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1. 发明申请

WO1996025383A1 ANTI-INFLAMMATORY BENZOIC ACID DERIVATIVES 审中-公开
标题翻译：抗炎剂苯甲酸衍生物
公开(公告)号：WO1996025383A1
公开(公告)日：1996-08-22
申请号：PCT/US1996001997
申请日：1996-02-15
申请人： SCIOS NOVA INC.
发明人： SCIOS NOVA INC. , MEWSHAW, Richard , HAMILTON, Gregory, Scott
IPC分类号： C07C63/36
CPC分类号： C07C323/62 , C07C45/00 , C07C45/292 , C07C59/68 , C07C63/331 , C07C63/66 , C07C69/76 , C07C69/92 , C07C47/575 , C07C47/546 , C07C47/55
摘要： Novel benzoic acid derivatives have formula (I) wherein: -X- represents C1 to C6 alkylene, C2 to C6 alkenylene or a divalent moiety having the structure -(CH2)m-Z- in which m is an integer from 0 to 3 and Z represents -O-, -S- or -NH-; -Y- represents a direct bond, C1 to C6 alkylene, C2 to C6 alkenylene or a divalent moiety having the structure -(CH2)m-Z-(CH2)n in which m and n are each, independently, an integer from 0 to 3 and -Z- represents -O-, -S- or -NH-; R represents a 5- or 6-membered carbocyclic or heterocyclic ring or a carbocyclic or heterocyclic fused ring system containing up to 10 members in the ring, which carbocyclic, heterocyclic or fused ring system may be saturated or unsaturated and may contain up to two substituents selected from lower alkyl, methoxy, halo and trifluoromethyl; and R and R are each, independently, selected from hydrogen, lower alkyl, methoxy, halo and trifluoromethyl. The benzoic acid derivates are useful as anti-inflammatory agents.
摘要翻译：新颖的苯甲酸衍生物具有式（I），其中：-X-表示C1-C6亚烷基，C2-C6亚链烯基或具有结构 - （CH2）mZ-的二价部分，其中m是0-3的整数，Z代表 -O - ， - S-或-NH-; -Y-表示直接键合，C1至C6亚烷基，C2至C6亚烯基或具有 - （CH2）mZ-（CH2）n结构的二价部分，其中m和n各自独立地为0至3的整数和-Z-表示-O - ， - S-或-NH-; R表示在环中含有至多10个成员的5-或6-元碳环或杂环或碳环或杂环稠合环系，该碳环，杂环或稠环体系可以是饱和或不饱和的，并且可以含有至多两个取代基选自低级烷基，甲氧基，卤素和三氟甲基; R 1和R 2各自独立地选自氢，低级烷基，甲氧基，卤素和三氟甲基。苯甲酸衍生物可用作抗炎剂。

2. 发明申请

WO1994008607A1 NOVEL PSEUDOPEPTIDE BRADYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译：新型抗体药物BRADYKININ受体拮抗剂
公开(公告)号：WO1994008607A1
公开(公告)日：1994-04-28
申请号：PCT/US1993009130
申请日：1993-09-27
申请人： SCIOS NOVA INC.
发明人： SCIOS NOVA INC. , KYLE, Donald, James , MAVUNKEL, Babu, Joseph
IPC分类号： A61K37/02
CPC分类号： C07K7/18 , A61K38/00
摘要： The substitution of at least one of the amino acids in positions 2 to 5 of the bradykinin peptide with a fatty acid amine converts bradykinin agonists into a bradykinin antagonist. The invention further includes the intermediate compounds and additional modifications at other positions within the modified bradykinin antagonists which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected as by insect bites.
摘要翻译：将缓激肽肽的2至5位中的至少一个氨基酸与脂肪酸胺的取代将缓激肽激动剂转化为缓激肽拮抗剂。本发明进一步包括中间体化合物和改性缓激肽拮抗剂内其它位置的其它改变，其增加新的缓激肽拮抗剂的抗酶性，拮抗剂效力和/或特异性。所产生的类似物可用于治疗哺乳动物和人的疾病和疾病，其中通过昆虫叮咬产生或注射过量的缓激肽或相关激肽。

3. 发明申请

WO1996002562A1 PROCESS FOR THE PURIFICATION OF BASIC FIBROBLAST GROWTH FACTOR 审中-公开
标题翻译：碱性成纤维细胞生长因子的纯化方法
公开(公告)号：WO1996002562A1
公开(公告)日：1996-02-01
申请号：PCT/US1994008016
申请日：1994-07-18
申请人： SCIOS NOVA INC.
发明人： SCIOS NOVA INC. , SHADLE, Paula, J. , SILVERNESS, Kate, B. , KING, Robert, S.
IPC分类号： C07K01/00
CPC分类号： C07K14/503
摘要： The invention relates to a method of purifying basic fibroblast growth factor. The method involves the use of strong cation exchange chromatography followed by hydrophobic interaction chromatography and then by weak cation exchange chromatography.
摘要翻译：本发明涉及纯化碱性成纤维细胞生长因子的方法。该方法包括使用强阳离子交换层析，然后进行疏水相互作用层析，然后通过弱阳离子交换层析。

