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1. 发明申请

US20170368190A1 Hydrophobic Core Carrier Compositions for Delivery of Therapeutic Agents, Methods of Making and Using the Same 审中-公开
公开(公告)号：US20170368190A1
公开(公告)日：2017-12-28
申请号：US15672802
申请日：2017-08-09
申请人： PharmaIN Corporation
发明人： Gerardo M. Castillo , Elijah M. Bolotin
IPC分类号： A61K47/60 , A61K38/22 , A61K47/64 , A61K47/69 , A61K31/4439 , A61K38/26 , A61K38/18
CPC分类号： A61K47/6907 , A61K31/4439 , A61K38/1808 , A61K38/1841 , A61K38/2207 , A61K38/26 , A61K47/60 , A61K47/645
摘要： The present invention relates, in part, to a biocompatible hydrophobic-core carrier comprising a carrier, and a plurality of hydrophobic groups covalently linked to the polymeric carrier. The hydrophobic groups are capable of dissociably linking load molecules such as therapeutic agents. The hydrophobic-core carrier may also comprise protective side chains, orienting molecules, and targeting molecules.

2. 发明申请

US20200254100A1 ANIONIC-CORE COMPOSITION FOR DELIVERY OF THERAPEUTIC AGENTS, AND METHODS OF MAKING AND USING THE SAME 审中-公开
公开(公告)号：US20200254100A1
公开(公告)日：2020-08-13
申请号：US16829843
申请日：2020-03-25
申请人： PharmaIN Corporation
发明人： Gerardo M. Castillo , Elijah M. Bolotin , Akiko Nashimoto-Ashfield
IPC分类号： A61K47/34 , A61K47/64 , A61K47/61 , A61K47/58 , A61K9/14
摘要： The present invention is directed to compositions comprising a polymer backbone with protective chain and anionic groups, and a cationic therapeutic agent. The present invention is directed to compositions for treating infections, inflammatory diseases, excess growth, and damaged cells and organs.

3. 发明申请

US20180280516A1 ANIONIC-CORE COMPOSITION FOR DELIVERY OF THERAPEUTIC AGENTS, AND METHODS OF MAKING AND USING THE SAME 审中-公开
公开(公告)号：US20180280516A1
公开(公告)日：2018-10-04
申请号：US16009132
申请日：2018-06-14
申请人： PharmaIN Corporation
发明人： Gerardo Castillo , Elijah M. Bolotin , Akiko Nashimoto-Ashfield
IPC分类号： A61K47/34 , A61K9/14 , A61K47/64 , A61K47/61 , A61K47/58
摘要： The present invention is directed to compositions comprising a polymer backbone with protective chain and anionic groups, and a cationic therapeutic agent. The present invention is directed to compositions for treating infections, inflammatory diseases, excess growth, and damaged cells and organs.

4. 发明授权

US09090664B2 Composition for long-acting peptide analogs 有权
标题翻译：长效肽类似物的组成
公开(公告)号：US09090664B2
公开(公告)日：2015-07-28
申请号：US13952411
申请日：2013-07-26
申请人： PharmaIn Corporation
发明人： Gerardo M. Castillo , Elijah M. Bolotin
IPC分类号： A61K47/48 , C07K7/16 , A61K38/00
CPC分类号： C07K14/57563 , A61K38/00 , A61K47/542 , C07K7/16 , C07K14/485 , C07K14/575
摘要： The invention describes compositions of peptide analogs that are active in blood or cleavable in blood to release an active peptide. The peptide analogs have a general formula: A-(Cm)x-Peptide (SEQ ID NO: 76), wherein A is hydrophobic moiety or a metal binding moiety, e.g., a chemical group or moiety containing 1) an alkyl group having 6 to 36 carbon units, 2) a nitrilotriacetic acid group, 3) an imidodiacetic acid group, or 4) a moiety of formula (ZyHisw)p (SEQ ID NO: 50), wherein Z is any amino acid residue other than histidine, His is histidine, y is an integer from 0-6; w is an integer from 1-6; and p is an integer from 1-6; wherein if A has alkyl group with 6 to 36 carbon units x is greater than 0; and Cm is a cleavable moiety consisting of glycine or alanine or lysine or arginine or N-Arginine or N-lysine, wherein x is an integer between 0-6 and N may be any amino acid or none. The peptide analogs are complexed with polymeric carrier to provide enhanced half-life.
摘要翻译：本发明描述了在血液中有活性的或可裂解的血液中释放活性肽的肽类似物的组合物。肽类似物具有以下通式：A-（Cm）x-肽（SEQ ID NO：76），其中A是疏水部分或金属结合部分，例如化学基团或部分，其含有1）具有6个至36个碳单元，2）次氮基三乙酸基团，3）亚氨基二乙酸基团，或4）式（ZyHisw）p（SEQ ID NO：50）的部分，其中Z是组氨酸以外的任何氨基酸残基，His 是组氨酸，y是0-6的整数; w是1-6的整数; p为1-6的整数; 其中如果A具有6至36个碳单元的烷基，x大于0; 和Cm是由甘氨酸或丙氨酸或赖氨酸或精氨酸或N-精氨酸或N-赖氨酸组成的可切割部分，其中x是0-6之间的整数，N可以是任何氨基酸或没有氨基酸。肽类似物与聚合物载体复合以提供增强的半衰期。

