公开(公告)号：US4895856A

公开(公告)日：1990-01-23

申请号：US280857

申请日：1988-12-07

Applicant: Francesco Makovec ,  Rolando Chiste ,  Walter Peris ,  Luigi Rovati

Inventor： Francesco Makovec ,  Rolando Chiste ,  Walter Peris ,  Luigi Rovati

IPC: A61K31/195 ,  A61K31/34 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/47 ,  A61P1/00 ,  A61P25/00 ,  A61P43/00 ,  C07C231/00 ,  C07C231/02 ,  C07C237/06 ,  C07C237/08 ,  C07C237/22 ,  C07D209/42 ,  C07D215/48 ,  C07D215/54 ,  C07D307/84 ,  C07D307/85 ,  C07D333/68 ,  C07D333/70

CPC classification number: C07D215/48 ,  C07D209/42 ,  C07D307/84 ,  C07D307/85 ,  C07D333/70

Abstract: New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

公开(公告)号：US4868195A

公开(公告)日：1989-09-19

申请号：US165045

申请日：1988-03-07

Applicant: Mary E. Carethers ,  Wiaczeslaw A. Cetenko ,  David T. Connor ,  Elizabeth A. Johnson ,  John S. Kiely ,  Charles F. Schwender ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Robert F. Bruns

Inventor： Mary E. Carethers ,  Wiaczeslaw A. Cetenko ,  David T. Connor ,  Elizabeth A. Johnson ,  John S. Kiely ,  Charles F. Schwender ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Robert F. Bruns

IPC: C07D209/36 ,  C07D209/42 ,  C07D279/02 ,  C07D307/83 ,  C07D307/84 ,  C07D307/92 ,  C07D311/22 ,  C07D311/24 ,  C07D333/64 ,  C07D333/68 ,  C07D335/06 ,  C07D491/04

CPC classification number: C07D307/92 ,  C07D209/36 ,  C07D209/42 ,  C07D279/02 ,  C07D307/83 ,  C07D307/84 ,  C07D311/22 ,  C07D311/24 ,  C07D333/64 ,  C07D333/68 ,  C07D335/06 ,  C07D491/04

Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.

Abstract translation: 本发明涉及新型烯醇酰胺型化合物，药物组合物及其使用方法，其可用于治疗其中脂肪氧合酶活性产物或白细胞三烯作用有助于病理状况的疾病。

公开(公告)号：US4826878A

公开(公告)日：1989-05-02

申请号：US133844

申请日：1987-12-16

Applicant: Francesco Makovec ,  Rolando Chiste ,  Walter Peris ,  Luigi Rovati

Inventor： Francesco Makovec ,  Rolando Chiste ,  Walter Peris ,  Luigi Rovati

IPC: A61K31/195 ,  A61K31/34 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/47 ,  A61P1/00 ,  A61P25/00 ,  A61P43/00 ,  C07C231/00 ,  C07C231/02 ,  C07C237/06 ,  C07C237/08 ,  C07C237/22 ,  C07D209/42 ,  C07D215/48 ,  C07D215/54 ,  C07D307/84 ,  C07D307/85 ,  C07D333/68 ,  C07D333/70 ,  C07C101/42

CPC classification number: C07D215/48 ,  C07D209/42 ,  C07D307/84 ,  C07D307/85 ,  C07D333/70

Abstract: New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutasnoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

公开(公告)号：US4260632A

公开(公告)日：1981-04-07

申请号：US123926

申请日：1980-02-22

Applicant: Leslie H. Smith

Inventor： Leslie H. Smith

IPC: C07D209/08 ,  C07D209/18 ,  C07D209/42 ,  C07D213/81 ,  C07D215/22 ,  C07D215/233 ,  C07D215/48 ,  C07D231/14 ,  C07D231/40 ,  C07D235/16 ,  C07D239/34 ,  C07D277/30 ,  C07D277/34 ,  C07D307/68 ,  C07D307/79 ,  C07D307/84 ,  C07D311/22 ,  C07D319/18 ,  C07D333/24 ,  C07D333/38 ,  C07D333/54 ,  A61K31/34 ,  C07D307/46 ,  C07D307/60 ,  C07D307/66

CPC classification number: C07D209/08 ,  C07D209/18 ,  C07D209/42 ,  C07D213/81 ,  C07D215/233 ,  C07D215/48 ,  C07D231/14 ,  C07D231/40 ,  C07D235/16 ,  C07D239/34 ,  C07D277/30 ,  C07D277/34 ,  C07D307/68 ,  C07D307/79 ,  C07D307/84 ,  C07D311/22 ,  C07D319/18 ,  C07D333/24 ,  C07D333/38 ,  C07D333/54 ,  Y02P20/55 ,  Y10S514/802

Abstract: Novel 1-heterocyclyloxy-or 1-aryloxy-3-amidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. The compounds possess .beta.-adrenergic blocking activity. Representative of the compounds disclosed is 1-(4-indolyloxy)-3-.beta.-isobutyramidoethylamino-2-propanol.

