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1. 发明授权

US06521606B2 Matrix metalloproteinase inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US06521606B2
公开(公告)日：2003-02-18
申请号：US09899017
申请日：2001-07-06
申请人： Morten Dahl Sørensen , Lars Kristian Albert Blæhr , Mette Knak Christensen
发明人： Morten Dahl Sørensen , Lars Kristian Albert Blæhr , Mette Knak Christensen
IPC分类号： A61K3166
CPC分类号： A61K31/675 , C07F9/65842
摘要： A compound of the general formula I wherein Y is O or S; n is 1, 2, 3 or 4; X represents hydroxamic acid, carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R1 is wherein E, when present represents, a bond or optionally substituted methylene or ethylene; s and t are independently 0, 1, 2 or 3; A and A′ independently represent a bond, or a saturated or unsaturated, optionally substituted cyclic or heterocyclic hydrocarbon di- or triradical; Z represents a bond, O, S, C(O), C(O)NR7, NR7C(O) or NR7, wherein R7 is hydrogen, hydroxy, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R5 represents a bond, alkane or alkene diradical, one or more ether diradicals (R—O—R′) or amine diradicals (R—N—R′), wherein R and R′ independently represent alkane or alkene diradicals with a C-content from 0 to 3; R6 represents hydrogen, hydroxy, halogen, cyano, nitro, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical, unsaturated optionally substituted cyclic or heterocyclic hydrocarbon radical, NR8R9, C(O)NR8R9, C(O)R8, CO(O)R8, S(O)2R9, wherein each R8 and R9 independently represent hydrogen, halogen, a branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R2 represents hydrogen, (C1-8)alkyl, (C2-6)alkenyl, (C3-8)cycloalkyl, aryl(C0-6)alkyl or heteroaryl(C0-6)alkyl; provided that if A, A′, Z and R5 are all bonds, and s and t are both 0 (zero), then R6 is different from hydrogen; or a salt, hydrate or solvate thereof. The compounds are valuable for human and veterinary therapy.
摘要翻译：通式I的化合物，其中Y为O或S; n为1,2,3或4; X为异羟肟酸，羧酸，膦酸，乙酰硫代甲基或巯基甲基; R1为E时，当存在时为键或任选取代的亚甲基或亚乙基; s和t独立地为0,1,2或3; A和A'独立地表示键，或饱和或不饱和的任选取代的环状或杂环烃二取代或杂芳基; Z表示键，O，S，C（O），C（O）NR7，NR7C（O）或NR7，其中R7是氢，羟基，支链或直链，饱和或不饱和的任选取代的烃基; R 5表示键，或二烯基双基，一个或多个醚双基（RO-R'）或胺二基（RN-R'），其中R和R'独立地表示C含量为0至3的烷烃或烯烃双基; R 6表示氢，羟基，卤素，氰基，硝基，支链或直链，饱和或不饱和的，任选取代的氢化物芳基，不饱和的任选取代的环状或杂环烃基，NR 8 R 9，C（O）NR 8 R 9，C（O）R 8，CO（O）R 8，S（O）2 R 9，其中各R 8和R 9分别代表氢，卤素，分支或直链，饱和或不饱和的任选取代的烃基; R 2表示氢，（C 1-8）烷基，（C 2-6）烯基，（C 3-8）环烷基，芳基（C 0-6）烷基或杂芳基 6）烷基;条件是如果A，A'，Z和R5都是键，并且s和t均为0（零），则R6不同于氢;或其盐，水合物或溶剂化物。化合物是有价值的用于人类和兽医治疗。

