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1. 发明申请

WO1997005133A1 PRODRUGS OF 4-[3-(TRANS-3-DIMETHYLAMINOCYCLOBUTYL)-1H-INDOL-5-YL-METHYL]-4(S)OXAZOLIDIN-2-ONE, THEIR PREPARATION AND THEIR USE AS 5HT1-LIKE RECEPTOR AGONISTS 审中-公开
标题翻译： 4- [3-（反式-3-二甲基氨基环己基）-1H-吲哚-5-基甲基] -4（S）氧杂环丁烷-2-酮的制备及其作为5HT1样受体激动剂的制备及其用途
公开(公告)号：WO1997005133A1
公开(公告)日：1997-02-13
申请号：PCT/EP1996003251
申请日：1996-07-24
申请人： GLAXO GROUP LIMITED , SELWOOD, David, Lawrence , BLADE, Robert, John
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention provides compounds of formula (I), wherein A is a C1-6alkyl, -O-C1-6alkyl, -O-phenyl or phenyl group and may optionally be substituted by one or more substituents selected from C1-3alkyl and halogen. These compounds act as prodrugs of 4-[3-( trans -5-dimethylaminocyclobutyl)-1H-indol-5-yl-methyl]-4(S)oxazolidin-2-one. The invention is also concerned with use of compounds of formula (I) in medicine, particularly as "5HT1-like" receptor agonists for prophylaxis and treatment of migraine, pharmaceutical compounds containing them and processes for their preparation.
摘要翻译：本发明提供式（I）化合物，其中A为C 1-6烷基，-O-C 1-6烷基，-O-苯基或苯基，并且可任选被一个或多个选自C 1-3烷基和卤素的取代基取代。这些化合物作为4- [3-（反式-5-二甲基氨基环丁基）-1H-吲哚-5-基 - 甲基] -4（S）恶唑烷-2-酮的前药。本发明还涉及式（I）化合物在药物中的用途，特别是用作预防和治疗偏头痛的“5HT1样”受体激动剂，含有它们的药物化合物及其制备方法。

2. 发明申请

WO1995032966A1 INDOLE DERIVATIVES AS PRODRUGS OF 5-HT1-LIKE RECEPTOR AGONISTS 审中-公开
标题翻译：作为5-HT1样受体激动剂的单克隆抗体衍生物
公开(公告)号：WO1995032966A1
公开(公告)日：1995-12-07
申请号：PCT/GB1995001249
申请日：1995-05-31
申请人： THE WELLCOME FOUNDATION LIMITED , BLADE, Robert, John , PANG, Yih, Sang , SELWOOD, David, Lawrence
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： A compound of formula (I), wherein A is C1-6alkyl, -O-C1-6alkyl, -O-phenyl or phenyl, optionally substituted by C1-3alkyl or halogen; n is an integer of from 0 to 3; W is a group of formula (i), (ii) or (iii) wherein R is hydrogen or C1-4alkyl, x is -O-, -S-, -NH-, or -CH2-, Y is oxygen or sulphur and the chiral centre * in formula (i) or (ii) is in its (S) or (R) form or is a mixture thereof in any proportions; and Z is a group of formula (iv) -CH2CH2NR R , (v) or (vi) wherein R and R are independently selected from hydrogen and C1-4alkyl and R is hydrogen or C1-4alkyl; and salts, solvates and physiologically functional derivatives thereof.
摘要翻译：式（I）的化合物，其中A为C1-6烷基，-O-C1-6烷基，-O-苯基或苯基，任选被C 1-3烷基或卤素取代; n为0〜3的整数， W是式（ⅰ），（ⅱ）或（ⅲ）的基团，其中R是氢或C 1-4烷基，x是-O - ， - S - ， - NH-或-CH 2 - ，Y是氧或硫式（i）或（ii）中的手性中心*为其（S）或（R）形式，或其为任何比例的混合物; 并且Z是式（ⅳ）-CH 2 CH 2 NR R 2，（ⅴ）或（vi）的基团，其中R 1和R 2独立地选自氢和C 1-4烷基，R 3 >是氢或C 1-4烷基; 及其盐，溶剂合物及其生理功能衍生物。

