公开(公告)号：US5234925A

公开(公告)日：1993-08-10

申请号：US744917

申请日：1991-08-14

申请人： Andre Rosowsky

发明人： Andre Rosowsky

IPC分类号： C07D253/08 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D253/08 ,  C07D409/12 ,  C07D417/12

摘要： 2-Aza-2-desamino analogues of 5,8-dideazafolic acid, which analogues have the formula ##STR1## wherein X is an aryl or heteroaryl moiety;R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, or C.sub.3 -C.sub.4 alkynyl; andR.sup.2 is OH, an L-.alpha.-amino acid, or a peptide comprising L-.alpha.-amino acids.

摘要翻译： 5,8-二氮杂萘酸的2-氮杂-2-脱氨基类似物，其类似物具有式（IMAGE），其中X是芳基或杂芳基部分; R1是H，C1-C4烷基，C3-C4烯基或C3-C4炔基; 并且R 2是OH，L-α-氨基酸或包含L-α-氨基酸的肽。

公开(公告)号：US4806641A

公开(公告)日：1989-02-21

申请号：US741866

申请日：1985-06-06

申请人： Alexander Volk ,  Wolfgang Konig

发明人： Alexander Volk ,  Wolfgang Konig

IPC分类号： C07B31/00 ,  C07B63/00 ,  C07C67/00 ,  C07C209/00 ,  C07C209/86 ,  C07C211/01 ,  C07C211/02 ,  C07C213/10 ,  C07C227/00 ,  C07C227/28 ,  C07C227/40 ,  C07C229/02 ,  C07D253/08 ,  C07K1/10 ,  C07K1/113 ,  C07K1/14 ,  C07K5/06 ,  C07K5/08

CPC分类号： C07D253/08 ,  C07K1/10 ,  C07K1/14 ,  C07K5/0606

摘要： The invention relates to salts of 3-hydroxy-4-oxo-3,4-dihydro-1,2,3-benzotriazine (HOObt) and compounds containing a primary amino group, a process for their preparation and their use.

摘要翻译： 本发明涉及3-羟基-4-氧代-3,4-二氢-1,2,3-苯并三嗪（HOObt）和含有伯氨基的化合物的盐，其制备方法及其应用。

公开(公告)号：US4242507A

公开(公告)日：1980-12-30

申请号：US880436

申请日：1978-02-23

申请人： Masumi Itoh ,  Jiyoji Notani

发明人： Masumi Itoh ,  Jiyoji Notani

IPC分类号： C07D249/18 ,  C07D253/08 ,  C07D257/04 ,  C07D277/68 ,  C07K1/08 ,  C07K5/06 ,  C07K5/072 ,  C07K5/078 ,  C07K5/097

CPC分类号： C07D253/08 ,  C07D249/18 ,  C07D257/04 ,  C07D277/68 ,  C07K1/086 ,  C07K5/0606 ,  C07K5/06095 ,  C07K5/06165 ,  C07K5/0823

摘要： A novel process for the amidation or esterification which comprises reacting a compound having a carboxy group with a compound having an amino or imino group which can be acylated or with a compound having a hydroxy group in the presence of a sulfonic acid ester of the formula:R.sub.1 --SO.sub.2 --OR.sub.2wherein R.sub.1 is an organic group and R.sub.2 O-- is a residue of a strongly acidic N-hydroxy compound as a condensation agent, and a novel sulfonic acid ester useful as such a condensation agent and a process for the preparation thereof.

摘要翻译： 一种用于酰胺化或酯化的新方法，其包括在下式的磺酸酯存在下使具有羧基的化合物与可被酰化的氨基或亚氨基的化合物或具有羟基的化合物反应： R1-SO2-OR2，其中R1是有机基团，R2O-是作为缩合剂的强酸性N-羟基化合物的残基，和用作这种缩合剂的新型磺酸酯及其制备方法。

公开(公告)号：US4138263A

公开(公告)日：1979-02-06

申请号：US604312

申请日：1975-08-13

申请人： Immo Boie ,  Gunter Renner ,  Friedrich-Wilhelm Kunitz

发明人： Immo Boie ,  Gunter Renner ,  Friedrich-Wilhelm Kunitz

IPC分类号： C07D215/22 ,  C07D237/16 ,  C07D237/32 ,  C07D239/36 ,  C07D239/54 ,  C07D239/90 ,  C07D239/96 ,  C07D241/20 ,  C07D241/44 ,  C07D251/30 ,  C07D253/08 ,  G03C7/305 ,  G03C1/40 ,  G03C7/00

