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    • 31. 发明申请
    • SULFONAMIDE-BASED ORGANOCATALYSTS AND METHOD FOR THEIR USE
    • 基于磺酰胺的有机化合物及其使用方法
    • WO2009039181A3
    • 2009-07-16
    • PCT/US2008076688
    • 2008-09-17
    • STATE OF OREGON ACTING BY & THCARTER RICH GARRETTYANG HUA
    • CARTER RICH GARRETTYANG HUA
    • B01J31/00C07C311/18C07C313/00
    • B01J31/0237B01J31/0222B01J31/0247B01J31/0271B01J2231/32B01J2231/341B01J2231/346B01J2231/4283B01J2231/46
    • Organocatalysts, particularly proline sulfonamide organocatalysts, having a first general formula as follows are disclosed. Embodiments of a method for using these organocatalysts also are disclosed. The method comprises providing a disclosed organocatalyst, and performing a reaction, often an enantioselective or diastereoselective reaction, using the organocatalyst. Solely by way of example, disclosed catalysts can be used to perform aldol reactions, conjugate additions, Michael additions, Robinson annulations, Mannich reactions, a-aminooxylations, a-hydroxyaminations, a-aminations and alkylation reactions. Certain of such reactions are intramolecular cyclizations used to form cyclic compounds, such as 5- or 6-membered rings, having one or more chiral centers. Disclosed organocatalysts generally are much more soluble in typical solvents used for organic synthesis than are known compounds. Moreover, the reaction yield is generally quite good with disclosed compounds, as is their enantioselective and diastereoselective effectiveness.
    • 公开了具有如下第一通式的有机催化剂,特别是脯氨酸磺酰胺有机催化剂。 也公开了使用这些有机催化剂的方法的实施方式。 该方法包括提供公开的有机催化剂,并使用有机催化剂进行反应,通常是对映选择性或非对映选择性反应。 仅举例而言,公开的催化剂可用于进行醛醇缩合反应,缀合物加成,迈克尔加成,罗宾逊环,曼尼希反应,α-氨氧基化,α-羟胺化,α-胺化和烷基化反应。 某些这样的反应是用于形成具有一个或多个手性中心的环状化合物例如5元或6元环的分子内环化。 披露的有机催化剂通常比已知化合物更易溶于用于有机合成的典型溶剂。 此外,所公开的化合物的反应收率通常相当好,它们的对映选择性和非对映选择性效果也是如此。
    • 37. 发明申请
    • THROMBOXANE ANTAGONISTS IN THE TREATMENT OF HORMONE-DEPENDENT NEOPLASIAS
    • 治疗依赖于雌激素的血栓素拮抗剂
    • WO8604234A3
    • 1986-09-12
    • PCT/GB8600028
    • 1986-01-16
    • NAT RES DEVSENIOR JUDITHTROUGHTON KAY MARIE
    • SENIOR JUDITHTROUGHTON KAY MARIE
    • C07C281/06A61K31/175A61K31/557C07C67/00C07C239/00C07C313/00C07C323/44C07C325/00C07C337/06C07C405/00C07D493/00
    • C07C405/0091A61K31/175A61K31/557
    • Compounds having thromboxane antagonist activity are of use in the treatment of hormone-dependent neoplasias for example oestrogen-dependent neoplasias. Thromboxane antagonists of particular value are compounds of formula (I) wherein formula (II) represents one of the divalent cyclic groups (III). The letters a and b indicating in each case the points of attachment of the substituents R1 and CV(R2)-NV'R, respectively; R1 is a 6-carboxyhex-2-enyl group or a modification thereof in which the group is altered by one, or an appropriate combination of two or more, of the following: (a) alteration of the position of the double bond, (b) reduction of the double bond, (c) alteration of the chain length through a decrease of one or two methylene groups or an increase of one to six methylene groups, (d) replacement of one or two methylene groups each separately by an oxygen or sulphur atom with the proviso that in the modified group no oxygen or sulphur atom is in an alpha position relative to either a doubly bonded carbon atom or to the carboxy group or a derivative thereof and that at least 2 carbon atoms separate any pair of oxygen and/or sulphur atoms; and (e) formation of an amide, ester or salt derivative of the carboxy groups; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group -NH.CO.NH-R3 or -NH.CS.NH-R3 wherein R3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by one or more aromatic groups directly or through an oxygen or sulphur atom.