3. 发明申请

WO2006051314A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2006051314A2
公开(公告)日：2006-05-18
申请号：PCT/GB2005004361
申请日：2005-11-11
申请人： UCL BIOMEDICA PLC , VALLANCE PATRICK JOHN THOMPSON , LEIPER JAMES MITCHELL , SELWOOD DAVID LAWRENCE , ROSSITER SHARON , HARTZOULAKIS BASIL
发明人： VALLANCE PATRICK JOHN THOMPSON , LEIPER JAMES MITCHELL , SELWOOD DAVID LAWRENCE , ROSSITER SHARON , HARTZOULAKIS BASIL
IPC分类号： C07C279/14 , A61K31/16 , A61K31/198 , A61K31/223 , A61K31/40 , A61K31/445 , A61K31/5375 , A61P9/10 , A61P11/06 , A61P19/02 , C07C279/16 , C07C279/18 , C07C323/52 , C07D295/215
CPC分类号： C07C279/14 , A61K31/16 , A61K31/198 , A61K31/223 , A61K31/40 , A61K31/445 , A61K31/4453 , A61K31/5375 , C07C279/16 , C07C279/18 , C07C323/44 , C07C2601/02 , C07D295/215 , C07D295/32
摘要： Compounds of formula (I) have been found to be useful as inhibitors of DDAH use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the treatment of a disease whose pathology is affected by DDAH formula (I) wherein: either - (a) R 1 is C 3 -C 12 alkyl, C 3 -C 12 alkenyl, C 3 -C 12 alkynyl, C 6 -C 10 aryl, C 3 -C 8 carbocyclyl, 5- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, -L-A, -L-Het-L', -L-Y-L', -L-Het-A or -L-Y-A, wherein: L is C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; L' is C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; A is C 6 -C 10 aryl, C 3 -C 8 carbocyclyl, 5- to 10-membered heterocyclyl or 5- to 10-membered heteroaryl; Het is -O-, -S- or -NR'-, wherein R' is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl; and Y is -CO-, -SO-, -SO 2 -, -CO-O-, -CO-NR'-, -O-CO- or -NR'-CO-, wherein R' is as defined above; - R 2 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; and - R 3 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl, - or (b) R 1 and R 2 form, together with the nitrogen to which they are attached, a 5- to 10-membered heterocyclic or heteroaryl ring, and R 3 is as defined above, - or (c) R 1 and R 3 form, together with the -N-C=N- moiety to which they are attached, a 5- to 10-membered heterocyclic or heteroaryl ring, and R 2 is as defined above; - R 4 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; B is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, -O-L-, -S-L- or-L-Het-L'-, wherein L, L' and Het are as defined above; - X is -O-, -S- or -NR'-, wherein R' is as defined above; -R 5 is hydrogen, C 1 -C 6 alkyl, C 2 - 6 alkenyl, C 2 -C 6 alkynyl, aryl, C 3 -C 8 carbocyclyl, 5- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, -L-A, -L-Het-L', -L-Y-L', -L-Het-A, -L-Y-A, -L-A-Het-A, -L-A-L'-A or -L-A-Het-L'-A, wherein L, L', Het and Y are as defined above and wherein each A is the same or different and is as defined above; -R 6 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; - R 7 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl, or R 7 is a bond, a C 1 -C 4 alkyl or C 2 -C 4 alkenyl moiety which is joined to one of the carbon atoms of B to form, together with the -N-C- moiety to which R 7 and B are attached, a 5- to 10-membered heterocyclic ring; and - R 8 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl.
摘要翻译：已经发现式（I）化合物可用作DDAH抑制剂用于式（I）化合物或其药学上可接受的盐在制备用于治疗病症为受DDAH式（I）影响，其中： - （a）R 1是C 3 -C 12烷基，C 3 C 12 - 12链烯基，C 3 -C 12炔基，C 6-C≡N C 10 -C 10芳基，C 3 -C 8碳环基，5至10元杂环基，5至10元杂芳基，-LA，-L -Het-L'，-LY-L'，-L-Het-A或-LYA，其中：L为C 1 -C 6烷基，C _{如上所定义; R 4是氢，C 1 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，烯基或C 2 -C 6 - 炔基; B是C 1 -C 6烷基，C 2 -C 6链烯基，-OL-，-SL - 或-L-Het-L'-，其中L，L'和Het如上所定义; -X是-O - ， - S-或-NR'-，其中R'如上定义; R 5是氢，C 1 -C 6烷基，C 2 -C 6 - 亚烷基，C 2 -C 6炔基，芳基，C 3 -C 8碳环基，5- 至10元杂环基，5至10元杂芳基，-LA，-L-Het-L'，-LY-L'，-L-Het-A，-LYA，-LA-Het-A，-LA -L'-A或-LA-Het-L'-A，其中L，L'，Het和Y如上所定义，并且其中每个A相同或不同，如上所定义; R 6是氢，C 1 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烯基或C 2 -C 6 - 炔基; R 7是氢，C 1 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 12烷基或C 2 -C 6 - 炔基，或R 7是键，C 1〜 -C 4烷基或C 2 -C 4亚烷基部分，其与B的一个碳原子连接形成，与 R 7和B连接的-NC-部分，5至10元杂环; 和 - R 8是氢，C 1 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烯基或C 2 -C 6炔基。}

