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1. 发明申请

WO2002034921A3 FERMENTATIVE PRODUCTION OF D-p-HYDROXYPHENYLGLYCINE AND D-PHENYLGLYCINE 审中-公开
公开(公告)号：WO2002034921A3
公开(公告)日：2002-05-02
申请号：PCT/NL2001/000772
申请日：2001-10-22
申请人： DSM N.V. , DSM BIOTECH GMBH , JOHNS HOPKINS UNIVERSITY , TOWNSEND, Craig, A. , GUNSIOR, Michele , MÜLLER, Ulrike , ASSEMA VAN, Friso, Bernard, Jan , SONKE, Theodorus
发明人： TOWNSEND, Craig, A. , GUNSIOR, Michele , MÜLLER, Ulrike , ASSEMA VAN, Friso, Bernard, Jan , SONKE, Theodorus
IPC分类号： C12N15/53
摘要： A new fermentative process for the preparation of D- p -hydroxyphenylglycine (D-HPG) or D-henylglycine (D-PG) in enantiomerically pure form is disclosed. Precursors for the formation of D-HPG and D-PG are withdrawn form the common aromatic amino acid pathway, converted to p -hydroxyphenylglyoxylate or phenylglyoxylate, and are finally converted to D-HPG or D-PG by the action of a stero-inverting D-aminotransferase.

2. 发明申请

WO2007014247A3 NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME 审中-公开
公开(公告)号：WO2007014247A3
公开(公告)日：2007-02-01
申请号：PCT/US2006/028979
申请日：2006-07-26
申请人： JOHNS HOPKINS UNIVERSITY , FASGEN, INC. , KUHAJDA, Francis, P. , TOWNSEND, Craig, A. , MEDGHALCHI, Susan, M. , MCFADDEN, Jill, M.
发明人： KUHAJDA, Francis, P. , TOWNSEND, Craig, A. , MEDGHALCHI, Susan, M. , MCFADDEN, Jill, M.
IPC分类号： C07D305/12 , C07D307/62 , A01N43/08 , A61K31/34
摘要： A pharmaceutical diluent and a compound of formula VI: wherein: R10 = H, or C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R11 = H3 or C]-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R12 = H, or C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, -C(O)R13, where R13 is H, Ci-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, or -OH, -OR14 or -NR14, where R14 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms.

3. 发明申请

WO2004005277A1 NOVEL COMPUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME 审中-公开
标题翻译：新型组合物，含有该组合物的药物组合物及其使用方法
公开(公告)号：WO2004005277A1
公开(公告)日：2004-01-15
申请号：PCT/US2003/021700
申请日：2003-07-09
申请人： FASGEN, INC. , THE JOHNS HOPKINS UNIVERSITY , KUHAJDA, Francis, P. , MEDGHALCHI, Susan, M. , MCFADDEN, Jill, M. , THUPARI, Jagan , TOWNSEND, Craig, A.
发明人： KUHAJDA, Francis, P. , MEDGHALCHI, Susan, M. , MCFADDEN, Jill, M. , THUPARI, Jagan , TOWNSEND, Craig, A.
IPC分类号： C07D333/32
CPC分类号： C07D409/12 , C07D333/32
摘要： A pharmaceutical composition comprising a phamaceurtical diluent and a compound of formula IV wherein R 21 = H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, -CH 2 OR 25 , -C(O)R 25 , -CO(O)R 25 , -C(O)NR 25 R 26 , -CH 2 C(O)R 25 , or -CH 2 C(O)NHR 25 , where R 25 and R 26 are each independently H, C 1 -C 10 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing one or more halogen atoms. R 22 = -OH, -OR 27 , -OCH 2 C(O)R 27 , -OCH 2 C(O)NHR 27 , -OC(O)R 27 , -OC(O)OR 27 , -OC(O)NHNH-R 5 , or -OC(O)NR 27 R 28 , where R 27 and R 28 are each independentlyH, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, and where R 27 and R 28 can each optionally contain halogen atoms; R 23 and R 24 , the same or different from each other, are C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. Methods of using such formulations for the treatment of cancer, to effect weight loss, to treat microbially-based infections, to inhibit neuropeptide-Y and/or fatty acid synthase, and to stimulate CPT-1.
摘要翻译：其中R 21 = H，C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基，-CH 2 OR 25，-C（O）R 5，（O）R 25，-C（O）NR 25 R 26，-CH 2 C（O）R 25或-CH 2 C（O）NHR 25，其中 R 25和R 26各自独立地为H，C 1 -C 10烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基，任选地含有一个或多个卤素原子。 R 22 = -OH，-OR 27，-OCH 2 C（O）R 27，-OCH 2 C（O）NHR 27，-OC（O）R 27，-OC（O）OR -OC（O）NHNH-R 5或-OC（O）NR 27 R 28，其中R 27和R 28各自独立地为H，C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基，其中R 27和R 28各自可以含有卤素原子; R 23和R 24彼此相同或不同，为C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基。使用这些制剂治疗癌症，减轻体重，治疗基于微生物的感染，抑制神经肽Y和/或脂肪酸合成酶以及刺激CPT-1的方法。

