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1. 发明申请

US20150152047A1 BENZAMIDE DERIVATIVE 有权
标题翻译：苯甲酸衍生物
公开(公告)号：US20150152047A1
公开(公告)日：2015-06-04
申请号：US14396678
申请日：2013-04-24
申请人： Chugai Seiyaku Kabushiki Kaisha
发明人： Takeshi Murata , Satoshi Niizuma , Sousuke Hara , Hatsuo Kawada , Kihito Hada , Hideaki Shimada , Hiroshi Tanaka , Yoshito Nakanishi
IPC分类号： C07C321/28 , C07D487/08 , C07D309/14 , C07C317/14 , C07D213/82
CPC分类号： C07C321/28 , C07C317/14 , C07C317/34 , C07C317/40 , C07C323/42 , C07C323/48 , C07C2601/02 , C07D205/04 , C07D207/09 , C07D207/12 , C07D207/14 , C07D211/26 , C07D211/56 , C07D211/68 , C07D213/62 , C07D213/82 , C07D241/04 , C07D263/34 , C07D295/14 , C07D295/16 , C07D309/14 , C07D401/12 , C07D403/04 , C07D487/08
摘要： The present invention relates to benzamide derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及由式（I）表示的苯甲酰胺衍生物或其药学上可接受的盐。

2. 发明授权

US06277865B1 Piperididinyl and N-amidinopiperidinyl derivatives 有权
标题翻译：哌啶基和N-脒基哌啶基衍生物
公开(公告)号：US06277865B1
公开(公告)日：2001-08-21
申请号：US09273618
申请日：1999-03-22
申请人： Scott I. Klein , Kevin R. Guertin
发明人： Scott I. Klein , Kevin R. Guertin
IPC分类号： A61K31445
CPC分类号： C07C45/63 , A01N43/40 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4462 , A61K31/4465 , A61K31/454 , A61K31/4545 , A61K31/47 , C07C205/57 , C07C255/60 , C07C257/18 , C07C259/18 , C07C2601/14 , C07C2603/08 , C07D205/08 , C07D207/327 , C07D209/08 , C07D209/48 , C07D211/00 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/34 , C07D211/68 , C07D211/70 , C07D213/40 , C07D213/54 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/70 , C07D213/82 , C07D213/89 , C07D215/04 , C07D215/48 , C07D231/12 , C07D231/14 , C07D233/56 , C07D233/64 , C07D235/06 , C07D249/06 , C07D249/08 , C07D277/56 , C07D285/08 , C07D317/60 , C07D319/18 , C07D401/04 , C07D401/12 , C07D409/04 , C07D409/14 , C07D417/04 , C07D471/04 , C07C47/565
摘要： This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
摘要翻译：本发明涉及通过将所述化合物与含有因子Xa的组合物组合而可用于抑制因子Xa的活性的式I化合物。本发明还涉及包含式I化合物的组合物，其制备方法，其用途，例如抑制凝血酶的形成或用于治疗患有或与生理学相关的疾病状态患者或受其影响的患者有害的过量凝血酶。

3. 发明授权

US3851059A Method for the stimulation of appetite in patients 失效
标题翻译：刺激患者感冒的方法
公开(公告)号：US3851059A
公开(公告)日：1974-11-26
申请号：US28068372
申请日：1972-08-14
申请人： MERCK & CO INC
发明人： PRUGH J
IPC分类号： A61K31/445 , C07D211/68 , A61K27/00
CPC分类号： C07D211/68 , A61K31/445
摘要： 1. A METHOD FOR THE STIMULATION OF APPETITE IN HUMAN PATIENTS HAVING A LOW APPETITE OR WHO EXHIBIT SYMPTOMS OF MALNUTRITION WHICH COMPRISES ADMINISTERING TO SAID PATIENT AN EFFECTIVE APPETITE STIMULATING AMOUNT OF FROM 0.1 TO 50 MG. OF 1-METHYL-4-(10,11-DIHYDRO-10-OXO-5HDIBENZO(A,D)CYCLOHEPTEN-5 -YLIDENE)PIPERIDINE OR AN ACID ADDITION SALT THEREOF.

4. 发明授权

US3845211A Method for treating allergic disorders due to histamine 失效
标题翻译：用于治疗组胺的过敏性疾病的方法
公开(公告)号：US3845211A
公开(公告)日：1974-10-29
申请号：US18009571
申请日：1971-09-13
申请人： MERCK & CO INC
发明人： PRUGH J
IPC分类号： A61K31/445 , C07D211/68 , A61K27/00
CPC分类号： C07D211/68 , A61K31/445
摘要： 1. A METHOD FOR THE TREATMENT OF ALLERGIC DISORDERS DUE TO HISTAMINE WHICH COMPRISES ADMINISTERING TO HUMAN PATIENTS AN EFFECTIVE ANTIHISTAMINIC AMOUNT OF COMPOUND HAVING THE FORMULA

