公开(公告)号：US20020128490A1

公开(公告)日：2002-09-12

申请号：US09801269

申请日：2001-03-07

Inventor： Jeffrey N. Johnston ,  Rajesh Viswanathan

IPC: C07D29/14 ,  C07D27/14 ,  G01N033/53

CPC classification number: C07D471/04 ,  C07C251/16 ,  C07D207/16 ,  C07D209/08 ,  C07D209/36

Abstract: The present invention provides methodology for carbon-nitrogen bond formation via vinyl or aryl amination. In the process of the invention, an sp2 hybridized radical is reacted with an azomethine moiety to form pyrrolidine and indole compounds. The methodology provides a facile process for the synthesis of compounds having the pyrrolidine or indole subunit and is especially advantageous for compounds having acid or base labile functional groups andor is comprised of chiral centers susceptible to acidbase epimerization.

Abstract translation: 本发明提供通过乙烯基或芳基胺化形成碳 - 氮键的方法。 在本发明的方法中，sp2杂化的基团与偶氮甲碱部分反应形成吡咯烷和吲哚化合物。 该方法为合成具有吡咯烷或吲哚亚基的化合物提供了一种简便的方法，对于具有酸或碱不稳定官能团的化合物尤其有利，并且由含有酸碱差向异构化的手性中心组成。

公开(公告)号：US20030191174A1

公开(公告)日：2003-10-09

申请号：US10258817

申请日：2002-10-28

Inventor： Shunichi Ikuta ,  Shiro Miyoshi ,  Kohei Ogawa

IPC: A61K031/404 ,  A61K031/381 ,  A61K031/343 ,  C07D29/14 ,  C07D333/72

CPC classification number: C07D307/79 ,  C07D209/08 ,  C07D209/12 ,  C07D333/54

Abstract: Compounds of the general formula (I): 1 or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.

Abstract translation: 通式（I）的化合物或其盐，其中R 1是氢，羟基或卤素; R 2是NHSO 2 CH 3，SO 2 NHCH 3等; R 5和R 6各自独立地是氢，C 1-6烷基，任选取代的苯基或任选取代的苄基; X是NH，硫，氧或亚甲基; Y是氧，NR 7，硫，亚甲基或键; 和*表示不对称碳原子。 该化合物可用作治疗或预防糖尿病，肥胖症，高脂血症，消化系统疾病，抑郁症或尿失调的药物。

公开(公告)号：US3634434A

公开(公告)日：1972-01-11

申请号：US3634434D

申请日：1969-05-09

Applicant: AMERICAN HOME PROD

Inventor： SALLAY STEPHEN I ,  CHILDRESS SCOTT J

IPC: C07D211/70 ,  C07D29/14

CPC classification number: C07D211/70

Abstract: PIPERIDINE AND TROPANE DERIVATIVES HAVING AN OLEFINIC COMPONENT IN THE 3 OR 4-POSITION OF THE RING HAVE BEEN PREPARED, THE COMPOUNDS DEMONSTRATING A CENTRAL NERVOUS SYSTEM STIMULATING ACTION.

公开(公告)号：US20010020035A1

公开(公告)日：2001-09-06

申请号：US09088522

申请日：1998-06-01

Inventor： PAMELA ALBAUGH ,  GANG LIU ,  ALAN HUTCHISON

IPC: C07D29/14 ,  C07D41/02

CPC classification number: C07D401/12 ,  C07D209/42 ,  C07D409/12 ,  C07D471/04

Abstract: Disclosed are compounds of the formula 1 or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

Abstract translation: 公开了下式的化合物或其药学上可接受的无毒盐，其中：W表示取代或未取代的芳基或杂芳基; T是氢，卤素，羟基，氨基或烷基; X是氢，羟基或低级烷基; m为0,1或2; n为0,1或2; 并且R 3和R 4表示取代或未取代的有机残基。 这些化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 这些化合物可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆增强。

公开(公告)号：US3475428A

公开(公告)日：1969-10-28

申请号：US3475428D

申请日：1966-05-23

Applicant: MONSANTO CO

Inventor： ALT GERHARD H

IPC: C07D295/073 ,  C07D87/30 ,  C07D27/04 ,  C07D29/14

CPC classification number: C07D295/073

公开(公告)号：US20020002286A1

公开(公告)日：2002-01-03

申请号：US09779080

申请日：2001-02-08

Inventor： Daniel Michael Ketcha ,  Lawrence Joseph Wilson

IPC: C07D29/14 ,  C07F009/547

CPC classification number: C07D209/42

Abstract: The subject invention involves a solid-phase process for the synthesis of indole compounds comprising the steps: (a) treating an amino resin with diketene to provide a resin-bound acetoacetamide; (b) treating the product from Step (a) with a primary amine in the presence of a dehydrating agent to provide a resin-bound enaminone; (c) treating the product from Step (b) with a 1,4-benzoquinone, and releasing the resulting indole product from the resin.

