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1. 发明申请

WO1993008211A1 TRIPEPTIDE DERIVATIVE ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译： TRIPEPTIDE衍生抗炎剂
公开(公告)号：WO1993008211A1
公开(公告)日：1993-04-29
申请号：PCT/US1992008901
申请日：1992-10-19
申请人： THE PROCTER & GAMBLE COMPANY
发明人： THE PROCTER & GAMBLE COMPANY , McIVER, John, McMillan
IPC分类号： C07K05/06
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086
摘要： The subject invention involves anti-inflammatory compounds having structure (1), wherein (a) n is an integer of from 0 to about 2; (b) -R is selected from straight or branched alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to about 6 carbon atoms; and cyclic alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 13 carbon atoms; and the carbon atom to which -R is bonded is in either D or L configuration; (c) -R' is selected from branched alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 6 carbon atoms; cyclic alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 13 carbon atoms; and arylalkyl, the alleyl portion being saturated and having from 1 to about 3 carbon atoms; and the carbon atom to which -R' is bonded is in L configuration; (d) -R'' is -(CH2)m-A-NH2 or -(CH2)m-A-B-C(NH2)=NH, wherein m is an integer of from 1 to about 5; -A- is a covalent bond, or p-phenyl or p-cyclohexyl; and -B- is a covalent bond or -NH-; and the carbon atom to which -R'' is bonded is in L configuration; (e) -Y is hydrogen or trifluoromethyl; (f) -Z- is -O- or -NH-; (g) -V- is selected from -OC(O)-, -N(Q)C(O)-, -N(Q)C(S)-, -C(O)-, -SO2- and -P(O)(OH)-; when -V- is -OC(O)-, -Z- is -NH-; (h) -X is selected from the group consisting of cyclic alkyl, branched alkyl having at least two branches, and aryl, each having from 5 to about 20 carbon atoms; and (i) -Q is selected from the group consisting of hydrogen; and straight or branched chain alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to about 6 carbon atoms; or -Q and -X are covalently linked forming a cyclic moiety which includes the nitrogen to which -Q is bonded and from 5 to about 20 carbon atoms. The subject invention also involves pharmaceutical compositions comprising the above compounds, and methods for treating inflammation or pain using such compounds and compositions.
摘要翻译：本发明涉及具有结构（1）的抗炎化合物，其中（a）n为0至约2的整数; （b）-R选自具有1至约6个碳原子的具有1或2个双键的饱和或不饱和的直链或支链烷基; 具有3至约13个碳原子的具有1或2个双键的饱和或不饱和环状烷基; R结合的碳原子为D或L构型; （c）-R'选自具有3至约6个碳原子的具有1或2个双键的饱和或不饱和的支链烷基; 具有3至约13个碳原子的具有1或2个双键的饱和或不饱和环状烷基; 和芳基烷基，所述烷基部分是饱和的且具有1至约3个碳原子; 且R'键合的碳原子为L构型; （d）-R“是 - （CH 2）m -A-NH 2或 - （CH 2）m -A-B-C（NH 2）= NH，其中m是1至约5的整数; -A-是共价键，或对 - 苯基或对 - 环己基; 和-B-是共价键或-NH-; 并且与R“结合的碳原子为L构型; （e）-Y是氢或三氟甲基; （f）-Z-是-O-或-NH-; （O） - ， - N（Q）C（O） - ， - N（Q）C（S） - ， - （O） - ， - SO 2 - 呸）-; 当-V-为-OC（O） - 时，-Z-为-NH-; （h）-X选自具有至少两个分支的环烷基，支链烷基和具有5至约20个碳原子的芳基; 和（i）-Q选自氢; 和具有1至约6个碳原子的具有1或2个双键的饱和或不饱和的直链或支链烷基; 或-Q和-X共价连接形成环状部分，其包括与Q键合的氮和5至约20个碳原子。本发明还涉及包含上述化合物的药物组合物，以及使用这些化合物和组合物治疗炎症或疼痛的方法。

2. 发明公开

EP0929639A1 LIQUID DETERGENTS CONTAINING PROTEOLYTIC ENZYME, PEPTIDE ALDEHYDE AND CALCIUM IONS 失效
标题翻译：液体清洁剂，蛋白水解酶，其肽和钙离子CONTAIN
公开(公告)号：EP0929639A1
公开(公告)日：1999-07-21
申请号：EP97942579.0
申请日：1997-09-19
申请人： THE PROCTER & GAMBLE COMPANY
发明人： McIVER, John, McMillan , HUBER, Alan, Carl , McKILLOP, Kirsten, Louise , SMITH, Laurence, Anthony
IPC分类号： C11D17 , C11D3
CPC分类号： C11D3/38663
摘要： Aqueous liquid detergent compositions are described which comprise a proteolytic enzyme wherein the proteolytic activity is reversibly inhibited by a peptide aldehyde and calcium. More specifically, liquid detergent compositions are disclosed which contain a detersive surfactant, a proteolytic enzyme, a peptide aldehyde, and calcium ions. The combination of peptide aldehyde and calcium ions acts to provide synergistic protease inhibitor benefits.

