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1. 发明授权

US07385086B2 Antimicrobial compounds 失效
标题翻译：抗菌化合物
公开(公告)号：US07385086B2
公开(公告)日：2008-06-10
申请号：US10764451
申请日：2004-01-27
申请人： Craig A. Townsend , James D. Dick , Gary R. Pasternack , Francis P. Kuhajda , Nicole M. Parrish
发明人： Craig A. Townsend , James D. Dick , Gary R. Pasternack , Francis P. Kuhajda , Nicole M. Parrish
IPC分类号： C07C317/00 , C07C317/02 , C07C317/04 , C07C317/06 , C07C317/08
CPC分类号： C40B40/04 , C07C311/06 , C07C317/44
摘要： This invention provides compounds and methods for treating, with said compound, a mycobacterial infection by administering to an animal a pharmaceutical composition containing a compound having the formula R—SOn-Z-CO—Y, where R is an alkyl groups having 6-20 carbon atoms, unsaturated hydrocarbon groups having 6-20 carbon atoms, or alkyl groups having 6-20 carbon atoms interrupted by at least one aromatic ring; Z is —CH2—, —CH2CH2—, —NH—NH—, —O—, ——NH—, —O—NH—, —CH2—NH—, —CH2—O—, —NH—O—, —NH—CH2—, —O—CH2—, and —CH═CH—; Y is —NH2, —O—CH2—C6H5, —CO—CO—O—CH3, and —O—CH3; and n is 1 or 2. It has been discovered that these compounds treat microbially-based infections caused by corynebacteria, nocardiae, rhodococcus, and mycobacteria. These compounds may be used to treat mycobacterial cells, such as Mycobacteria tuberculosis, drug resistant M. tuberculosis, M. avium intracellulare, M. leprae, M. paratuberculosis, and pathogenic Mycobacteria sp.
摘要翻译：本发明提供了通过向动物施用含有具有式R-SO n -Z-CO-Y的化合物的药物组合物，通过向所述化合物处理分枝杆菌感染的化合物和方法，其中R 是具有6-20个碳原子的烷基，具有6-20个碳原子的不饱和烃基或具有6-20个碳原子的烷基被至少一个芳环中断; Z是-CH 2 - ， - CH 2 CH 2 - ， - NH-NH-， - O - ， - NH-， -O-NH-，-CH 2 -NH-，-CH 2 -O-，-NH-O-，-NH-CH 2， -O - CH 2 - 和-CH-CH-; Y是-NH 2，-O-CH 2 -C 6 H 5，-CO-CO- O-CH 3，和-O-CH 3; 已发现这些化合物治疗由棒状杆菌，诺卡氏菌，罗红球菌和分枝杆菌引起的基于微生物的感染。这些化合物可用于治疗分枝杆菌细胞，例如结核分枝杆菌，耐药性结核分枝杆菌，胞内分枝杆菌，麻疯病，副结核分枝杆菌和致病性分枝杆菌属。

2. 发明授权

US06713654B1 Antimicrobial compounds 失效
标题翻译：抗菌化合物
公开(公告)号：US06713654B1
公开(公告)日：2004-03-30
申请号：US09486550
申请日：2000-08-28
申请人： Craig A. Townsend , James D. Dick , Gary R. Pasternack , Francis P. Kuhajda , Nicole M. Parrish
发明人： Craig A. Townsend , James D. Dick , Gary R. Pasternack , Francis P. Kuhajda , Nicole M. Parrish
IPC分类号： C07C31500
CPC分类号： C40B40/04 , C07C311/06 , C07C317/44
摘要： This invention provides methods for treating a mycobacterial infection by administering to an animal a pharmaceutical composition containing a compound having the formula R—SOn—Z—CO—Y, where R is an alkyl group having 6-20 carbons; Z is a radical selected from —CH2—, —O—, and —NH—, two of these radicals coupled together, or —CH2═CH2—; Y is —NH2, O—CH2—C6H5, —CO—CO—O—CH3, or O—CH3; and n is 1 or 2. It has been discovered that these compounds inhibit growth of microbial cells which synthesize &agr;-substitued, &bgr;-hydroxy fatty acids, particularly corynemycolic acid, nocardic acid, and mycolic acid. These compounds may be used to inhibit growth of mycobacterial cells, such as Mycobacterium tuberculosis, drug-resistant M. tuberculosis, M. avium intracellulare, and M. leprae.
摘要翻译：本发明提供了通过向动物施用含有具有式R-SOn-Z-CO-Y的化合物的药物组合物来治疗分枝杆菌感染的方法，其中R是具有6-20个碳原子的烷基; Z是选自-CH 2 - ， - O-和-NH-的基团，这些基团中的两个连接在一起，或-CH 2 = CH 2 - ; Y是-NH 2，O-CH 2 -C 6 H 5，-CO-CO-O-CH 3或O-CH 3; 已经发现，这些化合物抑制合成α-取代的β-羟基脂肪酸，特别是氯霉素酸，诺卡酸和霉菌酸的微生物细胞的生长。这些化合物可用于抑制分枝杆菌细胞的生长，例如结核分枝杆菌，耐药性结核分枝杆菌，胞内分枝杆菌和麻疯病。

