公开(公告)号：US4735966A

公开(公告)日：1988-04-05

申请号：US900025

申请日：1986-08-25

Applicant: Helen Y. Wu ,  Walter Kurz

Inventor： Helen Y. Wu ,  Walter Kurz

IPC: C07C27/00 ,  C07C35/31 ,  C07C35/52 ,  C07C41/00 ,  C07C43/196 ,  C07C43/23 ,  C07C45/00 ,  C07C45/29 ,  C07C45/30 ,  C07C45/45 ,  C07C45/59 ,  C07C45/71 ,  C07C45/78 ,  C07C47/267 ,  C07C47/27 ,  C07C47/273 ,  C07C47/277 ,  C07C59/46 ,  C07C59/54 ,  C07C59/62 ,  C07C59/72 ,  C07C67/00 ,  C07C69/732 ,  C07C231/00 ,  C07C231/12 ,  C07C233/25 ,  C07C235/64 ,  C07C275/28 ,  A61K31/045 ,  A61K31/11 ,  A61K31/19 ,  A61K31/215

CPC classification number: C07C59/62 ,  C07C35/31 ,  C07C43/196 ,  C07C45/292 ,  C07C45/305 ,  C07C45/455 ,  C07C45/59 ,  C07C45/71 ,  C07C45/78 ,  C07C47/267 ,  C07C47/27 ,  C07C47/273 ,  C07C47/277 ,  Y10S514/824

Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): ##STR1## wherein: A is --C.tbd.C--, trans --HC.dbd.CH--, --CH.sub.2 CH.sub.2 -- or --CH.dbd.CHCH.sub.2 --;X is lower alkoxy, hydroxy, or (2,2,2)-trifluoroethoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);is an integer of 2-4;R.sub.1 is --CH.sub.2 OH, --CHO, --CO.sub.2 R or --CO.sub.2 H, and the olefin formed by the R.sub.1 (CH.sub.2).sub.n CH.dbd. moiety is either (E) or (Z);R.sub.2 is hydrogen or methyl, or optionally --CH.dbd.CH.sub.2 when A is --CH.dbd.CHCH.sub.2 --; andR.sub.3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, ##STR2## --(CH.sub.2).sub.m -phenyl or CH.sub.2 O-phenyl; in which each phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen;in which:a is an integer of 0, 1 or 2;b is an integer of 3-7;m is an integer of 0, 1 or 2; andR is ##STR3## wherein x is ##STR4## in which each R.sub.4 is independently hydrogen or lower alkyl having 1-6 carbon atoms,and the pharmaceutically acceptable, non-toxic salts and esters thereof.

Abstract translation: （1），（2）和（3）中描述了可用于治疗心血管疾病如血栓形成，高血压和动脉粥样硬化的化合物：其中：A 是-C 3 D C，反-HC = CH - ， - CH 2 CH 2 - 或-CH = CHCH 2 - ; X是低级烷氧基，羟基或（2,2,2） - 三氟乙氧基; Y是氢，外 - （低级烷基）或内 - （低级烷基）; 是2-4的整数; R 1是-CH 2 OH，-CHO，-CO 2 R或-CO 2 H，由R 1（CH 2）n CH =部分形成的烯烃是（E）或（Z）; 当A为-CH = CHCH 2 - 时，R 2为氢或甲基，或任选地-CH = CH 2; 并且R 3是具有5-10个碳原子的直链或支链烷基，烯基或炔基，（CH 2）m - 苯基或CH 2 O-苯基; 其中每个苯基可以任选被低级烷基，低级烷氧基，三氟甲基或卤素取代; 其中：a为0,1或2的整数; b是3-7的整数; m是0,1或2的整数; 并且R是其中每个R 4独立地是氢或具有1-6个碳原子的低级烷基，其中x是其中X是 + TR＆lt; IMAGE＆gt;和其药学上可接受的无毒盐和酯。