5-(1-(H3C-)-PIPERIDIN-4-YL=),10-(O=)-10,11-DIHYDRO-5H-

DIBENZO(A,D)CYCLOHEPTENE

5. 发明授权

US08481527B2 Benzamide derivatives as bradykinin antagonists 有权
标题翻译：苯甲酰胺衍生物作为缓激肽拮抗剂
公开(公告)号：US08481527B2
公开(公告)日：2013-07-09
申请号：US12447157
申请日：2007-10-27
申请人： Istvan Vago , Gyula Beke , Eva Bozo , Sandor Farkas , Katalin Hornok , Gyorgy Keseru , Eva Schmidt , Eva Szentirmay , Monika Vastag
发明人： Istvan Vago , Gyula Beke , Eva Bozo , Sandor Farkas , Katalin Hornok , Gyorgy Keseru , Eva Schmidt , Eva Szentirmay , Monika Vastag
IPC分类号： C07D207/08 , C07D211/18 , C07D211/44 , C07D211/22 , C07D211/58 , C07D211/26 , C07D211/62 , C07D207/26 , C07D211/34 , C07D211/68 , A61K31/18 , A61P29/00
CPC分类号： C07D295/185 , C07D207/08 , C07D207/26 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/44 , C07D211/58 , C07D211/62 , C07D211/68 , C07D211/76 , C07D219/06 , C07D223/10 , C07D239/42 , C07D241/06 , C07D241/20 , C07D243/08 , C07D279/12 , C07D295/20 , C07D295/26 , C07D307/14 , C07D307/24 , C07D307/68 , C07D401/06 , C07D487/08
摘要： The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I) wherein R1-R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要翻译：本发明涉及式（I）的新的苯基氨磺酰基苯甲酰胺衍生物，其中R 1 -R 5和Z如权利要求中所定义，和作为选择性拮抗剂的光学对映体或外消旋物和/或其盐和/或水合物和/或溶剂合物缓激肽B1，制备这些化合物的方法，含有它们的药物组合物及其在治疗或预防疼痛和炎症病症中的用途。

6. 发明授权

US08076329B2 Histamine H3-receptor ligands and their therapeutic applications 有权
标题翻译：组胺H3受体配体及其治疗应用
公开(公告)号：US08076329B2
公开(公告)日：2011-12-13
申请号：US11912816
申请日：2006-04-25
申请人： Isabelle Bertrand , Marc Capet , Jeanne-Marie Lecomte , Nicolas Levoin , Xavier Ligneau , Olivia Poupardin-Olivier , Philippe Robert , Jean-Charles Schwartz , Olivier Labeeuw
发明人： Isabelle Bertrand , Marc Capet , Jeanne-Marie Lecomte , Nicolas Levoin , Xavier Ligneau , Olivia Poupardin-Olivier , Philippe Robert , Jean-Charles Schwartz , Olivier Labeeuw
IPC分类号： A61K31/4418 , A61K31/4453 , A61K31/4545 , A61K31/5355 , C07D213/30 , C07D211/14 , C07D413/12
CPC分类号： C07D213/30 , C07D207/20 , C07D207/30 , C07D207/335 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/68 , C07D211/70 , C07D213/61 , C07D213/64 , C07D213/89 , C07D231/12 , C07D295/088 , C07D295/192 , C07D333/16 , C07D333/20 , C07D401/12 , C07D401/14 , C07D409/12 , C07D413/12
摘要： The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2与它们所连接的氮原子一起形成单或双环饱和含氮环; 它们的制备及其作为H3受体配体的用途，用于治疗例如中枢神经系统疾病如阿尔茨海默病。

7. 发明授权

US6096761A Esters of 3-hydroxy-piperidinemethanol derivatives 有权
公开(公告)号：US6096761A
公开(公告)日：2000-08-01
申请号：US117980
申请日：1998-08-11
申请人： Jean-Paul Rene Marie Bosmans , John Christopher Love , Michel Anna Jozef Decleyn , Henri Elisabeth Frans D'Haen
发明人： Jean-Paul Rene Marie Bosmans , John Christopher Love , Michel Anna Jozef Decleyn , Henri Elisabeth Frans D'Haen
IPC分类号： A01N43/40 , A01N43/58 , C07D211/68 , C07D237/30 , C07D401/00
CPC分类号： A01N43/40 , A01N43/58 , C07D211/68 , C07D237/30 , C07D401/00
摘要： The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R.sup.1 is C.sub.1-6 alkyloxy, C.sub.2-6 alkenyloxy or C.sub.2-6 alkynyloxy; R.sup.2 is hydrogen or C.sub.1-6 alkyloxy, or when taken together R.sup.1 and R.sup.2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl; R.sup.3 is hydrogen or halo; R.sup.4 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.2-6 alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R.sup.5 -, Alk-X--R.sup.6, -Alk-Y--C(.dbd.O)--R.sup.8, or -Alk-Y--C(.dbd.O)--NR.sup.10 R.sup.11 wherein each Alk is C.sub.1-12 alkanediyl; and R.sup.5 is hydrogen, cyano, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, aryl, di(aryl)methyl or a heterocyclic ringsystem; R.sup.6 is hydrogen, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, aryl or heterocyclic ringsystem; X is O, S, SO.sub.2 or NR.sup.7 ; said R.sub.7 being hydrogen, C.sub.1-6 alkyl or aryl; R.sup.8 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, aryl, arylC.sub.1-6 alkyl, di(aryl)methyl, C.sub.1-6 alkyloxy or hydroxy; Y is NR.sup.9 or a direct bond; said R.sup.9 being hydrogen, C.sub.1-6 alkyl or aryl R.sup.10 and R.sup.11 each independently are hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, aryl or arylC.sub.1-6 alkyl, or R.sup.10 and R.sup.11 combined with the nitrogen atom bearing R.sup.10 and R.sup.11 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C.sub.1-6 alkyl, amino or mono or di(C.sub.1-6 alkyl)amino, or said R.sup.10 and R.sup.11 combined with the nitrogen bearing R.sup.10 and R.sup.11 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C.sub.1-6 alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