3. 发明授权

US5614551A Inhibitors of fatty acid synthesis as antimicrobial agents 失效
标题翻译：脂肪酸合成抑制剂作为抗菌剂
公开(公告)号：US5614551A
公开(公告)日：1997-03-25
申请号：US188421
申请日：1994-01-24
申请人： James D. Dick , Francis P. Kuhajda
发明人： James D. Dick , Francis P. Kuhajda
IPC分类号： A61K45/00 , A61K31/20 , A61K31/335 , A61K31/34 , A61K31/455 , A61P3/06 , A61P31/00 , A61P31/04 , A61P31/06 , A61P33/00 , A61P43/00 , A01N43/20 , A01N25/26 , A61K9/127
CPC分类号： A61K31/34 , A61K31/335
摘要： Fatty acid synthase (FAS) is overexpressed by certain infectious organisms that are resistant to most currently available antibiotics. Contrarywise, little FAS expression is identified in patient tissues. Inhibition of fatty acid synthesis is thus selectively toxic to invasive cells, while patient cells with low FAS activity are resistant. This invention provides a method of treating septic patients where fatty acid synthesis by invading cells is inhibited with resultant interruption of the disease process.
摘要翻译：脂肪酸合成酶（FAS）被某些对大多数现有抗生素具有抗性的感染性生物体过度表达。相反，在患者组织中鉴定出少量FAS表达。脂肪酸合成的抑制因此对侵入性细胞有选择性毒性，而具有低FAS活性的患者细胞具有抗性。本发明提供一种治疗败血症患者的方法，其中通过侵入细胞的脂肪酸合成被抑制并导致疾病过程的中断。

4. 发明申请

US20100022639A1 Methods of Inducing Weight Loss 审中-公开
标题翻译：诱导减肥的方法
公开(公告)号：US20100022639A1
公开(公告)日：2010-01-28
申请号：US12558313
申请日：2009-09-11
申请人： Thomas M. Loftus , Craig A. Townsend , Gabriele Ronnett , M. Daniel Lane , Francis P. Kuhajda
发明人： Thomas M. Loftus , Craig A. Townsend , Gabriele Ronnett , M. Daniel Lane , Francis P. Kuhajda
IPC分类号： A61K31/365 , C12Q1/68 , A61K31/336
CPC分类号： C12Q1/6883 , A61K31/365 , C12Q2600/106 , C12Q2600/136 , C12Q2600/158
摘要： This invention provides a method for inducing weight loss in an animal by administering to the animal a compound which reduces the expression and/or secretion of neuropeptide Y (NPY). The effect may be accomplished directly, indirectly, or humorally. Preferably, administration of this compound has the effect of increasing malonyl CoA levels in the animal. Compounds administered according to this invention may be inhibitors of fatty acid synthase (FAS), including substituted α-methylene-β-carboxyl-γ-butyrolactones, or inhibitors of malonyl Coenzyme A decarboxylase (MCD). Preferably, the compound is administered in an amount sufficient to reduce the amount and/or duration of expression and/or secretion of NPY to levels at or below those observed for lean animals. In another preferred embodiment, the administration will reduce expression and/or secretion to levels observed for fed or satiated animals; more preferably, administration will reduce the level of NPY below that of fed animals. In a particular embodiment, this invention provides a method for inducing weight loss in an animal by administering a compound which inhibits feeding behavior in the animal. The method is particularly useful for inducing weight loss in animals deficient in expression of the hormone leptin or animals resistant to the action of leptin.
摘要翻译：本发明提供一种通过向动物施用降低神经肽Y（NPY）的表达和/或分泌的化合物来诱导动物体内的体重减轻的方法。效果可以直接，间接或幽默地完成。优选地，该化合物的给药具有增加动物中丙二酰辅酶A水平的作用。根据本发明施用的化合物可以是脂肪酸合酶（FAS）的抑制剂，包括取代的α-亚甲基-β-羧基-γ-丁内酯或丙二酰辅酶A脱羧酶（MCD）的抑制剂。优选地，化合物以足以将NPY的表达和/或分泌的量和/或持续时间降低至对于瘦动物观察到的水平或以下的量施用。在另一个优选的实施方案中，施用将将表达和/或分泌降低至饲喂或饱食动物观察到的水平; 更优选地，施用将降低NPY的水平低于饲养动物的水平。在一个具体实施方案中，本发明提供了通过施用抑制动物中的进食行为的化合物来诱导动物体重减轻的方法。该方法特别可用于诱导缺乏激素瘦素或对瘦素作用的动物的表达的动物的体重减轻。