Abstract translation: 新的1-杂环氧基或1-芳氧基-3-酰氨基烷基氨基-2-丙醇衍生物，其制备方法，含有它们的药物组合物以及将其用于治疗心脏病的方法。 该化合物具有β-肾上腺素能阻滞活性。 所公开的化合物的代表是1-（4-吲哚氧基）-3-β-异丁酰胺基乙基氨基-2-丙醇。

公开(公告)号：US4054585A

公开(公告)日：1977-10-18

申请号：US694479

申请日：1976-06-09

Applicant: Ethel E. Felauer ,  Marshall Kulka ,  Bogislav Von Schmeling ,  Robert A. Davis

Inventor： Ethel E. Felauer ,  Marshall Kulka ,  Bogislav Von Schmeling ,  Robert A. Davis

IPC: A01N43/08 ,  A01N43/78 ,  C07D307/68 ,  C07D307/84

CPC classification number: A01N43/78 ,  A01N43/08 ,  C07D307/68 ,  C07D307/84

Abstract: A broad class of furan-3-Carboxamide derivatives, including many novel compounds, can be made reliably and in good yields by a novel one step reaction between an .alpha.-hydroxyketone and an acetamide in the presence of a Friedel-Crafts agent in an inert solvent. The broad class of derivatives has fungicidal and insecticidal utility.

Abstract translation: 通过在惰性的Friedel-Crafts试剂存在下，通过α-羟基酮和乙酰胺之间的新的一步反应可以可靠地且以良好的收率制备广泛的呋喃-3-羧酰胺衍生物，包括许多新型化合物 溶剂。 广泛的衍生物具有杀菌杀虫效用。

公开(公告)号：US3983141A

公开(公告)日：1976-09-28

申请号：US469528

申请日：1974-05-13

Applicant: Alexei Nikolaevich Grinev ,  Alexandr Alexandrovich Stolyarchuk ,  Pavel Alexandrovich Galenko-Yaroshevsky ,  Vladimir Spiridonovich Tantsjura ,  Natalya Vitalievna Arkhangelskaya

Inventor： Alexei Nikolaevich Grinev ,  Alexandr Alexandrovich Stolyarchuk ,  Pavel Alexandrovich Galenko-Yaroshevsky ,  Vladimir Spiridonovich Tantsjura ,  Natalya Vitalievna Arkhangelskaya

IPC: C07D307/84

CPC classification number: C07D307/84 ,  Y10S514/816

Abstract: Derivatives of 5-oxy-6-aminomethylbenzofuran having the general formula ##SPC1##Where R is alkyl, R' is alkyl, aryl, R.sup.2 is alkyl, R.sup.3 is alkyl, or R.sup.2 and R.sup.3, together with a nitrogen atom to which they are bonded, form a heterocycle comprising one or two hetero-atoms, and X is a halogen.Said compounds are prepared by aminomethylation of derivatives of 5-oxybenzofuran having the formula ##SPC2##Where R is alkyl, R' is alkyl, aryl, and X is a halogen.The reaction of aminomethylation can be carried out with a substituted bisaminomethane or with a mixture, consisting of a secondary amine and formaldehyde.Said compounds possess pharmacological activity.

Abstract translation: 具有通式为R 6为烷基的5-氧基-6-氨基甲基苯并呋喃的衍生物，R'为烷基，芳基，R 2为烷基，R 3为烷基或R 2和R 3与它们所键合的氮原子一起形成 包含一个或两个杂原子的杂环，X是卤素。

公开(公告)号：US3920707A

公开(公告)日：1975-11-18

申请号：US39584773

申请日：1973-09-10

Applicant: LABAZ

Inventor： DESCAMPS MARCEL ,  GUBIN JEAN ,  CLAEYS NORBERT

IPC: C07D307/80 ,  C07D307/84 ,  C07D307/78

CPC classification number: C07D307/80 ,  C07D307/84

Abstract: Benzofuran compounds of the general formula:

AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, WHEREIN R represents a branched- or straight-chain alkyl group containing from 1 to 4 carbon atoms or a cyclohexyl radical; R1 and R2, which are identical, each represent a hydrogen atom or a straight-chain alkyl group containing from 1 to 3 carbon atoms; Am represents a dimethylamino, diethylamino, di-n-propylamino, di-n-butylamino, piperidino, N-methyl-piperazino, N-ethylpiperazino, N-n-propyl-piperazino, N-phenyl-piperazino, methyl-nbutylamino, ethyl-n-butylamino, methylamino, ethylamino, npropylamino, isopropylamino or n-butylamino group and n is an integer in the range of from 3 to 6 inclusive.

