公开(公告)号：US12012383B2

公开(公告)日：2024-06-18

申请号：US17553637

申请日：2021-12-16

申请人： Clear Creek Bio, Inc.

发明人： Vikram S. Kumar ,  David P. Hesson ,  Ping Huang ,  Mo Jia ,  Xianjun You

IPC分类号： C07D215/52

CPC分类号： C07D215/52

摘要： The invention provides therapeutic compositions that contain an inhibitor of dihydroorotate dehydrogenase (DHODH) and promote sustained elevation of dihydroorotate (DHO) levels in a patient. The compositions are useful for treating disorders associated with unregulated DHODH activity, such as acute myeloid leukemia. The invention also provides methods of determining therapeutically effective doses of compositions that contain a DHODH inhibitor. The invention further provides methods of synthesis of 2-(2′-halo-1-1′-biphenyl-4-yl)-quinoline carboxylic acids, which are useful as DHODH inhibitors.

公开(公告)号：US20220177435A1

公开(公告)日：2022-06-09

申请号：US17553637

申请日：2021-12-16

申请人： Clear Creek Bio, Inc.

发明人： Vikram S. Kumar ,  David P. Hesson ,  Ping Huang ,  Mo Jia ,  Xianjun You

IPC分类号： C07D215/52

摘要： The invention provides therapeutic compositions that contain an inhibitor of dihydroorotate dehydrogenase (DHODH) and promote sustained elevation of dihydroorotate (DHO) levels in a patient. The compositions are useful for treating disorders associated with unregulated DHODH activity, such as acute myeloid leukemia. The invention also provides methods of determining therapeutically effective doses of compositions that contain a DHODH inhibitor. The invention further provides methods of synthesis of 2-(2′-halo-1-1′-biphenyl-4-yl)-quinoline carboxylic acids, which are useful as DHODH inhibitors.

公开(公告)号：US20220169640A1

公开(公告)日：2022-06-02

申请号：US17441978

申请日：2020-03-19

申请人： KABUSHIKI KAISHA YAKULT HONSHA

发明人： Takahide SHIGEYAMA ,  Takuya SUGIMOTO ,  Hideyuki KOMATSU ,  Hiroyuki NISHIYAMA

IPC分类号： C07D413/14 ,  C07D215/52 ,  C07D209/38

摘要： Provided is a method for industrially advantageously synthesizing a production intermediate of a quinolinecarboxamide derivative or a salt thereof. The present invention provides a method for producing a quinolinecarboxylic acid derivative of formula (4) or a salt thereof, including reacting an aniline of the following formula (1), in the presence of boron trifluoride-tetrahydrofuran complex or boron trifluoride-diethyl ether complex, with an aldehyde of formula (2) and subsequently reacting the resulting compound with an α-keto acid of formula (3), wherein R1, R2, R3 and R4 are the same or different and each represent a hydrogen atom, a halogen atom, a lower alkyl group, or the like, R5 represents a hydrogen atom, a lower alkyl group, or the like, and R6 represents a hydrogen atom, a lower alkyl group, or the like.

公开(公告)号：US11092594B2

公开(公告)日：2021-08-17

申请号：US15665291

申请日：2017-07-31

申请人： Ventana Medical Systems, Inc.

发明人： Jerome W. Kosmeder, II ,  Mark Lefever ,  Donald Johnson ,  Michael Farrell ,  Zhanna Zhilina ,  Christopher Bieniarz

IPC分类号： G01N33/532 ,  C07D495/04 ,  G01N33/58 ,  G01N33/53 ,  G01N33/533 ,  C07D491/147 ,  C07D277/76 ,  C07D241/44 ,  C07D493/04 ,  C07D243/12 ,  C07D277/48 ,  C07D215/52 ,  C07D231/16 ,  C07D493/14 ,  C07D491/056 ,  C07D498/04 ,  C07D311/12 ,  C07D491/052 ,  C07D271/12 ,  C07D417/12 ,  C07D271/08 ,  C12Q1/6804 ,  C12Q1/6841 ,  C12Q1/6886

摘要： A method for performing a multiplexed diagnostic assay, such as for two or more different targets in a sample, is described. One embodiment comprised contacting the sample with two or more specific binding moieties that bind specifically to two or more different targets. The two or more specific binding moieties are conjugated to different haptens, and at least one of the haptens is an oxazole, a pyrazole, a thiazole, a nitroaryl compound other than dinitrophenyl, a benzofurazan, a triterpene, a urea, athiourea, a rotenoid, a coumarin, a cyclolignan, a heterobiaryl, an azo aryl, or a benzodiazepine. The sample is contacted with two or more different anti-hapten antibodies that can be detected separately. The two or more different anti-hapten antibodies may be conjugated to different detectable labels.

公开(公告)号：US20210230135A1

公开(公告)日：2021-07-29

申请号：US17208474

申请日：2021-03-22

申请人： MITSUI CHEMICALS, INC.

发明人： 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分类号： 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 ,  C07C237/42 ,  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

摘要： A compound represented by Formula (1): The compound can be used as insecticides.

公开(公告)号：US20210087146A1

公开(公告)日：2021-03-25

申请号：US17111701

申请日：2020-12-04

申请人： Clear Creek Bio, Inc.

