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公开(公告)号：US5200328A
公开(公告)日：1993-04-06
申请号：US494702
申请日：1990-03-16
CPC分类号： C07H15/04 , A61K8/602 , A61Q11/00 , A61Q19/10 , C11D1/662 , C12P19/44 , C12P7/62 , Y10S435/874 , Y10S435/931
摘要： Fatty acid esters of methyl glycosides are prepared by reacting a fatty acid or ester with a methyl glycoside in the presence of an enzyme catalyst, in particular a lipase. The resulting fatty acid esters are preferably monoesters.The methyl glycoside fatty acid esters may be used as surface-active agents in cleaning compositions or personal care products.
摘要翻译： 通过使脂肪酸或酯与甲基糖苷在酶催化剂，特别是脂肪酶的存在下反应来制备甲基糖苷的脂肪酸酯。 所得的脂肪酸酯优选为单酯。 甲基糖苷脂肪酸酯可以用作清洁组合物或个人护理产品中的表面活性剂。
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2.发明申请PYRIDINYL DERIVATIVES AS INHIBITORS OF ENZYME NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE 审中-公开吡啶衍生物作为酶抑制剂磷酸化磷酸酯酶的抑制剂公开(公告)号：US20120264755A1
公开(公告)日：2012-10-18
申请号：US13377408
申请日：2010-06-09
IPC分类号： A61K31/5377 , C07D405/12 , A61K31/4433 , C07D213/72 , A61K31/44 , A61K31/5355 , A61P29/00 , A61P3/10 , A61P19/02 , A61P1/00 , A61P11/06 , A61P11/00 , A61P19/10 , A61P17/00 , A61P17/06 , A61P37/06 , A61P25/28 , A61P9/10 , A61P35/00 , A61P35/02 , A61P31/12 , A61P31/18 , C07D413/12
CPC分类号： C07D213/75 , C07D213/38 , C07D213/40 , C07D405/12 , C07D413/12
摘要： The present application discloses a compound of the formula (I) wherein Q is optionally substituted pyridyl; p is 0-6. Y is formulae (i), (ii) and (iii) where X is ═O, ═S and ═N—CN, r is 1-12, R is —Z-A, Z is a single bond, —S(═O)2—, >P═O, >C═O, —C(═O)NH—, and —C(═S)NH—; and A is hydrogen, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, and heteroaryl; B is a single bond, —NRN—, —S(═O)2— and —O—; wherein RN is selected from hydrogen, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, and heteroaryl; s is 0-6; and Cy is aryl, cycloalkyl, heterocyclyl, and heteroaryl. The compounds are useful for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT).
摘要翻译： 本申请公开了式（I）的化合物，其中Q是任选取代的吡啶基; p为0-6。 Y是式（ⅰ），（ⅱ）和（ⅲ），其中X是= O，≡S和≡N-CN，r是1-12，R是-ZA，Z是单键，-S（= ）=，P = O，> C = O，-C（= O）NH-和-C（= S）NH-; A为氢，C 1-12 - 烷基，C3-12 - 环烷基， - [CH2CH2O] 1-10-（C1-6 - 烷基），C1-12 - 烯基，芳基，杂环基和杂芳基; B是单键，-NRN - ， - S（= O）2 - 和-O-; 其中RN选自氢，C 1-12 - 烷基，C3-12 - 环烷基， - [CH2CH2O] 1-10-（C1-6 - 烷基），C1-12 - 烯基，芳基，杂环基和杂芳基; s是0-6; Cy是芳基，环烷基，杂环基和杂芳基。 该化合物可用作用于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。
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公开(公告)号：US20080090842A1
公开(公告)日：2008-04-17
申请号：US11998575
申请日：2007-11-30
申请人： Fredrik Bjorkling
发明人： Fredrik Bjorkling
IPC分类号： A61K31/4709 , A61K31/44 , A61K31/4439 , A61P35/00 , A61K31/444
CPC分类号： C07D213/89 , A61K31/4439 , A61K45/06 , C07D401/12
摘要： Compounds according to formula I wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, 0, C(O), S, S(O), S(0)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, aminoalkyl or straight or branched, saturated or unsaturated C1-4 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl or aminoalkyl; provided that R1 is not attached to the nitrogen-atom in the pyridyl ring; and pharmaceutically acceptable salts, solvates, hydrates, N-oxides and prodrugs thereof are disclosed. The compounds are useful in therapy.
