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51. 发明授权

US07776855B2 Antimicrobial oxazolidinone prodrugs 有权
标题翻译：抗菌恶唑烷酮前药
公开(公告)号：US07776855B2
公开(公告)日：2010-08-17
申请号：US11774746
申请日：2007-07-09
申请人： Mark J. Macielag , Manomi A. Tennakoon
发明人： Mark J. Macielag , Manomi A. Tennakoon
IPC分类号： A61K31/42 , A61K31/497 , C07D263/04 , C07D403/00 , C07D413/14
CPC分类号： C07D487/04
摘要： This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.
摘要翻译：本发明包括如本文定义的式（I）和式（II）的恶唑烷酮前药化合物。前药可通过天然生物学过程转化成具有抗微生物特性的活性成分，其可用于治疗哺乳动物的细菌感染。

52. 发明申请

US20100160289A1 SULFONAMIDES AS TRPM8 MODULATORS 有权
标题翻译：磺酰胺作为TRPM8调节剂
公开(公告)号：US20100160289A1
公开(公告)日：2010-06-24
申请号：US12638550
申请日：2009-12-15
申请人： Mark J. Macielag , James J. McNally
发明人： Mark J. Macielag , James J. McNally
IPC分类号： A61K31/381 , C07D333/66 , A61K31/4535 , C07D409/12 , A61K31/496 , A61K31/541 , C07D417/12 , A61K31/4025 , A61K31/551 , C07D413/12 , A61K31/5377 , A61K31/397 , A61K31/4725 , C07C311/32 , A61K31/18 , A61K31/5375 , C07D295/16 , A61K31/54 , C07D211/30 , A61K31/451 , A61K31/472 , C07D217/04 , C07D205/04 , A61K31/495 , A61P29/00
CPC分类号： C07D333/66 , C07C311/32 , C07D205/04 , C07D211/14 , C07D217/04 , C07D295/10 , C07D295/18 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
摘要翻译：公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。这样的化合物由式（I）和式（II）表示如下：其中Y，R 1，R 2，R 3，R 4，RA和RB在本文中定义。

53. 发明申请

US20090275594A1 3-HYDRAZONE PIPERAZINYL RIFAMYCIN DERIVATIVES USEFUL AS ANTIMICROBIAL AGENTS 审中-公开
标题翻译：作为抗微生物剂有效的3-氢氯吡嗪类维生素D衍生物
公开(公告)号：US20090275594A1
公开(公告)日：2009-11-05
申请号：US12434832
申请日：2009-05-04
申请人： Mark J. MACIELAG , Manomi Tennakoon
发明人： Mark J. MACIELAG , Manomi Tennakoon
IPC分类号： A61K31/496 , C07D413/14 , A61P31/04
CPC分类号： C07D498/08
摘要： The present invention is directed to novel 3-hydrazone piperazinyl rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.
摘要翻译：本发明涉及新的3-腙哌嗪基利福霉素衍生物，含有它们的药物组合物，以及所述衍生物和药物组合物作为抗病原微生物，特别是抗性微生物的抗微生物剂的用途。

54. 发明申请

US20090270379A1 QUINOLONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：喹诺酮衍生物作为抗菌药物有用
公开(公告)号：US20090270379A1
公开(公告)日：2009-10-29
申请号：US12426442
申请日：2009-04-20
申请人： Mark J. Macielag , Bin Zhu
发明人： Mark J. Macielag , Bin Zhu
IPC分类号： A61K31/5383 , C07D487/04 , A61K31/498 , C07D498/06 , A61P31/04
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention is directed to quinolone derivatives, useful as antimicrobial compounds, pharmaceutical compositions comprising said derivatives and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes
摘要翻译：本发明涉及用作抗微生物化合物的喹诺酮衍生物，包含所述衍生物的药物组合物以及所述衍生物和药物组合物作为抗病原微生物的抗微生物剂的用途，特别是针对抗性微生物

