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81. 发明申请

WO2003011829A1 PROCESS FOR THE PRODUCTION OF QUINAZOLINES 审中-公开
标题翻译：生产喹喔啉的方法
公开(公告)号：WO2003011829A1
公开(公告)日：2003-02-13
申请号：PCT/IB2002/002872
申请日：2002-07-19
申请人： PFIZER LIMITED , PFIZER INC. , BOULTON, Lee, Terence , CROOK, Robert, James , PETTMAN, Alan, John , WALTON, Robert
发明人： BOULTON, Lee, Terence , CROOK, Robert, James , PETTMAN, Alan, John , WALTON, Robert
IPC分类号： C07D213/57
CPC分类号： C07D401/04 , C07D213/57
摘要： The invention provides a process for the production of a compound of formula (A), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 represents C 1-4 alkoxy optionally substituted by one or more fluorine atoms; R 2 represents H or C 1-6 alkoxy optionally substituted by one or more fluorine atoms; R 3 represents a 5- or 6-membered heterocyclic ring which is optionally substituted; R 4 is a 4-, 5-, 6- or 7-membered heterocyclic ring which is optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted; the process comprising condensing a compound of formula (B), wherein R 1 to R 3 are as defined above; with a compound of formula (C), wherein R 5 and R 6 taken together with the N atom to which they are attached represent a 4-, 5-, 6-, or 7-membered N-containing heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted.
摘要翻译：本发明提供了制备式（A）化合物或其药学上可接受的盐或溶剂合物的方法，其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R 2表示任选被一个或多个氟原子取代的H或C 1-6烷氧基; R 3表示任选被取代的5或6元杂环; R 4是任选地与苯环或5-或6-元杂环稠合的4-，5-，6-或7-元杂环，该环系统作为整体任选被取代; 该方法包括将式（B）化合物（其中R 1至R 3如上所定义）缩合; 与式（C）的化合物反应，其中R 5和R 6与它们所连接的N原子一起代表4-，5-，6-或7-元的含N的杂环该环任选地与苯环或5-或6-元杂环稠合，整个环系统任选被取代。

82. 发明申请

WO02062301A3 METHOD AND COMPOSITION FOR REJUVINATING CELLS, TISSUES, ORGANS, HAIR AND NAILS 审中-公开
标题翻译：重组细胞，组织，器官，头发和指甲的方法和组合
公开(公告)号：WO02062301A3
公开(公告)日：2002-10-17
申请号：PCT/US0203714
申请日：2002-02-07
申请人： FARRINGTON PHARMACEUTICALS LLC , ULRICH PETER C , FANG SHENG DING , BRINES MICHAEL , XIE QIAO WEN , CERAMI ANTHONY
发明人： ULRICH PETER C , FANG SHENG DING , BRINES MICHAEL , XIE QIAO WEN , CERAMI ANTHONY
IPC分类号： C07D233/60 , A61K8/49 , A61K31/415 , A61K31/4174 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/452 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/519 , A61K31/535 , A61K31/5377 , A61K31/5383 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P17/00 , A61P19/02 , A61P25/02 , A61P25/28 , A61P27/02 , A61P27/12 , A61P27/16 , A61P43/00 , A61Q3/00 , A61Q3/02 , A61Q5/00 , A61Q5/12 , A61Q19/00 , A61Q19/08 , C07D213/20 , C07D213/50 , C07D213/57 , C07D213/73 , C07D233/54 , C07D239/26 , C07D239/42 , C07D265/36 , C07D277/22 , C07D277/24 , C07D277/84 , C07D417/06 , C07D487/04 , C07D498/02 , C07D513/04 , C07D521/00 , C07D213/02 , C07D239/02 , C07D277/20 , C07D277/30 , C07D277/60 , C07D401/00 , C07D403/02 , C07D413/02 , C07D417/00
CPC分类号： C07D213/20 , A61K8/49 , A61K8/4986 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/535 , A61Q3/00 , A61Q3/02 , A61Q5/00 , A61Q5/02 , A61Q5/12 , A61Q7/00 , A61Q19/08 , A61Q19/10 , C07D213/50 , C07D213/57 , C07D213/73 , C07D231/12 , C07D233/54 , C07D233/56 , C07D233/64 , C07D239/26 , C07D239/42 , C07D249/08 , C07D277/22 , C07D277/24 , C07D277/84 , C07D417/06 , C07D487/04 , C07D513/04
摘要： In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated coupling of proteins, lipids, nucleic acids, and other biomaterials, and any combination thereof. In another embodiment, the compositions and associated methods have utility in vivo to reduce the deleterious effects of sugar-mediated coupling processes in an organism, when the organism is exposed to the compound or composition internally, by ingestion, transdermal application, or other means. In yet another embodiment, the compositions and associated methods are useful for the ex-vivo treatment of organs, cells and tissues and external treatment of hair, nails and skin to rejuvenate them by changing deformability and increase the tissue fissuion coefficient. In a further embodiment, the present invention relates to novel compounds and pharmaceutical compositions.
摘要翻译：在一个实施方案中，本发明涉及包含药物组合物的化合物和组合物，所述药物组合物含有化合物和解离糖介导的蛋白质，脂质，核酸和其他生物材料偶联的相关方法及其任何组合。在另一个实施方案中，组合物和相关方法在体内通过摄入，经皮施用或其它方式在生物体内部暴露于化合物或组合物时，有效地降低糖介导的生物体中的偶联过程的有害作用。在另一个实施方案中，组合物和相关方法可用于器官，细胞和组织的离体处理以及毛发，指甲和皮肤的外部治疗，以通过改变变形性和增加组织裂隙系数来使其恢复活力。在另一个实施方案中，本发明涉及新化合物和药物组合物。

