公开(公告)号：WO2007137107A2

公开(公告)日：2007-11-29

申请号：PCT/US2007/069112

申请日：2007-05-17

Applicant: ABBOTT LABORATORIES ,  IYENGAR, Rajesh, R. ,  ZHAO, Gang ,  FREEMAN, Jennifer, C. ,  GAO, Ju ,  JUDD, Andrew, S. ,  KYM, Philip, R. ,  LYNCH, John, K. ,  MULHERN, Mathew, M. ,  SOUERS, Andrew, J.

Inventor： IYENGAR, Rajesh, R. ,  ZHAO, Gang ,  FREEMAN, Jennifer, C. ,  GAO, Ju ,  JUDD, Andrew, S. ,  KYM, Philip, R. ,  LYNCH, John, K. ,  MULHERN, Mathew, M. ,  SOUERS, Andrew, J.

IPC: C07C211/22 ,  C07C275/30 ,  C07C279/18 ,  C07C335/16 ,  C07D213/55 ,  C07D213/75

CPC classification number: C07C335/22 ,  C07C229/46 ,  C07C275/30 ,  C07C275/32 ,  C07C275/38 ,  C07C279/28 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/55 ,  C07D213/75 ,  C07D277/30 ,  C07D333/22 ,  C07D333/36 ,  C07D401/04 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: The present invention relates to compounds of formula (I) wherein R 1 , R 3 , X, Q, Z, A, D, m, and n are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.

Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 3，X，Q，Z，A，D，m和n如本文所定义。 还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。

公开(公告)号：WO02044139A1

公开(公告)日：2002-06-06

申请号：PCT/FR2001/003784

申请日：2001-11-30

IPC: C07D295/18 ,  A61K31/18 ,  A61K31/235 ,  A61K31/40 ,  A61K31/421 ,  A61K31/423 ,  A61K31/553 ,  A61P1/00 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P15/00 ,  A61P17/02 ,  C07C69/76 ,  C07C211/40 ,  C07C225/20 ,  C07C229/46 ,  C07C237/30 ,  C07C255/58 ,  C07C311/08 ,  C07C311/13 ,  C07C311/21 ,  C07C311/24 ,  C07C317/22 ,  C07D263/10 ,  C07D263/58 ,  C07D267/02 ,  A61K31/195

CPC classification number: C07C311/21 ,  C07C229/46 ,  C07C311/08 ,  C07C317/22 ,  C07C2601/14

Abstract: The invention concerns compounds of formula (I), wherein: A is a group of formula (a) or (b), their salts or solvates, pharmaceutical compositions containing them, a method for preparing them and intermediates used in said method. The compounds of formula (I) can be prescribed for treating gastro-intestinal diseases such as inflammatory diseases of the intestine such as irritable colon syndrome (IBS), as modulators of intestinal motricity, as lipolytic agents against obesity, anti-diabetic agents, psychotropic agents, anti-glaucoma agents, healing agents, antidepressants, as uterine contraction inhibitors, as tocolytic agents for preventing or delaying premature deliveries, for treating and/or preventing dysmenorrhea. In addition, the compounds of formula (I) can be used in the treatment of certain diseases of the central nervous system, such as for example depression, and certain disorders of the urinary system such as urinary incontinence.

Abstract translation: 本发明涉及式（I）化合物，其中：A为式（a）或（b）的基团，其盐或溶剂化物，含有它们的药物组合物，其制备方法和用于所述方法的中间体。 式（I）化合物可用于治疗诸如肠易激综合征（IBS）等胃肠疾病，肠易激综合征的调节剂，作为抗肥胖症的抗脂解剂，抗糖尿病药，精神药物 代谢剂，抗青光眼剂，愈合剂，抗抑郁药，作为子宫收缩抑制剂，作为用于预防或延缓过早输送的溶瘤剂，用于治疗和/或预防痛经。 此外，式（I）化合物可用于治疗中枢神经系统的某些疾病，例如抑郁症，以及泌尿系统的某些疾病如尿失禁。

公开(公告)号：WO01092213A2

公开(公告)日：2001-12-06

申请号：PCT/US2001/010832

申请日：2001-05-24

IPC: A61K31/17 ,  A61K31/18 ,  A61K31/27 ,  A61P25/00 ,  C07C229/46 ,  C07C271/12 ,  C07C271/22 ,  C07C271/24 ,  C07C271/28 ,  C07C271/30 ,  C07C275/18 ,  C07C275/24 ,  C07C275/28 ,  C07C311/19 ,  C07C335/16 ,  C07C271/00