2. 发明授权

US06784169B2 MMP inhibitors 失效
标题翻译： MMP抑制剂
公开(公告)号：US06784169B2
公开(公告)日：2004-08-31
申请号：US10345304
申请日：2003-01-16
申请人： Mette Knak Christensen , Lars Kristian Albert Blæhr
发明人： Mette Knak Christensen , Lars Kristian Albert Blæhr
IPC分类号： A61K3166
CPC分类号： C07F9/65842 , C07F9/6584
摘要： Novel compounds according to formula I n is 0, 1, 2 or 3; X represents hydroxamic acid (CONHOH), carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R2, R10 and R11 independently represent hydrogen or (C1-8)alkyl, (C2-6)alkenyl, (C3-8)cycloalkyl, aryl(C0-6)alkyl or heteroaryl(C0-6)alkyl, all of which may optionally be substituted; R3 and R4 independently represent hydrogen, hydroxy or alkoxy; provided that if A, A′, Z and R5 are all bonds, and s and t are both 0 (zero), then R6 is different from hydrogen, and that at least one of R3, R4, R10 and R11 is different from hydrogen; or a salt, hydrate or solvate thereof; pharmaceutical compositions comprising said compound; therapeutical methods comprising administering said compounds; and the use of said compounds in the manufacture of medicaments.
摘要翻译：式（I）的新型化合物是0,1,2或3; X代表异羟肟酸（CONHOH），羧酸，膦酸，乙酰硫代甲基或巯基甲基; R2，R10和R11独立地表示氢或（C1-8）烷基，（C2-6）烯基，（C3-8）环烷基，芳基（C0-6）烷基或杂芳基（C0-6）烷基，任选被取代; R3和R4独立地表示氢，羟基或烷氧基; 条件是如果A，A'，Z和R5都是键，并且s和t都是0（零），则R6不同于氢，R3，R4，R10和R11中的至少一个不同于氢 ;或其盐，水合物或溶剂合物; 包含所述化合物的药物组合物; 治疗方法包括施用所述化合物; 以及所述化合物在制备药物中的用途。

3. 发明授权

US08871747B2 Urea and thiourea derivatives 有权
标题翻译：尿素和硫脲衍生物
公开(公告)号：US08871747B2
公开(公告)日：2014-10-28
申请号：US13060789
申请日：2009-08-31
申请人： Mette Knak Christensen , Fredrik Bjorkling
发明人： Mette Knak Christensen , Fredrik Bjorkling
IPC分类号： A61K31/675 , C07D253/07 , C07D213/40 , C07D231/40 , C07D413/12 , C07D213/75 , C07D239/42
CPC分类号： C07F9/6533 , A61K31/4409 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/5355 , A61K31/5377 , A61K31/55 , A61K31/675 , A61K45/06 , C07D213/40 , C07D213/75 , C07D231/40 , C07D239/42 , C07D253/07 , C07D401/12 , C07D413/12 , C07F9/58
摘要： The present application discloses compounds of formula (I) wherein X is ═O, ═S, ═NH, ═NOH and ═NO-Me; A is —C(═O)—, —S(═O)2—, —C(═S)— and P(═O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt. sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
摘要翻译：本申请公开了式（I）的化合物，其中X为= O，= S，= NH，= NOOH和= NO-Me; A是-C（= O） - ， - S（= O）2 - ， - C（= S） - 和P（= O）（R5） - ; B是-O - ， - （CH 2）3-6 - 和O-（CH 2）2-5-; D是-O - ， - CR 7 R 8 - 和-NR 9; m为0-12，n为0-12，m + n为1-20; p为0-4; R1是选择。子杂芳基; 及其药学上可接受的盐及其前药。本申请还公开了用作治疗由升高水平的烟酰胺磷酸核糖转移酶（NAMPRT）引起的疾病或病症的药物的化合物，例如，炎症和组织修复障碍; 皮肤病; 自身免疫性疾病，阿尔茨海默氏病，中风，老年痴呆，再狭窄，糖尿病，肾小球性肾炎，癌症，恶病质，与感染和某些病毒感染有关的炎症，包括获得性免疫缺陷综合征（AIDS），成人呼吸窘迫综合征，共济失调致远端发育不良。

4. 发明申请

US20100227863A1 SUBSTITUTED 3-(4-HYDROXYPHENYL)-INDOLIN-2-ONE COMPOUNDS 审中-公开
标题翻译：取代的3-（4-羟基苯基） - 茚满-2-酮化合物
公开(公告)号：US20100227863A1
公开(公告)日：2010-09-09
申请号：US12597208
申请日：2008-04-28
申请人： Mette Knak Christensen , Fredrik Bjoerkling
发明人： Mette Knak Christensen , Fredrik Bjoerkling
IPC分类号： A61K31/5377 , C07D209/34 , A61K31/4015 , C07D401/04 , A61K31/4439 , C07D413/04 , A61P35/00
CPC分类号： C07D209/34 , C07D209/40 , C07D401/04 , C07D403/04 , C07D409/04 , C07D417/04
摘要： The present application discloses substituted 3-(4-hydroxyphenyl)-indolin-2-one compounds (oxindole compounds) of the formula and the use of such compounds for the preparation of a medicament for the treatment of cancer in a mammal, in particular in humans.
摘要翻译：本申请公开了下式的取代的3-（4-羟基苯基） - 二氢吲哚-2-酮化合物（羟吲哚化合物），以及这些化合物在制备用于治疗哺乳动物癌症的药物中的用途，特别是人类。