83. 发明申请

WO01081316A2 SUBSTITUTED PHENYL FARNESYLTRANSFERASE INHIBITORS 审中-公开
标题翻译：取代的苯基呋喃基酯抑制剂
公开(公告)号：WO01081316A2
公开(公告)日：2001-11-01
申请号：PCT/US2001/013678
申请日：2001-04-25
IPC分类号： C07D233/22 , A61K31/381 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/4245 , A61K31/426 , A61K31/4406 , A61K31/4412 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61P17/06 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07D213/30 , C07D213/36 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/80 , C07D213/82 , C07D213/84 , C07D213/85 , C07D231/12 , C07D233/26 , C07D233/54 , C07D249/04 , C07D249/08 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/30 , C07D333/16 , C07D333/24 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/10 , C07D405/12 , C07D409/10 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/10 , C07D417/12 , C07D233/00
CPC分类号： C07D213/30 , C07D213/36 , C07D231/12 , C07D233/64 , C07D249/04 , C07D249/08 , C07D277/24 , C07D277/28 , C07D277/30 , C07D333/16 , C07D333/24 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D409/10 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof, inhibit farnesyltransferase. Methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
摘要翻译：式（I）化合物或其药学上可接受的盐抑制法呢基转移酶。公开了制备该化合物的方法，含该化合物的药物组合物和使用该化合物的治疗方法。

84. 发明申请

WO01017968A1 INTEGRASE INHIBITORS CONTAINING AROMATIC HETEROCYCLE DERIVATIVES 审中-公开
标题翻译：含有芳香杂环衍生物的综合抑制剂
公开(公告)号：WO01017968A1
公开(公告)日：2001-03-15
申请号：PCT/JP2000/005754
申请日：2000-08-25
IPC分类号： A61P31/12 , A61P43/00 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/64 , C07D213/65 , C07D213/68 , C07D215/22 , C07D215/233 , C07D235/16 , C07D239/26 , C07D239/52 , C07D241/12 , C07D241/18 , C07D241/20 , C07D263/32 , C07D277/30 , C07D285/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D473/00 , C07F9/6512 , A61K31/41 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/44 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/47 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/519 , C07D213/53 , C07D215/14 , C07D215/20 , C07D217/16 , C07D235/12 , C07D261/12 , C07D409/06 , C07D487/04
CPC分类号： C07D213/64 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/65 , C07D213/68 , C07D215/233 , C07D235/16 , C07D239/26 , C07D239/52 , C07D241/12 , C07D241/18 , C07D241/20 , C07D263/32 , C07D277/30 , C07D285/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D473/00 , C07F9/65122
摘要： Compounds represented by general formula (I), tautomers thereof, prodrugs of both, pharmaceutically acceptable salts of them, or solvates thereof exhibit an integrase-inhibiting activity. In said formula, X is hydroxyl or the like; Y is -C(=R )-R -R (wherein R and R are each oxygen or the like; and R is hydrogen or optionally substituted alkyl), optionally substituted heteroaryl, or the like; Z is hydrogen or the like; Z and Z are each independently a single bond, alkylene, or the like; Z is a single bond, alkylene, -O-, or the like; R is optionally substituted aryl, optionally substituted heteroaryl, or the like; p is 0 to 2; and A is an optionally substituted aromatic heterocycle.
摘要翻译：由通式（I）表示的化合物，其互变异构体，它们的前药，它们的药学上可接受的盐或其溶剂合物表现出整合酶抑制活性。在所述式中，X是羟基等; Y为-C（= R 2）-R 3 -R 4（其中R 2和R 3各自为氧等，R 4为氢或任选取代的烷基），任选取代的杂芳基等; Z是氢等; Z 1和Z 3各自独立地为单键，亚烷基等; Z 2是单键，亚烷基，-O-等; R 1是任选取代的芳基，任选取代的杂芳基等; p为0〜2; 并且A是任选取代的芳族杂环。

