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1. 发明申请

WO2014070965A2 SOMATOSTATIN ANALOGS AND DIMERS THEREOF 审中-公开
标题翻译： SOMATOSTATIN类似物及其二聚体
公开(公告)号：WO2014070965A2
公开(公告)日：2014-05-08
申请号：PCT/US2013067651
申请日：2013-10-31
申请人： IPSEN PHARMA SAS , DONG ZHENG XIN , FERRANDIS ERIC
发明人： DONG ZHENG XIN , FERRANDIS ERIC
IPC分类号： A61K38/12
CPC分类号： C07K7/64 , A61K38/12 , G01N33/74 , G01N2333/726
摘要： The present invention relates to novel somatostatin analogs, dimers thereof, and methods of using the same to treat various diseases.
摘要翻译：本发明涉及新型促生长素抑制素类似物，其二聚体及其用途来治疗各种疾病。

2. 发明申请

WO2014070965A8 SOMATOSTATIN ANALOGS AND DIMERS THEREOF 审中-公开
标题翻译： SOMATOSTATIN类似物及其二聚体
公开(公告)号：WO2014070965A8
公开(公告)日：2015-06-04
申请号：PCT/US2013067651
申请日：2013-10-31
申请人： IPSEN PHARMA SAS
发明人： DONG ZHENG XIN , FERRANDIS ERIC
IPC分类号： A61K38/00
CPC分类号： C07K7/64 , A61K38/12 , G01N33/74 , G01N2333/726
摘要： The present invention relates to novel somatostatin analogs, dimers thereof, and methods of using the same to treat various diseases. Naturally occurring somatostatins (SSTs), which are also known as somatotropin release-inhibiting factors (SRIFs), have diverse biological effects in many cells and organs 10 throughout the body. They are produced by normal endocrine, gastrointestinal, immune and neuronal cells, as well as by certain tumors (Patel, Y. C, Frontiers in Neuroendocrinology, 20(3): 157-198 (1999); Froidevaux, et al., Biopolymers, 66(3): 161-83 (2002)).
摘要翻译：本发明涉及新型促生长素抑制素类似物，其二聚体及其用途来治疗各种疾病。天然存在的促生长素抑制因子（SSTs）也称为生长激素释放抑制因子（SRIF），在整个身体的许多细胞和器官10中具有不同的生物学作用。它们由正常的内分泌，胃肠道，免疫和神经元细胞以及某些肿瘤产生（Patel，Y.C，Frontiers in Neuroendocrinology，20（3）：157-198（1999）; Froidevaux等人，Biopolymers ，66（3）：161-83（2002））。

3. 发明公开

EP2914276A4 SOMATOSTATIN ANALOGS AND DIMERS THEREOF 审中-公开
标题翻译： SOMATOSTATIN-ANALOGA UND DIMERE DARAUS
公开(公告)号：EP2914276A4
公开(公告)日：2016-07-13
申请号：EP13850219
申请日：2013-10-31
申请人： IPSEN PHARMA SAS
发明人： DONG ZHENG XIN , FERRANDIS ERIC
IPC分类号： A61K38/00 , A61K38/12 , C07K7/64 , G01N33/74
CPC分类号： C07K7/64 , A61K38/12 , G01N33/74 , G01N2333/726
摘要： The present invention relates to novel somatostatin analogs, dimers thereof, and methods of using the same to treat various diseases. Naturally occurring somatostatins (SSTs), which are also known as somatotropin release-inhibiting factors (SRIFs), have diverse biological effects in many cells and organs 10 throughout the body. They are produced by normal endocrine, gastrointestinal, immune and neuronal cells, as well as by certain tumors (Patel, Y. C, Frontiers in Neuroendocrinology, 20(3): 157-198 (1999); Froidevaux, et al., Biopolymers, 66(3): 161-83 (2002)).
摘要翻译：本发明涉及新型促生长素抑制素类似物，其二聚体，及其用于治疗各种疾病的方法。自然发生的生长激素抑制因子（SSTs）也称为生长激素释放抑制因子（SRIF），在整个身体的许多细胞和器官10中具有多种生物学作用。它们由正常的内分泌，胃肠道，免疫和神经元细胞以及某些肿瘤产生（Patel，Y.C，Frontiers in Neuroendocrinology，20（3）：157-198（1999）; Froidevaux等人，Biopolymers ，66（3）：161-83（2002））。

