| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 二萜化合物单体及其制法和在制备治疗抗癌药物中的应用 | CN200410041150.3 | 2004-07-02 | CN1594267A | 2005-03-16 | 章永红 |
| 一种抗癌药物贝壳衫烷型二萜化合物单体ent－kauran－19－al－17－oic acid，它是从圆滑番荔枝茎中提取得到的抗癌化合物单体，其制备方法是首先将风干的圆滑荔枝茎粉碎后用乙醇提取，浓缩得浸膏；其次，再用氯仿提取，经柱层析，用洗脱剂脱洗后再柱层析；最后再用洗脱剂脱洗而得到贝壳杉烷型二萜化合物单体，经抗癌药理实验，对人肝癌细胞、人胃癌细胞的生长有明显的抑制作用，并具有高效低毒、毒副作用小、抗癌谱广、抗癌活性高等优点。 | ||||||
| 2 | PD-1/PD-L1抑制剂的盐及结晶形式 | CN202080086507.7 | 2020-11-10 | CN114829366A | 2022-07-29 | Z·贾; S·陈; Y·李; T·马丁; 沈博; N·苏; J·周; Q·李 |
| 本申请涉及PD‑1/PD‑L1抑制剂4,4'‑(((((2,2'‑二氯‑[1,1'‑联苯]‑3,3'‑二基)双(氮烷二基))双(羰基))双(1‑甲基‑1,4,6,7‑四氢‑5H‑咪唑并[4,5‑c]吡啶‑2,5‑二基))双(乙烷‑2,1‑二基))双(双环[2.2.1]庚烷‑1‑甲酸)的固体形式和盐形式，包括其制备过程，其中所述固体形式和盐形式可用于治疗包括感染性疾病和癌症在内的各种疾病。 | ||||||
| 3 | 3,3－二甲基－2－甲酰基环丙烷羧酸衍生物的制造方法 | CN02828520.4 | 2002-12-26 | CN1622929A | 2005-06-01 | 吉川享志 |
| 通式(2)的3，3－二甲基－2－甲酰基环丙烷羧酸衍生物的制造方法，该方法包括在钌化合物存在下，使通式(1)的3，3－二甲基－2－(2－甲基－1－丙烯基)环丙烷羧酸化合物与高碘酸化合物进行反应：如(2)式其中R是氢、取代的或未取代的烷基、取代的或未取代的芳基或取代的或未取代的芳烷基，如(1)式其中R如上面所定义。 | ||||||
| 4 | 3,3－二甲基－2－甲酰基环丙烷羧酸衍生物的制造方法 | CN02828520.4 | 2002-12-26 | CN1289457C | 2006-12-13 | 吉川享志 |
| 通式(2)的3，3-二甲基-2-甲酰基环丙烷羧酸衍生物的制造方法，该方法包括在钌化合物存在下，使通式(1)的3，3-二甲基-2-(2-甲基-1-丙烯基)环丙烷羧酸化合物与高碘酸化合物进行反应：1式其中R是氢、取代的或未取代的烷基、取代的或未取代的芳基或取代的或未取代的芳烷基，2式其中R如上面所定义。 | ||||||
| 5 | 2－(羟甲基)环丙烷羧酸化合物的制备方法 | CN03821517.9 | 2003-09-05 | CN1681767A | 2005-10-12 | 南田龙; 板垣诚 |
| 本发明提供式(2)所示2－(羟甲基)环丙烷羧酸化合物的制备方法，其特征在于，在选自钌催化剂、钴催化剂、铑催化剂、镍催化剂、钯催化剂和铂催化剂的催化剂的存在下，使式(1)所示的化合物与氢供体反应，(式中，R1表示氢原子，直链状、支链状或环状烷基，或者取代或未取代的芳基；R2和R3相同或不同，表示氢原子或甲基；R4表示被选自取代芳基和未取代芳基中的至少一个基团取代的C1－2烷基)，(式2中，R1、R2和R3表示与上述相同的含义)。 | ||||||
| 6 | Prostaglandins | US449720 | 1989-12-12 | US5028733A | 1991-07-02 | Robert L. Jones; Norman H. Wilson |
| Bicyclooctane and bicycloheptane prostaglandin intermediates have been synthesized. | ||||||
| 7 | Novel process for preparing semi-caronic aldehydes | US282382 | 1988-12-09 | US5004840A | 1991-04-02 | Alain Krief; Willy Dumont |
| A novel process for the preparation of compounds of the formula ##STR1## with cis or trans structure in racemic or optically active form wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl of 6 to 12 carbon atoms comprising reacting an optically active isomer, or racemate of the formula ##STR2## wherein R has the above definition and the way line indicates Z or E geometry with a gem-dimethyl cyclopropanation agent if there is Z geometry to obtain a compound of the formula ##STR3## or if the geometry is E with a gem-dimethyl cyclopropanation agent other than isopropylidene triphenyl phosphorane to obtain a compound of the formula ##STR4## wherein R has the above definition and the cyclopropane ring has the trans configuration and either hydrolyzing the compound of formula III or IIIa to obtain a compound of the formula ##STR5## and then cleaving the 4,5 bond to obtain the corresponding compound of formula I or simultaneously cleaving the 4,5 bond and hydrolyzing the dioxolane group to obtain the corresponding compound of formula I and novel intermediates. | ||||||