4. 发明申请

WO2006051314A8 GUANIDINE DERIVATIVES AS INHIBITORS OF DDAH 审中-公开
标题翻译：作为DDAH的抑制剂的胍衍生物
公开(公告)号：WO2006051314A8
公开(公告)日：2006-09-28
申请号：PCT/GB2005004361
申请日：2005-11-11
申请人： UCL BIOMEDICA PLC , VALLANCE PATRICK JOHN THOMPSON , LEIPER JAMES MITCHELL , SELWOOD DAVID LAWRENCE , ROSSITER SHARON , HARTZOULAKIS BASIL
发明人： VALLANCE PATRICK JOHN THOMPSON , LEIPER JAMES MITCHELL , SELWOOD DAVID LAWRENCE , ROSSITER SHARON , HARTZOULAKIS BASIL
IPC分类号： C07C279/14 , A61K31/16 , A61K31/198 , A61K31/223 , A61K31/40 , A61K31/4453 , A61K31/5375 , A61P9/10 , A61P11/06 , A61P19/02 , C07C279/16 , C07C279/18 , C07C323/44 , C07D295/215
CPC分类号： C07C279/14 , A61K31/16 , A61K31/198 , A61K31/223 , A61K31/40 , A61K31/445 , A61K31/4453 , A61K31/5375 , C07C279/16 , C07C279/18 , C07C323/44 , C07C2601/02 , C07D295/215 , C07D295/32
摘要： Compounds of formula (I) have been found to be useful as inhibitors of DDAH. The present invention thus provides the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the treatment of a disease whose pathology is affected by DDAH.
摘要翻译：已经发现式（I）化合物可用作DDAH的抑制剂。因此，本发明提供式（I）化合物或其药学上可接受的盐在制备用于治疗其病理学受DDAH影响的疾病的药物中的用途。

5. 发明申请

WO2006051314A3 GUANIDINE DERIVATIVES AS INHIBITORS OF DDAH 审中-公开
公开(公告)号：WO2006051314A3
公开(公告)日：2006-05-18
申请号：PCT/GB2005/004361
申请日：2005-11-11
申请人： UCL BIOMEDICA PLC , VALLANCE, Patrick, John, Thompson , LEIPER, James, Mitchell , SELWOOD, David, Lawrence , ROSSITER, Sharon , HARTZOULAKIS, Basil
发明人： VALLANCE, Patrick, John, Thompson , LEIPER, James, Mitchell , SELWOOD, David, Lawrence , ROSSITER, Sharon , HARTZOULAKIS, Basil
IPC分类号： C07C279/14 , C07C279/16 , C07C279/18 , C07C323/44 , C07D295/215 , A61P9/10 , A61P11/06 , A61P19/02 , A61K31/40 , A61K31/4453 , A61K31/5375 , A61K31/198 , A61K31/223 , A61K31/16
摘要： Compounds of formula (I) have been found to be useful as inhibitors of DDAH. The present invention thus provides the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the treatment of a disease whose pathology is affected by DDAH.

6. 发明申请

WO1997003983A1 4-[3-(TRANS-3-DIMETHYLAMINOCYCLOBUTYL)-1H-INDOL-5-YLMETHYL]-4(S)OXAZOLIDIN-2-ONE MONOBENZOATE AND SULPHATE SALT 审中-公开
标题翻译： 4- [3-（反式-3-二甲氨基环己基）-1H-吲哚-5-基]甲基] -4（S）氧杂环丁烷-2-酮单烯酸盐和硫酸盐
公开(公告)号：WO1997003983A1
公开(公告)日：1997-02-06
申请号：PCT/EP1996003188
申请日：1996-07-19
申请人： GLAXO GROUP LIMITED , SELWOOD, David, Lawrence , BROCKWELL, Michael, John
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： 4-[3-( trans -3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S )oxazolidin-2-one displays potentially selective inhibition of neurogenic inflammation and the nerve pathways responsible for transmission of head pain. The present invention provides the monobenzoate and sulphate salts of 4-[3-( trans -3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S )oxazolidinone. These salts have particularly good properties and may be obtained in substantially pure form. They are useful in therapy, particularly in the treatment and prophylaxis of migraine. The invention also provides a process for the preparation of these salts and pharmaceutical compositions containing at least one such salt as active ingredient.
摘要翻译： 4- [3-（反式-3-二甲基氨基环丁基）-1H-吲哚-5-基甲基] - （4S）恶唑烷-2-酮显示潜在的选择性抑制神经源性炎症和负责头痛的传播。本发明提供4- [3-（反式-3-二甲基氨基环丁基）-1H-吲哚-5-基甲基] - （4S）恶唑烷酮的单苯甲酸盐和硫酸盐。这些盐具有特别好的性质，可以以基本上纯的形式获得。它们可用于治疗，特别是治疗和预防偏头痛。本发明还提供了制备这些盐和含有至少一种这样的活性成分盐的药物组合物的方法。