4. 发明专利

AU2002335492B2 Polynucleotide useful for modulating cancer cell proliferation 未知
公开(公告)号：AU2002335492B2
公开(公告)日：2006-11-02
申请号：AU2002335492
申请日：2002-03-01
申请人： CENTRE NAT RECH SCIENT , IPSEN PHARMA SAS
发明人： FERRER JOSE-ANTONIO CAMARA Y , THURIEAU CHRISTOPHE , FERRANDIS ERIC , MARTINEZ JEAN
IPC分类号： C12N15/09 , C12N15/12 , A61K38/00 , A61K38/17 , A61P35/00 , C07K14/435 , C07K14/47 , C07K14/82 , C07K16/18 , C07K16/32 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/63 , C12P21/08
摘要： The invention concerns a novel protein modulating cancer cell proliferation. The proteins encoded by the polynucleotides of the invention enable to determine the degree of malignity of abnormal cell proliferation.

5. 发明专利

HK1213486A1 促生長素抑制素類似物及其二聚體未知
公开(公告)号：HK1213486A1
公开(公告)日：2016-07-08
申请号：HK16101502
申请日：2016-02-11
申请人： IPSEN PHARMA SAS
发明人： DONG ZHENG XIN , FERRANDIS ERIC
IPC分类号： A61K20060101

6. 发明专利

AU2003274281B2 Heterocarpin, a plant-derived protein with anti-cancer properties 未知
公开(公告)号：AU2003274281B2
公开(公告)日：2009-02-26
申请号：AU2003274281
申请日：2003-08-25
申请人： IPSEN PHARMA SAS
发明人： TENG BENG POON , THURIEAU CHRISTOPHE , FERRANDIS ERIC , SOHIER CHRISTINE
IPC分类号： A61P35/00 , C07K14/415 , A61K36/75 , A61K38/16
摘要： Use of a protein (I), isolated by extraction of Pilocarpus heterophyllus, to treat cancers that require growth hormone-releasing hormone (GHRH) for their growth. Use of a protein (I), isolated by extraction of Pilocarpus heterophyllus, to treat cancers that require growth hormone-releasing hormone (GHRH) for their growth. (I), designated heterocarpin, has molecular weight about 90.9 kD; contains the peptide fragments (1)-(3) and exists in glycosylated or non-glycosylated forms. Lys-Leu-Ile-Gly-Ala-Arg-Tyr-Phe-Asp-Lys (1) Tyr-Gly-Glu-Asp-Ile-Ile-Val-Gly-Val-Ile-Asp-Ser-Gly-Val (2) Pro-Glu-Ser-Glu-Ser-Tyr (3).

