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公开(公告)号：US20090069272A1
公开(公告)日：2009-03-12
申请号：US12001318
申请日：2007-12-11
IPC分类号： A61K31/675 , C07F9/38
CPC分类号： C07F9/5765
摘要： Disclosed is a new composition of matter, substantially enantiomerically pure (1R,6S)-2-Azabicyclo-[4.3.0]nonane-8,8-diphosphonic acid, methods of preparing this new composition of matter, a pharmaceutical composition comprising the new composition, and administration of the composition in methods of treating bone disorders such as osteoporosis, osteolytic bone metastasis, rheumatoid arthritis and osteoarthritis.
摘要翻译： 公开了一种新的物质组合物，基本上为对映异构体纯的（1R，6S）-2-氮杂双环[4.3.0]壬烷-8,8-二膦酸，制备这种新的物质组合物的方法，包含新的 组合物和组合物在治疗骨质疏松症，溶骨性骨转移，类风湿性关节炎和骨关节炎等骨病的方法中的用途。
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公开(公告)号：US07132539B2
公开(公告)日：2006-11-07
申请号：US10689022
申请日：2003-10-20
IPC分类号： C07D403/12 , C07D241/04 , A61K31/495 , A61K31/496
CPC分类号： C07D401/12 , C07D241/04 , C07D241/08 , C07D403/12
摘要： The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched alkyl, C3–C8 cyclic alkyl, C2–C12 linear or branched alkenyl, or haloalkyl, for example, the 2-keto-3-alkylpiperazines having the formula: wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, and 4-chlorophenyl; R1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, sec-butyl, tert-butyl, cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl, benzyl, allyl, 1-methylallyl, 2-methylallyl, but-2-enyl, and propargyll; R7a is selected from the group consisting of hydrogen, —CO2H, —CONH2, —CONHCH3, and —CON(CH3)2; R8 is benzyl, substituted benzyl, or naphthalen-2-ylmethyl.
摘要翻译： 本发明涉及包含由选自C 1 -C 12烷基的R 1烷基单元取代的含氮环支架的化合物， 直链或支链烷基，C 3 -C 8环烷基，C 2 -C 12直链状 或支链烯基或卤代烷基，例如具有下式的2-酮-3-烷基哌嗪：其中R选自苯基，3-氟苯基，4-氟苯基，3,5-二氟苯基和4-氟苯基， 氯苯基; R 1选自甲基，乙基，丙基，异丙基，丁基，异丁基，仲丁基，叔丁基，环丙基，环丙基甲基，环戊基，环戊基甲基，环己基， 环己基甲基，苄基，烯丙基，1-甲基烯丙基，2-甲基烯丙基，丁-2-烯基和炔丙基; R 7a选自氢，-CO 2 H，-CONH 2，-CONHCH 3，/ SUB >和-CON（CH 3 3）2。 R 8是苄基，取代的苄基或萘-2-基甲基。
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公开(公告)号：US5856314A
公开(公告)日：1999-01-05
申请号：US240303
申请日：1994-05-09
IPC分类号： A61K31/675 , A61P3/00 , A61P3/14 , A61P19/10 , A61P29/00 , A61P43/00 , C07F9/38 , C07F9/40 , C07F9/553 , C07F9/572 , C07F9/576 , C07F9/58 , C07F9/59 , C07F9/6506 , C07F9/6512 , C07F9/653 , C07F9/6539 , C07F9/6561 , A61K31/67 , A61K31/665
CPC分类号： C07F9/6561 , C07F9/3808 , C07F9/5532 , C07F9/5721 , C07F9/5765 , C07F9/582 , C07F9/588 , C07F9/592 , C07F9/598 , C07F9/65061 , C07F9/65127
摘要： The present invention relates to thio-substituted, nitrogen-containing heterocyclic phosphonate compounds, including bisphosphonates, phosphonoalkylphosphinates, phosphonocarboxylates, and phosphonosulfonates, and the pharmaceutically-acceptable salts and esters thereof useful for the treatment and prevention of osteoporosis and arthritis. These compounds have the general structure: ##STR1## (a) Z is a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N, at least one of which is N;(b) Q is covalent bond; O, S, N, or NR.sub.1 ;(c) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is substituted or unsubstituted C.sub.1 -C.sub.8 alkyl;(d) each R1 is independently selected from --SR.sup.6 ; --R.sup.8 SR.sup.6 ; nil; hydrogen; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; unsubstituted or substituted aryl; hydroxy; --CO.sub.2 R.sup.3 ; --O.sub.2 CR.sup.3 ; --NR.sup.3.sub.2 ; --OR.sup.3 ; --C(O)N(R.sup.3).sub.2 ; --N(R.sup.3)C(O)R.sup.3 ; substituted or unsubstituted benzyl; nitro; or combinations thereof;(e) R.sup.2 is one or more substituents on atoms in the Z moiety and is independently selected from --SR.sup.6 and --R.sup.8 SR.sup.6 ; where R.sup.6 is H; --CO.sub.2 R.sup.3 ; --O.sub.2 CR.sup.3 ; --NR.sup.3.sub.2 ; --N(R).sup.3 C(O)R.sup.3 ; and nil; hydrogen; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; unsubstituted or substituted aryl; hydroxy; substituted or unsubstituted benzyl; nitro; or combinations thereof;(f) each R.sup.3 is independently selected from hydrogen; substituted or unsubstituted C.sub.1 -C.sub.8 alkyl; or R.sup.8 SR.sup.6 ;(g) R.sup.5 is selected from --SR.sup.6 ; R.sup.8 SR.sup.6, hydrogen; hydroxy; amino; halogen; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; and(h) R.sup.6 is independently selected from H; --C(O)R.sup.7 ; C(S)R.sup.7 ; C(O)NR.sup.7.sub.2 ; C(S)NR.sup.7.sub.2 ; .sup.C(O)(OR7); and C(S)(OR.sup.7); wherein R.sup.7 is hydrogen; or unsubstituted or substituted C.sub.1 -C.sub.8 alkyl;(i) R.sup.8 is a substituted or unsubstituted C.sub.1 -C.sub.8 alkyl; and at least one of R.sup.1, R.sup.2, R.sup.3 or R.sup.5 must be SR.sup.6 or R.sup.8 SR.sup.6.
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14.发明授权
公开(公告)号：US5824661A
公开(公告)日：1998-10-20
申请号：US301514
申请日：1994-09-07
IPC分类号： A61K31/66 , A61K31/662 , A61K31/663 , A61K31/665 , A61K31/67 , A61K31/675 , A61P3/00 , A61P3/14 , A61P19/08 , A61P19/10 , A61P29/00 , A61P43/00 , C07F20060101 , C07F9/30 , C07F9/38 , C07F9/40 , C07F9/547 , C07F9/553 , C07F9/572 , C07F9/576 , C07F9/58 , C07F9/59 , C07F9/6506 , C07F9/6512 , C07F9/655 , C07F9/6553 , C07F9/6561
CPC分类号： C07F9/6561 , C07F9/3808 , C07F9/5532 , C07F9/5721 , C07F9/5765 , C07F9/582 , C07F9/588 , C07F9/592 , C07F9/598 , C07F9/65061 , C07F9/65127
摘要： Compounds of the formula ##STR1## where m and n are integers 0 to 10 and m+n equals 0 to 10, (a) X is O or S(b) Z is a covalent bond; a monocyclic or polycyclic carbocycle ring moiety; or a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N; (c) Q is covalent bond; O; or S; (d) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is C.sub.1 -C.sub.8 alkyl; (e) R.sup.1, R.sup.2 and R.sup.5 are as defined in the claims. are useful in the treatment of calcium and phosphate elated disorders, such as arthritis and the like.
摘要翻译： 其中m和n为整数0至10且m + n的化合物等于0至10，（a）X为O或S（b）Z为共价键; 单环或多环碳环部分; 或含有一个或多个选自O，S或N的杂原子的单环或多环杂环部分; （c）Q是共价键; O; 或S; （d）R是COOH，SO 3 H，PO 3 H 2或P（O）（OH）R 4，其中R 4是C 1 -C 8烷基; （e）R1，R2和R5如权利要求中所定义。 可用于治疗钙和磷酸盐激动症，例如关节炎等。
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15.发明授权Phosphonocarboxylate compounds pharmaceutical compositions, and methods for treating abnormal calcium and phosphate metabolism 失效膦酰基化合物化合物药物组合物，以及治疗异常钙和磷酸盐代谢的方法
公开(公告)号：US5760021A
公开(公告)日：1998-06-02
申请号：US55810
申请日：1993-05-07
IPC分类号： A61K20060101 , A61K31/215 , A61K31/66 , A61K31/662 , A61K31/665 , A61K31/67 , A61K31/675 , C07F20060101 , C07F9/38 , C07F9/547 , C07F9/572 , C07F9/576 , C07F9/6503 , C07F9/6561 , A01N57/00
CPC分类号： C07F9/3873
摘要： The present invention relates to compositions comprising pharnaceutically-acceptable carriers and a phosphonocarboxylate, or a pharmaceutically-acceptable salt thereof, having a structure according to formula (I): ##STR1##