| 8 | Prostaglandins | US377760 | 1989-07-06 | US4945106A | 1990-07-31 | Robert L. Jones; Norman H. Wilson |
| Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared. | ||||||
| 9 | Preparation of caronaldehyde acid and derivatives thereof | US355034 | 1982-03-05 | US4435597A | 1984-03-06 | Dieter Arlt |
| A process for the preparation of caronaldehyde acid or a derivative thereof of the formula ##STR1## in which R is O.sup.- Me.sup.+, or OH, andMe.sup.+ is an equivalent of an alkali metal, alkaline earth metal or ammonium cation, comprising reacting a 2-halogeno-3,3-dimethyl-5,5-dichloropentanoic acid halide of the formula ##STR2## wherein X and Y each independently is a halogen atom, with a base in the presence of water. | ||||||
| 10 | Synthesis of pyrethric acid | US3694472D | 1970-05-12 | US3694472A | 1972-09-26 | MARTEL JACQUES; BUENDIA JEAN |
| BY REACTING 3,3-DIMETHYL-2-FORMYL-1-CYCLOPROPANECARBOXYLIC (1R, 2R) acid or a salt thereof with methyl propionate under anhydrous basic conditions.
A novel process for the preparation of 3,3-dimethyl-2-(2''methoxycarbonyl-trans 1''-propenyl)-1-cyclopropane carboxylic (1R, 2R) acid or d-trans pyrethric (1R,2R) acid of the formula |
||||||
| 11 | SALTS AND CRYSTALLINE FORMS OF A PD-1/PD-L1 INHIBITOR | PCT/US2020/059817 | 2020-11-10 | WO2021096849A1 | 2021-05-20 | JIA, Zhongjiang; CHEN, Shili; LI, Yi; MARTIN, Timothy; SHEN, Bo; SU, Naijing; ZHOU, Jiacheng; LI, Qun |
This application relates to solid forms and salt forms of the PD-1/PD-L1 inhibitor 4,4'-(((((2,2'-dichloro-[1,1'-biphenyl]-3,3'-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-2,5-diyl))bis(ethane-2,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid), including processes of preparation thereof, where the solid forms and salt forms are useful in the treatment of various diseases including infectious diseases and cancer. |
||||||
| 12 | LEUKOTRIENE ANALOGUES. | EP83900154 | 1982-11-29 | EP0094963A4 | 1984-09-19 | NICOLAOU KYRIACOS C; PETASIS NICOS A; SEITZ STEVEN P |
| 13 | Process for the preparation of substituted alpha-halopropionic acids and of their derivatives; substituted vinylidene chloride | EP82102028 | 1982-03-13 | EP0061629A3 | 1983-01-26 | ARLT, DIETER, PROF. DR. |
| 14 | Enantioselective process | US791905 | 1991-11-13 | US5142099A | 1992-08-25 | Alain Krief |
| An enantioselective process for the preparation of hemicaronic aldehyde with a cis or trans structure and novel intermediates. | ||||||
| 15 | Enantioselective process | US482647 | 1990-02-21 | US4996349A | 1991-02-26 | Alain Krief; Willy Dumont |
| An enantioselective process for the preparation of hemicaronic aldehyde with a cis or trans structure and novel intermediates. | ||||||
| 16 | Prostaglandins | US349084 | 1982-02-12 | US4596823A | 1986-06-24 | Robert L. Jones; Norman H. Wilson |
| Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo[2,2,1]hept-2Z-ene, bicyclo[2,2,1]heptane, 7-oxabicyclo[2,2,1]hept-2Z-ene, 7-oxabicyclo[2,2,1]heptane, bicyclo[2,2,2]oct-2Z-ene or bicyclo[2,2,2]octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group C(R.sup.2).dbd.NR, a 6,6-dimethyl-bicyclo[3,1,1]heptane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group C(R.sup.2).dbd.NR or at the 5-position by the group C(R.sup.2).dbd.NR and at the 6-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group C(R.sup.2).dbd.NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group C(R.sup.2).dbd.NR, R.sup.1 is a 6-caboxyhex-2-enyl group or a modification thereof as defined herein, R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R is a group --OR.sup.3, --OR.sup.4, --A--R.sup.3 or -- N.dbd.R.sup.5 in which A is --NH--, --NH.CO--, --NH.CO.CH.sub.2 N(R.sup.6)--, --NH.SO.sub.2 --, --NH.CO.NH or --NH.CS.NH-- and wherein R.sup.3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, R.sup.4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom ay an aliphatic hydrocarbon group which is itself substituted by an aromatic group, R.sup.5 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R.sup.6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, with the proviso that when R is a group --OR.sup.3, --NH.COR.sup.3 or --NH.CO.NHR.sup.3 then ##STR3## excludes bicyclo[2,2,1]hept-2Z-enes and bicyclo[2,2,1]heptanes. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity. | ||||||
| 17 | Preparation of substituted alpha-halogeno-propionic acids and their derivatives | US355042 | 1982-03-05 | US4440947A | 1984-04-03 | Dieter Arlt |
| Substituted .alpha.-halogenopropionic acids and their derivatives of the general formula ##STR1## wherein R.sup.1 to R.sup.3, Y and X have the meanings given in the description, are prepared by a process which is characterized in that substituted vinylidene chlorides of the general formula ##STR2## are reacted with chlorine or bromine chloride in the presence of compounds of the formulaR.sup.5 --SO.sub.3 R.sup.6 (III)wherein R.sup.5 and R.sup.6 have the meaning given in the description, and the products obtained are treated, if appropriate, with water or alcohol. Certain of the substituted .alpha.-halogeno-propionic acids and the substituted vinylidene chloride of the formula ##STR3## are new. The end products are useful as herbicides and intermediates for insecticides. | ||||||
| 18 | 4-Methyl-3-formyl-pentanoic acid esters | US352259 | 1982-02-25 | US4421928A | 1983-12-20 | Jacques Martel; Jean Tessier; Jean-Pierre Demoute |
| Novel 4-methyl-3-formyl-pentanoic acid derivative of the formula ##STR1## wherein Hal is a halogen, R.sub.1 is alkyl of 1 to 12 carbon atoms and A and B are .dbd.0 or A is halogen and B is --OR.sub.2 and R.sub.2 is alkyl of 1 to 12 carbon atoms, their preparation and their use as intermediates. | ||||||
| 19 | Prostaglandins | US143506 | 1988-01-13 | US5081282A | 1992-01-14 | Robert L. Jones; Norman H. Wilson |
| Bicyclo prostaglandin analogues have been prepared. | ||||||
| 20 | Prostaglandins | US476562 | 1990-02-07 | US5025034A | 1991-06-18 | Robert L. Jones; Norman H. Wilson |
| Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared. | ||||||
QQ群二维码
意见反馈
意见反馈