 | 2021-05-25 | Nicox Sa | composto derivado de nitróxi de prostaglandina, processo para preparar dito composto, composição farmacêutica compreendendo dito composto e usos destes |
| US7569594B2 (en) * | 2005-02-07 | 2009-08-04 | The University Of Chicago | Analogs of leucascandrolide A |
-
2006
- 2006-11-08 DE DE102006052755A patent/DE102006052755A1/de not_active Withdrawn
-
2007
- 2007-11-08 CA CA2662876A patent/CA2662876C/en active Active
- 2007-11-08 SI SI200731651T patent/SI2086993T1/sl unknown
- 2007-11-08 PT PT78463049T patent/PT2086993E/pt unknown
- 2007-11-08 CN CNA2007800413318A patent/CN101563359A/zh active Pending
- 2007-11-08 AU AU2007317045A patent/AU2007317045B2/en active Active
- 2007-11-08 DK DK07846304.9T patent/DK2086993T3/en active
- 2007-11-08 EP EP07846304.9A patent/EP2086993B1/de active Active
- 2007-11-08 RU RU2009121559/04A patent/RU2501806C2/ru active
- 2007-11-08 PL PL07846304T patent/PL2086993T3/pl unknown
- 2007-11-08 US US12/513,476 patent/US8471063B2/en active Active
- 2007-11-08 JP JP2009534984A patent/JP5528113B2/ja active Active
- 2007-11-08 ES ES07846304.9T patent/ES2538262T3/es active Active
- 2007-11-08 CN CN201510641538.5A patent/CN105218632A/zh active Pending
- 2007-11-08 WO PCT/DE2007/002014 patent/WO2008055488A1/de not_active Ceased
-
2009
- 2009-05-05 IL IL198588A patent/IL198588A/en active IP Right Grant
-
2016
- 2016-07-06 HK HK16107848.1A patent/HK1219745A1/zh unknown
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