摘要翻译： 根据式I的化合物，其中R 1表示氢，卤素或一个或多个直链或支链，饱和或不饱和的C 1-6 - 烃基，任选被卤素，羟基，氰基，硝基，羧基，烷氧基 烷氧基羰基，烷基羰基，甲酰基，氨基，氨基烷基，氨基羰基，烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基，羟基磺酰氧基，二羟基磷酰氧基或膦酰基; X代表直链或支链饱和或不饱和的C 1-12烃二价基，任选被卤素，羟基，氰基，硝基，羧基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基，氨基烷基，氨基羰基 烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基，羟基磺酰氧基，二羟基亚磷酰氧基或膦酰基; Y表示0，C（O），S，S（O），S（O）2，C（O）O，NH，C（O）NH，OC（O） 或NHC（O）; Z代表具有5-12个环原子的芳族或非芳族杂环基团，任选被卤素，羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基烷基或直链或支链，饱和或不饱和的C 1 羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基或氨基烷基; 条件是R1不连接在吡啶环中的氮原子上; 及其药学上可接受的盐，溶剂化物，水合物，N-氧化物和前体药物。 这些化合物可用于治疗。
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公开(公告)号：US08871747B2
公开(公告)日：2014-10-28
申请号：US13060789
申请日：2009-08-31
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。
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公开(公告)号：US6071960A
公开(公告)日：2000-06-06
申请号：US202348
申请日：1998-12-14
CPC分类号： A61K31/225 , C07C69/40
摘要： Compounds of general formula (I) in which Y and Q are the same or different and are hydrogen atoms or C.sub.1-6 alkyl groups, optionally substituted by 1-4 hydroxy or 1-4 R.sup.3 O.sub.2 CCH.sub.2 CH.sub.2 CO.sub.2 -- groups, where R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl group which may be straight or branched and saturated or unsaturated, and R.sup.1 and R.sup.2 are the same or different and are C.sub.1-6 alkyl groups, which may be straight or branched and saturated or unsaturated, and solvates and prodrugs of these compounds and the salts of compounds in which R.sup.3 is a hydrogen atom. These compounds can be used in the treatment of diseases caused by or resulting in metabolic dysfunction and/or energy deprivation, such as diabetes, acute starvation, endotoxemia, sepsis, systemic inflammatory response syndrome and multiple orgen dysfunction syndrome. ##STR1##
摘要翻译： PCT No.PCT / EP97 / 02966 Sec。 371 1998年12月14日第 102（e）日期1998年12月14日PCT提交1997年6月4日PCT公布。 公开号WO97 / 47584 日期：1997年12月18日通式（I）的化合物，其中Y和Q相同或不同，为氢原子或C1-6烷基，任选被1-4个羟基或1-4个R3O2CCH2CH2CO2-基团取代，其中R3 是氢原子或C 1-6烷基，其可以是直链或支链和饱和或不饱和的，并且R 1和R 2相同或不同并且是C 1-6烷基，其可以是直链或支链和饱和或不饱和的， 这些化合物的溶剂合物和前药以及其中R3是氢原子的化合物的盐。 这些化合物可用于治疗由代谢功能障碍和/或能量缺乏引起的疾病，如糖尿病，急性饥饿，内毒素血症，败血症，全身性炎症反应综合征和多发性发育不全综合征。
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6.发明申请公开(公告)号：US20120225847A1
公开(公告)日：2012-09-06
申请号：US13000522
申请日：2009-06-24
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）。
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公开(公告)号：US07807682B2
公开(公告)日：2010-10-05
申请号：US11998575
申请日：2007-11-30
申请人： Fredrik Bjorkling
发明人： Fredrik Bjorkling
IPC分类号： C07D213/72 , A61K31/44
CPC分类号： C07D213/89 , A61K31/4439 , A61K45/06 , C07D401/12
摘要： Compounds according to formula I wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, 0, C(O), S, S(O), S(0)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, aminoalkyl or straight or branched, saturated or unsaturated C1-4 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl or aminoalkyl; provided that R1 is not attached to the nitrogen-atom in the pyridyl ring; and pharmaceutically acceptable salts, solvates, hydrates, N-oxides and prodrugs thereof are disclosed. The compounds are useful in therapy.
摘要翻译： 根据式I的化合物，其中R 1表示氢，卤素或一个或多个直链或支链的饱和或不饱和C 1-6烃基，任选被卤素，羟基，氰基，硝基，羧基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基 氨基烷基，氨基羰基，烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基，羟基磺酰氧基，二氢氧膦基氧基或膦酰基; X代表直链或支链饱和或不饱和的C 1 -C 12烃基，其任选被卤素，羟基，氰基，硝基，羧基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基，氨基烷基，氨基羰基，烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基 ，羟基磺酰氧基，二羟基磷酰氧基或膦酰基; Y表示0，C（O），S，S（O），S（O）2，C（O）O，NH，C（O）NH，OC（O）或NHC（O） 羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基烷基或直链或支链，饱和或不饱和的C 1-4烃基，其中Z代表具有5-12个环原子的芳族或非芳族杂环基团 羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基或氨基烷基; 条件是R1不连接在吡啶环中的氮原子上; 及其药学上可接受的盐，溶剂化物，水合物，N-氧化物和前体药物。 这些化合物可用于治疗。
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公开(公告)号：US4859589A
公开(公告)日：1989-08-22
申请号：US121918
申请日：1987-11-17
摘要： An epoxy group in a molecule can enzymatically be transferred to another molecule, thereby synthesizing carbohydrates carrying an epoxy group in the aglycone position.
摘要翻译： 分子中的环氧基可以酶促转移到另一个分子中，从而合成在糖苷配基中携带环氧基团的碳水化合物。
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公开(公告)号：US09006426B2
公开(公告)日：2015-04-14
申请号：US13000522
申请日：2009-06-24
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）。
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公开(公告)号：US20120010172A1
公开(公告)日：2012-01-12
申请号：US13060789
申请日：2009-08-31
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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