JP2002513801A5 - - Google Patents
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- JP2002513801A5 JP2002513801A5 JP2000547108A JP2000547108A JP2002513801A5 JP 2002513801 A5 JP2002513801 A5 JP 2002513801A5 JP 2000547108 A JP2000547108 A JP 2000547108A JP 2000547108 A JP2000547108 A JP 2000547108A JP 2002513801 A5 JP2002513801 A5 JP 2002513801A5
- Authority
- JP
- Japan
- Prior art keywords
- missing
- phe
- aib
- acc
- amino acid
- 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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- 150000001413 amino acids Chemical class 0.000 description 64
- 108090000445 Parathyroid hormone Proteins 0.000 description 16
- 150000003839 salts Chemical class 0.000 description 15
- 125000000923 (C1-C30) alkyl group Chemical group 0.000 description 14
- 102100030869 Parathyroid hormone 2 receptor Human genes 0.000 description 13
- 101710149426 Parathyroid hormone 2 receptor Proteins 0.000 description 13
- 150000001875 compounds Chemical class 0.000 description 12
- 125000000739 C2-C30 alkenyl group Chemical group 0.000 description 10
- 125000000217 alkyl group Chemical group 0.000 description 10
- -1 hydroxy-naphthyl Chemical group 0.000 description 10
- 150000008574 D-amino acids Chemical class 0.000 description 7
- 230000002159 abnormal effect Effects 0.000 description 6
- 125000002252 acyl group Chemical group 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 5
- 125000001183 hydrocarbyl group Chemical group 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- NNRMZXDHMCWWRV-RHBZDGMUSA-N (2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]acetyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoic acid Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(O)=O)[C@@H](C)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)C1=CN=CN1 NNRMZXDHMCWWRV-RHBZDGMUSA-N 0.000 description 3
- 108700020797 Parathyroid Hormone-Related Proteins 0.000 description 3
- 102000043299 Parathyroid hormone-related Human genes 0.000 description 3
- 108010045398 parathyroid hormone-related peptide (1-36) Proteins 0.000 description 3
- ODKSFYDXXFIFQN-UHFFFAOYSA-N Arginine Chemical compound OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 2
- 208000027796 Blood pressure disease Diseases 0.000 description 2
- 208000028482 Hypothalamic disease Diseases 0.000 description 2
- 208000007466 Male Infertility Diseases 0.000 description 2
- 102000003982 Parathyroid hormone Human genes 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 230000036772 blood pressure Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 125000001475 halogen functional group Chemical group 0.000 description 2
- 230000013632 homeostatic process Effects 0.000 description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 239000011707 mineral Substances 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 239000000199 parathyroid hormone Substances 0.000 description 2
- 108010073230 parathyroid hormone (1-38) Proteins 0.000 description 2
- 210000000952 spleen Anatomy 0.000 description 2
- OGBMKVWORPGQRR-UMXFMPSGSA-N teriparatide Chemical compound C([C@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)C1=CNC=N1 OGBMKVWORPGQRR-UMXFMPSGSA-N 0.000 description 2
- ZOWOHMFPXMYFKJ-WBTWNKCNSA-N (4S)-4-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]acetyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-5-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(1S)-1-carboxyethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C1=CN=CN1 ZOWOHMFPXMYFKJ-WBTWNKCNSA-N 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 108010054971 parathyroid hormone-related protein (1-34) Proteins 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7295698A | 1998-05-05 | 1998-05-05 | |
| US09/072,956 | 1998-05-05 | ||
| PCT/US1999/009521 WO1999057139A2 (en) | 1998-05-05 | 1999-05-03 | Pth2 receptor selective compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002513801A JP2002513801A (ja) | 2002-05-14 |
| JP2002513801A5 true JP2002513801A5 (https=) | 2006-02-16 |
| JP4460157B2 JP4460157B2 (ja) | 2010-05-12 |
Family
ID=22110801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000547108A Expired - Fee Related JP4460157B2 (ja) | 1998-05-05 | 1999-05-03 | Ｐｔｈ２レセプター選択的化合物 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7531621B1 (https=) |
| EP (1) | EP1075491B1 (https=) |
| JP (1) | JP4460157B2 (https=) |
| AT (1) | ATE392431T1 (https=) |
| AU (1) | AU3673699A (https=) |
| CA (1) | CA2327509A1 (https=) |
| DE (1) | DE69938548T2 (https=) |
| ES (1) | ES2302374T3 (https=) |
| HU (1) | HUP0300891A2 (https=) |
| NO (1) | NO20005556L (https=) |
| PL (1) | PL344645A1 (https=) |
| WO (1) | WO1999057139A2 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK40599A3 (en) | 1996-09-26 | 2000-06-12 | Chugai Pharmaceutical Co Ltd | Antibody against human parathormone related peptides |
| WO1998051329A1 (en) | 1997-05-15 | 1998-11-19 | Chugai Seiyaku Kabushiki Kaisha | Cachexia remedy |
