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1. 发明公开

EP4426306A1 NOVEL COMBINED ADMINISTRATION 审中-实审
公开(公告)号：EP4426306A1
公开(公告)日：2024-09-11
申请号：EP22802517.7
申请日：2022-10-04
申请人： F. Hoffmann-La Roche AG
发明人： HELLBACH, Nicole , KLETZL, Heidemarie , METZGER, Friedrich , SICILIANI SCALCO, Renata
IPC分类号： A61K31/519 , A61P21/00 , A61K39/395 , A61K9/00 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/26 , A61K39/00 , C07K16/22
CPC分类号： A61K31/519 , A61P21/00 , A61K9/0095 , A61K47/26 , A61K47/10 , A61K47/183 , A61K47/22 , A61K47/12 , C07K16/22 , A61K2039/50520130101 , A61K39/395

2. 发明公开

EP3035935A2 SCREENING METHOD 有权
标题翻译：筛选方法
公开(公告)号：EP3035935A2
公开(公告)日：2016-06-29
申请号：EP14750760.2
申请日：2014-08-15
申请人： F. Hoffmann-La Roche AG
发明人： EBELING, Martin , METZGER, Friedrich , SIVARAMAKRISHNAN, Manaswini
IPC分类号： A61K31/519 , A61P35/00
摘要： The invention discloses a screening method for the identification of new compounds for use in the treatment of cancer.
摘要翻译：本发明公开了用于鉴定用于治疗癌症的新化合物的筛选方法。

3. 发明授权

EP2274016B1 PEGYLATED IGF-I VARIANTS FOR USE IN THE TREATMENT OF NEUROMUSCULAR DISORDERS 有权
标题翻译： PEG化的IGF-I变数使用在治疗神经肌肉疾病
公开(公告)号：EP2274016B1
公开(公告)日：2012-07-25
申请号：EP09727511.9
申请日：2009-03-24
申请人： F. Hoffmann-La Roche AG
发明人： HOLTMANN, Bettina , METZGER, Friedrich , SENDTNER, Michael
IPC分类号： A61K47/48 , A61P25/00
CPC分类号： A61K38/30 , A61K47/60 , C07K14/475
摘要： The present invention relates to the pharmaceutical use of polyethylene glycol-(PEG)ylated IGF-I variants for the treatment, prevention and/or delay of progression of neuromuscular disorders, in particular amyotrophic lateral sclerosis (ALS). More specifically, the present invention relates to the use of a PEGylated IGF-I variant for the manufacture of a pharmaceutical composition for the treatment, prevention and/or delay of neuromuscular disorders, in particular ALS wherein the PEGylated IGF-I variant is characterized in that it is derived from the wild- type human IGF-I amino acid sequence (SEQ ID NO: 1) and carries one or two amino acid alterations at amino acid positions 27, 65 and 68 so that one or two of amino acids at positions 27, 65 and 68 is/are a polar amino acid but not lysine and PEG is attached to at least one lysine residue.

4. 发明公开

EP1830889A2 CONJUGATES OF INSULIN-LIKE GROWTH FACTOR-1 (IGF-1) AND POLY(ETHYLENE GLYCOL) 有权
标题翻译： KONJUGATE VONINSULINÄHNLICHEMWACHSTUMSFAKTOR-1（IGF-1）UND POLY（ETHYLINGLYKOL）
公开(公告)号：EP1830889A2
公开(公告)日：2007-09-12
申请号：EP05849990.6
申请日：2005-12-21
申请人： F. HOFFMANN-LA ROCHE AG
发明人： AMREIN, Beat , FOSER, Stefan , LANG, Kurt , METZGER, Friedrich , REGULA, Jörg , SCHAUBMAR, Andreas , HESSE, Friederike , KUENKELE, Klaus-Peter , LANZENDOERFER,Martin
IPC分类号： A61K47/48
CPC分类号： A61K47/60 , C07K14/475 , C07K14/65
摘要： A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and one or two poly(ethylene glycol) group(s), characterized in that said IGF-I variant has an amino acid alteration at up to three amino acid positions 27, 37, 65, 68 of the wild-type IGF-I amino acid sequence so that one or two of said amino acids is/are lysine and amino acid 27 is a polar aminio acid but not lysine, is conjugated via the primary amino group(s) of said lysine(s) and said poly(ethylene glycol) group(s) have an overall molecular weight of from 20 to 100 kDa is disclosed. This conjugate is useful for the treatment of neurodegenerative disorders like Alzheimer's Disease.
摘要翻译：由胰岛素样生长因子-1（IGF-I）变体和一个或两个聚（乙二醇）基团组成的缀合物，其特征在于所述IGF-1变体在最多三个氨基酸处具有氨基酸改变野生型IGF-I氨基酸序列的酸位置27,37,65,68，使得一个或两个所述氨基酸是赖氨酸，氨基酸27是极性氨基酸而不是赖氨酸，通过所述赖氨酸和所述聚（乙二醇）基团的伯氨基具有20至100kDa的总分子量。该缀合物可用于治疗神经变性疾病如阿尔茨海默病。