5. 发明申请

US20140051628A1 COMPOSITION FOR LONG-ACTING PEPTIDE ANALOGS 有权
标题翻译：用于长效肽模拟物的组合物
公开(公告)号：US20140051628A1
公开(公告)日：2014-02-20
申请号：US13952411
申请日：2013-07-26
申请人： PharmaIn Corporation
发明人： Gerardo M. Castillo , Elijah M. Bolotin
IPC分类号： C07K7/16
CPC分类号： C07K14/57563 , A61K38/00 , A61K47/542 , C07K7/16 , C07K14/485 , C07K14/575
摘要： The invention describes compositions of peptide analogs that are active in blood or cleavable in blood to release an active peptide. The peptide analogs have a general formula: A-(Cm)x-Peptide (SEQ ID NO: 76), wherein A is hydrophobic moiety or a metal binding moiety, e.g., a chemical group or moiety containing 1) an alkyl group having 6 to 36 carbon units, 2) a nitrilotriacetic acid group, 3) an imidodiacetic acid group, or 4) a moiety of formula (ZyHisw)p (SEQ ID NO: 50), wherein Z is any amino acid residue other than histidine, His is histidine, y is an integer from 0-6; w is an integer from 1-6; and p is an integer from 1-6; wherein if A has alkyl group with 6 to 36 carbon units x is greater than 0; and Cm is a cleavable moiety consisting of glycine or alanine or lysine or arginine or N-Arginine or N-lysine, wherein x is an integer between 0-6 and N may be any amino acid or none. The peptide analogs are complexed with polymeric carrier to provide enhanced half-life.
摘要翻译：本发明描述了在血液中有活性的或可裂解的血液中释放活性肽的肽类似物的组合物。肽类似物具有以下通式：A-（Cm）x-肽（SEQ ID NO：76），其中A是疏水部分或金属结合部分，例如化学基团或部分，其含有1）具有6个至36个碳单元，2）次氮基三乙酸基团，3）亚氨基二乙酸基团，或4）式（ZyHisw）p（SEQ ID NO：50）的部分，其中Z是组氨酸以外的任何氨基酸残基，His 是组氨酸，y是0-6的整数; w是1-6的整数; p为1-6的整数; 其中如果A具有6至36个碳单元的烷基，x大于0; 和Cm是由甘氨酸或丙氨酸或赖氨酸或精氨酸或N-精氨酸或N-赖氨酸组成的可切割部分，其中x是0-6之间的整数，N可以是任何氨基酸或没有氨基酸。肽类似物与聚合物载体复合以提供增强的半衰期。

