SK3893A3 - Bombesine antagonists - Google Patents
Bombesine antagonists Download PDFInfo
- Publication number
- SK3893A3 SK3893A3 SK3893A SK3893A SK3893A3 SK 3893 A3 SK3893 A3 SK 3893A3 SK 3893 A SK3893 A SK 3893A SK 3893 A SK3893 A SK 3893A SK 3893 A3 SK3893 A3 SK 3893A3
- Authority
- SK
- Slovakia
- Prior art keywords
- pro
- phe
- ala
- phenyl
- histrpalavald
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract description 6
- 108090000765 processed proteins & peptides Proteins 0.000 claims abstract description 106
- -1 Phe Chemical group 0.000 claims abstract description 91
- 102000004196 processed proteins & peptides Human genes 0.000 claims abstract description 68
- 229920001184 polypeptide Polymers 0.000 claims abstract description 57
- 238000011282 treatment Methods 0.000 claims abstract description 23
- 125000000174 L-prolyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(*)=O 0.000 claims abstract description 22
- 150000003839 salts Chemical class 0.000 claims abstract description 19
- ONIBWKKTOPOVIA-SCSAIBSYSA-N D-Proline Chemical compound OC(=O)[C@H]1CCCN1 ONIBWKKTOPOVIA-SCSAIBSYSA-N 0.000 claims abstract description 15
- 125000005843 halogen group Chemical group 0.000 claims abstract description 12
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical group OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 claims abstract description 11
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims abstract description 10
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 claims abstract description 8
- ODKSFYDXXFIFQN-SCSAIBSYSA-N D-arginine Chemical compound OC(=O)[C@H](N)CCCNC(N)=N ODKSFYDXXFIFQN-SCSAIBSYSA-N 0.000 claims abstract description 7
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical group OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims abstract description 7
- 125000001711 D-phenylalanine group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims abstract description 6
- VNYDHJARLHNEGA-RYUDHWBXSA-N Tyr-Pro Chemical compound C([C@H](N)C(=O)N1[C@@H](CCC1)C(O)=O)C1=CC=C(O)C=C1 VNYDHJARLHNEGA-RYUDHWBXSA-N 0.000 claims abstract description 6
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- 125000003118 aryl group Chemical group 0.000 claims abstract description 4
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- 238000004090 dissolution Methods 0.000 description 1
- 239000003534 dna topoisomerase inhibitor Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000000921 elemental analysis Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 229940066758 endopeptidases Drugs 0.000 description 1
- 230000003628 erosive effect Effects 0.000 description 1
- 230000032050 esterification Effects 0.000 description 1
- 238000005886 esterification reaction Methods 0.000 description 1
- PQJJJMRNHATNKG-UHFFFAOYSA-N ethyl bromoacetate Chemical compound CCOC(=O)CBr PQJJJMRNHATNKG-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 description 1
- 229960005420 etoposide Drugs 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000004992 fast atom bombardment mass spectroscopy Methods 0.000 description 1
- 230000002344 fibroplastic effect Effects 0.000 description 1
- 239000003063 flame retardant Substances 0.000 description 1
- 229960002949 fluorouracil Drugs 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 230000002538 fungal effect Effects 0.000 description 1
- 230000027119 gastric acid secretion Effects 0.000 description 1
- 239000012362 glacial acetic acid Substances 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 229960002885 histidine Drugs 0.000 description 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
