JP2005526010A5 - - Google Patents
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- JP2005526010A5 JP2005526010A5 JP2003550737A JP2003550737A JP2005526010A5 JP 2005526010 A5 JP2005526010 A5 JP 2005526010A5 JP 2003550737 A JP2003550737 A JP 2003550737A JP 2003550737 A JP2003550737 A JP 2003550737A JP 2005526010 A5 JP2005526010 A5 JP 2005526010A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- hif
- compound
- subject
- hifα
- 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
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- 239000000203 mixture Substances 0.000 claims 39
- 150000001875 compounds Chemical class 0.000 claims 23
- 230000000694 effects Effects 0.000 claims 11
- 206010021143 Hypoxia Diseases 0.000 claims 9
- KPGXRSRHYNQIFN-UHFFFAOYSA-N 2-oxoglutaric acid Chemical compound OC(=O)CCC(=O)C(O)=O KPGXRSRHYNQIFN-UHFFFAOYSA-N 0.000 claims 8
- 108010028143 Dioxygenases Proteins 0.000 claims 8
- 102000016680 Dioxygenases Human genes 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 6
- 230000000302 ischemic effect Effects 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 108010043005 Prolyl Hydroxylases Proteins 0.000 claims 5
- 102000004079 Prolyl Hydroxylases Human genes 0.000 claims 5
- 239000012634 fragment Substances 0.000 claims 3
- 230000033444 hydroxylation Effects 0.000 claims 3
- 238000005805 hydroxylation reaction Methods 0.000 claims 3
- 230000007954 hypoxia Effects 0.000 claims 3
- 208000028867 ischemia Diseases 0.000 claims 3
- 210000000056 organ Anatomy 0.000 claims 3
- 230000000087 stabilizing effect Effects 0.000 claims 3
- 239000005541 ACE inhibitor Substances 0.000 claims 2
- 102100037249 Egl nine homolog 1 Human genes 0.000 claims 2
- 101000881648 Homo sapiens Egl nine homolog 1 Proteins 0.000 claims 2
- 101000881650 Homo sapiens Prolyl hydroxylase EGLN2 Proteins 0.000 claims 2
- 101000881678 Homo sapiens Prolyl hydroxylase EGLN3 Proteins 0.000 claims 2
- 102100037248 Prolyl hydroxylase EGLN2 Human genes 0.000 claims 2
- 102100037247 Prolyl hydroxylase EGLN3 Human genes 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- -1 heterocyclic carboxamides Chemical class 0.000 claims 2
- 208000014674 injury Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- PHIQHXFUZVPYII-ZCFIWIBFSA-N (R)-carnitine Chemical compound C[N+](C)(C)C[C@H](O)CC([O-])=O PHIQHXFUZVPYII-ZCFIWIBFSA-N 0.000 claims 1
- 108010050451 2-oxoglutarate 3-dioxygenase proline Proteins 0.000 claims 1
- 102000008873 Angiotensin II receptor Human genes 0.000 claims 1
- 108050000824 Angiotensin II receptor Proteins 0.000 claims 1
- 200000000007 Arterial disease Diseases 0.000 claims 1
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 1
- 208000020446 Cardiac disease Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- LTMHDMANZUZIPE-AMTYYWEZSA-N Digoxin Natural products O([C@H]1[C@H](C)O[C@H](O[C@@H]2C[C@@H]3[C@@](C)([C@@H]4[C@H]([C@]5(O)[C@](C)([C@H](O)C4)[C@H](C4=CC(=O)OC4)CC5)CC3)CC2)C[C@@H]1O)[C@H]1O[C@H](C)[C@@H](O[C@H]2O[C@@H](C)[C@H](O)[C@@H](O)C2)[C@@H](O)C1 LTMHDMANZUZIPE-AMTYYWEZSA-N 0.000 claims 1
- 229940097420 Diuretic Drugs 0.000 claims 1
- 101000595915 Drosophila melanogaster Procollagen-lysine,2-oxoglutarate 5-dioxygenase Proteins 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 101001046870 Homo sapiens Hypoxia-inducible factor 1-alpha Proteins 0.000 claims 1
- 101001082574 Homo sapiens Hypoxia-inducible factor 1-alpha inhibitor Proteins 0.000 claims 1
- 101000614354 Homo sapiens Transmembrane prolyl 4-hydroxylase Proteins 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 102100022875 Hypoxia-inducible factor 1-alpha Human genes 0.000 claims 1
- 102100030481 Hypoxia-inducible factor 1-alpha inhibitor Human genes 0.000 claims 1
- 206010061216 Infarction Diseases 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 108010050808 Procollagen Proteins 0.000 claims 1