7. 发明专利

AU2002365016B2 Benzimidazole derivatives and their use as GnRH antagonists 未知
公开(公告)号：AU2002365016B2
公开(公告)日：2008-11-20
申请号：AU2002365016
申请日：2002-12-20
申请人： IPSEN PHARMA SAS
发明人： BRAULT VALERIE , FERRANDIS ERIC , POITOUT LYDIE , THURIEAU CHRISTOPHE
IPC分类号： C07D235/28 , A61K31/4184 , A61K31/427 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61P5/24 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D235/30 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D471/04 , C07D471/10 , C07D521/00
摘要： 2-(Alkylamino or alkylthio)-5-(aminocarbonyl or aminomethyl)-benzimidazole derivatives (I) are new. 2-(Alkylamino or alkylthio)-5-(aminocarbonyl or aminomethyl)-benzimidazole derivatives of formula (I), in racemic or enantiomer form or any combination of these forms, and their salts are new. A = CH2 or CO; Y = S or NH; R1, R2 = H, 1-8C alkyl, 5-9C bicycloalkyl (optionally substituted (os) by one or more T) or -(CH2)a-X; or NR1R2 = heterocycloalkyl, heterobicycloalkyl or a spiro or fused piperidine group of formula (i), (ii), (iii) or (iv) (all os by one or more of -(CH2)c-X''-Y'', oxo, hydroxy, halo, nitro or cyano); T = 1-6C alkyl; X = NH2, NHT, NT2, adamantyl, arylcarbonyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, indanyl or tetralinyl or 3-7C cycloalkyl, heterocycloalkyl, aryl or heteroaryl (os by one or more of -(CH2)b-X'-Y', halo, oxo, NO2, CN, NH2, NHT, NT2, OH or N3); X' = O, S, C(O), C(O)O, NHC(O), NHSO2 or direct bond; Y' = T (os by one or more halo) or heteroaryl, aryl or heterocycloalkyl (all os by one or more of T, OT, halo, NO2, CN, NH2, CF3, OCF3, OH, N3, NHT or NT2); X'' = O, C(O), C(O)O or direct bond; Y'' = T, NH2, NHT, NT2, 3-7C cycloalkyl, heterocycloalkyl or aralkyl; aryl or heteroaryl (both os by one or more of T, OT, COT, halo, OH, NO2, CN, CF3, OCF3, NH2, NHT or NT2); or 1,4-benzodioxanyl, 1,3-benzodioxolyl or benzimidazol-2-on-1-yl; a = 0-6; b = 0-2; c = 0-4; R3 = -(CH2)c-W3-(CH)2d-Z3; W3 = direct bond, CH(OH) or C(O); Z3 = T, adamantyl, aryl, heteroaryl, 1,4-benzodioxanyl, 1,3-benzodioxolyl or anthraquinonyl (where all aryl groups are os by one or more of -(CH2)e-V3-Y3, halo, NO2, CN, N3 or OH; V3 = O, S, C(O), C(O)O, SO2 or direct bond; Y3 = T, os by one or more halo, NH2, NHT, NT2, CH2COPh, heterocycloalkyl or aryl; c, d, e = 0-4; R4 = -(CH2)f-R''4; R''4 = heterocycloalkyl containing at least one N (os by T or aralkyl); heteroaryl containing at least one N (os by T); or -NW4W'4; W4 = H, T or cycloalkyl; W'4 = -(CH2)g-Q4-Z4; Q4 = -CH2CH(OH)-(CH2)h-(O)i-(CH2)j or -C(O)O; Z4 = H, 1-8C alkyl (os by one or more of OT, ST, SST and OH), 2-6C alkenyl, 2-6C alkynyl, 3-7C cycloalkyl (os by one or more alkyl, COOT or -T-OH), cyclohexenyl, adamantyl, heteroaryl, aryl (os by one or more of -(CH2)k-V4-Y4, OH, NO2, halo or CN), 1,4-benzodioxanyl or 1,3-benzodioxolyl; V4 = O, S, NHC(O) or direct bond; Y4 = T (os by NT2 or one or more halo), NH2, NHT, NT2, aralkyl or heterocycloalkyl; f, g = 0-4; h, i, j = 0 or 1; and k = 0-4.

8. 发明专利

AU2002241065B2 Heterocarpine, a human GHRH-binding protein 未知
公开(公告)号：AU2002241065B2
公开(公告)日：2006-09-28
申请号：AU2002241065
申请日：2002-02-26
申请人： IPSEN PHARMA SAS
发明人： SOHIER CHRISTINE , TENG BENG POON , THURIEAU CHRISTOPHE , FERRANDIS ERIC
IPC分类号： C07K14/415 , C12N15/02 , A61K36/75 , A61K38/00 , A61K38/27 , A61P3/10 , A61P5/00 , A61P5/04 , A61P9/10 , A61P13/12 , A61P25/02 , A61P27/02 , A61P35/00 , A61P43/00 , C07K7/06 , C07K7/08 , C07K16/16 , C12P21/08
摘要： The invention relates to a human GHRH-binding protein (human Growth Hormone-releasing hormone). Said protein, which is obtained from the Pilocarpus Heterophyllus plant, can be used to prepare medicaments intended to antagonise the effects of GHRH and to treat proliferative diseases (particularly cancer), acromegaly or diabetic nephropathies and retinopathies.

9. 发明专利

HK1092701A1 HETEROCARPIN, A PLANT-DERIVED PROTEIN WITH ANTI-CANCER PROPERTIES 未知
公开(公告)号：HK1092701A1
公开(公告)日：2007-02-16
申请号：HK06113390
申请日：2006-12-06
申请人： IPSEN PHARMA SAS
发明人： FERRANDIS ERIC , TENG BENG POON , SOHIER CHRISTINE , THURIEAU CHRISTOPHE
IPC分类号： C07K14/415 , A61K20090101 , A61K36/75 , A61K38/16 , A61P20090101 , A61P35/00
摘要： Use of a protein (I), isolated by extraction of Pilocarpus heterophyllus, to treat cancers that require growth hormone-releasing hormone (GHRH) for their growth. Use of a protein (I), isolated by extraction of Pilocarpus heterophyllus, to treat cancers that require growth hormone-releasing hormone (GHRH) for their growth. (I), designated heterocarpin, has molecular weight about 90.9 kD; contains the peptide fragments (1)-(3) and exists in glycosylated or non-glycosylated forms. Lys-Leu-Ile-Gly-Ala-Arg-Tyr-Phe-Asp-Lys (1) Tyr-Gly-Glu-Asp-Ile-Ile-Val-Gly-Val-Ile-Asp-Ser-Gly-Val (2) Pro-Glu-Ser-Glu-Ser-Tyr (3).

