公开(公告)号：US5563169A

公开(公告)日：1996-10-08

申请号：US204420

申请日：1994-07-06

Applicant: Akira Yoshida ,  Kozo Oda ,  Takashi Kasai ,  Teiichiro Koga ,  Kazuo Hasegawa

Inventor： Akira Yoshida ,  Kozo Oda ,  Takashi Kasai ,  Teiichiro Koga ,  Kazuo Hasegawa

IPC: A61K31/352 ,  A61K31/382 ,  A61P9/10 ,  C07D311/82 ,  C07D311/84 ,  C07D311/90 ,  C07D335/12 ,  C07D335/14 ,  C07D335/20 ,  C07D407/12 ,  A61K31/35

CPC classification number: C07D407/12 ,  C07D311/82 ,  C07D311/84 ,  C07D311/90 ,  C07D335/12 ,  C07D335/14 ,  C07D335/20

Abstract: ConstitutionTricyclic heterocyclyl compounds having a general formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 each represents H, a lower alkyl or lower alkoxy group, a halogen atom or halogeno-lower alkyl; R.sup.3 represents H or a lower alkyl group; R.sup.4 represents a substituted phenyl or naphthyl group; R.sub.5 represents H or a lower alkyl group; A represents a lower alkylene group; B represents an --O-- or --S-- group; and n is 0-1.EffectThe compounds have an excellent activity in the inhibition of acyl-CoA: cholesterol acyltransferase (ACAT) and are useful for the treatment and prophylaxis of atherosclerosis.

Abstract translation: PCT No.PCT / JP92 / 01164 Sec。 371日期：1994年7月6日 102（e）日期1994年7月6日PCT提交1992年9月11日PCT公布。 出版物WO93 / 03740 日期：1993年4月3日构造具有通式（I）的三环杂环基化合物：其中：R1和R2各自表示H，低级烷基或低级烷氧基，卤素原子或卤代低级烷基; R3代表H或低级烷基; R4表示取代的苯基或萘基; R5代表H或低级烷基; A表示低级亚烷基; B表示-O-或-S-基; n为0-1。 作用该化合物在酰基辅酶A：胆固醇酰基转移酶（ACAT）的抑制中具有优异的活性，可用于治疗和预防动脉粥样硬化。

公开(公告)号：US5532266A

公开(公告)日：1996-07-02

申请号：US453811

申请日：1995-05-30

Applicant: Rudolf Gottschlich ,  Karl-August Ackermann ,  Helmut Prucher ,  Christoph Seyfried ,  Hartmut Greiner ,  Gerd Bartoszyk ,  Frank Mauler ,  Manfred Stohrer ,  Andrew Barber

Inventor： Rudolf Gottschlich ,  Karl-August Ackermann ,  Helmut Prucher ,  Christoph Seyfried ,  Hartmut Greiner ,  Gerd Bartoszyk ,  Frank Mauler ,  Manfred Stohrer ,  Andrew Barber

IPC: A61K31/435 ,  A61K31/165 ,  A61K31/17 ,  A61K31/35 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/47 ,  A61K31/472 ,  A61K31/495 ,  A61K31/535 ,  A61P7/10 ,  A61P11/08 ,  A61P11/14 ,  A61P25/04 ,  A61P25/08 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07C233/00 ,  C07C233/05 ,  C07C233/08 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D215/00 ,  C07D217/06 ,  C07D217/14 ,  C07D295/12 ,  C07D295/135 ,  C07D311/84 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  C07D207/36 ,  C07D207/325

CPC classification number: C07D405/06 ,  C07D207/09 ,  C07D207/12 ,  C07D217/14 ,  C07D311/84 ,  C07D405/12

Abstract: Novel arylacetamides of the formula I ##STR1## in which Q is R.sup.4 --CH(CH.sub.2 Z)--NA--, ##STR2## R.sup.1 is Ar, cycloalkyl with 3-7 C atoms or C.sub.4 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.7 -alkyl,R.sup.2 is Ar,R.sup.3 is H, OH, OA or A,R.sup.4 is A or phenyl which can optionally be substituted once or twice by F, Cl, Br, I, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A or NA.sub.2,R.sup.5 and R.sup.6 are each, independently of one another, H, F, Cl, Br, I, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or taken together are methylenedioxy,A is alkyl with 1-7 C atoms, and physiologically acceptable salts thereof.