公开(公告)号：US4608388A

公开(公告)日：1986-08-26

申请号：US716872

申请日：1985-03-27

Applicant: Arthur F. Kluge ,  Anthony L. Willis ,  Counde O'Yang

Inventor： Arthur F. Kluge ,  Anthony L. Willis ,  Counde O'Yang

IPC: C07C43/178 ,  A61K31/045 ,  A61K31/085 ,  A61K31/11 ,  A61K31/19 ,  A61K31/215 ,  A61P3/06 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07C27/00 ,  C07C29/147 ,  C07C33/05 ,  C07C35/31 ,  C07C41/00 ,  C07C45/00 ,  C07C45/29 ,  C07C45/30 ,  C07C47/26 ,  C07C47/267 ,  C07C47/27 ,  C07C47/273 ,  C07C47/277 ,  C07C49/743 ,  C07C49/747 ,  C07C51/00 ,  C07C53/136 ,  C07C59/42 ,  C07C59/46 ,  C07C59/56 ,  C07C59/62 ,  C07C67/00 ,  C07C69/02 ,  C07C69/73 ,  C07C69/732 ,  C07C69/734 ,  C07C233/12 ,  C07C233/16 ,  C07C233/24 ,  C07C233/25 ,  C07C233/75 ,  C07C275/34 ,  C07F7/18 ,  H04N9/79 ,  C07C69/74

CPC classification number: C07F7/1856 ,  C07C35/31 ,  C07C403/08 ,  C07C403/16 ,  C07C45/292 ,  C07C45/305 ,  C07C47/267 ,  C07C47/27 ,  C07C47/273 ,  C07C47/277 ,  C07C49/743 ,  C07C49/747 ,  C07C59/46 ,  C07C59/56 ,  H04N9/7921 ,  C07B2200/07 ,  C07B2200/09 ,  C07C2101/14

Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): ##STR1## wherein: n is 2 or 3;R.sub.1 is CH.sub.2 OH, CHO, CO.sub.2 R or CO.sub.2 H;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl having 5-10 carbon atoms, ##STR2## optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen,in whicha is 0, 1 or 2;b is 3-7;m is 1 or 2; andR is ##STR3## in which each R.sub.4 is independently hydrogen or lower alkyl having 1-6 carbon atoms,and the pharmaceutically acceptable, non-toxic salts and esters thereof.

Abstract translation: （1），（2）和（3）中描述的化合物是：治疗心血管疾病如血栓形成，高血压和动脉粥样硬化的化合物是：（1） 其中：n为2或3; R1是CH2OH，CHO，CO2R或CO2H; R2是氢或甲基; 并且R 3是具有5-10个碳原子的直链或支链烷基，其中a是0,1或2，或者被低级烷基，低级烷氧基，三氟甲基或卤素任选取代的（CH 2） b为3-7; m为1或2; 并且R是每个R 4独立地是氢或具有1-6个碳原子的低级烷基的化合物，和其药学上可接受的无毒盐和酯。

公开(公告)号：US4988823A

公开(公告)日：1991-01-29

申请号：US372062

申请日：1989-06-27

Applicant: Johannes Kaulen

Inventor： Johannes Kaulen

IPC: A01N43/24 ,  C07B53/00 ,  C07C45/00 ,  C07C47/273 ,  C07C67/00 ,  C07C309/65 ,  C07D249/08 ,  C07D411/04 ,  C07D521/00

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D411/04

Abstract: Optically active oxiranes of the formula ##STR1## in which R represents substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or represents substituted or unsubstituted phenyl, andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent hydrogen or alkyl, at least one of the radicals representing alkyl, orR.sup.4 and R.sup.5 together represent alkanediyl, which is unsubstituted or substituted by alkyl, or R.sup.4 and R.sup.5 together with the adjacent carbon atoms represent a fused bicyclic hydrocarbon radical, which is unsubstituted or substituted by alkylare produced by reacting an enantiomerically pure oxathiane ketone of the formula ##STR2## with a sulphonium or sulphoxonium salt. The product can be converted to optically active 2-hydroxyethylazole derivatives of the formula ##STR3##