5. 发明授权

US5872217A Antibodies which specifically bind a cancer related antigen 失效
标题翻译：特异性结合癌症相关抗原的抗体
公开(公告)号：US5872217A
公开(公告)日：1999-02-16
申请号：US469007
申请日：1995-06-05
申请人： Francis P. Kuhajda , Gary R. Pasternack
发明人： Francis P. Kuhajda , Gary R. Pasternack
IPC分类号： A61K31/00 , A61K31/20 , A61K31/23 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/341 , C07K14/47 , C07K16/18 , C07K16/30 , C12N9/10 , G01N33/574
CPC分类号： A61K31/00 , A61K31/20 , A61K31/23 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/341 , C07K14/47 , C07K14/4748 , C07K16/18 , C07K16/3015 , C12N9/1029 , G01N33/57415 , G01N33/57488 , Y10S435/975 , Y10S530/806 , Y10S530/85 , Y10S530/851
摘要： A method of determining the prognosis of a solid tumor is provided, in which a sample from a patient bearing a tumor is assayed for the presence of a protein which is immunologically cross-reactive with the hpr gene product, but not with haptoglobin 1 or haptoglobin 2. Also provided is a method for preparing antibodies specific for this diagnostic marker which correlates with early relapse and metastasis of breast and other cancers. The marker can be detected using immunological methods employing antibodies specific for Hpr protein and not cross-reactive with haptoglobins 1 or 2.
摘要翻译：提供了确定实体瘤的预后的方法，其中来自患有肿瘤的患者的样品被测定与hpr基因产物具有免疫交叉反应性的蛋白质的存在，但不与触珠蛋白1或触珠蛋白还提供了一种制备与该诊断标记物特异性的抗体相关的方法，其与乳腺癌和其他癌症的早期复发和转移相关。可使用采用Hpr蛋白特异性抗体并且不与触珠蛋白1或2交叉反应的免疫学方法检测标记。

6. 发明授权

US07649012B2 Compounds, pharmaceutical compositions containing same, and methods of use for same 失效
标题翻译：含有其的化合物，药物组合物及其用途方法
公开(公告)号：US07649012B2
公开(公告)日：2010-01-19
申请号：US10520505
申请日：2003-07-09
申请人： Francis P. Kuhajda , Susan M. Medghalchi , Jill M. McFadden , Jagan Thupari
发明人： Francis P. Kuhajda , Susan M. Medghalchi , Jill M. McFadden , Jagan Thupari
IPC分类号： A61K31/381 , C07D333/32
CPC分类号： C07D409/12 , C07D333/32
摘要： A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula IV wherein R21=H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —CH2OR25, —C(O)R25, —CO(O)R25, —C(O)NR25R26, —CH2C(O)R25, or —CH2C(O)NHR25, where R25 and R26 are each independently H, C1-C10 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing one or more halogen atoms. R22=—OH, —OR27, —OCH2C(O)R27, —OCH2C(O)NHR27, —OC(O)R27, —OC(O)OR27, —OC(O)NHNH—R5, or —OC(O)NR27R28, where R27 and R28 are each independently H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, and where R27 and R28 can each optionally contain halogen atoms; R23 and R24, the same or different from each other, are C1-C20 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：包含药物稀释剂和式IV化合物的药物组合物，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 25，-CO（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，芳烷基或烷芳基，一个或多个卤素原子。 R22 = -OH，-OR27，-OCH2C（O）R27，-OCH2C（O）NHR27，-OC（O）R27，-OC（O）OR27，-OC（O）NHNH-R5或-OC ）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，并且其中R 27和R 28可各自任选含有卤素原子; 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。