CPC classification number: C07C335/16 ,  C07B2200/07 ,  C07C229/46 ,  C07C271/22 ,  C07C271/24 ,  C07C271/28 ,  C07C271/30 ,  C07C275/18 ,  C07C275/24 ,  C07C275/28 ,  C07C311/19 ,  C07C2601/02 ,  C07C2601/14

Abstract: Compounds of the formula (I) in which: R is (CH2)nY; n is 1 or 2; Y is NHSO2R or X -W-X -R ; X is O or NH; W is C=O, C=S, C=NH, or SO2; X is O or NH, provided that X and X are not both O; R is C1-10 alkyl; C2-10 alkenyl; C2-10 alkynyl; aryl; aryl-C1-10 alkyl; aryl-C2-10 alkenyl; aryl-C2-10 alkynyl; C3-8 cycloalkyl or C3-8-cycloalkyl-C1-10 alkyl; and R is hydrogen, C1-10 alkyl; C2-10 alkenyl; C2-10 alkynyl; aryl; aryl-C1-10 alkyl; aryl-C2-10 alkenyl; aryl-C2-10 alkynyl; C3-8 cycloalkyl; or C3-8-cycloalkyl-C1-10 alkyl; or a salt or ester thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system.

Abstract translation: 式（I）的化合物，其中：R 1是（CH 2）n Y; n为1或2; Y是NHSO 2 R 2或X 1 -W-X 2 -R 3; X 1是O或NH; W为C = O，C = S，C = NH或SO 2; X 2是O或NH，条件是X 1和X 2不都是O; R 2为C 1-10烷基; C 2-10烯基; C 2-10炔基; 芳基; 芳基-C 1-10烷基; 芳基-C 2-10烯基; 芳基-C 2-10炔基; C 3-8环烷基或C 3-8 - 环烷基-C 1-10烷基; 和R 3是氢，C 1-10烷基; C 2-10烯基; C 2-10炔基; 芳基; 芳基-C 1-10烷基; 芳基-C 2-10烯基; 芳基-C 2-10炔基; C3-8环烷基; 或C 3-8 - 环烷基-C 1-10烷基; 或其盐或酯调节代谢型谷氨酸受体功能，并且可用于治疗中枢神经系统疾病。

公开(公告)号：WO01085669A1

公开(公告)日：2001-11-15

申请号：PCT/CA2001/000650

申请日：2001-05-11

IPC: A61P25/00 ,  C07C229/46 ,  C07C229/50 ,  A61K31/196

CPC classification number: C07C229/50 ,  C07C229/46 ,  C07C2603/94

Abstract: The present invention relates to therapeutically active novel spiro[2.4]heptane amino carboxy compounds and derivatives thereof. Also provided is a method of preparing compounds of Formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract translation: 本发明涉及治疗活性的新型螺[2.4]庚烷氨基羧基化合物及其衍生物。 还提供制备式（I）化合物的方法和包含该化合物的药物组合物。 新型化合物作为代谢型谷氨酸受体的调节剂，因此可用于治疗与代谢型谷氨酸受体系统相关的中枢神经系统疾病。

公开(公告)号：WO00075102A1

公开(公告)日：2000-12-14

申请号：PCT/EP2000/004896

申请日：2000-05-26

IPC: A61K31/195 ,  C07C229/46

CPC classification number: C07C229/46 ,  C07B2200/07 ,  C07C2601/02

Abstract: Compounds of the formula (I) in which R is C1-10 alkyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system.

Abstract translation: 其中R 1为C 1-10烷基的式（I）化合物; C2-10烯基; C 2-10炔基; 苯基-C 2-10烷基或苯基-C 2-10烯基; 及其盐和酯，调节代谢型谷氨酸受体功能，可用于治疗中枢神经系统疾病。

公开(公告)号：WO00043000A1

公开(公告)日：2000-07-27

申请号：PCT/JP2000/000247

申请日：2000-01-20

IPC: A61K38/00 ,  A61P35/00 ,  A61P43/00 ,  C07C229/46 ,  C07C237/22 ,  C07C271/22 ,  C07C327/22 ,  C07C327/28 ,  C07D305/12 ,  C07K5/06 ,  A61K31/215 ,  A61K31/27 ,  A61K31/337 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07C237/10 ,  C07D405/12

CPC classification number: C07K5/06026 ,  A61K38/00 ,  C07C229/46 ,  C07C237/22 ,  C07C271/22 ,  C07C327/22 ,  C07C327/28 ,  C07C2601/02 ,  C07D305/12 ,  C07K5/06191