| WO2001002011A1 (fr) * | 1999-07-02 | 2001-01-11 | Chugai Seiyaku Kabushiki Kaisha | REMEDES CONTRE LES MALADIES CAUSEES PAR PTH OU PTHrP |
| TWI255718B (en) | 1999-07-02 | 2006-06-01 | Chugai Pharmaceutical Co Ltd | Ameliorative agent for low vasopressin concentration |
| US8029793B2 (en) | 2000-04-28 | 2011-10-04 | Chugai Seiyaku Kabushiki Kaisha | Methods for inhibiting cell proliferation |
| WO2002024943A2 (en) * | 2000-09-19 | 2002-03-28 | Curagen Corporation | Method of identifying osteoregenerative agents using differential gene expression |
| WO2004071396A2 (en) * | 2003-02-17 | 2004-08-26 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with parathyroid hormone receptor 2 (pthr2) |
| AU2007313001B2 (en) | 2006-10-13 | 2012-03-22 | Eli Lilly And Company | Pegylated PTH as PTH receptor modulators and uses thereof |
| AU2008282805B2 (en) | 2007-08-01 | 2014-05-01 | Chugai Pharmaceutical Co., Ltd. | Screening methods using G-protein coupled receptors and related compositions |
| WO2011143406A2 (en) | 2010-05-13 | 2011-11-17 | The General Hospital Corporation | Parathyroid hormone analogs and uses thereof |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5001223A (en) * | 1987-05-26 | 1991-03-19 | Merck & Co., Inc. | Parathyroid hormone antagonists with enhanced metabolic properties |
| EP0293158A3 (en) | 1987-05-26 | 1990-05-09 | Merck & Co. Inc. | Parathyroid hormone antagonists |
| US5527772A (en) | 1987-10-20 | 1996-06-18 | Holick; Michael F. | Regulation of cell proliferation and differentiation using peptides |
| US4968669A (en) | 1988-05-09 | 1990-11-06 | Merck & Co., Inc. | Parathyroid hormone antagonists |
| EP0341962B1 (en) | 1988-05-09 | 1995-03-15 | Merck & Co. Inc. | Humoral hypercalcemic factor antagonists |
| CA2040264A1 (en) | 1990-04-12 | 1991-10-13 | Tatsuhiko Kanmera | Parathyroid hormone antagonists |
| US5093233A (en) | 1990-04-25 | 1992-03-03 | Merck & Co., Inc. | Antagonists with position 13 modification |
| US5087562A (en) | 1990-04-25 | 1992-02-11 | Merck & Co., Inc. | Humoral hypercalcemic factor antagonists with modification at position 13 . . . |
| US5149779A (en) | 1990-07-26 | 1992-09-22 | Merck & Co., Inc. | Humoral hypercalcemic factor antagonists |
| JPH0532696A (ja) | 1990-09-28 | 1993-02-09 | Takeda Chem Ind Ltd | 副甲状腺ホルモン誘導体 |
| AU9103791A (en) * | 1990-12-21 | 1992-07-22 | Allelix Biopharmaceuticals Inc. | Oxidation resistant variants of parathyroid hormone |
| DE4203040A1 (de) | 1992-02-04 | 1993-08-05 | Boehringer Mannheim Gmbh | Neue parathormonfragmente, deren herstellung und diese enthaltende arzneimittel |
| US5589452A (en) | 1992-07-14 | 1996-12-31 | Syntex (U.S.A.) Inc. | Analogs of parathyroid hormone and parathyroid hormone related peptide: synthesis and use for the treatment of osteoporosis |
| AU672790B2 (en) | 1992-07-15 | 1996-10-17 | Novartis Ag | Variants of parathyroid hormone and its fragments |
| CA2126299C (en) * | 1994-06-20 | 2000-12-12 | Gordon E. Willick | Parathyroid hormone analogues for the treatment of osteoporosis |
| US5747456A (en) | 1994-12-19 | 1998-05-05 | Beth Israel Deaconess Medical Center | Continuous low-dose administration of parathyroid hormone or its agonist |
| US5717062A (en) | 1995-06-07 | 1998-02-10 | Beth Israel Hospital Association | Cyclic analogs of PTH and PTHrP |
| US5955574A (en) * | 1995-07-13 | 1999-09-21 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A. | Analogs of parathyroid hormone |
| US5969095A (en) | 1995-07-13 | 1999-10-19 | Biomeasure, Inc. | Analogs of parathyroid hormone |
| US5723577A (en) * | 1995-07-13 | 1998-03-03 | Biomeasure Inc. | Analogs of parathyroid hormone |
| JP3259011B2 (ja) * | 1995-08-02 | 2002-02-18 | ミヤチテクノス株式会社 | インバータ式抵抗溶接制御方法及び装置 |
| DE69734157T2 (de) | 1996-07-31 | 2006-07-13 | The General Hospital Corp., Boston | Parathyroidhormon-verwandthe peptidanaloge |
-
1999
- 1999-05-03 HU HU0300891A patent/HUP0300891A2/hu unknown
- 1999-05-03 AT AT99918938T patent/ATE392431T1/de not_active IP Right Cessation
- 1999-05-03 PL PL99344645A patent/PL344645A1/xx not_active Application Discontinuation
- 1999-05-03 EP EP99918938A patent/EP1075491B1/en not_active Expired - Lifetime
- 1999-05-03 US US09/674,597 patent/US7531621B1/en not_active Expired - Fee Related
- 1999-05-03 JP JP2000547108A patent/JP4460157B2/ja not_active Expired - Fee Related
- 1999-05-03 CA CA002327509A patent/CA2327509A1/en not_active Abandoned
- 1999-05-03 WO PCT/US1999/009521 patent/WO1999057139A2/en not_active Ceased
- 1999-05-03 AU AU36736/99A patent/AU3673699A/en not_active Abandoned
- 1999-05-03 DE DE69938548T patent/DE69938548T2/de not_active Expired - Lifetime
- 1999-05-03 ES ES99918938T patent/ES2302374T3/es not_active Expired - Lifetime
-
2000
- 2000-11-03 NO NO20005556A patent/NO20005556L/no not_active Application Discontinuation
-
2009
- 2009-03-27 US US12/413,303 patent/US20090226477A1/en not_active Abandoned
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