4. 发明申请

WO2002089847A1 CYTOSTATIC EFFECTS OF FATTY ACID SYNTHASE INHIBITION 审中-公开
标题翻译：脂肪酸合成酶抑制的细胞毒作用
公开(公告)号：WO2002089847A1
公开(公告)日：2002-11-14
申请号：PCT/US2002/004408
申请日：2002-02-15
申请人： THE JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE , PIZER, Ellen, Sarah , KUHAJDA, Francis, Paul , TOWNSEND, Craig, A.
发明人： PIZER, Ellen, Sarah , KUHAJDA, Francis, Paul , TOWNSEND, Craig, A.
IPC分类号： A61K45/00
CPC分类号： A61K31/336 , A61K31/00 , A61K31/16 , A61K31/365
摘要： This invention provides a method for treating an individual having a tumor by administering to the individual an inhibitor of fatty acid synthase (FAS) in an amount sufficient to retard growth of cells in the tumor. Preferably, the method of this invention is applied to an individual having a tumor comprising cells which do not overexpress FAS or a tumor comprising cells which are resistant to induction of apoptosis by inhibitors of FAS. Administration of an inhibitor of FAS according to this invention can induce a cellular response equivalent to a genotoxic stress response in the absence of substantial DNA damage. This invention also provides for use of a FAS inhibitor in the preparation of a medicament for treating a tumor in an individual whose tumor exhibits reduced p53 function.
摘要翻译：本发明提供一种通过向个体施用足以抑制肿瘤细胞生长的量的脂肪酸合酶抑制剂（FAS）来治疗患有肿瘤的个体的方法。优选地，本发明的方法适用于具有肿瘤的个体，所述肿瘤包含不过表达FAS的细胞或包含对FAS抑制剂诱导凋亡有抗性的细胞的肿瘤。根据本发明的FAS抑制剂的施用可以在没有实质的DNA损伤的情况下诱导与基因毒性应激反应相当的细胞反应。本发明还提供了FAS抑制剂在制备用于治疗其肿瘤显示出降低的p53功能的个体中的肿瘤的药物中的用途。

5. 发明申请

WO2007030772A2 IMPROVED PRODUCTION OF CLAVULANIC ACID BY GENETIC ENGINEERING OF STREPTOMYCES CLAVULIGERUS 审中-公开
标题翻译：通过基因工程改进CLAVUIGICUS的生产方法
公开(公告)号：WO2007030772A2
公开(公告)日：2007-03-15
申请号：PCT/US2006/035172
申请日：2006-09-08
申请人： THE JOHNS HOPKINS UNIVERSITY , TOWNSEND, Craig, A. , LI, Rong-feng
发明人： TOWNSEND, Craig, A. , LI, Rong-feng
IPC分类号： C12P37/00
CPC分类号： C12P17/188
摘要： Genetically engineered Streptomyces clavuligerus strains with improved capabilities to produce clavulanic acid are provided. The strains are genetically engineered by disrupting newly identified glyceraldehyde-3-phosphate dehydrogenase (GAPDH) genes. This results in an increased intracelluar pool of the clavulanic acid precursor D-glyceraldehyde-3-phosphate (D-G3P), and increased clavulanic acid production. Clavulanic acid production may be further increased by supplying arginine to the medium in which the S. clavuligerus is grown.
摘要翻译：提供了具有改进的克拉维酸能力的遗传工程链霉菌（Streptomyces clavuligerus）菌株。通过破坏新鉴定的甘油醛-3-磷酸脱氢酶（GAPDH）基因，遗传工程菌株。这导致克拉维酸前体D-甘油醛-3-磷酸（D-G3P）的增加的胞内池，并且增加了克拉维酸的产生。将精氨酸提供给S的培养基可以进一步提高克拉维酸的产生。