公开(公告)号：US3122551A

公开(公告)日：1964-02-25

申请号：US23550762

申请日：1962-11-05

Applicant: ABBOTT LAB

Inventor： ELMER ZAUGG HAROLD ,  DE NET ROBERT WILLIAM ,  MICHAELS JR RAYMOND JOHN

IPC: C07D307/80 ,  C07D307/81 ,  C07D307/84 ,  C07D307/87 ,  C07D311/58 ,  C07D313/08

CPC classification number: C07D307/87 ,  C07D307/80 ,  C07D307/81 ,  C07D307/84 ,  C07D311/58 ,  C07D313/08

公开(公告)号：US11760742B2

公开(公告)日：2023-09-19

申请号：US17208474

申请日：2021-03-22

Applicant: MITSUI CHEMICALS, INC.

Inventor： Kei Yoshida ,  Takeo Wakita ,  Hiroyuki Katsuta ,  Akiyoshi Kai ,  Yutaka Chiba ,  Kiyoshi Takahashi ,  Hiroko Kato ,  Nobuyuki Kawahara ,  Michikazu Nomura ,  Hidenori Daido ,  Junji Maki ,  Shinichi Banba

IPC: C07C237/42 ,  C07D333/38 ,  A01N37/44 ,  A01N43/08 ,  A01N43/10 ,  A01N43/12 ,  A01N43/16 ,  A01N43/30 ,  A01N43/42 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/78 ,  A01N43/80 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07D207/416 ,  C07D213/64 ,  C07D213/73 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D215/52 ,  C07D231/14 ,  C07D231/16 ,  C07D239/30 ,  C07D241/24 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D307/24 ,  C07D307/68 ,  C07D307/84 ,  C07D309/08 ,  C07D309/28 ,  C07D317/62 ,  C07D333/68 ,  A01N43/40 ,  A01N37/22 ,  A01N43/60 ,  C07C237/48 ,  C07D207/34 ,  C07D239/28 ,  C07D261/18 ,  C07D307/85 ,  C07D317/46

CPC classification number: C07D333/38 ,  A01N37/22 ,  A01N37/44 ,  A01N43/08 ,  A01N43/10 ,  A01N43/12 ,  A01N43/16 ,  A01N43/30 ,  A01N43/40 ,  A01N43/42 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/78 ,  A01N43/80 ,  C07C237/42 ,  C07C237/48 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07D207/34 ,  C07D207/416 ,  C07D213/64 ,  C07D213/73 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D215/52 ,  C07D231/14 ,  C07D231/16 ,  C07D239/28 ,  C07D239/30 ,  C07D241/24 ,  C07D261/18 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D307/24 ,  C07D307/68 ,  C07D307/84 ,  C07D307/85 ,  C07D309/08 ,  C07D309/28 ,  C07D317/46 ,  C07D317/62 ,  C07D333/68

Abstract: A compound represented by Formula (1):




The compound can be used as insecticides.

公开(公告)号：US20180237407A1

公开(公告)日：2018-08-23

申请号：US15752126

申请日：2016-08-12

Applicant: James HSIEH ,  Evripidis GAVATHIOTIS ,  Memorial Sloan-Kettering Cancer Center ,  Albert Einstein College of Medicine, Inc.

Inventor： Emily H. Cheng ,  Paul Jeng ,  Ouathek Ouerfelli ,  James Hsieh ,  Guangli Yang ,  Evripidis Gavathiotis

IPC: C07D307/84 ,  A61P35/00

CPC classification number: C07D307/84 ,  A61K31/343 ,  A61P19/02 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  C07D307/82

Abstract: Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, methods, uses, and kits involving compounds of Formulae (I), (II), (III), (IV), (V), or (VI) for treating and/or preventing proliferative diseases (e.g. cancers, inflammatory diseases, and autoimmune diseases) in a subject. The compounds and pharmaceutical compositions as described herein inhibit at least one protein of the BCL-2 family in a biological sample or subject to treat and/or prevent a proliferative disease. In certain embodiments, compounds described herein are selective inhibitors of MCL-1, a BCL-2 family member protein.