LV11549B - Therapeutic peptide derivatives - Google Patents
Therapeutic peptide derivatives Download PDFInfo
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- LV11549B LV11549B LVP-96-71A LV960071A LV11549B LV 11549 B LV11549 B LV 11549B LV 960071 A LV960071 A LV 960071A LV 11549 B LV11549 B LV 11549B
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- 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
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
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- A—HUMAN NECESSITIES
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
- A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
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- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
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- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/655—Somatostatins
- C07K14/6555—Somatostatins at least 1 amino acid in D-form
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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Claims (12)
- LV 11549 PATENTA FORMULA 1. Peptida atvasinājums, kas satur: bioloģiski aktīvu peptida daļu, un 5 vismaz vienu aizvietotāju, kas pievienots pie minētās peptida daļas, kur minētais aizvietotājs ir izvēlēts no grupas, kas ietver savienojumus I, II un III, kur savienojums I ir:kur: R0 ir O, S vai NR5, kur R5 ir H vai (C,-C6)alkilgrupa; 15 katrs no R, un R2 neatkarīgi ir H, (CH2)mOR6 vai CH(OR7)CH2OR8, kur R6 ir H vai (C2-C;.)acilgrupa, un katrs no R7 and R8 neatkarīgi ir H, (C2-C7)acilgrupa vai C(Rg)(R10), kur katrs no R9 un R10 neatkarīgi ir H vai (C,-C6)alkilgrupa; vai katrs no R, un R2 ir grupa =CHCH2OR,,, kur aizvietotājā R, un R2 20 neatkarīgi R1t ir H vai (C2-C7)acilgrupa, un m ir vesels skaitlis starp 1 un 5, ieskaitot; un viens no R3 vai R4 ir (CH2)nR12 vai (CH2)nCH(OH)R12, kur R12 ir CO, CH2 vai S02, un n ir vesels skaitlis starp 1 un 5, ieskaitot; un atlikušais R3 vai R4 ir H, (C^Cgjhidroksialkilgrupa vai (C2-C7)acilgrupa; 25 un savienojums II ir: Rt3-0-CH2 30 R.4-0-CH2-C-(CH2)m-R,6-R17-(CH2)n-Rl8 r!5-o-ch2 35 kur: katrs no R,3, R,4 un R1S neatkarīgi ir H vai (C2-C24)acilgrupa; R16 ir NH vai nav vispār; 2 R17 ir CO, O vai nav vispār; R18 ir CO, CH2, S02 vai nav vispār; m ir vesels skaitlis starp 1 un 5, ieskaitot; n ir vesels skaitlis starp 0 un 5, ieskaitot; un savienojums III ir:kur: R)9 ir H, NH2, aromātiska funkcionāla grupa, OH, (C,-C6)hidroksialkilgrupa, H(R27)(R28), S03H vai nav vispār; kur katrs no R27 un R28 neatkarīgi ir H vai (Cļ-Cg) alkilgrupa; R^ ir O vai nav vispār; R21 ir (Cļ-Cgjalkilgrupa vai nav vispār; R22 ir N, 0, C vai CH; -R23- ir (C,-C6)alki(grupa vai nav vispār; R24 ir N, CH vai C; R25 ir NH, 0 vai nav vispār; R26 ir S02, CO, CH2 vai nav vispār; m ir vesels skaitlis starp 0 un 5, ieskaitot; n ir vesels skaitlis starp 0 un 5, ieskaitot; p ir vesels skaitlis starp 0 un 5, ieskaitot; q ir vesels skaitlis starp 0 un 5, ieskaitot; un kur minētā peptīda daļa ir pievienota pie katra no minētajiem aizvietotājiem ar CO-N, CH2-N vai S02*N saiti starp minēto aizvietotāju un minētās peptīda daļas N-gala vai sānu virknes slāpekļa atomu.
- 2. Peptīda atvasinājums saskaņā ar 1. punktu, kur minētais aizvietotājs ir savienojums II.
- 3. Peptīda atvasinājums saskaņā ar 2. punktu, kur minētais aizvietotājs ir (H0CH2)3C-NH-(CH)2-S02 vai (HOCH2)3C-CH2. 3 LV 11549
- 4. Peptīda atvasinājums saskaņā ar 1. punktu, kur minētais aizvietotājs ir savienojums III.