85. 发明申请

WO00042014A2 1-(6- METHYLPYRIDINE- 3-YL)-2-[4- (METHYLSULFONYL) PHENYL] ETHANONE AND METHOD FOR ITS PREPARATION 审中-公开
标题翻译： 1-（6-甲基吡啶-3-基）-2- [4-（甲磺酰基）苯基]乙酮及其制造方法
公开(公告)号：WO00042014A2
公开(公告)日：2000-07-20
申请号：PCT/EP2000/000240
申请日：2000-01-13
IPC分类号： C07D213/50 , C07D213/52 , C07D213/53 , C07D213/57
CPC分类号： C07D213/57 , C07D213/50
摘要： The invention relates to a new starting product for the preparation of COX-2 inhibitors, notably the compound 1-(6- methylpyridine- 3-yl)-2-[(4- (methylsulfonyl) phenyl] ethanone of the formula (I), and to a method for producing same.
摘要翻译：它是用于生产COX-2抑制剂的新的起始材料，化合物1-（6-甲基吡啶-3-基）-2- [4-（甲基磺酰基）苯基]式（I）和它的制备过程的乙酮描述。

86. 发明申请

WO00005210A1 N,N-SUBSTITUTED CYCLIC AMINE DERIVATIVES 审中-公开
标题翻译： N，N-取代的环状氨基衍生物
公开(公告)号：WO00005210A1
公开(公告)日：2000-02-03
申请号：PCT/JP1999/003900
申请日：1999-07-21
IPC分类号： C07D295/08 , A61K31/496 , A61P9/10 , A61P25/28 , C07D213/57 , C07D213/64 , C07D215/20 , C07D217/02 , C07D233/54 , C07D233/58 , C07D239/34 , C07D239/80 , C07D317/64 , C07D333/24 , C07D333/38 , C07D401/12 , C07D403/12 , C07D213/30 , A61K31/36 , A61K31/495 , A61K31/55 , C07D243/08 , C07D295/12 , C07D333/16
CPC分类号： C07D213/64 , C07D213/57 , C07D215/20 , C07D217/02 , C07D233/54 , C07D239/34 , C07D239/80 , C07D295/15 , C07D317/64 , C07D333/24 , C07D333/38
摘要： N,N-substituted cyclic amine derivatives represented by general formula (VIII) or pharmacologically acceptable salts thereof: wherein A represents aryl, etc.; E represents -CO- or -CHOH-; G represents oxygen, etc.; J represents optionally substituted aryl; R represents lower alkyl, etc.; Alk represents linear or branched lower alkylene; n, v, w, x and y independently represent each 0 or 1; and p represents 2 or 3. These compounds or salts thereof are efficacious in treating diseases against which calcium antagonism is efficacious. These diseases include cerebrovascular disorder at the acute stage, cerebral stroke, cerebral infarction, head injury, cerebral nerve cell death, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, brain circulatory disturbance, brain function disturbance, pain, convulsion, schizophrenia, hemicrania, epilepsy, circular psychosis, nerve degeneration diseases, brain ischemia, AIDS, complex dementia, edema, anxiety and diabetic nephropathy.
摘要翻译：由通式（VIII）表示的N，N-取代的环胺衍生物或其药理学上可接受的盐：其中A表示芳基等; E表示-CO-或-CHOH-; G代表氧气等; J表示任选取代的芳基; R 1表示低级烷基等; Alk表示直链或支链低级亚烷基; n，v，w，x和y独立地表示0或1; 并且p代表2或3.这些化合物或其盐在治疗有效钙拮抗作用的疾病中是有效的。这些疾病包括急性期的脑血管障碍，脑中风，脑梗塞，头部损伤，脑神经细胞死亡，阿尔茨海默病，帕金森病，肌萎缩性侧索硬化，亨廷顿病，脑循环障碍，脑功能障碍，疼痛，惊厥，精神分裂症，hemicrania，癫痫，圆形精神病，神经变性疾病，脑缺血，艾滋病，复杂性痴呆，水肿，焦虑和糖尿病肾病。