10. 发明专利

HU228339B1 BENZIMIDAZOLE DERIVATIVES PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE 未知
公开(公告)号：HU228339B1
公开(公告)日：2013-03-28
申请号：HU0500183
申请日：2002-12-20
申请人： IPSEN PHARMA SAS
发明人： POITOUT LYDIE , BRAULT VALERIE , FERRANDIS ERIC , THURIEAU CHRISTOPHE
IPC分类号： C07D401/14 , A61K31/4184 , A61K31/427 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61P5/24 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D235/28 , C07D235/30 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D471/04 , C07D471/10 , C07D521/00
摘要： 2-(Alkylamino or alkylthio)-5-(aminocarbonyl or aminomethyl)-benzimidazole derivatives (I) are new. 2-(Alkylamino or alkylthio)-5-(aminocarbonyl or aminomethyl)-benzimidazole derivatives of formula (I), in racemic or enantiomer form or any combination of these forms, and their salts are new. A = CH2 or CO; Y = S or NH; R1, R2 = H, 1-8C alkyl, 5-9C bicycloalkyl (optionally substituted (os) by one or more T) or -(CH2)a-X; or NR1R2 = heterocycloalkyl, heterobicycloalkyl or a spiro or fused piperidine group of formula (i), (ii), (iii) or (iv) (all os by one or more of -(CH2)c-X''-Y'', oxo, hydroxy, halo, nitro or cyano); T = 1-6C alkyl; X = NH2, NHT, NT2, adamantyl, arylcarbonyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, indanyl or tetralinyl or 3-7C cycloalkyl, heterocycloalkyl, aryl or heteroaryl (os by one or more of -(CH2)b-X'-Y', halo, oxo, NO2, CN, NH2, NHT, NT2, OH or N3); X' = O, S, C(O), C(O)O, NHC(O), NHSO2 or direct bond; Y' = T (os by one or more halo) or heteroaryl, aryl or heterocycloalkyl (all os by one or more of T, OT, halo, NO2, CN, NH2, CF3, OCF3, OH, N3, NHT or NT2); X'' = O, C(O), C(O)O or direct bond; Y'' = T, NH2, NHT, NT2, 3-7C cycloalkyl, heterocycloalkyl or aralkyl; aryl or heteroaryl (both os by one or more of T, OT, COT, halo, OH, NO2, CN, CF3, OCF3, NH2, NHT or NT2); or 1,4-benzodioxanyl, 1,3-benzodioxolyl or benzimidazol-2-on-1-yl; a = 0-6; b = 0-2; c = 0-4; R3 = -(CH2)c-W3-(CH)2d-Z3; W3 = direct bond, CH(OH) or C(O); Z3 = T, adamantyl, aryl, heteroaryl, 1,4-benzodioxanyl, 1,3-benzodioxolyl or anthraquinonyl (where all aryl groups are os by one or more of -(CH2)e-V3-Y3, halo, NO2, CN, N3 or OH; V3 = O, S, C(O), C(O)O, SO2 or direct bond; Y3 = T, os by one or more halo, NH2, NHT, NT2, CH2COPh, heterocycloalkyl or aryl; c, d, e = 0-4; R4 = -(CH2)f-R''4; R''4 = heterocycloalkyl containing at least one N (os by T or aralkyl); heteroaryl containing at least one N (os by T); or -NW4W'4; W4 = H, T or cycloalkyl; W'4 = -(CH2)g-Q4-Z4; Q4 = -CH2CH(OH)-(CH2)h-(O)i-(CH2)j or -C(O)O; Z4 = H, 1-8C alkyl (os by one or more of OT, ST, SST and OH), 2-6C alkenyl, 2-6C alkynyl, 3-7C cycloalkyl (os by one or more alkyl, COOT or -T-OH), cyclohexenyl, adamantyl, heteroaryl, aryl (os by one or more of -(CH2)k-V4-Y4, OH, NO2, halo or CN), 1,4-benzodioxanyl or 1,3-benzodioxolyl; V4 = O, S, NHC(O) or direct bond; Y4 = T (os by NT2 or one or more halo), NH2, NHT, NT2, aralkyl or heterocycloalkyl; f, g = 0-4; h, i, j = 0 or 1; and k = 0-4.

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