公开(公告)号：US20220055986A1

公开(公告)日：2022-02-24

申请号：US17521004

申请日：2021-11-08

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Toshihide WATANABE ,  Kensuke KUSUMI ,  Satomi IMAIDE ,  Toshimitsu ENDO ,  Takaki KOMIYA ,  Naomi TSUBURAYA

IPC: C07D205/04 ,  C07C49/252 ,  C07C49/577

Abstract: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

公开(公告)号：US4581377A

公开(公告)日：1986-04-08

申请号：US669455

申请日：1984-11-07

Applicant: Yoshihisa Shibata ,  Yoshihiko Yoshimoto

Inventor： Yoshihisa Shibata ,  Yoshihiko Yoshimoto

IPC: C07C43/23 ,  A61K31/045 ,  A61K31/085 ,  A61K31/12 ,  A61K31/135 ,  A61K31/22 ,  A61P25/04 ,  A61P29/00 ,  C07C27/00 ,  C07C33/34 ,  C07C33/38 ,  C07C33/50 ,  C07C41/00 ,  C07C45/00 ,  C07C49/225 ,  C07C49/237 ,  C07C49/252 ,  C07C49/255 ,  C07C49/675 ,  C07C49/683 ,  C07C49/747 ,  C07C67/00 ,  C07C69/157 ,  C07C69/63 ,  C07C69/67 ,  C07C201/00 ,  C07C205/00 ,  C07C205/19 ,  C07C205/42 ,  C07C205/45 ,  C07C209/00 ,  C07C211/61 ,  C07C225/22 ,  C07C49/792

CPC classification number: C07C49/747 ,  C07C205/19 ,  C07C205/42 ,  C07C205/45 ,  C07C49/225 ,  C07C49/237 ,  C07C49/252 ,  C07C49/255 ,  C07C49/675 ,  C07C2103/18

Abstract: Compounds of formula I below are useful as anti-inflammatory, analgesic and/or anti-pyretic agents: ##STR1## in which R.sup.1 is hydrogen, nitro, amino, hydroxyl, alkoxy of one to four carbon atoms, alkyl of one to four carbon atoms or halogen; R.sup.2 is hydrogen or alkyl of one to four carbon atoms; is a saturated or unsaturated bond; A is CO, CHOH, C(R.sup.5)OH or CHOCOR.sup.6, where R.sup.5 and R.sup.6 are alkyl of one to four carbon atoms; B is alkyl of one to twelve carbon atoms; and X is H.sub.2 or O.

Abstract translation: 式I化合物可用作抗炎，镇痛和/或抗热解剂：其中R1是氢，硝基，氨基，羟基，1-4个碳原子的烷氧基， 至四个碳原子或卤素; R2是氢或1-4个碳原子的烷基; 是饱和或不饱和键; A是CO，CHOH，C（R5）OH或CHOCOR6，其中R5和R6是1-4个碳原子的烷基; B是1-12个碳原子的烷基; X为H 2或O.

公开(公告)号：US4382959A

公开(公告)日：1983-05-10

申请号：US253197

申请日：1981-04-13

Applicant: Alexander C. Goudie

Inventor： Alexander C. Goudie

IPC: C07C41/26 ,  C07C43/23 ,  C07C45/27 ,  C07C45/30 ,  C07C45/45 ,  C07C49/255 ,  A61K31/12 ,  C07C49/252

CPC classification number: C07C49/255 ,  C07C41/26 ,  C07C43/23 ,  C07C45/27 ,  C07C45/30 ,  C07C45/45

Abstract: 4-(6-Methoxy-2-naphthyl)-3-hydroxybutan-2-one and 4-(6-methoxy-2-naphthyl)buta-2,3-diol have good degrees of anti-inflammatory and analgesic activity coupled with an advantageous therapeutic ratio based on gastric irritancy and are non-oestrogenic. Their preparation and use are described.