摘要翻译： 本发明涉及包含药物学上可接受的载体和具有根据式（I）的结构的膦酰基羧酸酯或其药学上可接受的盐的组合物：
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![Imidazo[1,2-a] pyridinyl bisphosphonates](/abs-image/US/2013/12/31/US08618079B2/abs.jpg.150x150.jpg)
公开(公告)号：US08618079B2
公开(公告)日：2013-12-31
申请号：US13120078
申请日：2009-09-22
IPC分类号： A61K31/675
CPC分类号： C07D471/04 , C07F9/65068
摘要： Novel imidazo[1,2-α]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
摘要翻译： 公开了新的咪唑并[1,2-α]吡啶基双膦酸盐化合物，以及制备化合物的方法，包括该化合物的药物组合物，以及在治疗异常钙和磷酸盐代谢的方法中施用化合物，包括骨和关节疾病 和其他疾病。
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公开(公告)号：US08314081B2
公开(公告)日：2012-11-20
申请号：US12912514
申请日：2010-10-26
IPC分类号： A61K31/675 , A61P19/00 , A61P29/00 , C07F9/6574
CPC分类号： C07F9/65746 , C07F9/657181
摘要： Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
摘要翻译： 公开了新的二膦酸酯环状缩醛化合物，以及制备化合物的方法，包括该化合物的药物组合物，以及在治疗骨代谢障碍（例如钙和磷酸钙代谢异常）的方法中给予化合物。
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公开(公告)号：US20110098251A1
公开(公告)日：2011-04-28
申请号：US12912514
申请日：2010-10-26
IPC分类号： A61K31/675 , C07F9/6574 , A61P19/00 , A61P29/00
CPC分类号： C07F9/65746 , C07F9/657181
摘要： Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
摘要翻译： 公开了新的二膦酸酯环状缩醛化合物，以及制备化合物的方法，包括该化合物的药物组合物，以及在治疗骨代谢障碍（例如钙和磷酸钙代谢异常）的方法中给予化合物。
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公开(公告)号：US06951916B2
公开(公告)日：2005-10-04
申请号：US10612104
申请日：2003-07-02
IPC分类号： A61K38/00 , A61K38/12 , A61K38/34 , A61P3/04 , A61P5/06 , A61P5/14 , A61P5/40 , A61P7/08 , A61P9/00 , A61P15/00 , A61P15/08 , A61P15/10 , A61P21/00 , A61P25/00 , A61P25/14 , A61P25/28 , A61P29/00 , A61P31/04 , A61P43/00 , C07K7/02 , C07K7/54 , C07K7/64 , C07K14/68 , C07K14/685 , C07K7/50
CPC分类号： C07K14/685 , A61K38/00 , C07K14/68
摘要： Disclosed are MC-4 and/or MC-3 receptor ligands having the formula: wherein B is a suitable linking group comprising a least one amino acid.
摘要翻译： 公开了具有下式的MC-4和/或MC-3受体配体：其中B是包含至少一个氨基酸的合适的连接基团。
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公开(公告)号：US06613874B1
公开(公告)日：2003-09-02
申请号：US09537789
申请日：2000-03-29
IPC分类号： C07K750
CPC分类号： C07K14/685 , A61K38/00 , C07K14/68
摘要： Disclosed are cyclic peptide analogs that are MC-4 and/or MC-3 receptor ligands, the analogs having a structure according to Formula (I): wherein B, X, E, Z, D, G, M′, W, R, R1, R1′, R11, m, n, p and q are as described in the specification. The peptide analogs are useful in treating diseases that are mediated by the MC-4 and/or the MC-3 receptor. As such, the invention is directed to methods of treating body weight disorders, such as obesity, anorexia, and cachexia. The invention also relates to the treatment of CNS depression, behavior-related disorders, memory-related disorders, cardiovascular function, inflammation, sepsis, septic shock, cardiogenic shock, hypovolemic shock, sexual dysfunction, erectile dysfunction, muscle atrophy, diseases associated with nerve growth and repair, and intrauterine fetal growth. Also disclosed are pharmaceutical compositions comprising the peptide analogs of Formula (I).
摘要翻译： 公开了作为MC-4和/或MC-3受体配体的环肽类似物，该类似物具有式（I）的结构：其中B，X，E，Z，D，G，M'，W，R ，R1，R1'，R11，m，n，p和q如说明书中所述。 肽类似物可用于治疗由MC-4和/或MC-3受体介导的疾病。 因此，本发明涉及治疗体重障碍，例如肥胖症，厌食症和恶病质的方法。 本发明还涉及CNS抑郁症，行为相关障碍，记忆相关障碍，心血管功能，炎症，败血症，败血症休克，心源性休克，血容量不足休克，性功能障碍，勃起功能障碍，肌肉萎缩，与神经相关的疾病 生长和修复，宫内胎儿生长。 还公开了包含式（I）的肽类似物的药物组合物。
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