- 125000000487 histidyl group Chemical group [H]N([H])C(C(=O)O*)C([H])([H])C1=C([H])N([H])C([H])=N1 0.000 description 1
- 210000005260 human cell Anatomy 0.000 description 1
- 229960001330 hydroxycarbamide Drugs 0.000 description 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 1
- 239000000367 immunologic factor Substances 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 125000001905 inorganic group Chemical group 0.000 description 1
- 239000012444 intercalating antibiotic Substances 0.000 description 1
- 229940079322 interferon Drugs 0.000 description 1
- 239000000543 intermediate Substances 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 210000004153 islets of langerhan Anatomy 0.000 description 1
- 239000008263 liquid aerosol Substances 0.000 description 1
- 238000011866 long-term treatment Methods 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 210000004962 mammalian cell Anatomy 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 238000006140 methanolysis reaction Methods 0.000 description 1
- UZKWTJUDCOPSNM-UHFFFAOYSA-N methoxybenzene Substances CCCCOC=C UZKWTJUDCOPSNM-UHFFFAOYSA-N 0.000 description 1
- QVDXUKJJGUSGLS-LURJTMIESA-N methyl L-leucinate Chemical compound COC(=O)[C@@H](N)CC(C)C QVDXUKJJGUSGLS-LURJTMIESA-N 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 230000002297 mitogenic effect Effects 0.000 description 1
- 230000000394 mitotic effect Effects 0.000 description 1
- 239000012452 mother liquor Substances 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 229940100662 nasal drops Drugs 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 229940097496 nasal spray Drugs 0.000 description 1
- 230000017066 negative regulation of growth Effects 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 108010088904 phenylalanylproline Proteins 0.000 description 1
- 229940117953 phenylisothiocyanate Drugs 0.000 description 1
- 229960005235 piperonyl butoxide Drugs 0.000 description 1
- 210000003635 pituitary gland Anatomy 0.000 description 1
- 238000011176 pooling Methods 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940097325 prolactin Drugs 0.000 description 1
- 239000005297 pyrex Substances 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000002390 rotary evaporation Methods 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 208000000649 small cell carcinoma Diseases 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- VYGIGVDDUBLRTI-UHFFFAOYSA-N tert-butyl 2-(3-ethoxy-1-hydroxy-3-oxopropyl)pyrrolidine-1-carboxylate Chemical compound CCOC(=O)CC(O)C1CCCN1C(=O)OC(C)(C)C VYGIGVDDUBLRTI-UHFFFAOYSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- LQTMEOSBXTVYRM-VIFPVBQESA-N tert-butyl n-[(2s)-1-hydroxy-4-methylpentan-2-yl]carbamate Chemical compound CC(C)C[C@@H](CO)NC(=O)OC(C)(C)C LQTMEOSBXTVYRM-VIFPVBQESA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 238000000954 titration curve Methods 0.000 description 1
- 229940044693 topoisomerase inhibitor Drugs 0.000 description 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000032258 transport Effects 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 229960003048 vinblastine Drugs 0.000 description 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 229910052724 xenon Inorganic materials 0.000 description 1
- FHNFHKCVQCLJFQ-UHFFFAOYSA-N xenon atom Chemical compound [Xe] FHNFHKCVQCLJFQ-UHFFFAOYSA-N 0.000 description 1
- JPZXHKDZASGCLU-LBPRGKRZSA-N β-(2-naphthyl)-alanine Chemical compound C1=CC=CC2=CC(C[C@H](N)C(O)=O)=CC=C21 JPZXHKDZASGCLU-LBPRGKRZSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