Abstract translation: 4-（6-甲氧基-2-萘基）-3-羟基丁-2-酮和4-（6-甲氧基-2-萘基）丁-2,3-二醇具有良好的抗炎和镇痛作用 基于胃刺激的有利的治疗比例是非雌激素的。 描述了它们的制备和使用。

公开(公告)号：US4247484A

公开(公告)日：1981-01-27

申请号：US76974

申请日：1979-09-20

Applicant: Victor Mark ,  Charles V. Hedges

Inventor： Victor Mark ,  Charles V. Hedges

IPC: C07C37/20 ,  C07C39/17 ,  C07C39/42 ,  C07C45/00 ,  C07C45/68 ,  C07C49/747 ,  C07C67/00 ,  C08G63/00 ,  C08G64/00 ,  C08G64/06 ,  C08G64/14 ,  C07C49/22 ,  C07C49/237 ,  C07C49/252

CPC classification number: C08G64/14 ,  C07C37/20 ,  C07C45/68 ,  C07C49/747 ,  C08G64/06 ,  C07C2101/14

Abstract: Novel keto-diphenol compounds are disclosed. These compounds are intermediates in the production of novel tetraphenolic compounds which have utility as branching agents in the production of novel, randomly branched polycarbonates.

Abstract translation: 公开了新的酮 - 二酚化合物。 这些化合物是生产新型四元酚化合物的中间体，其在生产新型无规支化的聚碳酸酯中可用作支化剂。

公开(公告)号：US20220001035A1

公开(公告)日：2022-01-06

申请号：US17448463

申请日：2021-09-22

Applicant: The General Hospital Corporation

Inventor： Chongzhao Ran ,  Anna Moore ,  Jian Yang

IPC: A61K51/04 ,  C07B59/00 ,  C07F5/02 ,  C07C49/248 ,  C07C49/252

Abstract: Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

公开(公告)号：US11198672B2

公开(公告)日：2021-12-14

申请号：US16970865

申请日：2019-02-21

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Toshihide Watanabe ,  Kensuke Kusumi ,  Satomi Imaide ,  Toshimitsu Endo ,  Takaki Komiya ,  Naomi Tsuburaya

IPC: C07D205/04 ,  C07C49/252 ,  C07C49/577

Abstract: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

公开(公告)号：US4456771A

公开(公告)日：1984-06-26

申请号：US415020

申请日：1982-09-07

Applicant: Charles R. Everly ,  Jerry M. Roper

Inventor： Charles R. Everly ,  Jerry M. Roper

IPC: B01J31/00 ,  C07C45/00 ,  C07C45/68 ,  C07C49/245 ,  C07C49/252 ,  C07C67/00 ,  C08K5/132 ,  C09K15/08 ,  C10L1/185 ,  C10M129/24 ,  C07C45/61

CPC classification number: C10M129/24 ,  C07C45/68 ,  C07C49/245 ,  C07C49/252 ,  C08K5/132 ,  C09K15/08 ,  C10L1/1857 ,  C10M2207/023 ,  C10M2207/08

Abstract: Novel (3',5'-dihydrocarbyl-4'-hydroxybenzyl)-1,3-diketones are prepared by reacting an N,N-dihydrocarbyl-2,6-dihydrocarbyl-4-aminomethylphenol with a 1,3-diketone and an alkyl halide in the presence of an alkali or an alkaline earth metal hydride. The products are useful as antioxidants.

Abstract translation: 通过使N，N-二烃基-2,6-二烃基-4-氨基甲基苯酚与1,3-二酮和1,3-二酮反应制备新的（3'，5'-二烃基-4'-羟基苄基）-1,3-二酮 烷基卤化物在碱或碱土金属氢化物的存在下反应。 该产品可用作抗氧化剂。

公开(公告)号：US4228105A

公开(公告)日：1980-10-14

申请号：US964046

申请日：1978-11-27

Applicant: Rudiger Jeck

Inventor： Rudiger Jeck

IPC: C07D295/10 ,  C07C45/00 ,  C07C45/51 ,  C07C45/66 ,  C07C49/20 ,  C07C49/223 ,  C07C49/225 ,  C07C49/235 ,  C07C49/24 ,  C07C49/252 ,  C07C67/00 ,  C07C213/00 ,  C07C225/22 ,  C07C241/00 ,  C07C251/16 ,  C07D295/112 ,  C07C49/82