55. 发明申请

US20090264474A1 SULFONAMIDES AS TRPM8 MODULATORS 有权
标题翻译：磺酰胺作为TRPM8调节剂
公开(公告)号：US20090264474A1
公开(公告)日：2009-10-22
申请号：US12175740
申请日：2008-07-18
申请人： Shawn T. Branum , Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Michele C. Jetter , Yi Liu , Donald Ludovici , Mark J. Macielag , Jay M. Matthews , James J. McNally , Laura M. Reaney , Ronald K. Russell , Ning Qin , Christopher Teleha , Kenneth M. Wells , Scott C. Youells , Mark A. Youngman
发明人： Shawn T. Branum , Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Michele C. Jetter , Yi Liu , Donald Ludovici , Mark J. Macielag , Jay M. Matthews , James J. McNally , Laura M. Reaney , Ronald K. Russell , Ning Qin , Christopher Teleha , Kenneth M. Wells , Scott C. Youells , Mark A. Youngman
IPC分类号： A61K31/4439 , C07D333/66 , A61K31/381 , C07D417/12 , C07D409/12 , A61K31/4196 , A61K31/427 , C07D401/14
CPC分类号： C07D333/66 , C07D333/36 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
摘要翻译：公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。这样的化合物由式I表示如下：其中A，B，G，Y，R 1，R 2，R 3和R 4在本文中定义。

56. 发明授权

US06825172B2 3-descladinosyl-6-O-carbamoyl and 6-O-carbonoyl macrolide antibacterial agents 有权
标题翻译： 3-脱酰基脯氨酰基-6-O-氨基甲酰基和6-O-碳酰基大环内酯类抗菌剂
公开(公告)号：US06825172B2
公开(公告)日：2004-11-30
申请号：US10447058
申请日：2003-05-28
申请人： Todd C. Henninger , Mark J. Macielag , Brett A. Marinelli , Bin Zhu
发明人： Todd C. Henninger , Mark J. Macielag , Brett A. Marinelli , Bin Zhu
IPC分类号： A61K3170
CPC分类号： C07H17/08
摘要： 3-Descladinosyl-6-O-carbamoyl and 6-O-carbonoyl macrolide antibacterial agents of the formula: wherein R1, W, R3, R4, R5, R6, X, X′, and Z are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
摘要翻译： 3-脱氨基腺苷基-6-O-氨基甲酰基和6-O-碳酰基大环内酯抗菌剂，其结构式如下：其中R 1，W，R 3，R 4，R 5，R 6， X，X'和Z如本文所述，其中取代基具有在说明书中指出的含义。这些化合物可用作抗菌剂。

57. 发明授权

US06713455B2 6-O-carbamate-11,12-lacto-ketolide antimicrobials 有权
标题翻译： 6-O-氨基甲酸酯-11,12-乳糖内酯抗微生物剂
公开(公告)号：US06713455B2
公开(公告)日：2004-03-30
申请号：US10244184
申请日：2002-09-16
申请人： Eugene B. Grant, III , Todd C. Henninger , Mark J. Macielag , Deodialsingh Guiadeen
发明人： Eugene B. Grant, III , Todd C. Henninger , Mark J. Macielag , Deodialsingh Guiadeen
IPC分类号： A61K3170
CPC分类号： C07H17/08
摘要： 6-O-Carbamate-11,12-lacto-ketolide antimicrobials of the formula: wherein R1, R2, R3 R7, and R8 are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
摘要翻译： 6-O-氨基甲酸酯-11,12-乳糖 - 内酯抗微生物剂，其结构式如下：其中R 1，R 2，R 3 R 7和R 8如本文所述，其中取代基具有说明书中指出的含义。这些化合物可用作抗菌剂。