Abstract translation: 式（I）的光学活性环氧乙烷，其中R表示取代或未取代的烷基，取代或未取代的环烷基或表示取代或未取代的苯基，且R 1，R 2，R 3，R 4，R 5和R 6表示氢或烷基， 代表烷基的至少一个基团，或者R 4和R 5一起表示未被取代或被烷基取代的烷二基，或者R4和R5与相邻的碳原子一起表示稠合的双环烃基，其未被取代或被烷基取代 通过将式（IMA）（II）的对映异构体纯的氧硫杂环己酮与锍盐或磺基锍盐反应。 该产物可以转化成式（VI）的光学活性2-羟基乙唑衍生物，

公开(公告)号：US4929772A

公开(公告)日：1990-05-29

申请号：US321171

申请日：1989-03-09

Applicant: Pietro Massardo ,  Franco Bettarini ,  Paolo Piccardi ,  Franco Rama

Inventor： Pietro Massardo ,  Franco Bettarini ,  Paolo Piccardi ,  Franco Rama

IPC: B01J23/00 ,  B01J27/00 ,  C07B31/00 ,  C07B41/02 ,  C07B61/00 ,  C07C27/00 ,  C07C29/64 ,  C07C41/30 ,  C07C43/23 ,  C07C45/00 ,  C07C45/68 ,  C07C47/195 ,  C07C47/273 ,  C07C47/56 ,  C07C49/82 ,  C07C51/367 ,  C07C67/00 ,  C07C69/675 ,  C07C69/757 ,  C07C201/00 ,  C07C205/26 ,  C07C205/58 ,  C07C213/00 ,  C07C215/68 ,  C07C253/00 ,  C07C255/53 ,  C07C313/00 ,  C07C319/20 ,  C07C323/12 ,  C07D213/30 ,  C07D307/42 ,  C07D333/16

CPC classification number: C07D213/30 ,  C07C205/26 ,  C07C29/64 ,  C07C37/20 ,  C07C41/30 ,  C07C45/68 ,  C07C47/195 ,  C07C47/56 ,  C07C67/343 ,  C07D307/42 ,  C07D333/16

Abstract: There is disclosed a process for preparing polyhalogenated carbinols having formula: ##STR1## by reacting a compound having formula: ##STR2## with a system consisting of a compound having formula: ##STR3## and of a divalent metal or of a metal salt, in protic dipolar solvents, in which formulaeR=H, an alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkadienyl, phenyl, naphthyl, anthracyl group, a heterocyclic radical, optionally substituted;R'=H, a haloalkyl, --CN, --COOR" group with R" equal to H or to an alkyl group;X.sup.1 =Cl, Br; =X.sub.2 =F, Cl, Br;X.sup.3 =Cl, Br, CF.sub.3, CCl.sub.3 ; Y=Br or Cl when X.sup.1, X.sup.2 and X.sup.3 are different from Br.

Abstract translation: 公开了一种制备具有下式的多卤代甲醇的方法：通过使具有下式的化合物：（II）与具有下列化学式的化合物：（IMA）（III）和式 二价金属或金属盐，在质子偶极溶剂中，其中式R = H，烷基，环烷基，烯基，环烯基，链二烯基，苯基，萘基，蒽基，杂环基，任选取代; R'= H，R“等于H的卤代烷基，-CN，-COOR”基团或烷基; X1 = Cl，Br; = X2 = F，Cl，Br; X3 = Cl，Br，CF3，CCl3; 当X1，X2和X3与Br不同时，Y = Br或Cl。

公开(公告)号：US4900846A

公开(公告)日：1990-02-13

申请号：US113153

申请日：1987-10-27

Applicant: Gregory P. Harris

Inventor： Gregory P. Harris

IPC: C07D319/06 ,  C07C45/59 ,  C07C47/27 ,  C07C47/273 ,  C07C47/277 ,  C07C51/00 ,  C07C51/353 ,  C07C59/48 ,  C07C59/52 ,  C07C59/56 ,  C07C59/64 ,  C07C67/00 ,  C07C69/035 ,  C07C201/00 ,  C07C205/56 ,  C07C231/00 ,  C07C231/12 ,  C07C233/18 ,  C07C233/25 ,  C07C233/33 ,  C07C301/00 ,  C07C303/40 ,  C07C311/03 ,  C07C311/51 ,  C07D307/20 ,  C07D307/33 ,  C07D319/08