- 108010061699 Procollagen-Proline Dioxygenase Proteins 0.000 claims 1
- 102000012293 Procollagen-Proline Dioxygenase Human genes 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- 102000018399 Prolyl 3-hydroxylases Human genes 0.000 claims 1
- 208000003782 Raynaud disease Diseases 0.000 claims 1
- 208000012322 Raynaud phenomenon Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 102100040472 Transmembrane prolyl 4-hydroxylase Human genes 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 229960001230 asparagine Drugs 0.000 claims 1
- 235000009582 asparagine Nutrition 0.000 claims 1
- 230000000975 bioactive effect Effects 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 229960004203 carnitine Drugs 0.000 claims 1
- LBGQERGEZNQMAT-UHFFFAOYSA-N cinnoline-3-carboxamide Chemical class C1=CC=C2N=NC(C(=O)N)=CC2=C1 LBGQERGEZNQMAT-UHFFFAOYSA-N 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- LTMHDMANZUZIPE-PUGKRICDSA-N digoxin Chemical compound C1[C@H](O)[C@H](O)[C@@H](C)O[C@H]1O[C@@H]1[C@@H](C)O[C@@H](O[C@@H]2[C@H](O[C@@H](O[C@@H]3C[C@@H]4[C@]([C@@H]5[C@H]([C@]6(CC[C@@H]([C@@]6(C)[C@H](O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)C[C@@H]2O)C)C[C@@H]1O LTMHDMANZUZIPE-PUGKRICDSA-N 0.000 claims 1
- 229960005156 digoxin Drugs 0.000 claims 1
- LTMHDMANZUZIPE-UHFFFAOYSA-N digoxine Natural products C1C(O)C(O)C(C)OC1OC1C(C)OC(OC2C(OC(OC3CC4C(C5C(C6(CCC(C6(C)C(O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)CC2O)C)CC1O LTMHDMANZUZIPE-UHFFFAOYSA-N 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 230000001882 diuretic effect Effects 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 210000005095 gastrointestinal system Anatomy 0.000 claims 1
- 208000019622 heart disease Diseases 0.000 claims 1
- 210000000777 hematopoietic system Anatomy 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000007574 infarction Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- YZDXFUGIDTUCDA-UHFFFAOYSA-N isoquinoline-1-carboxamide Chemical class C1=CC=C2C(C(=O)N)=NC=CC2=C1 YZDXFUGIDTUCDA-UHFFFAOYSA-N 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 210000002346 musculoskeletal system Anatomy 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 150000005041 phenanthrolines Chemical class 0.000 claims 1
- IBBMAWULFFBRKK-UHFFFAOYSA-N picolinamide Chemical class NC(=O)C1=CC=CC=N1 IBBMAWULFFBRKK-UHFFFAOYSA-N 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- ZEXKKIXCRDTKBF-UHFFFAOYSA-N quinoline-2-carboxamide Chemical class C1=CC=CC2=NC(C(=O)N)=CC=C21 ZEXKKIXCRDTKBF-UHFFFAOYSA-N 0.000 claims 1
- 239000003087 receptor blocking agent Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33708201P | 2001-12-06 | 2001-12-06 | |
| US60/337,082 | 2001-12-06 | ||
| US34965902P | 2002-01-16 | 2002-01-16 | |
| US60/349,659 | 2002-01-16 | ||
| US35968302P | 2002-02-25 | 2002-02-25 | |
| US60/359,683 | 2002-02-25 | ||
| US38648802P | 2002-06-05 | 2002-06-05 | |
| US60/386,488 | 2002-06-05 | ||
| PCT/US2002/038867 WO2003049686A2 (en) | 2001-12-06 | 2002-12-06 | Stabilization of hypoxia inducible factor (hif) alpha |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010243226A Division JP5498918B2 (ja) | 2001-12-06 | 2010-10-29 | 低酸素誘導性因子（ＨＩＦ）−αの安定化 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005526010A JP2005526010A (ja) | 2005-09-02 |
| JP2005526010A5 true JP2005526010A5 (enExample) | 2006-01-26 |
| JP5341293B2 JP5341293B2 (ja) | 2013-11-13 |
Family
ID=27502557
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003550737A Expired - Lifetime JP5341293B2 (ja) | 2001-12-06 | 2002-12-06 | 低酸素誘導性因子（ＨＩＦ）−αの安定化 |
| JP2003554713A Pending JP2005524612A (ja) | 2001-12-06 | 2002-12-06 | 内因性エリスロポエチン（ｅｐｏ）を増加させる方法 |
| JP2005351153A Expired - Lifetime JP4804131B2 (ja) | 2001-12-06 | 2005-12-05 | 内因性エリスロポエチン（ｅｐｏ）を増加させる方法 |
| JP2010208681A Expired - Lifetime JP5469572B2 (ja) | 2001-12-06 | 2010-09-17 | 内因性エリスロポエチン（ｅｐｏ）を増加させる方法 |