5. 发明公开

EP4360707A3 COMPOSITIONS FOR TREATING SPINAL MUSCULAR ATROPHY 审中-实审
公开(公告)号：EP4360707A3
公开(公告)日：2024-08-07
申请号：EP24156739.5
申请日：2016-11-08
申请人： F. Hoffmann-La Roche AG
发明人： ALSENZ, Jochem , GRASSMANN, Olaf , KUEHL, Peter , METZGER, Friedrich , MCCARTHY, Kathleen Dorothy , MORAWSKI VIANNA, Eduardo Paulo , WOODHOUSE, Marvin Lloyd
IPC分类号： A61K9/00 , A61K31/5025 , A61K31/519 , A61K31/575 , A61K9/08 , A61K9/14 , A61P21/00 , A61P25/00 , A61P25/28 , A61P25/02
CPC分类号： A61K9/0053 , A61K9/0095 , A61K9/08 , A61K9/14 , A61K31/5025 , A61K31/575 , A61K31/519 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/28
摘要： The present invention provides pharmaceutical compositions comprising a compound of formula (I)

wherein A, R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the pharmaceutical compositions comprising a compound of formula (I) and their use as medicaments.

6. 发明授权

EP1830889B1 CONJUGATES OF INSULIN-LIKE GROWTH FACTOR-1 (IGF-1) AND POLY(ETHYLENE GLYCOL) 有权
标题翻译：胰岛素样生长因子-1（IGF-1）和聚（乙二醇）的共轭物
公开(公告)号：EP1830889B1
公开(公告)日：2017-05-17
申请号：EP05849990.6
申请日：2005-12-21
申请人： F. Hoffmann-La Roche AG
发明人： AMREIN, Beat , FOSER, Stefan , LANG, Kurt , METZGER, Friedrich , REGULA, Jörg , SCHAUBMAR, Andreas , HESSE, Friederike , KUENKELE, Klaus-Peter , LANZENDOERFER,Martin
IPC分类号： A61K47/60 , A61P25/28
CPC分类号： A61K47/60 , C07K14/475 , C07K14/65
摘要： A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and one or two poly(ethylene glycol) group(s), characterized in that said IGF-I variant has an amino acid alteration at up to three amino acid positions 27, 37, 65, 68 of the wild-type IGF-I amino acid sequence so that one or two of said amino acids is/are lysine and amino acid 27 is a polar aminio acid but not lysine, is conjugated via the primary amino group(s) of said lysine(s) and said poly(ethylene glycol) group(s) have an overall molecular weight of from 20 to 100 kDa is disclosed. This conjugate is useful for the treatment of neurodegenerative disorders like Alzheimer's Disease.
摘要翻译：由胰岛素样生长因子-1（IGF-1）变体和一个或两个聚（乙二醇）基团组成的缀合物，其特征在于所述IGF-1变体具有至多三个氨基的氨基酸改变野生型IGF-I氨基酸序列的氨基酸位置27,37,65,68使得所述氨基酸中的一个或两个氨基酸是赖氨酸且氨基酸27是极性氨基酸但不是赖氨酸通过公开了所述赖氨酸和所述聚（乙二醇）基团的一个或多个伯氨基具有20至100kDa的总分子量。该缀合物对于治疗神经退行性疾病如阿尔茨海默病是有用的。