58. 发明授权

US06492358B2 &bgr;-carboline derivatives useful as inhibitors of phosphodiesterase 有权
标题翻译：可用作磷酸二酯酶抑制剂的β-咔啉衍生物
公开(公告)号：US06492358B2
公开(公告)日：2002-12-10
申请号：US09847767
申请日：2001-05-02
申请人： Zhihua Sui , Mark J. Macielag
发明人： Zhihua Sui , Mark J. Macielag
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07D495/04
摘要： The present invention relates to novel &bgr;-carboline derivatives of the general formula wherein all the variables are as described within the specification, useful as phosphodiesterase inhibitors. The present invention further relates to use of the described derivatives for the treatment of diseases and conditions related to PDE, for example male erectile dysfunction.
摘要翻译：本发明涉及一般制剂的新型β-咔啉衍生物，其全部变量如本说明书所述，可用作磷酸二酯酶抑制剂。本发明还涉及所述衍生物用于治疗与PDE有关的疾病和病症（例如雄性勃起功能障碍）的用途。

59. 发明授权

US5494898A Peptide skeletal muscle relaxants 失效
标题翻译：肽骨骼肌松弛剂
公开(公告)号：US5494898A
公开(公告)日：1996-02-27
申请号：US303975
申请日：1994-09-09
申请人： Yea-Shun Cheng , Zenon D. Konteatis , Mark J. Macielag , David C. Palmer
发明人： Yea-Shun Cheng , Zenon D. Konteatis , Mark J. Macielag , David C. Palmer
IPC分类号： A61K38/00 , C07K5/02 , C07K5/087 , C07K5/09 , C07K5/097 , A61K38/06
CPC分类号： C07K5/0821 , C07K5/0202 , C07K5/0812 , C07K5/0815 , C07K5/0823 , A61K38/00
摘要： Novel diquaternary polypeptides possessing skeletal muscle relaxation activity represented by the formulae: ##STR1## wherein: R is lower alkyl; R.sub.1 and R.sub.2 are lower alkyl or R.sub.1 and R.sub.2, together with the nitrogen to which they are attached form a heterocyclic ring having 5 to 7 member atoms; R.sub.3 is lower alkyl, [N,N-di(lower alkyl)-3-piperidinium].sup.(+), or [N,N-di(lower alkyl)-4-piperidinium].sup.(+) R.sub.4 is selected from the group consisting of t-butyl, benzyl or fluorenylmethyl; A.sub.1 is selected from the group consisting of trans-4-acetoxyproline, phenylalanine, glutamic acid-.gamma.-methyl ester, or proline; AA.sub.2 is selected from the group consisting of phenylalanine, leucine, 3-(2-naphthyl)alanine, 3-(1-naphthyl)alanine, and 3-cyclohexylalanine; AA.sub.3 is proline when R.sub.3 is [N,N-di(lower alkyl)-3-piperidinium].sup.(+) or [N,N-di(lower alkyl)-4-piperidinium].sup.(+), and is Orn(.delta.-N.sup.(+) --R--R.sub.1 --R.sub.2) or Lys(.epsilon.-N.sup.(+) --R--R.sub.1 --R.sub.2) when R.sub.3 ia lower alkyl; AA.sub.4 is Orn(.delta.-N.sup.(+)--R--R.sub.1 --R.sub.2) or Lys(.epsilon.-N.sup.(+) --R--R.sub.1 --R.sub.2); Z.sup.(-) is a pharmaceutically acceptable anion; and (R).sub.m R.sub.1 R.sub.2 N.sup.(+) represents the acceptable anion; (R).sub.m R.sub.1 R.sub.2 N.sup.(+) -- represents the alpha amino group of AA.sub.1 ; and m represents an integer of 0 or 1 with the proviso that m is zero only when AA.sub.1 is trans-4-acetoxyproline or proline.
摘要翻译：具有由下式表示的骨骼肌松弛活性的新型二季铵化多肽：其中：R为低级烷基; R 1和R 2是低级烷基或R 1和R 2与它们所连接的氮一起形成具有5至7个成员原子的杂环; R3是低级烷基，[N，N-二（低级烷基）-3-哌啶鎓]（+）或[N，N-二（低级烷基）-4-哌啶鎓]（+）R 4选自叔丁基，苄基或芴基甲基; A1选自反式-4-乙酰氧基脯氨酸，苯丙氨酸，谷氨酸-γ-甲酯或脯氨酸; AA2选自苯丙氨酸，亮氨酸，3-（2-萘基）丙氨酸，3-（1-萘基）丙氨酸和3-环己基丙氨酸; 当R3是[N，N-二（低级烷基）-3-哌啶鎓]（+）或[N，N-二（低级烷基）-4-哌啶鎓]（+）时，AA3是脯氨酸，并且是Orn 当R3低级烷基时，N（+） - R-R1-R2）或Lys（ε-N（+） - R-R1-R2） AA4是Orn（Δ-N（+）-R-R1-R2）或Lys（ε-N（+）-R-R1-R2）; Z（ - ）是药学上可接受的阴离子; 和（R）mR1R2N（+）表示可接受的阴离子; （R）mR1R2N（+） - 表示AA1的α氨基; m表示0或1的整数，条件是仅当AA1为反式-4-乙酰氧基脯氨酸或脯氨酸时，m为0。