- 5. Peptīda atvasinājums saskaņā ar 4. punktu, kur minētais aizvietotājs ir viens no: HO(CH.,)2-N_N-(CH2)2S02- un HQ(CH2)2-N n-ch2-cq-
- 6. Peptīda atvasinājums saskaņā ar 1. punktu, kur minētā peptīda daļa ir izvēlēta no grupas, kurā ietilpst: somatostatīns, bombezīns, kalcitonīns, kalcitonīna gēnam atbilstošais peptīds (CGRP), amilīns, paratiroidais hormons (PTH), gastrīna atbrīvotājpeptīds (GRP), melanocītus stimulējošais hormons (MSH), adrenokortikotropais hormons (ACTH), paratiroīdajam hormonam radniecīgais peptīds (PTHrP), luteinizējošā hormona rilīzinghormons (LHRH), augšanas hormona atbrīvotājfaktors (GHRF), augšanas hormona atbrīvotājpeptīds (GHRP), holecistokinīns (CCK), glikagons, bradikinīns, glikagonam līdzīgais peptīds (GLP), gastrins, enkefalīns, neiromedīns, endotelīns, viela P, neiropeptids Υ (ΝΡΥ), peptīds ΥΥ (ΡΥΥ), vazoaktīvais zarnu peptīds (VIP), guanilīns, hipofīzes adenilātciklāzi aktivējošais polipeptīds (PACAP), beta-šūnu tropīns, adrenomedulīns un to atvasinājumi, fragmenti un analogi.
- 7. Peptīda atvasinājums saskaņā ar 6. punktu, kur minētā peptīda daļa ir somatostatīns vai tā atvasinājums, fragments vai analogs.
- 8. Peptīda atvasinājums saskaņā ar 7. punktu, kur minētais somatostatīna analogs ir viens no: H-D-Phe-c[Cys-Tyr-D-Trp-Lys-Abu-Cys]-Thr-NH2, H-D-Phe-c[Cys-Tyr-D-Trp-Lys-Thr-Cys]-Nal-NH2 un H-D-Nal-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH2.
- 9. Peptīda atvasinājums saskaņā ar 6. punktu, kur minētā peptīda daļa ir bombezīns vai tā atvasinājums, fragments vai analogs. 4 I
- 10. Petīda atvasinājums saskaņā ar 1. punktu, kur minētais peptida atvasinājums ir viens no: HO(CH2)2-N^-(CH2)CO-D-Phe-c[Cys-Tyr-D-Trp-Lys-Abu-Cys]-Thr-NH2 un H0(CH2)2-N^N-(CH2)2S02-D-Phe-c[Cys-Tyr-D-Trp-Lys-Abu-Cys]-Thr-NH2
- 11. Dimērs peptida atvasinājums, kas satur: divas bioloģiski aktīvas peptida daļas un vismaz vienu aizvietotāju, kas pievienots pie vienas no minētajām peptida daļām, kur minētais aizvietotājs ir viens no savienojumiem IV un V, kur savienojums IV ir:R0 ir O, S vai NR5, kur Rs ir H vai (C,-C6)alkilgrupa; katrs no R, un R2 neatkarīgi ir H, (CH2)mOR6 vai CH(OR7)CH2OR0, kur R6 ir H vai (C2-C7)acilgrupa, un katrs no R7 un R0 neatkarīgi ir H, (C2-C7)acilgrupa vai C(R9)(R10), kur katrs no R9 un R,0 neatkarīgi ir H vai (C,-C6)alkilgrupa; vai katrs no R, un R2 ir grupa =CHCH2OR,,, kur Rn aizvietotājos R, un R2 neatkarīgi ir H vai (C2-C7)acilgrupa, un m ir vesels skaitlis starp 1 un 5, ieskaitot; un katrs R3 vai R4 neatkarīgi ir (CH?)nRt2 vai (CH2)nCH(OH)R.2, kur R,2 ir CO, CH2 vai S02, un n ir vesels skaitlis starp 1 un 5, ieskaitot; un savienojums V ir: LV 11549 (CH2)m / \ ^19* ^20* ^21*^22' ^23 'R24'(CH2)p-R25-(CH2)q-R26 \ / (CH,)n kur: R,g ir S02, CO, CH2vai nav vispār; ir 0 vai nav vispār; R21 ir (C,-C6)alkilgrupa vai nav vispār; R22ir N, CH, O vai C; -R23- ir (C,-C6)alkilgrupa vai nav vispār; R24 ir N, CH vai C; R25 ir NH, 0 vai nav vispār; R26 ir S02, CO, CH2 vai nav vispār; m ir vesels skaitlis starp 0 un 5, ieskaitot; n ir vesels skaitlis starp 0 un 5, ieskaitot; p ir vesels skaitlis starp 0 un 5, ieskaitot; q ir vesels skaitlis starp 0 un 5, ieskaitot; un kur vismaz viena no minētajām peptīda daļām ir pievienota pie katra no minētajiem aizvietotājiem ar CO-N, CH2-N vai S02-N saiti starp minēto aizvietotāju un minētās peptīda daļas N-gala vai sānu virknes slāpekļa atomu.