CPC classification number: C07D307/33 ,  C07C59/64 ,  C07D307/20 ,  C07D319/08

Abstract: The invention provides a novel process for making novel (4-phenyl-1,3-dioxan-cis-5-yl)alkenoic acids of the formula I in which Ra and Rb are independently hydrogen, alkenyl, alkyl, halogenoalkyl, pentafluorophenyl, aryl or aryl-(1,4C)alkyl; or Ra and Rb together are polymethylene; Rc is hydroxy or (1-6C)alkanesulphonamideo, A is vinylene, n is 1, Y is polymethylene, and benzene ring B bears various optional substituents. The process involves the reaction of an aldehyde of formula II with an ylid to give an erythro-diol of formula III which is then cyclized to the required dioxane derivative of formula I. The invention also provides a novel process for making the aldehydes of formula II from the corresponding lactols of formula IIa, which are themselves obtained with the correct trans-stereochemistry by two selective reductions of a trans-phenylparaconic acid of formula V. The compounds of formula I are useful as thereapeutic agents.

公开(公告)号：US09481660B2

公开(公告)日：2016-11-01

申请号：US14246741

申请日：2014-04-07

Applicant: Jonathan Daniel Heller ,  Qingqi Chen ,  Rocio Alejandra Lopez ,  Amanda Jean Morris

Inventor： Jonathan Daniel Heller ,  Qingqi Chen ,  Rocio Alejandra Lopez ,  Amanda Jean Morris

IPC: C07C33/26 ,  C07D295/088 ,  C07C37/50 ,  C07C39/367 ,  C07C43/225 ,  C07C43/23 ,  C07C47/27 ,  C07C47/273 ,  C07C217/20 ,  C07D277/24 ,  C07C39/21 ,  C07C43/205 ,  C07C217/54

CPC classification number: C07D295/088 ,  C07C37/50 ,  C07C39/21 ,  C07C39/367 ,  C07C43/2055 ,  C07C43/225 ,  C07C43/23 ,  C07C47/27 ,  C07C47/273 ,  C07C217/20 ,  C07C217/54 ,  C07C255/33 ,  C07D277/24 ,  C07C39/16

Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.

Abstract translation: 本发明涉及去甲二氢愈创木酸衍生物化合物，即丁烷桥改性的二氢愈创木酸（NDGA）化合物和丁烷桥改性的四-O-取代的NDGA化合物，含有它们的药物组合物，制备它们的方法及其使用方法和试剂盒 包括它们用于治疗疾病和病症，特别是由HIV感染，HPV感染或HSV感染引起的或与病毒感染相关的疾病，诸如各种类型的关节炎和炎症性肠病的炎性疾病， 代谢疾病，如糖尿病和高血压，或增殖性疾病，如各种类型的癌症。

公开(公告)号：US5113007A

公开(公告)日：1992-05-12

申请号：US610827

申请日：1990-11-08

Applicant: Jean-Claude Combret ,  Jean-Louis Klein ,  Joel Le Gaillard

Inventor： Jean-Claude Combret ,  Jean-Louis Klein ,  Joel Le Gaillard

IPC: C07C45/51 ,  C07C47/273 ,  C07C47/277 ,  C07F7/18

CPC classification number: C07F7/1856 ,  C07C45/511 ,  C07C47/273 ,  C07C47/277 ,  C07F7/1852

Abstract: New dienoxysilanes of the general formula: ##STR1## and new .alpha.-halo .alpha.-ethylene aldehydes to which they give access, having the general formula: ##STR2## These new compounds constitute important synthesis intermediates opening a new path for access to macrolides such as pyrenophorine, norpyrenophorine or vermiculine.