7. 发明公开

EP2274016A2 USE OF PEGYLATED IGF-I VARIANTS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS 有权
标题翻译： PEGYLIERTE IGF-I-VARIANTEN ZUR VERWENDUNG BEI DER BEHANDLUNGNEUROMUSKULÄRERERKRANKUNGEN
公开(公告)号：EP2274016A2
公开(公告)日：2011-01-19
申请号：EP09727511.9
申请日：2009-03-24
申请人： F. Hoffmann-La Roche AG
发明人： HOLTMANN, Bettina , METZGER, Friedrich , SENDTNER, Michael
IPC分类号： A61K47/48 , A61P25/00
CPC分类号： A61K38/30 , A61K47/60 , C07K14/475
摘要： The present invention relates to the pharmaceutical use of polyethylene glycol-(PEG)ylated IGF-I variants for the treatment, prevention and/or delay of progression of neuromuscular disorders, in particular amyotrophic lateral sclerosis (ALS). More specifically, the present invention relates to the use of a PEGylated IGF-I variant for the manufacture of a pharmaceutical composition for the treatment, prevention and/or delay of neuromuscular disorders, in particular ALS wherein the PEGylated IGF-I variant is characterized in that it is derived from the wild- type human IGF-I amino acid sequence (SEQ ID NO: 1) and carries one or two amino acid alterations at amino acid positions 27, 65 and 68 so that one or two of amino acids at positions 27, 65 and 68 is/are a polar amino acid but not lysine and PEG is attached to at least one lysine residue.
摘要翻译：本发明涉及含有衍生自野生型人IGF-I氨基酸序列的聚乙二醇化IGF-1变体的药物组合物，其中位置27,65和68上的一个或两个赖氨酸氨基酸被改变为除赖氨酸以外的极性氨基酸，其中PEG连接至至少一个赖氨酸残基。本发明还涉及通过施用治疗有效量的本发明的药物组合物来治疗，预防和/或延缓神经肌肉疾病，特别是肌萎缩性侧索硬化（ALS）的进展的方法。

8. 发明授权

EP3035935B1 COMPOUNDS FOR USE IN THE PROPHYLAXIS AND TREATMENT OF CANCER 有权
公开(公告)号：EP3035935B1
公开(公告)日：2020-03-11
申请号：EP14750760.2
申请日：2014-08-15
申请人： F. Hoffmann-La Roche AG
发明人： EBELING, Martin , METZGER, Friedrich , SIVARAMAKRISHNAN, Manaswini
IPC分类号： A61K31/519 , A61P35/00

9. 发明公开

EP3374362A1 COMPOUNDS FOR TREATING AMYOTROPHIC LATERAL SCLEROSIS 审中-公开
公开(公告)号：EP3374362A1
公开(公告)日：2018-09-19
申请号：EP16798661.1
申请日：2016-11-10
申请人： F. Hoffmann-La Roche AG
发明人： MCCARTHY, Kathleen Dorothy , METZGER, Friedrich , RATNI, Hasane
IPC分类号： C07D487/04 , A61K31/5025 , A61P21/00
CPC分类号： A61K31/519 , A61P25/28 , C07D487/04
摘要： The present invention provides compounds of formula (I) (I) wherein A, R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts thereof for use in the treatment, prevention and/or delay of progression of amyotrophic lateral sclerosis (ALS). Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.

10. 发明公开

EP4360707A2 COMPOSITIONS FOR TREATING SPINAL MUSCULAR ATROPHY 审中-实审
公开(公告)号：EP4360707A2
公开(公告)日：2024-05-01
申请号：EP24156739.5
申请日：2016-11-08
申请人： F. Hoffmann-La Roche AG
发明人： ALSENZ, Jochem , GRASSMANN, Olaf , KUEHL, Peter , METZGER, Friedrich , MCCARTHY, Kathleen Dorothy , MORAWSKI VIANNA, Eduardo Paulo , WOODHOUSE, Marvin Lloyd
IPC分类号： A61P21/00
CPC分类号： A61K45/06 , A61K9/0053 , A61K9/0095 , A61K9/08 , A61K9/14 , A61K31/5025 , A61K31/575 , A61K31/519 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/28
摘要： The present invention provides pharmaceutical compositions comprising a compound of formula (I)

wherein A, R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the pharmaceutical compositions comprising a compound of formula (I) and their use as medicaments.

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