3. 发明公开

EP0929642A1 LIQUID LAUNDRY DETERGENT COMPOSITIONS CONTAINING PROTEOLYTIC ENZYME AND PROTEASE INHIBITORS 失效
标题翻译：液体洗涤剂蛋白分解酶和蛋白酶抑制剂含
公开(公告)号：EP0929642A1
公开(公告)日：1999-07-21
申请号：EP97943377.0
申请日：1997-09-19
申请人： THE PROCTER & GAMBLE COMPANY
发明人： McIVER, John, McMillan , HUBER, Alan, Carl , SAUNDERS, Charles, Winston , SMITH, Laurence, Anthony
IPC分类号： C11D17 , C11D3
CPC分类号： C11D3/38663
摘要： Aqueous liquid detergent compositions are described which comprise a detersive surfactant, a proteolytic enzyme, and a protease inhibitor selected from the group consisting of proteins, peptides and peptide derivatives, such as peptide aldehydes and peptide trifluromethyl ketones, wherein the protease activity in the laundry detergent composition is less than 1 % of the activity without the protease inhibitor, and the ratio of the percent of free protease in the wash to the percent of free protease in the laundry detergent composition is greater than about 100, preferably greater than about 200, and more preferably greater than about 400.

4. 发明公开

EP0929640A1 LIQUID DETERGENTS CONTAINING PROTEOLYTIC ENZYME AND PROTEASE INHIBITORS 失效
标题翻译：液体洗涤剂蛋白分解酶和蛋白酶抑制剂含
公开(公告)号：EP0929640A1
公开(公告)日：1999-07-21
申请号：EP97942580.0
申请日：1997-09-19
申请人： THE PROCTER & GAMBLE COMPANY
发明人： McIVER, John, McMillan , HUBER, Alan, Carl , McKILLOP, Kristen, Louise
IPC分类号： C12N9 , C07K5 , C11D3 , C11D17
CPC分类号： C11D3/38663 , C07K5/06052 , C07K5/06191 , C07K5/0812 , C07K5/0827 , C11D3/26 , C11D3/32 , C11D3/349 , C11D3/364 , C11D3/368
摘要： Aqueous liquid detergent compositions are described which comprise a proteolytic enzyme wherein the proteolytic activity is reversibly inhibited by a peptide protease inhibitor selected from the group consisting of aldhehydes and trifluoromethyl ketones.

5. 发明公开

EP1061963A1 PROTEASE INHIBITORS IN ABSORBENT ARTICLES 有权
标题翻译：蛋白酶抑制剂用于吸水垫
公开(公告)号：EP1061963A1
公开(公告)日：2000-12-27
申请号：EP99912419.1
申请日：1999-03-11
申请人： THE PROCTER & GAMBLE COMPANY
发明人： ROURKE, Francis, James , OSBORNE, Scott, Edward , ROE, Donald, Carroll , UNDERINER, Todd, Laurence , McIVER, John, McMillan , BATES, Timothy
IPC分类号： A61L15/44
CPC分类号： A61B5/441 , A61L15/44 , A61L2300/434
摘要： The invention provides an absorbent article, at least a portion of which has a protease inhibitor incorporated therein to decrease the activity of fecal proteases that may otherwise initiate or contribute to inflammation of the skin of a wearer of the article resulting in diaper rash or diaper dermatitis. Preferably the article further comprises a delivery system for releasably containing and delivering the protease inhibitor to at least a portion of the skin of the wearer. More preferably, the delivery system comprises a skin care composition and at least a portion of the composition, including the protease inhibitor, is automatically transferred from the article to the wearer's skin without manual intervention during normal usage of the article to form a defense against fecal proteases at the skin-feces interface. Most preferably, repeated application of similarly treated articles to the wearer's skin provides an available source from which the protease inhibitor continuously transfers onto the skin over time and accumulatesto provide a proactive defense against fecal proteases for the reduction or prevention of diaper dermatitis due to proteolytic enzymes.

6. 发明公开

EP0929636A1 LIQUID DETERGENTS CONTAINING PROTEOLYTIC ENZYME, PEPTIDE ALDEHYDE AND A SOURCE OF BORIC ACID 失效
标题翻译：液体清洁剂，蛋白水解酶肽和BORSÄUREQUELLECONTAIN
公开(公告)号：EP0929636A1
公开(公告)日：1999-07-21
申请号：EP97941697.0
申请日：1997-09-19
申请人： THE PROCTER & GAMBLE COMPANY
发明人： McIVER, John, McMillan , HUBER, Alan, Carl , McKILLOP, Kirsten, Louise , SMITH, Laurence, Anthony
IPC分类号： C12N9 , C11D3 , C11D17
CPC分类号： C11D3/38663 , C11D3/38618
摘要： Aqueous liquid detergent compositions are described which comprise a proteolytic enzyme wherein the proteolytic activity is reversibly inhibited by a peptide aldehyde and a source of boric acid. In a particularly preferred embodiment, liquid detergent compositions are disclosed which contain a detersive surfactant, a proteolytic enzyme, a peptide aldehyde, boric acid, and diol ions. The combination of peptide aldehyde and boric acid act to provide improved stability of protease and other enzymes.