7. 发明申请

WO1995020588A1 INDOLE DERIVATIVES AS 5-HT1 AGONISTS 审中-公开
标题翻译：单独使用衍生物作为5-HT1激动剂
公开(公告)号：WO1995020588A1
公开(公告)日：1995-08-03
申请号：PCT/GB1995000142
申请日：1995-01-25
申请人： THE WELLCOME FOUNDATION LIMITED , GLEN, Robert, Charles , FOSTER, Christopher, James , SELWOOD, David, Lawrence , MARTIN, Graeme, Richard
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D209/48 , C07D209/14 , C07D401/06 , C07D403/06 , C07D413/04 , C07D413/06
摘要： Compounds of formula (I) wherein R and R are hydrogen, C1-4 alkyl or are linked to form a ring, A is a cycloalkyl or alkyl-cycloalkyl group, n is an integer from 0 to 3, W is an optionally substituted 5-or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; or W is a group -SO2NR R -NHC(O)R R or -C(O)NHR R ; are useful in treating clinical conditions for which a "5-HT1-like" receptor agonist is indicated.
摘要翻译：其中R和R 1为氢，C 1-4烷基或连接形成环的式（I）化合物，A为环烷基或烷基 - 环烷基，n为0-3的整数，W为任选取代的5-或6-元杂环; 或W是任选取代的芳基，杂芳基，芳氧基或硫代苯氧基; 或W是基团-SO 2 NR 6 R 7 -NHC（O）R 6 R 7或-C（O）NHR 6 R 7; 可用于治疗表现为“5-HT1样”受体激动剂的临床病症。

8. 发明申请

WO1994005687A1 ANTIVIRAL PYRIMIDINE NUCLEOSIDES 审中-公开
标题翻译：抗病毒吡嘧啶核苷
公开(公告)号：WO1994005687A1
公开(公告)日：1994-03-17
申请号：PCT/GB1993001858
申请日：1993-09-03
申请人： UNIVERSITY OF BIRMINGHAM , THE WELLCOME FOUNDATION LIMITED , MILLER, John, Allen , YOUNG, Robert, John , RAHIM, Saad, George , SELWOOD, David, Lawrence , WALKER, Richard
发明人： UNIVERSITY OF BIRMINGHAM , THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07H19/06
CPC分类号： C07H19/06
摘要： Antiviral nucleosides of formula (I), wherein: Y is hydroxy or amino; X is hydrogen, hydroxy, mercapto, halo, trifluoromethyl, methyl, C2-6alkyl, C1-6haloalkyl, hydroxyC1-3alkyl, formyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C1-6alkoxy, C1-6alkylthio, C1-6alkoxyC1-2alkyl, C1-6alkylthiomethyl, amino, monoC1-6alkylamino, diC1-6alkylamino, cyano, thiocyanate or nitro; R2 is hydrogen and R3 is hydroxy or hydrogen, or together R2 and R3 form a carbon-carbon bond; and physiologically functional derivatives thereof. Compositions containing the compounds, their use in treatment and therapy of viral disease, and processes for the production of the compounds are also provided.
摘要翻译：式（I）的抗病毒核苷，其中：Y是羟基或氨基; X是氢，羟基，巯基，卤素，三氟甲基，甲基，C 2-6烷基，C 1-6卤代烷基，羟基C 1-3烷基，甲酰基，C 2-6烯基，C 2-6卤代烯基，C 2-6炔基，C 1-6烷氧基，C 1-6烷硫基， C 1-6烷硫基甲基，氨基，一C 1-6烷基氨基，二C 1-6烷基氨基，氰基，硫氰酸酯或硝基; R2是氢，R3是羟基或氢，或者R2和R3一起形成碳 - 碳键; 及其生理功能衍生物。还提供了含有化合物的组合物，它们在治疗和治疗病毒性疾病中的用途以及生产化合物的方法。

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