60. 发明授权

US5470830A Motilin-like polypeptides that inhibit gastrointestinal motor activity 失效
公开(公告)号：US5470830A
公开(公告)日：1995-11-28
申请号：US103489
申请日：1993-08-06
申请人： Mark J. Macielag , Ramalinga Dharanipragada , Mary S. Marvin
发明人： Mark J. Macielag , Ramalinga Dharanipragada , Mary S. Marvin
IPC分类号： C07K7/04 , A61K38/00 , A61P1/00 , C07K14/575 , C07K14/63 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K14/63 , A61K38/00
摘要： This invention pertains to polypeptides having gastrointestinal motor inhibitory activity represented by the formula: ##STR1## including optically active isomeric forms and the pharmaceutically acceptable acid addition salts thereof wherein A is the L-stereoisomer of a lipophilic aliphatic or alicyclic amino acid; B is selected from the group consisting of L and D aromatic, heteroaromatic, lipophilic aliphatic, and alicyclic amino acids; D is the L-stereoisomer of a lipophilic aliphatic or alicyclic amino acid; E is the L-stereoisomer of an aromatic, aliphatic, or alicyclic amino acid; F is the L-stereoisomer of an aromatic or heteroaromatic amino acid; G is glycine or D-alanine; H is L-glutamic acid or L-glutamine; I is L-glutamine, L-glutamic acid, or L-alanine; J is a direct bond between I and group --NH-- or is selected from the group consisting of Z, Z-Leu, Z-Leu-Gln, Z-Leu-Gln-Glu (SEQ ID NO:2), Z-Leu-Gln-Glu-Lys (SEQ ID NO:3), Zleu-Gln-Glu-Lys-Glu (SEQ ID NO:4), Z-Leu-Gln-Glu-Lys-Glu-Arg (SEQ ID NO:5), ZLeu-Gln-Glu-Lys-Glu-Arg-Asn (SEQ ID NO:6), Z-Leu-Gln-Glu-Lys-Glu-Arg-AsnLys (SEQ ID NO:7), and Z-Leu-Gln-Glu-Lys-Glu-Arg-Asn-Lys-Gly (SEQ ID NO:8), wherein Z is selected from the group consisting of arginine, D-arginine, D-homoarginine, D-lysine, D-ornithine, D-2,4-diaminobutyric acid, D-glutamine, D-asparagine, and D-alanine; R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl; R.sub.3 is selected from the group consisting of lower-alkyl, cycloalkyl, substituted and unsubstituted aryl, and heteroaryl, wherein the aryl group may be substituted with one or more substituents selected from the group consisting of halogen, hydroxy, and lower-alkoxy; R.sub.4 is selected from the group consisting of --CH.sub.2 CONH.sub.2, aminoalkyl groups containing from 1 to 3 carbon atoms, and guanidinoalkyl groups containing 2 or 3 carbon atoms; R.sub.5 is --COOH or --CONH.sub.2 ; and the symbol * represents an asymmetric carbon atom which may be in the D or L configuration, and each lower-alkyl group contains from 1 to 4 carbon atoms, with the proviso that R.sub.4 is --CH.sub.2 CONH.sub.2 only when J is Z-Leu or Z-Leu-Gln-Glu-Lys-Glu-Arg-Asn-Lys-Gly (SEQ ID NO:8).

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