6. 发明申请

WO2009149066A1 NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME 审中-公开
标题翻译：新化合物，含有该化合物的药物组合物及其使用方法
公开(公告)号：WO2009149066A1
公开(公告)日：2009-12-10
申请号：PCT/US2009/045945
申请日：2009-06-02
申请人： FASGEN, INC. , THE JOHNS HOPKINS UNIVERSITY , TOWNSEND, Craig, A. , EL MESKINI, Rajaa , SUBBURAJ, Kandasamy , MEDGHAICHI, Susan , STURDIVANT, Jill, Marie
发明人： TOWNSEND, Craig, A. , EL MESKINI, Rajaa , SUBBURAJ, Kandasamy , MEDGHAICHI, Susan , STURDIVANT, Jill, Marie
IPC分类号： A01N43/08 , A61K31/34
CPC分类号： C07D333/32 , C07D307/60
摘要： The class compounds of the present invention may be represented by Formula (I), wherein X may be O, S, or N. R 1 and R 2 are independently either H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. R 3 and R 4 are independently either H, an aryl group, a heteroaryl group, and a heterocyclic ring group having 4 to 6 carbon atoms, wherein the aryl, heteroaryl, and heterocyclic moieties are optionally substituted with one or more of a first substitution group defined herein. In a further embodiment, R 3 and R 4 along with the atoms and bonds to which they are attached, form an optionally substituted 5-7 membered ring having at least one nitrogen atom within the ring structure.
摘要翻译：本发明的类化合物可以由式（I）表示，其中X可以是O，S或N.R 1和R 2独立地是H，C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基。 R 3和R 4独立地为H，芳基，杂芳基和具有4-6个碳原子的杂环基，其中芳基，杂芳基和杂环部分任选被一个或多个被定义的第一取代基取代于此。在另一个实施方案中，R 3和R 4连同它们所连接的原子和键，形成在环结构内具有至少一个氮原子的任选取代的5-7元环。

7. 发明申请

WO2007014249A2 NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME 审中-公开
标题翻译：新化合物，含有该化合物的药物组合物及其使用方法
公开(公告)号：WO2007014249A2
公开(公告)日：2007-02-01
申请号：PCT/US2006/028981
申请日：2006-07-26
申请人： JOHNS HOPKINS UNIVERSITY , FASGEN, INC. , KUHAJDA, Francis, P. , TOWNSEND, Craig, A. , MEDGHALCHI, Susan, M. , MCFADDEN, Jill, M.
发明人： KUHAJDA, Francis, P. , TOWNSEND, Craig, A. , MEDGHALCHI, Susan, M. , MCFADDEN, Jill, M.
IPC分类号： A61K39/02
CPC分类号： C07D333/38 , C07D409/12
摘要： A pharmaceutical composition containing a pharmaceutical diluent and a compound of formula II: wherein: R 8 = H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, -C(O)R 4 , where R 4 is H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, or -OH, -OR 7 or -NR 7 , where R 7 is H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R 9 = -OR 5 , -NR 5 , -NH-NH-R 5 where R 5 is H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl, optionally containing halogen atoms; R 10 = H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or- CH 2 C(O)R 6 , where R 6 is OR 7 and NR 7 , where R 7 = H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl and can optionally contain halogen atoms. Also included in the invention are methods of using the pharmaceutical compositions and the chemical compounds used in the compositions.
摘要翻译：含有药物稀释剂和式II化合物的药物组合物：其中：R 8 = H，C 1 -C 4 - C（O）R 4，其中R 4是H，C 1 -C 4烷基，芳基，芳基，芳烷基，任选地含有卤素原子，或-OH，-OR7或-NR9的环烷基，链烯基，芳基，芳基烷基或烷基芳基，其中R 7为H，C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基，芳基烷基，芳基烷基，或烷芳基，任选含有卤素原子; R 9 = -OR 5，-NR 5，-NH-NH-R 5其中R 5是H，C 1 -C 20烷基，环烷基，链烯基，芳基，芳基烷基，烯丙基或烷基芳基，任选含有卤素原子; R 10 = H，C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基，或-CH = （O）R 6，其中R 6是OR 7和NR 7，其中R 7是氢，其中R 7 = H，C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基，烯丙基或烷基芳基，并且可以任选含有卤素原子。本发明还包括使用药物组合物和组合物中使用的化学化合物的方法。

