UA73100C2 - Method for inhibiting proliferation of cancer cells by administering growth hormone releasing compound or its antagonist - Google Patents

Method for inhibiting proliferation of cancer cells by administering growth hormone releasing compound or its antagonist Download PDF

Info

Publication number: UA73100C2
Authority: UA; Ukraine
Prior art keywords: mgr; ttr; aia; rne; niz
Prior art date: 1998-11-16

Application number

UA2001064044A

Other languages

English (en)

Ukrainian (uk)

Original Assignee

Zentaris Ag

Priority date (The priority date 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 date listed.)

1998-11-16

Filing date

1999-11-11

Publication date

2005-06-15

1999-11-11 Application filed by Zentaris Ag filed Critical Zentaris Ag

2005-06-15 Publication of UA73100C2 publication Critical patent/UA73100C2/uk

Links

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Classifications

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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
- A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones

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Animal Behavior & Ethology (AREA)
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Pharmacology & Pharmacy (AREA)
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Proteomics, Peptides & Aminoacids (AREA)
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UA2001064044A 1998-11-16 1999-11-11 Method for inhibiting proliferation of cancer cells by administering growth hormone releasing compound or its antagonist UA73100C2 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US09/192,406 US6124263A (en)	1998-11-16	1998-11-16	Treatment of tumors by administration of growth hormone releasing compounds and their antagonists
PCT/EP1999/008662 WO2000029011A1 (en)	1998-11-16	1999-11-11	Treatment of tumors by administration of growth hormone releasing compounds and their antagonists

Publications (1)

Publication Number	Publication Date
UA73100C2 true UA73100C2 (en)	2005-06-15

Family

ID=22709509

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
UA2001064044A UA73100C2 (en)	1998-11-16	1999-11-11	Method for inhibiting proliferation of cancer cells by administering growth hormone releasing compound or its antagonist

Country Status (30)

Country	Link
US (1)	US6124263A (de)
EP (1)	EP1131083B1 (de)
JP (1)	JP2002529512A (de)
KR (1)	KR100704138B1 (de)
CN (3)	CN100368014C (de)
AR (1)	AR021286A1 (de)
AT (1)	ATE258062T1 (de)
BG (1)	BG105572A (de)
BR (1)	BR9915390A (de)
CA (1)	CA2350914A1 (de)
CO (1)	CO5140111A1 (de)
CZ (1)	CZ20011577A3 (de)
DE (1)	DE69914365T2 (de)
DK (1)	DK1131083T3 (de)
ES (1)	ES2212650T3 (de)
HK (1)	HK1040934A1 (de)
HU (1)	HUP0104374A3 (de)
IL (1)	IL142858A0 (de)
MX (1)	MXPA01004689A (de)
NO (1)	NO20012367L (de)
NZ (1)	NZ511280A (de)
PL (1)	PL347659A1 (de)
PT (1)	PT1131083E (de)
RU (1)	RU2240133C2 (de)
SK (1)	SK6352001A3 (de)
TR (1)	TR200101350T2 (de)
TW (2)	TWI237565B (de)
UA (1)	UA73100C2 (de)
WO (1)	WO2000029011A1 (de)
ZA (1)	ZA200103182B (de)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US6211156B1 (en) *	1999-11-10	2001-04-03	Asta Medica A.G.	Peptides for treatment of erectile dysfunction
CU23157A1 (es) *	2001-01-03	2006-07-18	Ct Ingenieria Genetica Biotech	COMPOSICION FARMACéUTICA PARA EL TRATAMIENTO DEL DANO TISULAR DEBIDO A FALTA DE IRRIGACION SANGUINEA ARTERIAL
DE10112882A1 (de) *	2001-03-15	2002-09-19	Max Delbrueck Centrum	Verwendung von Tryptophan-Derivaten zur spezifischen zytostatischen Behandlung von Serotonin-produzierenden Tumoren
US20040157227A1 (en) *	2001-05-10	2004-08-12	Chopin Lisa Kerstin	Reproductive cancer diagnosis and therapy
EP1312363A1 (de) *	2001-09-28	2003-05-21	Pfizer Products Inc.	Behandlungsverfahren und kits bestehend aus Wachstumshormonsekretionsförderern
TWI331922B (en)	2002-08-09	2010-10-21	Ipsen Pharma Sas	Growth hormone releasing peptides
WO2005027913A1 (en) *	2003-09-19	2005-03-31	Pfizer Products Inc.	Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and a growth hormone secretagogue
US20050164952A1 (en) *	2004-01-23	2005-07-28	Vital Pharmaceuticals, Inc.	Delivery system for growth hormone releasing peptides
EP2021015A2 (de) *	2006-04-28	2009-02-11	The Administrators Of The Tulane Educational Fund	Ghrelin/ghrp/ghsr-antagonisten und ihre verwendung
CN101541341B (zh)	2006-09-27	2013-06-05	益普生制药两合公司	N末端取代的生长素释放肽类似物
KR20090112720A (ko)	2007-02-13	2009-10-28	헬신 세라퓨틱스 (유.에스.) 인크.	성장 호르몬 분비촉진제를 이용한 세포 증식 질환의 치료방법
US8841257B2 (en) *	2009-04-10	2014-09-23	Board Of Regents, The University Of Texas System	Inhibitors of STAT3 and uses thereof
US9724381B2 (en)	2009-05-12	2017-08-08	The Administrators Of The Tulane Educational Fund	Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof
IT1399610B1 (it) *	2010-01-28	2013-04-26	Univ Milano Bicocca	Uso di agonisti e antagonisti dei recettori per i growth hormone secretagogues per la prevenzione e il trattamento di convulsioni ed epilessia
CA3129405A1 (en)	2019-02-08	2020-08-13	United States Government As Represented By The Department Of Veterans Affairs	Growth hormone-releasing hormone antagonists and uses thereof
WO2021011874A1 (en) *	2019-07-18	2021-01-21	University Of Miami	Ghrh antagonists for use in a method of treating sarcoidosis