5. 发明申请

US20100029646A1 PRODRUGS OF DIPHENYL OX-INDOL-2-ONE COMPOUNDS 审中-公开
标题翻译：二苯氧基-2-二醇化合物的制备方法
公开(公告)号：US20100029646A1
公开(公告)日：2010-02-04
申请号：US12518545
申请日：2007-12-11
申请人： Mette Knak Christensen , Fredrik Bjoerkling , Martins Ikaunieks , Andrei Zaichenko , Vija Gailite , Einars Loza , Ivars Kalvinsh , Marina Madre
发明人： Mette Knak Christensen , Fredrik Bjoerkling , Martins Ikaunieks , Andrei Zaichenko , Vija Gailite , Einars Loza , Ivars Kalvinsh , Marina Madre
IPC分类号： A61K31/404 , C07D209/34 , C07D403/06 , C07D413/06 , A61P35/00 , A61K31/496 , A61K31/5377
CPC分类号： C07D209/34
摘要： The present application discloses prodrugs of substituted 3,3-diphenyl-1,3-dihydro-indol-2-one compounds having the general formula (I). The 4-position of the phenyl moieties and the N-position of the indole represent useful handles for the introduction of particular prodrug groups, in particular those comprising an amino acid moiety. The prodrug compounds are believed to be useful for the treatment of cancer in a mammal, possibly in combination with one or more other chemotherapeutic agents. The application also discloses the compounds for use in a method of treating a mammal suffering from or being susceptible to cancer
摘要翻译：本申请公开了具有通式（I）的取代的3,3-二苯基-1,3-二氢 - 吲哚-2-酮化合物的前药。苯基部分的4-位和吲哚的N-位表示用于引入特定前药基团，特别是包含氨基酸部分的那些的有用的手段。认为前药化合物可用于治疗哺乳动物中的癌症，可能与一种或多种其它化学治疗剂组合。本申请还公开了用于治疗患有或易患癌症的哺乳动物的方法中的化合物

6. 发明申请

US20120225847A1 SQUARIC ACID DERIVATIVES AS INHIBITORS OF THE NICOTINAMIDE 有权
标题翻译：作为NICOTINAMIDE的抑制剂的SQUARIC酸衍生物
公开(公告)号：US20120225847A1
公开(公告)日：2012-09-06
申请号：US13000522
申请日：2009-06-24
申请人： Mette Knak Christensen , Fredrik Bjorkling
发明人： Mette Knak Christensen , Fredrik Bjorkling
IPC分类号： A61K31/675 , A61K31/5377 , A61K31/496 , A61K31/47 , A61K31/4409 , C07D413/12 , C07D413/14 , C07D401/12 , C07F9/28 , C07D213/72 , A61P29/00 , A61P19/02 , A61P1/00 , A61P11/06 , A61P11/00 , A61P19/10 , A61P17/00 , A61P17/06 , A61P37/00 , A61P25/00 , A61P41/00 , A61P25/28 , A61P9/10 , A61P3/10 , A61P35/00 , A61P35/02 , A61P31/00 , A61P31/12 , A61P31/14 , A61K31/55
CPC分类号： C07D413/12 , C07D213/74 , C07D401/12 , C07F9/58 , C07F9/65583
摘要： The present application discloses novel squaric acid derivatives of the formula A: from —C(═O)—, —S(═O)2—, —C(═S)— and —P(═O)(R5)—; B: -, —O—, —NR6— and —C(═O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and viral infections, adult respiratory distress syndrome, ataxia telengiectasia).
摘要翻译：本申请公开了式A的新型方酸衍生物：-C（= O） - ， - S（= O）2 - ， - C（= S） - 和-P（= O）（R5） - ; B： - ， - O - ， - NR6-和-C（= O）-NR6-; D： - ， - O - ， - CR 7 R 8 - 和-NR 9; m = 0-12; n = 0-12; m + n = 1-20; p = 0-2; R1：杂芳基，芳基; R2：H，C1-12 - 烷基，C3-12-环烷基， - [CH2CH2O] 1-10-（C1-6 - 烷基），C1-12 - 烯基，芳基，杂环基，杂芳基; R3：C1-12烷基，C3-12-环烷基， - [CH2CH2O] 1-10-（C1-6 - 烷基），C1-12 - 烯基，芳基，杂环基，杂芳基; 或R 2和R 3：含氮杂环/杂芳族环; R4和R4 *：H，C1-12 - 烷基，C1-12 - 烯基; 及其药学上可接受的盐和前药，以及它们在治疗由升高的NAMPRT水平引起的疾病/病症（炎症和组织修复障碍，特别是类风湿性关节炎，炎性肠病，哮喘和CPOD，骨关节炎，骨质疏松症和纤维化疾病皮肤病;自身免疫性疾病，包括系统性红斑狼疮，多发性硬化症，银屑病关节炎，强直性脊柱炎，组织和器官排斥反应，阿尔茨海默病，中风，动脉粥样硬化，再狭窄，糖尿病，肾小球肾炎，恶病质，与感染和病毒感染相关的炎症，成人呼吸窘迫综合征，共济失调远端传染性疾病）。