7. 发明授权

EP0929639B1 LIQUID DETERGENTS CONTAINING PROTEOLYTIC ENZYME, PEPTIDE ALDEHYDE AND CALCIUM IONS 失效
标题翻译：液体清洁剂，蛋白水解酶，其肽和钙离子CONTAIN
公开(公告)号：EP0929639B1
公开(公告)日：2002-11-13
申请号：EP97942579.0
申请日：1997-09-19
申请人： THE PROCTER & GAMBLE COMPANY
发明人： McIVER, John, McMillan , HUBER, Alan, Carl , McKILLOP, Kirsten, Louise , SMITH, Laurence, Anthony
IPC分类号： C11D3/386
CPC分类号： C11D3/38663

8. 发明公开

EP1117640A1 HETEROCYCLIC 2-SUBSTITUTED KETOAMIDES USEFUL FOR TREATING HAIR LOSS IN MAMMALS 审中-公开
标题翻译：杂环取代的2-酮酰胺FOR脱发治疗哺乳动物
公开(公告)号：EP1117640A1
公开(公告)日：2001-07-25
申请号：EP99949856.1
申请日：1999-09-24
申请人： THE PROCTER & GAMBLE COMPANY
发明人： McIVER, John, McMillan , DEGENHARDT, Charles, Raymond , EICKHOFF, David, Joseph
IPC分类号： C07D207/16 , C07D211/60 , C07D217/26 , A61K7/06 , A61K31/401 , A61K31/445 , A61K31/472
CPC分类号： A61Q7/00 , A61K8/41 , A61K8/4913 , A61K8/4926
摘要： The present disclosure describes novel compounds (formula (I)), wherein W is selected from nil, hydrogen, and lower alkyl; A is selected from nil and alkyl; X and Y are each, independently, selected from C(O), P(O), N, O and S, wherein: (i) when X is C(O) then R3 is nil and Y is selected from N, O, and S, (ii) when X is P(O) then R3 is nil and Y is selected from the group consisting of N and O; (iii) when X is N then R3 is selected from hydrogen, alkyl, and arylalkyl, Y is C(O), and R2 is nil; (iv) when X is O then R3 is nil, Y is C(O), and R2 is nil; and (v) when X is S then R3 is nil, Y is C(O), and R2 is nil; and wherein the substitutents R1 to R10 are defined herein, and compositions which are particularly useful for treating hair loss in mammals, including arresting and/or reversing hair loss and promoting hair growth. The present compounds and compositions may also be useful against a variety of disorders including, for example, multi-drug resistance, human immunodeficiency virus (HIV), cardiac injury, and neurological disorders, and may be useful for controlling parasites and invoking immunosuppression.

9. 发明公开

EP1062264A2 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：EP1062264A2
公开(公告)日：2000-12-27
申请号：EP99909957.5
申请日：1999-03-11
申请人： THE PROCTER & GAMBLE COMPANY
发明人： McIVER, John, McMillan , UNDERINER, Todd, Laurence , BATES, Timothy
IPC分类号： C08G65/48 , A61K31/155 , C07C279/18 , C07C257/18 , C07C257/14 , A61K31/77
CPC分类号： C08G65/333 , A61K8/0208 , A61K8/0216 , A61K8/86 , A61K31/155 , A61K31/77 , A61K2800/92 , A61Q19/00 , C07C257/14 , C07C257/18 , C07C279/18 , C08G65/3326 , Y10S514/844 , Y10S514/846
摘要： The present invention relates to compounds, compositions, and methods which are useful for the prevention and treatment of adverse health, skin, hair, and oral conditions. The compounds, compositions, and methods are also widely applicable for use in health, skin, hair, oral, beauty, and personal care applications. In particular, the present invention relates to compounds having structure (1): and the tautomers, acceptable salts, and biohydrolyzable amides, esters, and imides thereof, wherein A, Q, n, P, L1, L2, L3, L4, Z, X, B1 and B2 are defined herein.

10. 发明授权

EP1061963B1 PROTEASE INHIBITORS IN ABSORBENT ARTICLES 有权
标题翻译：蛋白酶抑制剂的吸收性文章
公开(公告)号：EP1061963B1
公开(公告)日：2003-05-07
申请号：EP99912419.1
申请日：1999-03-11
申请人： THE PROCTER & GAMBLE COMPANY
发明人： ROURKE, Francis, James , OSBORNE, Scott, Edward , ROE, Donald, Carroll , UNDERINER, Todd, Laurence , McIVER, John, McMillan , BATES, Timothy
IPC分类号： A61L15/44
CPC分类号： A61B5/441 , A61L15/44 , A61L2300/434

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