87. 发明申请

WO99040056A1 HYDROXYLATION ACTIVATED PRODRUGS 审中-公开
标题翻译：羟化活化剂
公开(公告)号：WO99040056A1
公开(公告)日：1999-08-12
申请号：PCT/GB1999/000155
申请日：1999-02-02
IPC分类号： A61K31/085 , A61K31/09 , A61K31/12 , A61K31/145 , A61K31/275 , A61K31/4406 , A61K31/4418 , A61P35/00 , A61P43/00 , C07C43/215 , C07C49/84 , C07C205/35 , C07C255/36 , C07C327/44 , C07C327/48 , C07D213/57
CPC分类号： C07C43/215 , C07C49/84 , C07C205/35 , C07C255/36 , C07C327/48 , C07C2602/10 , C07D213/57
摘要： The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.
摘要翻译：本发明涉及酶促芳族羟基化活化的前体药物，特别是抗肿瘤前体药物以及由CYP1B1酶的羟基化活性特异性活化的药物。

88. 发明申请

WO99005109A1 PYRIDYLACRYLAMIDE DERIVATIVES AND NEPHRITIS REMEDIES AND TGF- beta INHIBITORS CONTAINING THE SAME 审中-公开
标题翻译：吡啶酰胺衍生物和含有相同抗原的补体和TGF-β抑制剂
公开(公告)号：WO99005109A1
公开(公告)日：1999-02-04
申请号：PCT/JP1998/003312
申请日：1998-07-24
IPC分类号： C07D213/56 , C07D213/57 , A61K31/44 , A61K31/535 , C07D213/59 , C07D213/61 , C07D213/66 , C07D213/80 , C07D401/12
CPC分类号： C07D213/56
摘要： Compounds represented by general formula (I), and nephritis remedies and TGF- beta inhibitors containing the same, wherein Ar is (substituted) pyridyl; Ar is (substituted) phenyl; R is H, alkyl or aryl; R is H, alkyl, cyano or alkoxycarbonyl; R is H or (substituted) alkyl; X is O or S; A and B are each H, OH, alkoxy or alkylthio, or alternatively they together form oxo, thioxo, =N-Y (wherein Y is dialkylamino, OH, aralkyloxy or alkoxy) or -Z -M-Z - (wherein Z and Z are each O, S or optionally alkyl-substituted imino; and M is alkylene or phenylene), or B may be 1-alkylimidazol-2-yl with A being OH; and n is an integer of 1 to 3.
摘要翻译：由通式（I）表示的化合物，以及含有该化合物的肾炎疗法和TGF-β抑制剂，其中Ar 1是（取代的）吡啶基; Ar 2是（取代的）苯基; R 1是H，烷基或芳基; R 2是H，烷基，氰基或烷氧基羰基; R 3是H或（取代的）烷基; X是O或S; A和B各自为H，OH，烷氧基或烷硫基，或者它们一起形成氧代，硫代，= NY（其中Y是二烷基氨基，OH，芳烷氧基或烷氧基）或-Z 1 -MZ 2 - （其中 Z 1和Z 2各自为O，S或任选的烷基取代的亚氨基; M为亚烷基或亚苯基），或B可为具有A为OH的1-烷基咪唑-2-基; n为1〜3的整数。