Abstract: Proteasome inhibitors containing as the active ingredient carboxylic acid derivatives represented by general formula (I) or pharmacologically acceptable salts thereof: wherein m and n are each independently an integer of 0 to 10; p is 0 or 1; R is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, or the like; and R is hydrogen, COR or CH2OR , or alternatively R and R together represent formula (II), wherein X is a linkage, substituted or unsubstituted alkylene, substituted or unsubstituted cycloalkylene, or the like; X is oxygen, sulfur, or NR ; R is as defined for R ; and R is hydroxyl, mercapto, substituted or unsubstituted alkoxy, or the like, or alternatively R and R together represent a linkage; and R is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or the like.

Abstract translation: 含有作为活性成分的通式（I）表示的羧酸衍生物或其药学上可接受的盐的蛋白酶体抑制剂，其中m和n各自独立地为0〜10的整数， p为0或1; R 1是氢，取代或未取代的烷基，取代或未取代的环烷基等; 和R 2是氢，COR 13或CH 2 OR 3a，或者R 1和R 2一起表示式（II），其中X 1是连接，取代或未取代的亚烷基， 取代或未取代的亚环烷基等; X 2是氧，硫或NR 17; R 3如对R 3a所定义; R 4为羟基，巯基，取代或未取代的烷氧基等，或者R 3和R 4一起表示键; R 5为氢，取代或未取代的烷基，取代或未取代的链烯基等。

公开(公告)号：WO1997021666A1

公开(公告)日：1997-06-19

申请号：PCT/EP1996005470

申请日：1996-12-06

Applicant: GLAXO GROUP LIMITED ,  HARTLEY, Charles, David ,  CARTER, Malcolm, Clive ,  FOXTON, Michael, Walter

Inventor： GLAXO GROUP LIMITED

IPC: C07C229/42

CPC classification number: C07D257/04 ,  C07C229/42 ,  C07C229/46 ,  C07C237/20 ,  C07C275/40 ,  C07C309/24 ,  C07C311/35 ,  C07C2601/08 ,  C07F9/3882

Abstract: The present invention relates to phenethanolamine derivatives of formula (I), wherein R represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents hydrogen or C1-6alkyl; R represents a group (A) where the aromatic ring may be optionally substituted by up to four substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; R represents hydrogen, or C1-6alkyl; R represents CO2R , C1-6alkylCO2R , CONR R , NHCONR R , SO2NHR , P(O)(OR )2, SO3H, C1-6alkylSO3H, NHSO2R , NHCOR or tetrazol-5-yl; R and R independently represent hydrogen, C1-6alkyl, trifluoromethyl, CN, OH, CO2R , CH2CO2R , or R and R form a 5-6 membered cycloalkyl ring; R represents hydrogen, or C1-6alkyl; R represents hydrogen, C1-6alkyl, or C1-6alkylOR ; R , R , R , R -R , and R -R each independently represent hydrogen, or C1-6alkyl; R represents C1-6alkyl or trifluoromethyl; R represents C1-6alkyl or trifluoromethyl; with the proviso that when R and R are both hydrogen, R is other than hydrogen; and physiologically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.

Abstract translation: 本发明涉及式（I）的苯乙醇胺衍生物，其中R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基和三氟甲基的取代基取代的芳基 ; R 2表示氢或C 1-6烷基; R 3表示芳基可以任选被至多四个选自C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基的取代基取代的基团（A）; R 4表示氢或C 1-6烷基; R 5表示CO 2 R 8，C 1-6烷基CO 2 R 16，CONR 9 R 10，NHCONR 11 R 12，SO 2 NHR 13，P（O）（OR 14） 2，SO 3 H，C 1-6烷基SO 3 H，NHSO 2 R 15，NHCOR 17或四唑-5-基; R 6和R 7独立地表示氢，C 1-6烷基，三氟甲基，CN，OH，CO 2 R 18，CH 2 CO 2 R 19或R 6和R 7形成5-6元环烷基 环; R 8表示氢或C 1-6烷基; R 9表示氢，C 1-6烷基或C 1-6烷基OR 20; R 10，R 11，R 12，R 14 -R 16和R 18 -R 20各自独立地表示氢或C 1-6烷基; R 13表示C 1-6烷基或三氟甲基; R 17表示C 1-6烷基或三氟甲基; 条件是当R 6和R 7都是氢时，R 8不是氢; 及其生理上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