7. 发明授权

US06277876B1 Matrix metalloproteinase inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US06277876B1
公开(公告)日：2001-08-21
申请号：US09623428
申请日：2000-09-05
申请人： Mette Knak Christensen
发明人： Mette Knak Christensen
IPC分类号： A61K31404
CPC分类号： C07D249/18 , C07C327/42 , C07C327/44 , C07D209/20 , C07D317/36
摘要： Compounds of the formula (I) where X is a —CO2H or —CONHOH group; Y and Z are independently sulphur or oxygen, at least one being sulphur; R1 is hydrogen, hydroxy, (C1-C6)alkyl, (C2-C6)alkenyl, or (C3-C8cycloalkyl; R2 is a (C1-C24)alkyl, phenyl(C1-C6)alkyl, or phenyl(C0-C6alkyl)O)C1-C6)alkyl, any of which may be optionally substituted by (C1-C6)alkyl, (C1-C6)alkoxy, halo or cyano (CN); R3 is the characterising side chain of a natural &agr;-amino acid in which any functional groups may be protected, (C1-C6)alkyl which may be optionally substituted, or cycloalkyl(C1-C6)alkyl; R4 is hydrogen, (C1-C6)alkyl, phenyl(C1-C6)alkyl, optionally substituted phenyl or heteroaryl, or a group of formula —(Q—O)n—Q where Q is a straight or branched (C1-C6)alkyl, where n is an integer >1 and no continuous linear sequence of atoms in the group R4 is >12; or a salt, hydrate or solvate thereof. The compounds are useful for treating various medical conditions such as tissue breakdown and inflammation.
摘要翻译：其中X为-CO 2 H或-CONHOH基团的式（I）化合物; Y和Z独立地是硫或氧，至少一个是硫; R 1是氢，羟基，（C 1 -C 6）烷基，（C 2 -C 6）烯基或（C 3 -C 8环烷基; R 2是（C 1 -C 24）烷基，苯基（C 1 -C 6）烷基或苯基（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，卤素或氰基（CN）中的任何一个可以被任选取代。 R3是其中任何官能团可以被保护的天然α-氨基酸的表征侧链，可以被任选取代的（C 1 -C 6）烷基或环烷基（C 1 -C 6）烷基; R4是氢，（C1-C6）烷基，苯基（C1-C6）烷基，任意取代的苯基或杂芳基，或式 - （QO）nQ基团，其中Q是直链或支链（C1-C6）烷基，其中 n是整数> 1，并且基团R4中的原子的连续线性序列不大于12; 或其盐，水合物或溶剂合物。该化合物可用于治疗各种医疗条件如组织分解和炎症。