4. 发明申请

WO1993003758A1 PRODUCTION OF HOMOGENEOUS NEUROTROPHIC FACTOR 审中-公开
标题翻译：均质神经营养因子的产生
公开(公告)号：WO1993003758A1
公开(公告)日：1993-03-04
申请号：PCT/US1992007070
申请日：1992-08-21
申请人： SCIOS NOVA INC.
发明人： SCIOS NOVA INC. , HIGAKI, Jeffrey, N. , TISCHER, Edmund, G. , CORDELL, Barbara , THOMPSON, Stewart, A.
IPC分类号： A61K37/36
CPC分类号： C07K14/475 , A61K38/00
摘要： There are disclosed neurotrophic factors which are capable of being expressed as polypeptides lacking the microheterogeneity associated with a related native-sequence factor, CNTF. Also disclosed are DNA sequences encoding the neurotrophic factors and methods for expressing and recovering the factors as homogeneous polypeptides.
摘要翻译：已经公开了能够被表达为缺乏与相关天然序列因子CNTF相关的微不同性的多肽的神经营养因子。还公开了编码神经营养因子的DNA序列和用于表达和恢复因子作为均质多肽的方法。

5. 发明申请

WO1995007294A1 PSEUDO- AND NON-PEPTIDE BRADYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译： PSEUDO-非非肽类BRADYKININ受体拮抗剂
公开(公告)号：WO1995007294A1
公开(公告)日：1995-03-16
申请号：PCT/US1994010128
申请日：1994-09-09
申请人： SCIOS NOVA INC. , KYLE, Donald, James , MAVUNKEL, Babu, Joseph , LU, Zhijian
发明人： SCIOS NOVA INC.
IPC分类号： C07K07/18
CPC分类号： C07K7/18 , A61K38/00
摘要： The invention provides bradykinin antagonist compounds wherein many (or all) of the peptide bonds of bradykinin are eliminated to yield compounds which specifically compete with bradykinin for binding to the bradykinin receptor. More particularly, the invention relates to compounds having, in appropriate spatial arrangement, two positively charged moieties flanking a hydrophobic organic moiety and a moiety which mimics a beta turn conformation.
摘要翻译：本发明提供缓激肽拮抗剂化合物，其中消除缓激肽的许多（或全部）肽键，以产生与缓激肽特异性竞争结合缓激肽受体的化合物。更具体地说，本发明涉及在适当的空间排列中具有侧翼于疏水性有机部分的两个带正电荷的部分和模拟β转角构象的部分的化合物。

6. 发明申请

WO1994019372A1 CYCLIC BRADYKININ ANTAGONIST PEPTIDES 审中-公开
公开(公告)号：WO1994019372A1
公开(公告)日：1994-09-01
申请号：PCT/US1994001393
申请日：1994-02-08
申请人： SCIOS NOVA INC.
发明人： SCIOS NOVA INC. , KYLE, Donald, James , CHAKRAVARTY, Sarvajit
IPC分类号： C07K07/18
CPC分类号： C07K7/18 , A61K38/00 , Y10S930/27
摘要： Cyclic compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acid substitutions are made at positions 2 and 5 or 6 to facilitate the cyclization of the peptide through covalent bonding of the amino acid side chains. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.
摘要翻译：基于修饰的缓激肽序列的环化合物是有效的缓激肽受体拮抗剂。在位置2和5或6进行氨基酸取代，以促进肽通过氨基酸侧链的共价结合而环化。所产生的类似物可用于治疗其中产生或注射过量的缓激肽或相关激肽的哺乳动物和人的病症和疾病，例如通过昆虫叮咬。

7. 发明申请

WO1993011764A1 FLUORENYL DERIVATIVES AND THEIR USE AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：氟代衍生物及其作为抗炎剂的用途
公开(公告)号：WO1993011764A1
公开(公告)日：1993-06-24
申请号：PCT/US1992010487
申请日：1992-12-10
申请人： SCIOS NOVA INC.
发明人： SCIOS NOVA INC. , PERUMATTAM, John, Joseph
IPC分类号： A61K31/41
CPC分类号： C07D257/04 , C07C271/28 , C07C311/51 , C07C2603/18
摘要： The compound having formula (I) and a method of treating an inflammatory condition comprising administering to an animal in need of such treatment an effective amount of at least one compound represented by the formula.
摘要翻译：具有式（I）的化合物和治疗炎性病症的方法包括向需要这种治疗的动物施用有效量的至少一种由式表示的化合物。

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