公开(公告)号：WO1995015944A1

公开(公告)日：1995-06-15

申请号：PCT/EP1994003914

申请日：1994-11-26

Applicant: BASF AKTIENGESELLSCHAFT ,  ALBRECHT, Hans-Peter ,  BÖHM, Hans-Joachim ,  RASCHACK, Manfred ,  UNGER, Liliane ,  WERNET, Wolfgang

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07D209/18

CPC classification number: C07C205/56 ,  C07C62/06 ,  C07C62/18 ,  C07C62/38 ,  C07C69/757 ,  C07C229/46 ,  C07C229/50 ,  C07C235/34 ,  C07C2602/28 ,  C07D209/18

Abstract: The invention describes compounds of formula (I), where A is an oxygen atom or a NH group; B is the radical -Zm-(CHQ)p-(CH=CH)q-(CH2)r-P, where Z is a -CO- group or -SO2-group, m is 0 or 1, p is 0, 1 or 2, q is 0, 1 or 2, r is 0, 1 or 2, Q is a hydrogen atom, a C1-4 alkyl radical, a carboxyl-, carboxamido- or carboxy-C1-4 alkyl group, and P is a hydrogen atom, an indolyl radical, or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkyl groups, and/or a C1-2 alkylenedioxy group; D is an amino-, hydroxy-, C1-4 alkoxy, C1-4 alkylamino-, aryl-C1-4 alkylenoxy- or aryl-C1-4 alkyleneamino, where the aryl radicals represent a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group; X is a C1-4 alkyl radical or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group; Y is a hydrogen atom, a C1-4 alkyl radical or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group, or X and Y together represent a -(CH2)s group, where s is 3, 4 or 5, and 1 or 2 hydrogen atoms can be replaced by methyl groups, and n is 0 or 1, and possibly their salts with physiologically tolerable acids and bases. The compounds can be used to combat diseases.

Abstract translation: 有式（I），其中A是氧原子或NH基团的发明中，B是基团-Zm-（CHQ）对 - （CH = CH）Q（CH 2）RP，其中Z是-CO - 或-SO 2基团，m是0或1，p是阿尔0，1或2，q为0，1或2，r是0，1或2，Q是氢原子，C 1-4 烷基，羧基，甲酰氨基，或羧基-C 1-4 - 烷基且P为氢原子或任选地被1-3个C 1-4烷基，卤素原子，三氟甲基，羟基，C 1-4烷氧基，C 1 -C 4-酰氧基，氨基，C 1-5酰氨基，磺酰氨基，硝基，C 1-5酰基，羧基或硫代C 1-4 - 烷基基团和/或C1-2亚烷基二氧基取代的苯基或 代表吲哚基团，D是氨基，羟基，C 1-4 - 烷氧基，C 1-4 - 烷基氨基，芳基-C 1-4 - 亚烷基或芳基-C 1-4亚烷基氨基，其中所述芳基任选被取代的1- 3个C 1-4烷基，卤素原子，三氟甲基，羟基，C 1-4 - 烷氧基，C 1-4 - 酰氧基，氨基，C 1-5酰氨基，磺 namido-，硝基，C 1-5酰基，羧基或硫代C1-4亚烷基基团和/或C 1-2 - 亚烷基二氧基取代的苯基，X表示C 1-4 - 烷基或任选被1个 -3 C 1-4烷基，卤素，三氟甲基，羟基，C 1-4烷氧基，C 1-4酰氧基，氨基，C 1-5酰氨基，磺酰氨基，硝基，C1-5- 亚烷基硫基-C 1-4 - 酰基，羧基或和/或亚烷基二C1-2取代的苯基基团，Y表示氢原子，C 1-4烷基或任选地被1-3 C 1-4烷基的基团，卤原子 甲基，三氟甲基，羟基，C 1-4 - 烷氧基，C 1-4 - 酰氧基，氨基，C 1-5酰氨基，磺酰氨基，硝基，C 1-5酰基，羧基或硫代C1 -4 - 亚烷基和/或C 1-2 - 亚烷基二氧基取代的苯基基团，或X和Y一起形成 - （CH 2）平均的小组，其中s是在其通过甲基基团1个或2个氢原子的数目3，4或5个 可以被替换，并且n为数字0或1， 和任选其盐与生理上可接受的酸或碱。 所述化合物适于防治疾病。

公开(公告)号：WO1995015940A1

公开(公告)日：1995-06-15

申请号：PCT/GB1994002690

申请日：1994-12-09

Applicant: UNIVERSITY OF BRISTOL ,  TOCRIS COOKSON LIMITED ,  WATKINS, Jeffrey, Clifton ,  JANE, David, Edward