CPC classification number: C07D295/112 ,  C07C45/516 ,  C07C45/66 ,  C07C49/223 ,  C07C49/225 ,  C07C49/235 ,  C07C49/252

Abstract: A process for the production of compounds of formula I, ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms,R.sub.2 is hydrogen, fluorine, chlorine or bromine, andR.sub.3 is bromine, iodine, isobutyl, tert. butyl, cyclohexyl, cyclohexenyl; or phenyl, optionally substituted by fluorine, chlorine, bromine or alkoxy of 1 to 4 carbon atoms; or a radical of formula II, ##STR2## in which either R.sub.4 and R.sub.5 are the same or different and each signifies alkyl of 1 to 3 carbon atoms, orR.sub.4 and R.sub.5 together signify the radical --(CH.sub.2).sub.n --, in which n is 4 or 5, the radical --CH.sub.2 --CH.sub.2 --0--CH.sub.2 --CH.sub.2 --, the radical --CH.sub.2 --CH.dbd.CH--CH.sub.2 --, or the radical --CH.sub.2 --CH.sub.2 --N(R.sub.6)--CH.sub.2 --CH.sub.2 --, in which R.sub.6 is hydrogen or alkyl of 1 to 3 carbon atoms. Hydroxyketone and hydroxy imine intermediates are also disclosed.The compounds of formula I are known to exhibit anti-inflammatory activity.

Abstract translation: 制备式I化合物的方法，其中R 1为1至3个碳原子的烷基，R 2为氢，氟，氯或溴，R 3为溴，碘，异丁基，叔丁基。 丁基，环己基，环己烯基; 或苯基，任选被氟，氯，溴或具有1至4个碳原子的烷氧基取代; 或式II的基团，其中R 4和R 5相同或不同，并且各自表示1至3个碳原子的烷基，或者R 4和R 5一起表示基团 - （CH 2）n - ，其中 基团-CH 2 -CH 2 -O-CH 2 -CH 2 - ，基团-CH 2 -CH = CH-CH 2 - 或基团-CH 2 -CH 2 -N（R 6）-CH 2 -CH 2 - 其中R 6是氢或1至3个碳原子的烷基。 还公开了羟基酮和羟基亚胺中间体。 已知式I化合物具有抗炎活性。

公开(公告)号：US3876648A

公开(公告)日：1975-04-08

申请号：US34793173

申请日：1973-04-04

Applicant: CIBA GEIGY CORP

Inventor： HAAS GEORGES ,  ROSSI ALBERTO

IPC: C07C29/147 ,  C07C45/00 ,  C07C45/63 ,  C07C49/237 ,  C07C49/252 ,  C07C67/00 ,  C07C245/14 ,  C07D213/79 ,  C07D213/80 ,  C07D31/36

CPC classification number: C07D213/79 ,  C07C29/147 ,  C07C45/63 ,  C07C49/237 ,  C07C245/14 ,  C07C2601/16 ,  C07C33/34

Abstract: This invention describes new pyridine carboxylic acid esters of formula I

wherein R.sub.1 is 1-cycloalkenyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen, lower alkyl or cycloalkyl, A is a direct bond or methylene, or --A--O-- represents --CO--CH.sub.2 --O-- and Py is pyridyl. The compounds claimed possess an anti-inflammatory action and also an anti-nociceptive action and are therefore useful in particular as antiphlogistics and as non anaesthetic, peripheral analgesics.

公开(公告)号：US20240327342A1

公开(公告)日：2024-10-03

申请号：US18744303

申请日：2024-06-14

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Toshihide WATANABE ,  Kensuke KUSUMI ,  Satomi IMAIDE ,  Toshimitsu ENDO ,  Takaki KOMIYA ,  Naomi TSUBURAYA

IPC: C07D205/04 ,  C07C49/252 ,  C07C49/577

CPC classification number: C07D205/04 ,  C07C49/252 ,  C07C49/577

Abstract: A compound represented by the general formula (V)




wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.