8. 发明授权

US3981876A 1-Alkyl-4-(10[1-p iperidyl]-5H-dibenzo-[a,d]cyclohepten-5-ylidene)piperidine compounds 失效
标题翻译： 1-烷基-4-（10 {8 1-哌啶基{9 -5H-二苯并 - {8a，d {9环庚烯-5-亚基）哌啶化合物
公开(公告)号：US3981876A
公开(公告)日：1976-09-21
申请号：US280697
申请日：1972-08-14
申请人： John D. Prugh
发明人： John D. Prugh
IPC分类号： A61K31/445 , C07D211/68 , C07D211/28
CPC分类号： C07D211/68 , A61K31/445
摘要： The new 1-alkyl-4-(10-oxo or -hydroxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds are prepared from the corresponding 10-desoxy compounds having a double bond at the 10,11-position by a process involving bromination, dehydrobomination of the resulting dibromo compound, followed by enamine formation and hydrolysis to give the desired 10-oxo compound. The compounds prepared in this manner are active as antihistamines and as appetite stimulants.
摘要翻译：从相应的10-脱氧化合物制备新的1-烷基-4-（10-氧代或 - 羟基-10,11-二氢-5H-二苯并[a，d]环庚烯-5-亚基） - 哌啶化合物，其具有通过涉及溴化的方法在10,11位双键，得到的二溴化合物脱氢，然后进行烯胺形成和水解，得到所需的10-氧代化合物。以这种方式制备的化合物作为抗组胺剂和作为食欲兴奋剂是有活性的。

9. 发明授权

US3960872A 1 Alkyl-4-(10:oxo or hydroxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds 失效
标题翻译： 1烷基-4-（10：氧代或羟基-10,11-二氢-5H-二苯并{8a，d {9环庚烯-5-亚基） - 哌啶化合物
公开(公告)号：US3960872A
公开(公告)日：1976-06-01
申请号：US280685
申请日：1972-08-14
申请人： John D. Prugh
发明人： John D. Prugh
IPC分类号： A61K31/445 , C07D211/68 , C08F2/50 , C07D211/32
CPC分类号： C07D211/68 , A61K31/445 , C08F2/50
摘要： The new 1-alkyl-4-(10-oxo or -hydroxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds are prepared from the corresponding 10-desoxy compounds having a double bond at the 10,11-position by a process involving bromination, dehydrobromination of the resulting dibromo compound, followed by enamine formation and hydrolysis to give the desired 10-oxo compound. The compounds prepared in this manner are active as antihistamines and as appetite stimulants.
摘要翻译：从相应的10-脱氧化合物制备新的1-烷基-4-（10-氧代或 - 羟基-10,11-二氢-5H-二苯并[a，d]环庚烯-5-亚基） - 哌啶化合物，其具有通过涉及溴化的方法在10,11位双键，得到的二溴化合物的脱溴化氢，然后进行烯胺的形成和水解，得到所需的10-氧代化合物。以这种方式制备的化合物作为抗组胺剂和作为食欲兴奋剂是有活性的。

10. 发明授权

US09289430B2 Compounds and methods for inhibiting phosphate transport 有权
公开(公告)号：US09289430B2
公开(公告)日：2016-03-22
申请号：US14337028
申请日：2014-07-21
申请人： Ardelyx, Inc.
发明人： Jason G. Lewis , Jeffrey W. Jacobs , Nicholas Reich , Michael R. Leadbetter , Noah Bell , Han-Ting Chang , Tao Chen , Marc Navre , Dominique Charmot , Christopher Carreras , Eric Labonte
IPC分类号： A61K31/4439 , A61K31/454 , C07D401/12 , A61K31/5377 , A61K31/4965 , A61K31/505 , A61K45/06 , C07D211/68 , C07D231/40 , C07D233/88 , C07D255/02 , C07D277/46 , C07D285/135 , A61K31/415 , A61K31/4545 , A61K31/59 , C07D249/14
CPC分类号： A61K31/5377 , A61K31/415 , A61K31/454 , A61K31/4545 , A61K31/4965 , A61K31/505 , A61K31/59 , A61K45/06 , C07D211/68 , C07D231/40 , C07D233/88 , C07D249/14 , C07D255/02 , C07D277/46 , C07D285/135 , C07D401/12 , A61K2300/00
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

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