- 12. Peptīda atvasinājums saskaņā ar 1. punktu, kas izmantojams slimības, īpaši vēža, ārstēšanai.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US10419493A | 1993-08-09 | 1993-08-09 | |
PCT/US1994/008875 WO1995004752A1 (en) | 1993-08-09 | 1994-08-08 | Therapeutic peptide derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
LV11549A LV11549A (lv) | 1996-10-20 |
LV11549B true LV11549B (en) | 1997-04-20 |
Family
ID=22299154
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
LVP-96-71A LV11549B (en) | 1993-08-09 | 1996-03-08 | Therapeutic peptide derivatives |
Country Status (30)
Country | Link |
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US (1) | US5552520A (lv) |
EP (3) | EP0788509B1 (lv) |
JP (3) | JP3618750B2 (lv) |
KR (1) | KR100325972B1 (lv) |
CN (1) | CN1055700C (lv) |
AT (3) | ATE284413T1 (lv) |
AU (1) | AU689490B2 (lv) |
CA (1) | CA2168113C (lv) |
CZ (3) | CZ292586B6 (lv) |
DE (3) | DE69432758T2 (lv) |
DK (3) | DK0788509T3 (lv) |
ES (3) | ES2196031T3 (lv) |
FI (1) | FI960584A0 (lv) |
GE (1) | GEP20002146B (lv) |
HK (2) | HK1053314A1 (lv) |
HU (1) | HU224350B1 (lv) |
LT (1) | LT4078B (lv) |
LV (1) | LV11549B (lv) |
MD (1) | MD1591B2 (lv) |
NZ (1) | NZ271238A (lv) |
PL (1) | PL180612B1 (lv) |
PT (2) | PT788509E (lv) |
RO (1) | RO117259B1 (lv) |
RU (1) | RU2133252C1 (lv) |
SG (1) | SG75092A1 (lv) |
SI (2) | SI0788509T1 (lv) |
SK (1) | SK15096A3 (lv) |
UA (1) | UA44707C2 (lv) |
WO (1) | WO1995004752A1 (lv) |
ZA (1) | ZA945966B (lv) |
Families Citing this family (61)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2774769B2 (ja) * | 1993-04-26 | 1998-07-09 | 賢治 寒川 | アドレノメデュリン |
WO1996029343A1 (fr) * | 1995-03-20 | 1996-09-26 | Kyowa Hakko Kogyo Co., Ltd. | Nouveaux derives de calcitonine |
US5824772A (en) * | 1995-04-04 | 1998-10-20 | Advanced Bioconcept, Inc. | Fluorescent somatostatin |
US7048906B2 (en) | 1995-05-17 | 2006-05-23 | Cedars-Sinai Medical Center | Methods of diagnosing and treating small intestinal bacterial overgrowth (SIBO) and SIBO-related conditions |
US6861053B1 (en) | 1999-08-11 | 2005-03-01 | Cedars-Sinai Medical Center | Methods of diagnosing or treating irritable bowel syndrome and other disorders caused by small intestinal bacterial overgrowth |
US6479457B2 (en) * | 1995-06-06 | 2002-11-12 | Kinerton Limited | Ionic molecular conjugates of N-acylated derivatives of poly(2-amino-2-deoxy-D-glucose) and polypeptides |
US5830431A (en) * | 1995-06-07 | 1998-11-03 | Mallinckrodt Medical, Inc. | Radiolabeled peptide compositions for site-specific targeting |
US6544949B1 (en) | 1995-07-13 | 2003-04-08 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Analogs of parathyroid hormone |
US7410948B2 (en) | 1995-07-13 | 2008-08-12 | Societe De Conseils De Recherches Et D'applications Scientifiques, Sas | Analogs of parathyroid hormone |
US5766620A (en) * | 1995-10-23 | 1998-06-16 | Theratech, Inc. | Buccal delivery of glucagon-like insulinotropic peptides |
US7078413B2 (en) | 1996-04-19 | 2006-07-18 | Wisconsin Alumni Research Foundation | Compositions and methods of use for a bombesin peptide |
US6492330B1 (en) * | 1996-08-16 | 2002-12-10 | National Institute Of Immunology | Antiangiogenic drugs |
US5968903A (en) * | 1998-05-07 | 1999-10-19 | Biomeasure, Incorporated | Inhibition of H. pylori proliferation |
US6124263A (en) * | 1998-11-16 | 2000-09-26 | Asta Medica Ag | Treatment of tumors by administration of growth hormone releasing compounds and their antagonists |
US6864234B1 (en) | 1999-06-25 | 2005-03-08 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Somatostatin agonists |
BR0011919A (pt) * | 1999-06-25 | 2002-03-19 | Sod Conseils Rech Applic | Agonistas de somatostatina |
EP1348444B1 (en) * | 1999-08-18 | 2006-04-12 | Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. | Sustained release formulation of a peptide complexed with a polymer |
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1994
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1996
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