7. 发明授权

US5759837A Chemotherapy for cancer by inhibiting the fatty acid biosynthetic pathway 失效
标题翻译：通过抑制脂肪酸生物合成途径的化学疗法
公开(公告)号：US5759837A
公开(公告)日：1998-06-02
申请号：US188425
申请日：1994-01-24
申请人： Francis P. Kuhajda , Gary R. Pasternack
发明人： Francis P. Kuhajda , Gary R. Pasternack
IPC分类号： A61K31/00 , A61K31/20 , A61K31/23 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/341 , C07K14/47 , C07K16/18 , C07K16/30 , C12N9/10 , G01N33/574 , C12N9/04
CPC分类号： A61K31/00 , A61K31/20 , A61K31/23 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/341 , C07K14/47 , C07K14/4748 , C07K16/18 , C07K16/3015 , C12N9/1029 , G01N33/57415 , G01N33/57488
摘要： Fatty acid synthase (FAS) is overexpressed in carcinomas with poor prognosis, but little FAS expression is identified in normal tissues Inhibition of fatty acid synthesis is selectively toxic to carcinoma cells, while normal cells with low FAS activity are resistant. This invention provides a method of treating cancer patients where fatty acid synthesis by cells of the patient's tumor is inhibited with resultant interruption of the disease process.
摘要翻译：脂肪酸合成酶（FAS）在预后差的癌症中过表达，但在正常组织中鉴定出少量FAS表达。脂肪酸合成的抑制对癌细胞有选择性毒性，而FAS活性低的正常细胞具有抗性。本发明提供了一种治疗癌症患者的方法，其中抑制患者肿瘤细胞的脂肪酸合成，导致疾病过程的中断。

8. 发明申请

US20100168218A1 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：US20100168218A1
公开(公告)日：2010-07-01
申请号：US12309422
申请日：2006-07-26
申请人： Francis P. Kuhajda
发明人： Francis P. Kuhajda
IPC分类号： A61K31/381 , A61K31/365 , A61P3/04
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：一种减少受试者的食物摄入的方法，包括施用增加粮农组织的化合物，其中化合物不在中枢神经系统中起作用以降低食欲，其中化合物不是脂肪酸，或NPY抑制剂，或FAS抑制剂。

9. 发明申请

US20100029761A1 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：US20100029761A1
公开(公告)日：2010-02-04
申请号：US12309419
申请日：2006-07-26
申请人： Francis P. Kuhajda , Craig A. Townsend , Susan M. Medghalchi , Jill M. McFadden
发明人： Francis P. Kuhajda , Craig A. Townsend , Susan M. Medghalchi , Jill M. McFadden
IPC分类号： A61K31/341 , C07D307/04 , C07D307/26 , A61P3/04
CPC分类号： C07D307/68
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.
摘要翻译：药物稀释剂和式VI化合物：其中：R 10 = H或任选含有卤素原子的C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基; R 11 = H 3或C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基，任选地含有卤素原子; R 12 = H或任选含有卤素原子的C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基，-C（O）R 13，其中R 13是H，C 1 -C 20烷基，环烷基，烯基，芳基，或烷基芳基，任选地含有卤素原子，或-OH，-OR 14或-NR 14，其中R 14是H，C 1 -C 20烷基，环烷基，烯基，芳基，芳烷基或烷基芳基，任选地含有卤素原子。

10. 发明申请

US20090162870A1 FATTY ACID SYNTHASE IN LIVER DISEASE 审中-公开
标题翻译：肝脏脂肪酸合成酶
公开(公告)号：US20090162870A1
公开(公告)日：2009-06-25
申请号：US12038803
申请日：2008-02-27
申请人： Susan M. Medghalchi , Francis P. Kuhajda
发明人： Susan M. Medghalchi , Francis P. Kuhajda
IPC分类号： G01N33/573
CPC分类号： G01N33/573 , G01N2333/91045 , G01N2800/08
摘要： Methods and compositions for detecting elevated fatty acid synthase (FAS) expression in the liver of a subject are disclosed. The detection may be of expression in liver cells per se or in a bodily fluid of a subject. Also disclosed are methods for identifying the presence or absence of liver disease or pathology in relation to elevated FAS. The disclosed methods may be practiced with various compositions comprising reagents for detecting FAS expression as described herein.
摘要翻译：公开了用于检测受试者肝脏中升高的脂肪酸合成酶（FAS）表达的方法和组合物。检测可以在肝细胞本身或受试者的体液中表达。还公开了用于鉴定与升高的FAS相关的肝病或病理学存在或不存在的方法。所公开的方法可以用包含用于检测如本文所述的FAS表达的试剂的各种组合物来实施。

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