Inventor： UNIVERSITY OF BRISTOL ,  TOCRIS COOKSON LIMITED

IPC: C07C229/24

CPC classification number: C07F9/301 ,  C07C229/24 ,  C07C229/46 ,  C07C309/61 ,  C07C2601/02 ,  C07F9/091 ,  C07F9/3808

Abstract: Compounds of formula (I) are disclosed wherein: Y is selected from carboxy, phosphono, -PO2H(OR ), phosphinico, -PO2H(R ), -OPO3H2, -OPO2H(OR ), arsono, -AsO2H(OR ), arsinico, -AsO2H(R ), sulpho, sulphino, sulpheno, OSO3H, tetrazolyl, 3-hydroxyisoxazole, 1,2,4-oxadiazolidin-3,5-dione and hydantoin where R is C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkylene or optionally substituted aryl or aralkyl; B is selected from C1 to C8 alkylene, C3 to C8 cycloalkylene, C2 to C8 alkenylene and C2 to C8 alkynylene optionally chain substituted and optionally substituted on the chain; Q is selected from carboxy, C1 to C6 alkoxycarbonyl and hydroxamic acid; R is selected from C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkylene, haloalkyl and optionally substituted aryl, aralkyl or biaryl; and R and R are the same or different and are selected from hydrogen, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C1 to C6 acyl and optionally substituted benzoyl, two of Y, Q, R , R , R and the substituents on B being optionally condensed with each other to form a carbocyclic or heterocyclic ring system, and pharmaceutically acceptable salts thereof. The compounds may be used as agents to influence the central nervous system.

Abstract translation: 公开了式（I）的化合物，其中：Y选自羧基，膦酰基，-PO2H（OR 13），亚磷酰基，-PO2H（R13），-OPO3H2，-OPO2H（OR13） 亚砷基-AsO 2 H（OR 13），亚辛基，-AsO 2 H（R 13），磺基，亚磺酰基，苯酚基，OSO 3 H，四唑基，3-羟基异恶唑，1,2,4-恶二唑烷-3,5-二酮和 乙内酰脲，其中R 13为C 1至C 6烷基，C 2至C 6烯基，C 2至C 6炔基，C 3至C 8亚环烷基或任选取代的芳基或芳烷基; B选自C1至C8亚烷基，C3至C8亚环烷基，C2至C8亚烯基和C2至C8亚炔基任选被链取代并任选取代在链上; Q选自羧基，C1至C6烷氧基羰基和异羟肟酸; R 10选自C 1至C 6烷基，C 2至C 6烯基，C 2至C 6炔基，C 3至C 8亚环烷基，卤代烷基和任选取代的芳基，芳烷基或联芳基; 并且R 11和R 12相同或不同，并且选自氢，C 1至C 6烷基，C 2至C 6烯基，C 2至C 6炔基，C 1至C 6酰基和任选取代的苯甲酰基，Y，Q R 10，R 11，R 12和B上的取代基任选地彼此缩合形成碳环或杂环系统及其药学上可接受的盐。 该化合物可用作影响中枢神经系统的药剂。

公开(公告)号：WO1994000417A1

公开(公告)日：1994-01-06

申请号：PCT/JP1993000852

申请日：1993-06-21

Applicant: ZAIDAN HOJIN SEISAN KAIHATSU KAGAKU KENKYUSHO ,  FUJIMURA, Hajime ,  YABUUCHI, Takahiro ,  TANAKA, Teruo

Inventor： ZAIDAN HOJIN SEISAN KAIHATSU KAGAKU KENKYUSHO

IPC: C07C229/46

CPC classification number: C07C229/46 ,  C07C2601/14 ,  Y10S514/925 ,  Y10S514/926

Abstract: A zinc tranexamate compound represented by formula (I) and a pharmaceutically acceptable organic acid salt thereof. This compound exhibits anti-inflammatory and anti-ulcerous activities even when administered at a dose smaller than that of tranexamic acid or cetraxate hydrochloride, and is easy to administer because it is tasteless and odorless. The organic acid salt is water-soluble and hence can be used in liquid form as injection or external preparation.

Abstract translation: 由式（I）表示的硝酸锌锌化合物及其药学上可接受的有机酸盐。 该化合物即使以小于氨甲环酸或四乙酸盐酸盐的剂量施用时也显示出抗炎和抗溃疡活性，并且由于无味无味而容易施用。 有机酸盐是水溶性的，因此可以以液体形式用作注射剂或外用制剂。