6. 发明申请

US20200017567A1 NPRA AGONISTS, COMPOSITIONS, AND USES THEREOF 审中-公开
公开(公告)号：US20200017567A1
公开(公告)日：2020-01-16
申请号：US16577947
申请日：2019-09-20
申请人： PharmaIn Corporation
发明人： Gerardo M. Castillo , Akiko Nishimoto-Ashfield , Elijah M. Bolotin
IPC分类号： C07K14/575 , A61P9/00 , A61K47/54
摘要： This disclosure provides a natriuretic peptide derivative of Formula (I), and to compositions including a natriuretic peptide derivative of Formula (I), (fatty acyl)z-(B)x-(G)y-NP (I), wherein: z is 1, x is an integer from 2 to 4 and y is 3; or z is 0, x is an integer from 0 to 4 and y is an integer from 1 to 3; fatty acyl comprises from 12 to 24 (e.g., 12 to 18) carbons atoms; B is lysine or arginine; G is glycine; NP is a natriuretic peptide; if present, (fatty acyl)z- is covalently linked to the N-terminus of (B)x; (fatty acyl)z-(B)x- is covalently linked to the N-terminus of (G)y; and (fatty acyl)z-(B)x-(G)y- is covalently linked to the N-terminus of NP. The natriuretic peptide derivative according to the disclosure, and compositions thereof, are useful in the treatment of diseases such as hypertension, vascular congestion, and heart disease.

7. 发明授权

US10507248B2 Hydrophobic core carrier compositions for delivery of therapeutic agents, methods of making and using the same 有权
公开(公告)号：US10507248B2
公开(公告)日：2019-12-17
申请号：US15672802
申请日：2017-08-09
申请人： PharmaIn Corporation
发明人： Gerardo M. Castillo , Elijah M. Bolotin
IPC分类号： A61K38/00 , A61K38/18 , A61K47/30 , A61K47/69 , A61K47/64 , A61K38/22 , A61K38/26 , A61K31/4439 , A61K47/60
摘要： The present invention relates, in part, to a biocompatible hydrophobic-core carrier comprising a carrier, and a plurality of hydrophobic groups covalently linked to the polymeric carrier. The hydrophobic groups are capable of dissociably linking load molecules such as therapeutic agents. The hydrophobic-core carrier may also comprise protective side chains, orienting molecules, and targeting molecules.

8. 发明授权

US09737615B2 Hydrophobic core carrier compositions for delivery of therapeutic agents, methods of making and using the same 有权
公开(公告)号：US09737615B2
公开(公告)日：2017-08-22
申请号：US14087523
申请日：2013-11-22
申请人： PharmaIN Corporation
发明人： Gerardo M. Castillo , Elijah M. Bolotin
IPC分类号： A61K38/00 , A61K38/22 , A61K38/26 , A61K47/48 , A61K38/18 , A61K31/4439
CPC分类号： A61K47/6907 , A61K31/4439 , A61K38/1808 , A61K38/1841 , A61K38/2207 , A61K38/26 , A61K47/60 , A61K47/645
摘要： The present invention relates, in part, to a biocompatible hydrophobic-core carrier comprising a carrier, and a plurality of hydrophobic groups covalently linked to the polymeric carrier. The hydrophobic groups are capable of dissociably linking load molecules such as therapeutic agents. The hydrophobic-core carrier may also comprise protective side chains, orienting molecules, and targeting molecules.

9. 发明申请

US20140154203A1 Hydrophobic Core Carrier Compositions for Delivery of Therapeutic Agents, Methods of Making and Using The Same 审中-公开
标题翻译：用于递送治疗剂的疏水性核心载体组合物，制备和使用它们的方法
公开(公告)号：US20140154203A1
公开(公告)日：2014-06-05
申请号：US14087523
申请日：2013-11-22
申请人： PharmaIN Corporation
发明人： Gerardo M. Castillo , Elijah M. Bolotin
IPC分类号： A61K47/48 , A61K38/26 , A61K31/4439
CPC分类号： A61K47/6907 , A61K31/4439 , A61K38/1808 , A61K38/1841 , A61K38/2207 , A61K38/26 , A61K47/60 , A61K47/645
摘要： The present invention relates, in part, to a biocompatible hydrophobic-core carrier comprising a carrier, and a plurality of hydrophobic groups covalently linked to the polymeric carrier. The hydrophobic groups are capable of dissociably linking load molecules such as therapeutic agents. The hydrophobic-core carrier may also comprise protective side chains, orienting molecules, and targeting molecules.
摘要翻译：本发明部分涉及包含载体和与聚合物载体共价连接的多个疏水基团的生物相容的疏水性核心载体。疏水基团能够解离地连接载体分子例如治疗剂。疏水核心载体还可以包含保护性侧链，取向分子和靶向分子。

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