Abstract translation: 本发明涉及用于合成吲哚化合物的固相方法，其包括以下步骤：（a）用双烯酮处理氨基树脂以提供树脂结合的乙酰乙酰胺; （b）在脱水剂存在下用伯胺处理步骤（a）的产物以提供树脂结合的烯胺酮; （c）用1,4-苯醌处理步骤（b）的产物，并将所得的吲哚产物从树脂中释放出来。

公开(公告)号：US20010046960A1

公开(公告)日：2001-11-29

申请号：US09817507

申请日：2001-03-26

Inventor： Darryl DesMarteau ,  Vittorio Montanari

IPC: A61K038/05 ,  C07D29/14

CPC classification number: C07D317/58 ,  C07B2200/07 ,  C07C229/36 ,  C07C237/20 ,  C07K5/06191 ,  C07K5/1027 ,  C07K14/001

Abstract: Fluorinated alkyl compounds may be used as reaction intermediates or reaction products in polymerizing amino acid structures into peptides. Fluorinated methyl groups have been found to be particularly useful. A compound having a fluorinated methyl group such as that set forth below: 1 wherein R is selected from the group consisting of: alkyls, hydrogen, aryls, aromatic compounds, amines, sulfur-containing alkyl groups, sulfur-containing aryl groups, and heterocyclic compounds may be utilized alone, or reacted in combination with other amino acids, to form a dipeptide, or polypeptide.

Abstract translation: 氟化烷基化合物可以用作将氨基酸结构聚合成肽的反应中间体或反应产物。 已经发现氟化甲基是特别有用的。 具有如下所示的氟化甲基的化合物：其中R选自：烷基，氢，芳基，芳族化合物，胺，含硫烷基，含硫芳基和杂环化合物 可单独使用或与其它氨基酸组合反应以形成二肽或多肽。

公开(公告)号：US3507875A

公开(公告)日：1970-04-21

申请号：US3507875D

申请日：1966-01-17

Applicant: SANDOZ AG

Inventor： JUCKER ERNST ,  GMUNDER JOHN

IPC: C07D211/14 ,  C07D211/68 ,  C07D295/13 ,  C07D451/14 ,  C07D29/34 ,  C07D29/14 ,  C07D29/26

CPC classification number: C07D295/13 ,  C07D211/14 ,  C07D211/68 ,  C07D451/14

公开(公告)号：US20020007073A1

公开(公告)日：2002-01-17

申请号：US09898333

申请日：2001-07-03

Applicant: Max-Delbruck-Centrum fur molekulare Medizin

Inventor： Manfred Schneider ,  Oliver Keil ,  Regina Reszka ,  Detlef Groth

IPC: C07D233/44 ,  C07D29/14 ,  C07D27/14 ,  C07K005/078

CPC classification number: A61K48/00 ,  A61K9/1272 ,  C07C237/12 ,  C07C271/20 ,  C07C279/14 ,  C07J41/0055 ,  C07J41/0072 ,  C12N15/88

Abstract: This invention relates to the synthesis of novel cationic, amphiphilic lipids and their application as gene transfer vehicles in vitro and in vivo. For this a series of different lipids (diglycerides, steroids) were synthesized by modification with variable cationic molecules (amino acids, biogenic amines). Compounds of this kind are, due to their capability of producing complexes with polynucleotides (DNA, RNA, Antisense oligonucleotides, ribozymes etc) suitable as vectors for gene transfer (transfection).

Abstract translation: 本发明涉及新型阳离子，两亲性脂质的合成及其在体外和体内作为基因转运载体的应用。 为此，通过用可变阳离子分子（氨基酸，生物胺）进行修饰来合成一系列不同的脂质（甘油二酯，类固醇）。 由于它们与适合作为基因转移（转染）载体的多核苷酸（DNA，RNA，反义寡核苷酸，核酶等）产生复合物的能力，这类化合物。

公开(公告)号：US3674785A

公开(公告)日：1972-07-04

申请号：US3674785D

申请日：1964-01-09

Applicant: MINNESOTA MINING & MFG

Inventor： MITSCH RONALD A

IPC: C07D207/22 ,  C07D211/72 ,  C07D211/92 ,  C07D215/18 ,  C07D265/30 ,  C07D93/10 ,  C07D29/14 ,  C07D87/00

CPC classification number: C07D265/30 ,  C07D207/22 ,  C07D211/72 ,  C07D211/92 ,  C07D215/18 ,  Y10S149/119

Abstract: 8. A compound of the formula: WHEREIN EACH R is selected from the class consisting of fluorine and fluoroalkyl radicals and wherein R groups taken together can form ring systems, which compound comprises a ring which contains a plurality of hetero atoms therein, said ring containing only a single azomethine group, provided that said compound contains no atoms other than carbon, fluorine, nitrogen, oxygen and sulfur atoms. 10. Perfluoro-5,6-dihydro-2H-1,4-oxazine. 12. 1,1,1,1-TETRAFLUOROPERFLUORO-5,6-DIHYDRO-2H-1,4-thiazine.