89. 发明申请

WO99000356A1 SUBSTITUTED N-[(AMINOIMINOMETHYL OR AMINOMETHYL)PHENYL]PROPYL AMIDES 审中-公开
标题翻译：取代的N - [（氨基亚氨基或氨基甲基）苯基]丙烯酰胺
公开(公告)号：WO99000356A1
公开(公告)日：1999-01-07
申请号：PCT/US1998/013550
申请日：1998-06-26
IPC分类号： C07D249/04 , A61K31/00 , A61K31/165 , A61K31/166 , A61K31/195 , A61K31/215 , A61K31/216 , A61K31/24 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/4196 , A61K31/426 , A61K31/433 , A61K31/437 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4436 , A61K31/4439 , A61K31/4545 , A61K31/47 , A61P7/00 , A61P7/02 , A61P43/00 , C07C45/63 , C07C205/06 , C07C205/57 , C07C229/28 , C07C233/64 , C07C251/02 , C07C255/60 , C07C257/18 , C07C259/18 , C07D205/08 , C07D207/32 , C07D207/325 , C07D207/327 , C07D209/08 , C07D209/48 , C07D213/40 , C07D213/54 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/58 , C07D213/70 , C07D213/74 , C07D213/82 , C07D213/89 , C07D215/04 , C07D215/48 , C07D231/14 , C07D233/54 , C07D233/56 , C07D235/04 , C07D235/06 , C07D235/08 , C07D249/06 , C07D277/20 , C07D277/28 , C07D277/56 , C07D285/08 , C07D317/46 , C07D317/60 , C07D319/16 , C07D319/18 , C07D333/70 , C07D401/04 , C07D409/04 , C07D417/04 , C07D471/04 , C07D521/00
CPC分类号： C07D207/327 , C07C45/63 , C07C205/57 , C07C255/60 , C07C257/18 , C07C259/18 , C07C2601/14 , C07C2603/08 , C07D205/08 , C07D209/08 , C07D209/48 , 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 , C07D409/04 , C07D417/04 , C07D471/04 , C07C47/565
摘要： This invention relates to compounds of formula (I) which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
摘要翻译：本发明涉及抑制因子Xa的式（I）化合物，含有该化合物的药物组合物，以及该化合物用于治疗患有可通过施用因子Xa抑制剂而可以改善的病症的患者的用途。

90. 发明申请

WO1992018481A1 STYRYL-SUBSTITUTED HETEROARYL COMPOUNDS WHICH INHIBIT EGF RECEPTOR TYROSINE KINASE 审中-公开
标题翻译：抑制EGF受体酪氨酸激酶的异黄酮替代化合物
公开(公告)号：WO1992018481A1
公开(公告)日：1992-10-29
申请号：PCT/US1991007698
申请日：1991-10-15
申请人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS), ... , SPADA, Alfred, P. , PERSONS, Paul, E. , LEVITZKI, Alexander , GILON, Chaim , GAZIT, Aviv
发明人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS), ...
IPC分类号： C07D213/57
CPC分类号： C07D213/89 , A61K31/404 , A61K31/4406 , C07D209/18 , C07D213/57
摘要： Methods of inhibiting cell proliferation in a patient suffering from such disorder comprising the use of a styryl-substituted heteroaryl compound wherein the heteroaryl group is a monocyclic ring with 1 or 2 heteroatoms, or a bicyclic ring with 1 to about 4 heteroatoms, said compound optionally substituted or polysubstituted, with the proviso that when said ring is polysubstituted, the substituents do not have a common point of attachment to said ring, and those compounds wherein no substituent on the heteroaryl group is a carboxy group or an ester group, and pharmaceutical compositions comprising such compounds.
摘要翻译：抑制患有这种病症的患者的细胞增殖的方法包括使用苯乙烯基取代的杂芳基化合物，其中杂芳基是具有1或2个杂原子的单环，或具有1至约4个杂原子的双环，所述化合物任选地取代或多取代，条件是当所述环是多取代时，取代基不具有与所述环的共同连接点，并且其中杂芳基上没有取代基是羧基或酯基的那些化合物，以及药物组合物包括这样的化合物。

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