8. 发明申请

WO2007014248A2 METHOD OF REDUCING FOOD INTAKE 审中-公开
标题翻译：减少食物摄入的方法
公开(公告)号：WO2007014248A2
公开(公告)日：2007-02-01
申请号：PCT/US2006/028980
申请日：2006-07-26
申请人： JOHNS HOPKINS UNIVERSITY , FASGEN, INC. , KUHAJDA, Francis, P. , THUPARI, Jagan , TOWNSEND, Craig, A. , MCFADDEN, Jill, M.
发明人： KUHAJDA, Francis, P. , THUPARI, Jagan , TOWNSEND, Craig, A. , MCFADDEN, Jill, M.
IPC分类号： A61K31/137
CPC分类号： A61K31/137
摘要： A method of decreasing the food intake of a subject, comprising the administration of a compound which increases FAO, where the compound does not act in the central nervous system to decrease appetite, where the compound is not a fatty acid, or an NPY-inhibitor, or an FAS inhibitor.
摘要翻译：降低受试者的食物摄入量的方法，包括施用增加FAO的化合物，其中所述化合物不在中枢神经系统中起作用以降低食欲，其中所述化合物不是脂肪酸或NPY抑制剂或FAS抑制剂。

9. 发明申请

WO2005117590A3 NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME 审中-公开
公开(公告)号：WO2005117590A3
公开(公告)日：2005-12-15
申请号：PCT/US2005/018443
申请日：2005-05-25
申请人： FASGEN, LLC , THE JOHNS HOPKINS UNIVERSITY , MCFADDEN, Jill, M. , TOWNSEND, Craig, A. , MEDGHALCHI, Susan, M.
发明人： MCFADDEN, Jill, M. , TOWNSEND, Craig, A. , MEDGHALCHI, Susan, M.
IPC分类号： A61K31/381 , C07D333/32
摘要： A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula (II), wherein R 1 and R 2 , the same or different from each other, are H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, -CH 2 COR S , -CH 2 C(O)NR S , -C(O)R 5 , or -CH 2 OR 5 , and can optionally contain halogen atoms, where R 5 is a C 1 -C 12 alkyl group. R 3 and R 4 , the same or different from each other, are H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl.

10. 发明申请

WO2004006835A2 NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME 审中-公开
标题翻译：新化合物，含有该化合物的药物组合物及其使用方法
公开(公告)号：WO2004006835A2
公开(公告)日：2004-01-22
申请号：PCT/US2003/020960
申请日：2003-07-01
申请人： FASGEN, LLC. , THE JOHNS HOPKINS UNIVERSITY , KUHADJA, Francis, P. , MEDGHALCHI, Susan, M. , THUPARI, Jagan, N. , TOWNSEND, Craig, A. , McFADDEN, Jill, M.
发明人： KUHADJA, Francis, P. , MEDGHALCHI, Susan, M. , THUPARI, Jagan, N. , TOWNSEND, Craig, A. , McFADDEN, Jill, M.
IPC分类号： A61K
CPC分类号： C07D307/33 , C07D307/58 , C07D307/68
摘要： Pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula IX: R 29 = H, or C I -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, =CHR 31 , -C(O)OR 31 , - C(O)R 31 , -CH 2 C(O)OR 31 , CH 2 C(O)NHR 31 , where R 31 is H or C 1 -C 10 alkyl, cycloalkyl, or alkenyl; R 30 = C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl; X 5 = -OR 32 , or NHR 32 , Where R 32 is H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, the R 32 group optionally containing a carbonyl group, a carboxyl group, a carboxyamide group, an alcohol group, or an ether group, the R 32 group further optionally containing one or more halogen atoms; with the proviso that when R 29 is =CH 2 , then X 5 is not OH. Also disclosed are compounds within the scope of the formula IX, as well as uses of the pharmaceutical compositions for weight loss, anti-microbial and anti-cancer applications, inhibition of fatty acid synthase and neuropeptide-Y, and the stimulation of the activity of carnitine palmitoyl transferase-1.
摘要翻译： R 29 = H或C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷芳基，= CHR 31，-C（O）OR 3，（O）R 31，-CH 2 C（O）OR 31，CH 2 C（O）NHR 31，其中R 31是H或C 1 -C 10烷基，环烷基或链烯基; R 30 = C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基; X 5 = -OR 32或NHR 32，其中R 32是H，C 1 -C 20烷基，环烷基，烯基，芳基，芳烷基或烷芳基，R 32基任选地含有羰基，羧基，羧酰胺基，醇基或醚基，R 32基团还任选地含有一个或多个卤原子; 条件是当R 29是= CH 2时，则X 5不是OH。还公开了式IX范围内的化合物，以及药物组合物用于体重减轻，抗微生物和抗癌应用，抑制脂肪酸合酶和神经肽Y的用途以及刺激活性肉碱棕榈酰转移酶-1。

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