Abstract translation: 新的具有以下通式的新二烯氧基硅烷：和它们可以进入的新的α-卤代α-亚乙基醛，具有以下通式：这些新化合物构成重要的合成中间体，为获得大环内酯类如 芘炔，赤霉素或蛭石。

公开(公告)号：US4873329A

公开(公告)日：1989-10-10

申请号：US704038

申请日：1985-02-21

Applicant: Leslie R. Hughes ,  John Oldfield ,  Howard Tucker

Inventor： Leslie R. Hughes ,  John Oldfield ,  Howard Tucker

IPC: A61K31/045 ,  A61K31/075 ,  A61K31/095 ,  A61K31/10 ,  A61K31/12 ,  A61K31/135 ,  A61K31/165 ,  A61K31/18 ,  A61K31/22 ,  A61K31/235 ,  A61K31/27 ,  A61K31/275 ,  A61K31/44 ,  A61K31/47 ,  A61K31/473 ,  A61K31/52 ,  A61P17/00 ,  C07C17/23 ,  C07C17/26 ,  C07C33/28 ,  C07C33/34 ,  C07C33/40 ,  C07C33/48 ,  C07C33/50 ,  C07C43/14 ,  C07C43/20 ,  C07C43/23 ,  C07C45/26 ,  C07C45/54 ,  C07C45/72 ,  C07C45/74 ,  C07C47/273 ,  C07C49/213 ,  C07C49/227 ,  C07C49/235 ,  C07C49/245 ,  C07C49/248 ,  C07C49/255 ,  C07C59/56 ,  C07C69/02 ,  C07C205/19 ,  C07C205/26 ,  C07C205/34 ,  C07C215/28 ,  C07C215/68 ,  C07C235/06 ,  C07C255/32 ,  C07C255/53 ,  C07C317/00 ,  C07D213/34 ,  C07D213/57 ,  C07D213/61 ,  C07D213/70 ,  C07D213/71 ,  C07D215/06 ,  C07D215/14 ,  C07D215/16 ,  C07D215/36 ,  C07D219/04 ,  C07D219/16 ,  C07D233/84 ,  C07D239/38 ,  C07D239/46 ,  C07D239/47 ,  C07D239/56 ,  C07D249/12 ,  C07D251/38 ,  C07D277/24 ,  C07D277/36 ,  C07D303/08 ,  C07D333/16 ,  C07D333/28 ,  C07D333/38 ,  C07D333/44 ,  C07D339/06 ,  C07D339/08 ,  C07D473/00 ,  C07D473/24 ,  C07D473/38 ,  C07D487/04 ,  C07D521/00 ,  C07F7/08

CPC classification number: C07C17/23 ,  C07C17/278 ,  C07C205/26 ,  C07C205/45 ,  C07C255/00 ,  C07C317/00 ,  C07C323/00 ,  C07C33/483 ,  C07C33/50 ,  C07C45/26 ,  C07C45/54 ,  C07C45/72 ,  C07C45/74 ,  C07C47/273 ,  C07C49/235 ,  C07C49/245 ,  C07C49/248 ,  C07C59/56 ,  C07D213/34 ,  C07D213/57 ,  C07D213/61 ,  C07D213/70 ,  C07D213/71 ,  C07D215/14 ,  C07D215/36 ,  C07D219/04 ,  C07D233/84 ,  C07D239/38 ,  C07D239/47 ,  C07D239/56 ,  C07D249/12 ,  C07D251/38 ,  C07D277/24 ,  C07D277/36 ,  C07D303/08 ,  C07D333/28 ,  C07D333/38 ,  C07D333/44 ,  C07D339/06 ,  C07D473/24 ,  C07D473/38 ,  C07D487/04 ,  C07F7/0818