- C07K7/086—Bombesin; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB909016810A GB9016810D0 (en) | 1990-07-31 | 1990-07-31 | Peptides |
| PCT/GB1991/001289 WO1992002545A1 (en) | 1990-07-31 | 1991-07-30 | Bombesin antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SK3893A3 true SK3893A3 (en) | 1993-07-07 |
Family
ID=10679953
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK3893A SK3893A3 (en) | 1990-07-31 | 1991-09-30 | Bombesine antagonists |
Country Status (20)
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5877277A (en) | 1987-09-24 | 1999-03-02 | Biomeasure, Inc. | Octapeptide bombesin analogs |
| US5723578A (en) * | 1987-09-24 | 1998-03-03 | The Administrators Of Tulane Educational Fund | Peptide analogs of bombesin |
| US5436137A (en) * | 1992-07-27 | 1995-07-25 | Oregon Regional Primate Research Center | DNA sequence which encodes a peptide capable of promoting acrosome reaction |
| US5620955A (en) * | 1993-06-18 | 1997-04-15 | Peptide Technologies Corporation | Bombesin receptor antagonists and uses thereof |
| JP4954983B2 (ja) * | 2005-05-18 | 2012-06-20 | ファーマサイエンス・インコーポレイテッド | Ｂｉｒドメイン結合化合物 |
| BRPI0617751A2 (pt) | 2005-10-25 | 2011-08-02 | Aegera Therapeutics Inc | compostos de ligação do domìnio iap bir |
| US9284350B2 (en) | 2010-02-12 | 2016-03-15 | Pharmascience Inc. | IAP BIR domain binding compounds |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU618029B2 (en) * | 1987-11-02 | 1991-12-12 | Imperial Chemical Industries Plc | Polypeptide compounds |
-
1990
- 1990-07-31 GB GB909016810A patent/GB9016810D0/en active Pending
-
1991
- 1991-07-30 CA CA002088166A patent/CA2088166A1/en not_active Abandoned
- 1991-07-30 EP EP91914148A patent/EP0541654A1/en not_active Withdrawn
- 1991-07-30 PT PT98498A patent/PT98498A/pt not_active Application Discontinuation
- 1991-07-30 IL IL99009A patent/IL99009A0/xx unknown
- 1991-07-30 IE IE267191A patent/IE912671A1/en unknown
- 1991-07-30 WO PCT/GB1991/001289 patent/WO1992002545A1/en not_active Application Discontinuation
- 1991-07-30 NZ NZ239183A patent/NZ239183A/xx unknown
- 1991-07-30 MC MC912312D patent/MC2312A1/xx unknown
- 1991-07-30 JP JP3513218A patent/JPH05509100A/ja active Pending
- 1991-07-30 MY MYPI91001370A patent/MY107031A/en unknown
- 1991-07-30 PL PL91297652A patent/PL167322B1/pl unknown
- 1991-07-30 AU AU83111/91A patent/AU653544B2/en not_active Ceased
- 1991-07-30 TW TW080105951A patent/TW234130B/zh active
- 1991-07-30 CZ CS9380A patent/CZ8093A3/cs unknown
- 1991-07-30 ZA ZA915978A patent/ZA915978B/xx unknown
- 1991-07-30 HU HU93239A patent/HUT63178A/hu unknown
- 1991-09-30 SK SK3893A patent/SK3893A3/sk unknown
-
1993
- 1993-01-26 NO NO930262A patent/NO930262D0/no unknown
- 1993-01-29 FI FI930411A patent/FI930411A7/fi not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| FI930411A0 (fi) | 1993-01-29 |
| EP0541654A1 (en) | 1993-05-19 |
| PL297652A1 (enrdf_load_stackoverflow) | 1992-07-13 |
| PL167322B1 (pl) | 1995-08-31 |
| AU8311191A (en) | 1992-03-02 |
| CA2088166A1 (en) | 1992-02-01 |
| MY107031A (en) | 1995-08-30 |
| NO930262L (no) | 1993-01-26 |
| HU9300239D0 (en) | 1993-04-28 |
| NO930262D0 (no) | 1993-01-26 |
| PT98498A (pt) | 1992-05-29 |
| HUT63178A (en) | 1993-07-28 |
| FI930411A7 (fi) | 1993-01-29 |
| AU653544B2 (en) | 1994-10-06 |
| WO1992002545A1 (en) | 1992-02-20 |
| ZA915978B (en) | 1993-04-28 |
| IL99009A0 (en) | 1992-07-15 |
| IE912671A1 (en) | 1992-02-12 |
| MC2312A1 (fr) | 1993-09-27 |
| CZ8093A3 (en) | 1994-01-19 |
| GB9016810D0 (en) | 1990-09-12 |
| TW234130B (enrdf_load_stackoverflow) | 1994-11-11 |
| NZ239183A (en) | 1993-07-27 |
| JPH05509100A (ja) | 1993-12-16 |
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