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CA2053250A1 (en) *	1989-04-26	1990-10-27	David H. Coy	Linear somatostatin analogs
IT1240643B (it) *	1990-05-11	1993-12-17	Mediolanum Farmaceutici Spa	Peptidi biologicamente attivi contenenti in catena 2-alchiltriptofano
US5385682A (en) *	1990-05-15	1995-01-31	Exxon Research & Engineering Co.	Grease composition
EP1288224B1 (de) *	1993-08-09	2008-06-25	Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S.	Derivate therapeutischer Peptide
US5550212A (en) *	1993-12-17	1996-08-27	The Administrators Of The Tulane Educational Fund	Analogues of hGH-RH(1-29)NH2 having antagonistic activity
US5807985A (en) *	1996-06-11	1998-09-15	Deghenghi; Romano	Oligopeptide compounds containing D-2-alkyltryptophan capable of promoting the release of growth hormone
US6063796A (en) *	1997-04-04	2000-05-16	Merck & Co., Inc.	Somatostatin agonists

1998
- 1998-11-16 US US09/192,406 patent/US6124263A/en not_active Expired - Fee Related
1999
- 1999-10-28 CO CO99068206A patent/CO5140111A1/es unknown
- 1999-11-11 DK DK99955974T patent/DK1131083T3/da active
- 1999-11-11 RU RU2001116722/14A patent/RU2240133C2/ru not_active IP Right Cessation
- 1999-11-11 CN CNB2006100998244A patent/CN100368014C/zh not_active Expired - Fee Related
- 1999-11-11 IL IL14285899A patent/IL142858A0/xx unknown
- 1999-11-11 JP JP2000582057A patent/JP2002529512A/ja active Pending
- 1999-11-11 EP EP99955974A patent/EP1131083B1/de not_active Expired - Lifetime
- 1999-11-11 CN CNB200410045995XA patent/CN1277840C/zh not_active Expired - Fee Related
- 1999-11-11 KR KR1020017006163A patent/KR100704138B1/ko not_active Expired - Fee Related
- 1999-11-11 HK HK02102769.3A patent/HK1040934A1/zh unknown
- 1999-11-11 PT PT99955974T patent/PT1131083E/pt unknown
- 1999-11-11 CZ CZ20011577A patent/CZ20011577A3/cs unknown
- 1999-11-11 ES ES99955974T patent/ES2212650T3/es not_active Expired - Lifetime
- 1999-11-11 AT AT99955974T patent/ATE258062T1/de not_active IP Right Cessation
- 1999-11-11 PL PL99347659A patent/PL347659A1/xx unknown
- 1999-11-11 HU HU0104374A patent/HUP0104374A3/hu unknown
- 1999-11-11 BR BR9915390-4A patent/BR9915390A/pt not_active IP Right Cessation
- 1999-11-11 DE DE69914365T patent/DE69914365T2/de not_active Expired - Fee Related
- 1999-11-11 WO PCT/EP1999/008662 patent/WO2000029011A1/en not_active Ceased
- 1999-11-11 SK SK635-2001A patent/SK6352001A3/sk unknown
- 1999-11-11 UA UA2001064044A patent/UA73100C2/uk unknown
- 1999-11-11 TR TR2001/01350T patent/TR200101350T2/xx unknown
- 1999-11-11 CN CNB998133612A patent/CN1200726C/zh not_active Expired - Fee Related
- 1999-11-11 CA CA002350914A patent/CA2350914A1/en not_active Abandoned
- 1999-11-11 NZ NZ511280A patent/NZ511280A/xx unknown
- 1999-11-11 MX MXPA01004689A patent/MXPA01004689A/es not_active IP Right Cessation
- 1999-11-16 AR ARP990105814A patent/AR021286A1/es unknown
- 1999-11-30 TW TW088117984A patent/TWI237565B/zh not_active IP Right Cessation
- 1999-11-30 TW TW094111886A patent/TWI263642B/zh not_active IP Right Cessation
2001
- 2001-04-19 ZA ZA200103182A patent/ZA200103182B/en unknown
- 2001-05-14 NO NO20012367A patent/NO20012367L/no not_active Application Discontinuation
- 2001-06-07 BG BG105572A patent/BG105572A/xx unknown