CPC分类号： C07D215/22 ,  C07D237/16 ,  C07D237/32 ,  C07D239/36 ,  C07D239/54 ,  C07D239/90 ,  C07D239/96 ,  C07D241/20 ,  C07D241/44 ,  C07D251/30 ,  C07D253/08 ,  G03C7/30535

摘要： 2-Equivalent yellow couplers for the production of yellow dye images in color photographic silver halide materials have as splittable group a nitrogen-containing 6-membered heteroaromatic ring which is linked by the said nitrogen atom to the coupling position of the coupler molecule, contains a carbonyl group adjacent said nitrogen, and also contains one or two additional nitrogens as well as a fused-on aromatic carbocyclic ring. When the heteroaromatic ring contains two additional nitrogens, all three nitrogens are vicinal; when it contains only one additional nitrogen, the splittable group is a 1,3-quinazolinone-4 having at least one carboxy, with lower aliphatic alcohols esterified carboxy, nitro, methyl or chloro substituent.

摘要翻译： 用于在彩色照相卤化银材料中生产黄色染料图像的2-等效的黄色成色剂具有可分离的基团，由所述氮原子连接到成色剂分子的偶联位置的含氮6元杂芳环包含 邻近所述氮的羰基，并且还含有一个或两个另外的氮以及稠合的芳族碳环。 当杂芳环含有两个另外的氮时，所有三个氮都是邻位的; 当仅含有一个另外的氮时，可裂解基团是具有至少一个羧基的1,3-喹唑啉酮-4，其中低级脂族醇酯化羧基，硝基，甲基或氯取代基。

公开(公告)号：US3808318A

公开(公告)日：1974-04-30

申请号：US27149272

申请日：1972-07-13

申请人： SANDOZ AG

发明人： KATHAWALA F

IPC分类号： C07C243/38 ,  C07D253/08 ,  C07D295/13 ,  C07D491/04 ,  A61K27/00

CPC分类号： C07D253/08 ,  C07C243/38 ,  C07D295/13 ,  C07D491/04

摘要： DISCLOSED ARE COMPOUNDS OF THE CLASS OF 1,2,3-BENZOTRIAZIN-4(3H)-ONES WHICH ARE SUBSTITUTED AT THE 3-POSITION AND WHICH ARE SUBSTITUTED AT LEAST TWO OF THE 6, 7 AND 8-POSITIONS BY ALKOXY OR BY AN ADJACENT METHYLENEDIOXY, E.G. 6,7-DIMETHOXY-3-(3 - MORPHOLINOPROPYLAMINO)-1,2,3BENZOTRIAZIN-4(3H)-ONE. THE COMPOUNDS HAVE PHARMACOLOGICAL ACTIVITY IN ANIMALS, E.G., ANTI-INFLAMMATORY ACTIVITY. THE COMPOUNDS MAY BE PREPARED, FOR EXAMPLE, BY ALKYLATION OF THE CORRESPONDING 3-UNSUBSTITUTED COMPOUNDS AND BY REACTION OF AN APPROPRIATELY DISUBSTITUTED ANTHRANIL AMIDE WITH SODIUM NITRITE AND A STRONG INORGANIC ACID, E.G., SULFURIC ACID.

公开(公告)号：US3751413A

公开(公告)日：1973-08-07

申请号：US3751413D

申请日：1972-06-22

申请人： SCHRAVEN E ,  STACHEL A ,  NITZ R ,  STACHEL L ,  RESAG K ,  BEYERLE R

发明人： STACHEL A ,  SCHRAVEN E ,  NITZ R ,  RESAG K ,  STACHEL L ,  BEYERLE R

IPC分类号： C07D253/08 ,  C07D55/08

CPC分类号： C07D253/08 ,  Y10S514/929

摘要： THE PRESENT INVENTEION PERTAINS TO NEW, PHARMACOLOGICALLY VALUABLE BASICALLY SUBSTITUTED 1,2,3-BENZOTRIAZINE-4(3H)-ONE DERIVATIVES HAVING EXCELLENT CORONARY DILATOR PROPERTIES AND WHICH HAVE THE STRUCTURAL FORMULA