Abstract: A compound of the formula ##STR1## wherein X has the formula ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl; wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent selected from halogeno, nitro, cyano, trifluoromethyl, alkylthio, alkylsulphinyl and alkylsulphonyl or each is hydrogen, alkyl, alkoxy or dialkylamino provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent; wherein R.sup.5 and R.sup.6, which may be the same or different, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 is carbamoyl, alkyl, cycloalkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalkenyl, halogenoalkynyl, alkanoyl, alkylcarbamoyl, dialkylcarbamoyl or aroyl; or wherein R.sup.8 is alkyl or alkenyl which bears one or more substituents selected from cyano, carbamoyl, amino, hydroxy, alkanoyl, alkoxy, alkylthio, alkenylthio, alkylsulphinyl, alkenylsulphinyl, alkylsulphonyl, alkenylsulphonyl, alkanoylamino, alkoxycarbonylamino, alkylsulphonamido, alkylamino, dialkylamino, dialkylsulphamoyl, aroyl, aryl, arylthio, arylsulphinyl, arylsulphonyl, heterocyclylthio, heterocyclylsulphinyl and heterocyclylsulphonyl; or wherein R.sup.8 has the formula ##STR3## wherein ring B is phenyl, naphthyl or heterocyclyl and wherein R.sup.2, R.sup.3 and R.sup.4 have any of the meanings stated above, provided that when R.sup.7 is methyl R.sup.8 is not also methyl.

Abstract translation: 式（I）的化合物，其中X具有式“IMAGE”，其中环A是苯基，萘基或杂环基; 其中R1是氢，烷基，烷酰基或芳酰基; 其中R 2，R 3和R 4可以相同或不同，各自为选自卤素，硝基，氰基，三氟甲基，烷硫基，烷基亚磺酰基和烷基磺酰基的吸电子取代基，或者各自为氢，烷基，烷氧基或二烷基氨基，条件是当环 A是苯基或萘基，R 2，R 3和R 4中的至少一个是吸电子取代基; 其中R 5和R 6可以相同或不同，各自为氢，卤代或烷基; 其中R 7是烷基或卤代烷基; 并且其中R8是氨基甲酰基，烷基，环烷基，烯基，炔基，卤代烷基，卤代烯基，卤代炔基，烷酰基，烷基氨基甲酰基，二烷基氨基甲酰基或芳酰基。 或其中R8是具有一个或多个选自氰基，氨基甲酰基，氨基，羟基，烷酰基，烷氧基，烷硫基，烯硫基，烷基亚磺酰基，烯基亚磺酰基，烷基磺酰基，烯基磺酰基，烷酰基氨基，烷氧基羰基氨基，烷基磺酰氨基，烷基氨基，二烷基氨基，二烷基氨基磺酰基 ，芳酰基，芳基，芳硫基，芳基亚磺酰基，芳基磺酰基，杂环硫基，杂环基亚磺酰基和杂环基磺酰基; 或其中R 8具有式“IMAGE”，其中环B为苯基，萘基或杂环基，并且其中R2，R3和R4具有上述任何含义，条件是当R 7为甲基时，R 8也不是甲基。

公开(公告)号：US6028103A

公开(公告)日：2000-02-22

申请号：US822550

申请日：1997-03-19

Applicant: Carlo Brugnara ,  Jose Halperin ,  Emile M. Bellot, Jr. ,  Mark Froimowitz ,  Richard John Lombardy ,  John J. Clifford ,  Ying-Duo Gao ,  Reem M. Haidar ,  Eugene W. Kelleher ,  Falguni M. Kher ,  Adel M. Moussa ,  Yesh P. Sachdeva ,  Minghua Sun ,  Heather N. Taft

Inventor： Carlo Brugnara ,  Jose Halperin ,  Emile M. Bellot, Jr. ,  Mark Froimowitz ,  Richard John Lombardy ,  John J. Clifford ,  Ying-Duo Gao ,  Reem M. Haidar ,  Eugene W. Kelleher ,  Falguni M. Kher ,  Adel M. Moussa ,  Yesh P. Sachdeva ,  Minghua Sun ,  Heather N. Taft