Also Published As

Publication number	Publication date
IL142858A0 (en)	2002-03-10
KR20010089459A (ko)	2001-10-06
HUP0104374A2 (hu)	2002-04-29
DE69914365D1 (de)	2004-02-26
JP2002529512A (ja)	2002-09-10
CN1200726C (zh)	2005-05-11
NO20012367D0 (no)	2001-05-14
TR200101350T2 (tr)	2001-11-21
CO5140111A1 (es)	2002-03-22
CZ20011577A3 (cs)	2002-07-17
CN1326353A (zh)	2001-12-12
RU2240133C2 (ru)	2004-11-20
CN1277840C (zh)	2006-10-04
PT1131083E (pt)	2004-06-30
ZA200103182B (en)	2001-09-07
EP1131083B1 (de)	2004-01-21
CN1895660A (zh)	2007-01-17
NO20012367L (no)	2001-07-09
NZ511280A (en)	2002-10-25
PL347659A1 (en)	2002-04-22
MXPA01004689A (es)	2002-09-18
US6124263A (en)	2000-09-26
TWI263642B (en)	2006-10-11
HK1040934A1 (zh)	2002-06-28
HUP0104374A3 (en)	2003-03-28
AR021286A1 (es)	2002-07-03
EP1131083A1 (de)	2001-09-12
TWI237565B (en)	2005-08-11
DK1131083T3 (da)	2004-04-26
BR9915390A (pt)	2001-08-07
WO2000029011A1 (en)	2000-05-25
TW200530270A (en)	2005-09-16
ES2212650T3 (es)	2004-07-16
DE69914365T2 (de)	2004-11-04
KR100704138B1 (ko)	2007-04-09
SK6352001A3 (en)	2002-09-10
CA2350914A1 (en)	2000-05-25
CN100368014C (zh)	2008-02-13
BG105572A (en)	2002-01-31
ATE258062T1 (de)	2004-02-15
CN1594358A (zh)	2005-03-16

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EP1542716B1 (de)	2009-11-04	Wachstumshormon freisetzende peptide
US8524668B2 (en)	2013-09-03	Methods of protecting against apoptosis using lipopeptides
EP1131083B1 (de)	2004-01-21	Verwendung von wachstumshormon freisetzenden stoffen und ihren antagonisten zur behandlung von tumoren
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ITMI951670A1 (it)	1997-01-28	Peptidi ciclici analoghi della somatostatina ad attivita' inibitrice dell'ormone della crescita
AU768516B2 (en)	2003-12-18	Treatment of tumors by administration of growth hormone releasing compounds and their antagonists
Tsutsumi et al.	1993	Biphasic effects of suramin on125I-epidermal growth factor binding to human meningiomas
Teplán	2000	Peptides and antitumor activity: Development and investigation of some peptides with antitumor activity
US12024515B2 (en)	2024-07-02	Kifunensine derivatives
Bowers	2000	GHRP historical perspective: basic and clinical
Patchett et al.	2000	The design of peptidomimetic growth hormone secretagogues
EP1756142B1 (de)	2008-07-02	Pseudopeptide, die die sekretion von wachstumshormon anregen
AU2007202409B2 (en)	2009-01-29	Growth hormone releasing peptides
Chen et al.	1999	Intracellular GHRP signalling
Pleasanton et al.	0	Aurrecoechea et al.(43) Pub. Date: Jul. 20, 2006
HK1181684B (en)	2016-01-22	Methods of protecting against apoptosis using lipopeptides
HK1102373B (en)	2008-09-12	Pseudopeptides growth hormone secretagogues