3-(((R3)M-PHENYL)-COO-CH(-CH2-R'')-CH2-),(R1)N-1,2,3-BENZO-

TRIAZIN-4(3H)-ONE

WHEREIN R'' IS A RADICAL SELECTED FROM THE GROUP CONSISTING OF N,N - DI - LOWER-ALKYLAMINO, N-LOWER-ALKYL-N-ALLYLAMINO, N-LOWER-ALKYL-N-(METHOXY-LOWER-ALKYL)-AMINO, N-LOWER-ALKYL-N-(DIETHYLAMINO-LOWER-ALKYL)-AMINO AND N-LOWER-ALKYL-N-BENZYL-AMINO,LOWER ALKYL MEANING ALKYL HAVING 1 TO 4 CARBON ATOMS, SAID RADICAL BEING BOUND VIA IS NITROGEN ATOM, R1 IS A LOIWER ALKOXY GROUP HAVING 1-4 CARBON ATOMS WHICH MAY BE IN THE 6,7 OR 6,7,8-POSITION, R2 IS AN ALKOXY GROUP HAVING 1-4 CARBON ATOMS, M IS AN INTEGER SELECTED FROM 1,2 AND 3, AND N IS AN INTEGER SELECTED FROM THE GROUP CONSISTING OF 2 AND 3 AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF.

公开(公告)号：US3471489A

公开(公告)日：1969-10-07

申请号：US3471489D

申请日：1968-07-29

申请人： DOW CHEMICAL CO

发明人： RIGTERINK RAYMOND H

IPC分类号： C07D253/08 ,  C07D55/08 ,  A01N9/22 ,  A61K27/00

CPC分类号： C07D253/08

公开(公告)号：US20170348319A1

公开(公告)日：2017-12-07

申请号：US15683589

申请日：2017-08-22

申请人： Takeda Pharmaceutical Company Limited

发明人： Stephen Hitchcock ,  Betty Lam ,  Holger Monenschein ,  Holly Reichard

IPC分类号： A61K31/53 ,  C07D253/08

CPC分类号： A61K31/53 ,  C07D253/08

摘要： The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

公开(公告)号：US09730928B2

公开(公告)日：2017-08-15

申请号：US14896906

申请日：2014-06-13

申请人： University of Utah Research Foundation

发明人： Vincente Planelles ,  Alberto Bosque-Pardos ,  Chris M. Ireland ,  Ryan Van Wagoner ,  Mary Kay Harper-Ireland ,  John Alan Maschek

IPC分类号： A61K31/501 ,  A61K31/416 ,  A61K31/53 ,  A61K45/06 ,  C07D231/54 ,  C07D249/04 ,  A61K31/4192 ,  A61K31/437 ,  C07D249/18 ,  C07D253/08 ,  C07D403/04 ,  C07D471/04

CPC分类号： A61K31/501 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/53 ,  A61K45/06 ,  C07D231/54 ,  C07D249/04 ,  C07D249/18 ,  C07D253/08 ,  C07D403/04 ,  C07D471/04 ,  A61K2300/00

摘要： In one aspect, the invention relates to triazol-1-ol compounds, analogs thereof, compositions comprising same, and methods of using same, alone or in combination with other agents, to reactivate latent retroviruses, and more particularly to reactivate latent HIV-1. Such compounds, compositions, and methods can be used, for example, in connection with diagnosing and/or treating a retrovirus, and more specifically HIV-1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：US20160362421A1

公开(公告)日：2016-12-15

申请号：US15188701

申请日：2016-06-21

申请人： Gilead Sciences, Inc.

发明人： Britton Kenneth Corkey ,  Elfatih Elzein ,  Michael Graupe ,  Juan Guerrero ,  Robert H. Jiang ,  Rao V. Kalla ,  Tetsuya Kobayashi ,  Dmitry Koltun ,  Xiaofen Li ,  Ruben Martinez ,  Gregory Notte ,  Eric Q. Parkhill ,  Thao Perry ,  Chandrasekar Venkataramani ,  Jeff Zablocki

IPC分类号： C07D498/10 ,  C07D401/04 ,  C07D403/04 ,  C07D413/06 ,  C07D403/06 ,  C07D413/14 ,  C07D417/06 ,  C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D237/32 ,  C07D417/12 ,  C07D401/06 ,  C07D265/22 ,  C07D279/08 ,  C07D217/26 ,  C07D405/12 ,  C07D253/08

CPC分类号： C07D498/10 ,  C07D217/26 ,  C07D237/32 ,  C07D239/88 ,  C07D239/90 ,  C07D253/08 ,  C07D263/58 ,  C07D265/22 ,  C07D279/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D498/04

摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

摘要翻译： 其中Q，R 1，X 1，X 2，Y和R 2如本文所述，用于制备和使用化合物的方法以及含有该化合物的药物组合物。