发明人： Vikram S. Kumar ,  David P. Hesson ,  Ping Huang ,  Mo Jia ,  Xianjun You

IPC分类号： C07D215/52

摘要： The invention provides therapeutic compositions that contain an inhibitor of dihydroorotate dehydrogenase (DHODH) and promote sustained elevation of dihydroorotate (DHO) levels in a patient. The compositions are useful for treating disorders associated with unregulated DHODH activity, such as acute myeloid leukemia. The invention also provides methods of determining therapeutically effective doses of compositions that contain a DHODH inhibitor. The invention further provides methods of synthesis of 2-(2′-halo-1-1′-biphenyl-4-yl)-quinoline carboxylic acids, which are useful as DHODH inhibitors.

公开(公告)号：US10479765B2

公开(公告)日：2019-11-19

申请号：US16125645

申请日：2018-09-07

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Hartmut Beck ,  Tobias Thaler ,  Raimund Kast ,  Daniel Meibom ,  Mark Meininghaus ,  Carsten Terjung ,  Martina Delbeck ,  Klemens Lustig ,  Uwe Muenster ,  Britta Olenik

IPC分类号： C07D215/52 ,  C07D215/60 ,  C07D401/12 ,  C07D401/04

摘要： The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.

公开(公告)号：US10179770B2

公开(公告)日：2019-01-15

申请号：US14777917

申请日：2014-03-13

申请人： GENOSCIENCE PHARMA

发明人： Jerome Courcambeck ,  Philippe Halfon ,  Firas Bassissi ,  Sonia Brun ,  Gregory Nicolas ,  Antoine Beret ,  Serge Petit ,  Claire Camus ,  Jean Pierre Nallet

IPC分类号： A61K31/47 ,  C07D215/52 ,  C07D401/04 ,  A61K45/06 ,  C07D215/12 ,  C07D215/18 ,  C07D215/233 ,  C07D401/06 ,  C07D491/113 ,  C07D211/58 ,  C07D211/74 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/5377 ,  C07D215/42 ,  C07D401/12

摘要： The invention provides quinoline derivatives, their manufacture, pharmaceutical compositions containing them, and their use as medicaments. The active compounds of the present invention are useful for the treatment of proliferative neoplastic and non-neoplastic diseases.

公开(公告)号：US20160002198A1

公开(公告)日：2016-01-07

申请号：US14854627

申请日：2015-09-15

申请人： MITSUI CHEMICALS, INC.

发明人： 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分类号： C07D333/38 ,  C07C237/48 ,  C07D213/81 ,  C07D213/82 ,  C07D207/34 ,  C07D241/24 ,  C07D239/28 ,  C07D307/68 ,  C07D307/85 ,  C07D309/08 ,  C07D231/14 ,  C07D261/18 ,  C07D277/56 ,  C07D317/46 ,  C07D215/52 ,  C07C237/42

CPC分类号： 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

摘要： An object of the present invention is to provide a compound represented by Formula (1): wherein A1, A2, A3 and A4 each represent a carbon atom, a nitrogen atom or an oxidized nitrogen atom; R1 and R2 each represent a hydrogen atom, an optionally substituted alkyl group or an optionally substituted C1-C4 alkylcarbonyl group; G1 and G2 each represent an oxygen atom or a sulfur atom; X, which may be identical or different each other, represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a trifluoromethyl group; n is an integer of 0 to 4; and Q1 represents an optionally substituted phenyl group, an optionally substituted naphthyl group or an optionally substituted heterocyclic group; Q2 represents a phenyl group or heterocyclic group having one or more substituents, at least one of the substituent being any of a C1-C4 haloalkoxy group, a C2-C6 perfluoroalkyl group, a C1-C6 perfluoroalkylthio group, a C1-C6 perfluoroalkylsulfinyl group and a C1-C6 perfluoroalkylsulfonyl group, an insecticide comprising the compound as the active ingredient, and a process for preparation thereof.

摘要翻译： 本发明的目的是提供由式（1）表示的化合物：其中A1，A2，A3和A4各自表示碳原子，氮原子或氧化的氮原子; R 1和R 2各自表示氢原子，任选取代的烷基或任选取代的C 1 -C 4烷基羰基; G1和G2各自表示氧原子或硫原子; X可以相同或不同，表示氢原子，卤素原子，C1-C3烷基或三氟甲基; n为0〜4的整数。 并且Q 1表示任选取代的苯基，任选取代的萘基或任选取代的杂环基; Q2表示具有一个或多个取代基的苯基或杂环基，所述取代基中的至少一个为C1-C4卤代烷氧基，C2-C6全氟烷基，C1-C6全氟烷硫基，C1-C6全氟烷基亚磺酰基 和C1-C6全氟烷基磺酰基，其包含该化合物作为活性成分的杀虫剂及其制备方法。

公开(公告)号：US09185912B2

公开(公告)日：2015-11-17

申请号：US14220673

申请日：2014-03-20

申请人： MITSUI CHEMICALS, INC.

发明人： 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分类号： A01N43/40 ,  A01N43/60 ,  A01N37/44 ,  A01N43/08 ,  A01N43/10 ,  A01N43/12 ,  A01N43/16 ,  A01N43/30 ,  A01N43/42 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/78 ,  A01N43/80 ,  C07C237/42 ,  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 ,  C07D333/38 ,  C07D333/68 ,  A01N37/22

CPC分类号： 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

摘要： A compound represented by Formula (1): The compound can be used as insecticides.

摘要翻译： 由式（1）表示的化合物：该化合物可以用作杀虫剂。