8. 发明授权

US09006426B2 Squaric acid derivatives as inhibitors of the nicotinamide 有权
标题翻译：方酸衍生物作为烟酰胺的抑制剂
公开(公告)号：US09006426B2
公开(公告)日：2015-04-14
申请号：US13000522
申请日：2009-06-24
申请人： Mette Knak Christensen , Fredrik Bjorkling
发明人： Mette Knak Christensen , Fredrik Bjorkling
IPC分类号： A61K31/5355 , C07D413/08 , C07D413/12 , C07D213/74 , C07D401/12 , C07F9/58 , C07F9/6558
CPC分类号： C07D413/12 , C07D213/74 , C07D401/12 , C07F9/58 , C07F9/65583
摘要： The present application discloses novel squaric acid derivatives of the formula A: from —C(═O)—, —S(═O)2—, —C(═S)— and —P(═O)(R5)—; B: -, —O—, —NR6— and —C(═O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and viral infections, adult respiratory distress syndrome, ataxia telengiectasia).
摘要翻译：本申请公开了式A的新型方酸衍生物：-C（= O） - ， - S（= O）2 - ， - C（= S） - 和-P（= O）（R5） - ; B： - ， - O - ， - NR6-和-C（= O）-NR6-; D： - ， - O - ， - CR 7 R 8 - 和-NR 9; m = 0-12; n = 0-12; m + n = 1-20; p = 0-2; R1：杂芳基，芳基; R2：H，C1-12 - 烷基，C3-12-环烷基， - [CH2CH2O] 1-10-（C1-6 - 烷基），C1-12 - 烯基，芳基，杂环基，杂芳基; R3：C1-12烷基，C3-12-环烷基， - [CH2CH2O] 1-10-（C1-6 - 烷基），C1-12 - 烯基，芳基，杂环基，杂芳基; 或R 2和R 3：含氮杂环/杂芳族环; R4和R4 *：H，C1-12 - 烷基，C1-12 - 烯基; 及其药学上可接受的盐和前药，以及它们在治疗由升高的NAMPRT水平引起的疾病/病症（炎症和组织修复障碍，特别是类风湿性关节炎，炎性肠病，哮喘和CPOD，骨关节炎，骨质疏松症和纤维化疾病皮肤病;自身免疫性疾病，包括系统性红斑狼疮，多发性硬化症，银屑病关节炎，强直性脊柱炎，组织和器官排斥反应，阿尔茨海默病，中风，动脉粥样硬化，再狭窄，糖尿病，肾小球肾炎，恶病质，与感染和病毒感染相关的炎症，成人呼吸窘迫综合征，共济失调远端传染性疾病）。

9. 发明申请

US20120010172A1 NOVEL UREA AND THIOUREA DERIVATIVES 有权
标题翻译：新尿素和硫脲衍生物
公开(公告)号：US20120010172A1
公开(公告)日：2012-01-12
申请号：US13060789
申请日：2009-08-31
申请人： Mette Knak Christensen , Fredrik Bjorkling
发明人： Mette Knak Christensen , Fredrik Bjorkling
IPC分类号： A61K31/675 , A61K31/4409 , C07D413/12 , A61K31/5377 , C07D239/42 , A61K31/505 , C07D213/40 , A61K31/5355 , C07D253/07 , A61K31/53 , C07D261/14 , A61K31/42 , C07D241/20 , A61K31/4965 , C07F9/58 , A61K31/4406 , C07D401/12 , A61K31/4725 , C07F9/6533 , A61K31/496 , A61K31/55 , A61K31/4439 , A61K31/4545 , A61P35/00 , A61P29/00 , A61P9/00 , A61P9/10 , A61P37/06 , C07D213/75
CPC分类号： C07F9/6533 , A61K31/4409 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/5355 , A61K31/5377 , A61K31/55 , A61K31/675 , A61K45/06 , C07D213/40 , C07D213/75 , C07D231/40 , C07D239/42 , C07D253/07 , C07D401/12 , C07D413/12 , C07F9/58
摘要： The present application discloses compounds of formula (I) wherein X is ═O, ═S, ═NH, ═NOH and ═NO-Me; A is —C(═O)—, —S(═O)2—, —C(═S)— and P(═O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
摘要翻译：本申请公开了式（I）的化合物，其中X为= O，= S，= NH，= NOOH和= NO-Me; A是-C（= O） - ， - S（= O）2 - ， - C（= S） - 和P（= O）（R5） - ; B是-O - ， - （CH 2）3-6 - 和O-（CH 2）2-5-; D是-O - ， - CR 7 R 8 - 和-NR 9; m为0-12，n为0-12，m + n为1-20; p为0-4; R1是opt.sub。杂芳基; 及其药学上可接受的盐及其前药。本申请还公开了用作治疗由升高水平的烟酰胺磷酸核糖转移酶（NAMPRT）引起的疾病或病症的药物的化合物，例如，炎症和组织修复障碍; 皮肤病; 自身免疫性疾病，阿尔茨海默病，中风，老年硬化症，再狭窄，糖尿病，肾小球性肾炎，癌症，恶病质，与感染和某些病毒感染有关的炎症，包括获得性免疫缺陷综合征（AIDS），成人呼吸窘迫综合征，共济失调性致远端增生症。

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