| JP2010243226A Expired - Lifetime JP5498918B2 (ja) | 2001-12-06 | 2010-10-29 | 低酸素誘導性因子（ＨＩＦ）−αの安定化 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003554713A Pending JP2005524612A (ja) | 2001-12-06 | 2002-12-06 | 内因性エリスロポエチン（ｅｐｏ）を増加させる方法 |
| JP2005351153A Expired - Lifetime JP4804131B2 (ja) | 2001-12-06 | 2005-12-05 | 内因性エリスロポエチン（ｅｐｏ）を増加させる方法 |
| JP2010208681A Expired - Lifetime JP5469572B2 (ja) | 2001-12-06 | 2010-09-17 | 内因性エリスロポエチン（ｅｐｏ）を増加させる方法 |
| JP2010243226A Expired - Lifetime JP5498918B2 (ja) | 2001-12-06 | 2010-10-29 | 低酸素誘導性因子（ＨＩＦ）−αの安定化 |
Country Status (12)
| Country | Link |
|---|---|
| US (15) | US20030176317A1 (enExample) |
| EP (7) | EP2298301B2 (enExample) |
| JP (5) | JP5341293B2 (enExample) |
| CN (7) | CN102552263A (enExample) |
| AU (3) | AU2002357096B2 (enExample) |
| CA (4) | CA2916093C (enExample) |
| DK (3) | DK2298301T3 (enExample) |
| ES (3) | ES2414706T3 (enExample) |
| HU (1) | HU229475B1 (enExample) |
| IL (2) | IL162085A0 (enExample) |
| NO (1) | NO343732B1 (enExample) |
| WO (2) | WO2003053997A2 (enExample) |
Families Citing this family (135)
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| EP2295060B1 (en) | 2001-12-06 | 2018-10-31 | Fibrogen, Inc. | Treatment or prevention of ischemic or hypoxic conditions |
| US8318703B2 (en) | 2001-12-06 | 2012-11-27 | Fibrogen, Inc. | Methods for improving kidney function |
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| US7618940B2 (en) | 2002-12-06 | 2009-11-17 | Fibrogen, Inc. | Fat regulation |
| US8614204B2 (en) | 2003-06-06 | 2013-12-24 | Fibrogen, Inc. | Enhanced erythropoiesis and iron metabolism |
| DE602004031114D1 (de) | 2003-06-06 | 2011-03-03 | Fibrogen Inc | Stickstoffhaltige heteroarylverbindungen und deren verwendungen zur erhoehung des gehaltes von endogenem erythropoietin |
| US20060251638A1 (en) * | 2003-06-06 | 2006-11-09 | Volkmar Guenzler-Pukall | Cytoprotection through the use of hif hydroxylase inhibitors |
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2004
- 2004-05-20 IL IL162085A patent/IL162085A/en active IP Right Grant
- 2004-07-02 NO NO20042804A patent/NO343732B1/no not_active IP Right Cessation
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2005
- 2005-12-05 JP JP2005351153A patent/JP4804131B2/ja not_active Expired - Lifetime
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2006
- 2006-04-17 US US11/406,023 patent/US20060178316A1/en not_active Abandoned
- 2006-04-17 US US11/405,734 patent/US20060183695A1/en not_active Abandoned
- 2006-04-17 US US11/406,484 patent/US20060178317A1/en not_active Abandoned
- 2006-07-28 US US11/495,118 patent/US20060258702A1/en not_active Abandoned
- 2006-07-28 US US11/495,036 patent/US20060258660A1/en not_active Abandoned
- 2006-07-28 US US11/494,978 patent/US20060270699A1/en not_active Abandoned
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2009
- 2009-01-02 AU AU2009200018A patent/AU2009200018C1/en not_active Expired
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2010
- 2010-09-17 JP JP2010208681A patent/JP5469572B2/ja not_active Expired - Lifetime
- 2010-10-29 JP JP2010243226A patent/JP5498918B2/ja not_active Expired - Lifetime
- 2010-12-02 US US12/928,119 patent/US8466172B2/en not_active Expired - Fee Related
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2011
- 2011-02-17 US US12/932,151 patent/US20110166178A1/en not_active Abandoned
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2012
- 2012-09-13 US US13/614,917 patent/US20130203805A1/en not_active Abandoned
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2013
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2014
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2017
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2021
- 2021-08-05 US US17/394,602 patent/US20210369702A1/en not_active Abandoned
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