IPC: C07D295/14 ,  A61K31/015 ,  A61K31/02 ,  A61K31/045 ,  A61K31/11 ,  A61K31/135 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/275 ,  A61K31/34 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4453 ,  A61P35/00 ,  A61P43/00 ,  C07C15/16 ,  C07C17/35 ,  C07C22/04 ,  C07C25/18 ,  C07C33/24 ,  C07C33/28 ,  C07C33/34 ,  C07C33/46 ,  C07C39/15 ,  C07C39/367 ,  C07C43/164 ,  C07C43/225 ,  C07C43/23 ,  C07C45/00 ,  C07C45/44 ,  C07C47/23 ,  C07C47/24 ,  C07C47/273 ,  C07C49/163 ,  C07C49/215 ,  C07C49/233 ,  C07C57/38 ,  C07C57/40 ,  C07C57/46 ,  C07C57/58 ,  C07C69/616 ,  C07C69/65 ,  C07C69/76 ,  C07C211/27 ,  C07C211/52 ,  C07C211/54 ,  C07C215/68 ,  C07C229/14 ,  C07C233/11 ,  C07C239/20 ,  C07C239/22 ,  C07C255/33 ,  C07C255/35 ,  C07C259/06 ,  C07C321/10 ,  C07D207/26 ,  C07D213/06 ,  C07D213/16 ,  C07D213/20 ,  C07D213/30 ,  C07D295/145 ,  C07D307/33 ,  C07F7/08 ,  C07F7/10 ,  C07F7/30 ,  C07F9/50 ,  C07F9/535 ,  A61K31/28 ,  C07C255/04

CPC classification number: C07F9/5352 ,  C07C15/16 ,  C07C17/35 ,  C07C211/27 ,  C07C211/52 ,  C07C211/54 ,  C07C215/68 ,  C07C22/04 ,  C07C233/11 ,  C07C239/22 ,  C07C25/18 ,  C07C255/33 ,  C07C255/35 ,  C07C259/06 ,  C07C321/10 ,  C07C33/34 ,  C07C33/46 ,  C07C39/367 ,  C07C43/164 ,  C07C43/225 ,  C07C43/23 ,  C07C45/004 ,  C07C45/44 ,  C07C47/23 ,  C07C47/24 ,  C07C49/215 ,  C07C49/233 ,  C07C57/38 ,  C07C57/58 ,  C07C69/616 ,  C07C69/65 ,  C07C69/76 ,  C07D207/26 ,  C07D213/16 ,  C07D213/20 ,  C07D213/30 ,  C07D295/145 ,  C07D307/33 ,  C07F7/0818 ,  C07F7/30 ,  C07F9/5022 ,  C07C2101/14

Abstract: The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. The compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Abstract translation: 本发明提供了一类用于治疗镰状细胞病和有害或异常细胞增殖的有效药物的化学化合物。 活性化合物是取代的三芳基甲烷化合物或其类似物，其中一个或多个芳基被杂芳基，环烷基或杂环烷基代替，和/或叔碳原子被不同的原子代替，例如Si，Ge，N或 P.该化合物抑制哺乳动物细胞增殖，抑制红细胞的Gardos通道，减少镰状红细胞脱水和/或延迟红细胞镰状或变形的发生。

公开(公告)号：US5072008A

公开(公告)日：1991-12-10

申请号：US365699

申请日：1989-06-14

Applicant: Gregory D. Harris

Inventor： Gregory D. Harris

IPC: C07D307/30 ,  C07C45/59 ,  C07C47/27 ,  C07C47/273 ,  C07C47/277 ,  C07C59/48 ,  C07C205/44 ,  C07D307/20 ,  C07D307/33

CPC classification number: C07D307/20 ,  C07C201/12 ,  C07C45/59 ,  C07C47/27 ,  C07C47/273 ,  C07C47/277

Abstract: The invention concerns a novel process for the stereospecific manufacture of novel hydroxymethyl lactols of the formula I by a one step reduction of a corresponding lactone carboxylic ester of the formula II (many of which esters are novel) using a reducing agent such as diisobutylaluminium hydride at about ambient temperature. The lactols of formula I are intermediates for the production of pharmacologically active 1,3-dioxane alkenoic acids useful in the treatment of certain cardiovascular and pulmonary medical conditions. Certain of the esters of formula II are novel and are also included in the invention.