Abstract translation: 其中Q为R4-CH（CH2Z）-NA-，R1为Ar，具有3-7个C原子的环烷基或C 4 -C 8 - 环烷基-C 1 -C 4烷基的新的芳基乙酰胺， C7-烷基，R2是Ar，R3是H，OH，OA或A，R4是A或可以被F，Cl，Br，I，OH，OA，CF3，NO2，NH2等任意取代一次或两次的苯基， NHA，NHCOA，NHSO2A或NA2，R5和R6各自独立地为H，F，Cl，Br，I，OH，OA，CF3，NH2，NHA，NA2，NHCOA，NHCONH2， 亚甲二氧基，A是具有1-7个C原子的烷基，以及其生理上可接受的盐。

公开(公告)号：US5312936A

公开(公告)日：1994-05-17

申请号：US761127

申请日：1991-09-17

Applicant: Sherryl L. Lifer ,  Winston S. Marshall ,  Fariborz Mohamadi ,  Jon K. Reel ,  Richard L. Simon ,  Mitchell I. Steinberg ,  Celia A. Whitesitt

Inventor： Sherryl L. Lifer ,  Winston S. Marshall ,  Fariborz Mohamadi ,  Jon K. Reel ,  Richard L. Simon ,  Mitchell I. Steinberg ,  Celia A. Whitesitt

IPC: A61K31/075 ,  A61K31/00 ,  A61K31/085 ,  A61K31/13 ,  A61K31/16 ,  A61K31/18 ,  A61K31/19 ,  A61K31/35 ,  A61K31/352 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61P5/00 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07C63/331 ,  C07C65/24 ,  C07C65/34 ,  C07C69/76 ,  C07C205/56 ,  C07C229/42 ,  C07C235/24 ,  C07C255/41 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/38 ,  C07D233/88 ,  C07D233/90 ,  C07D249/04 ,  C07D249/06 ,  C07D249/08 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D257/04 ,  C07D257/06 ,  C07D311/82 ,  C07D311/84 ,  C07D311/86 ,  C07D311/88 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D233/44

CPC classification number: C07D257/04 ,  C07C229/42 ,  C07C255/41 ,  C07C65/24 ,  C07C65/34 ,  C07C69/76 ,  C07D207/34 ,  C07D231/14 ,  C07D233/88 ,  C07D233/90 ,  C07D249/10 ,  C07D257/06 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.

Abstract translation: 本发明提供新颖的苯基和杂环衍生物，它们的药物制剂及其在哺乳动物中拮抗血管紧张素II受体的用途。

公开(公告)号：US5219871A

公开(公告)日：1993-06-15

申请号：US416894

申请日：1989-10-04

Applicant: Peter E. Cross ,  Alexander R. MacKenzie

Inventor： Peter E. Cross ,  Alexander R. MacKenzie

IPC: A61K31/00 ,  A61K31/335 ,  A61K31/34 ,  A61K31/343 ,  A61K31/357 ,  A61K31/36 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61P25/02 ,  C07C237/20 ,  C07C237/24 ,  C07C255/42 ,  C07C255/47 ,  C07C255/58 ,  C07C311/08 ,  C07C311/29 ,  C07C311/39 ,  C07C323/25 ,  C07C323/36 ,  C07C323/38 ,  C07C323/49 ,  C07C323/62 ,  C07C323/67 ,  C07D213/38 ,  C07D213/74 ,  C07D241/12 ,  C07D307/79 ,  C07D311/84 ,  C07D313/12 ,  C07D317/58 ,  C07D319/16 ,  C07D319/18 ,  C07D335/14 ,  C07D337/12

CPC classification number: C07D307/79 ,  C07C237/20 ,  C07C237/24 ,  C07C255/42 ,  C07C255/47 ,  C07C255/58 ,  C07C311/08 ,  C07D213/38 ,  C07D317/58 ,  C07D319/16 ,  C07C2102/08 ,  C07C2103/38

Abstract: Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.

公开(公告)号：US5066680A

公开(公告)日：1991-11-19

申请号：US475301

申请日：1990-02-05

Applicant: Youichi Shiokawa ,  Kazuo Okumura ,  Kazuhiko Take ,  Kazunori Tsubaki

Inventor： Youichi Shiokawa ,  Kazuo Okumura ,  Kazuhiko Take ,  Kazunori Tsubaki

IPC: A61K31/165 ,  A61K31/35 ,  A61K31/352 ,  A61K31/415 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/451 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P1/00 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  C07C233/07 ,  C07C233/40 ,  C07C235/28 ,  C07C235/34 ,  C07C237/20 ,  C07C237/22 ,  C07D211/22 ,  C07D211/26 ,  C07D211/34 ,  C07D211/46 ,  C07D211/70 ,  C07D213/40 ,  C07D233/34 ,  C07D233/88 ,  C07D295/08 ,  C07D295/125 ,  C07D311/84 ,  C07D335/14 ,  C07D471/08

CPC classification number: C07D213/40 ,  C07C233/40 ,  C07C235/34 ,  C07C237/20 ,  C07C237/22 ,  C07D211/22 ,  C07D211/26 ,  C07D211/46 ,  C07D211/70 ,  C07D233/34 ,  C07D295/125 ,  C07D335/14 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2101/18

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s),R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.

公开(公告)号：US4918082A

公开(公告)日：1990-04-17

申请号：US243108

申请日：1988-09-02

Applicant: William M. Davis

Inventor： William M. Davis

IPC: C07D205/04 ,  C07D211/54 ,  C07D311/84

CPC classification number: C07D205/04 ,  C07D211/54 ,  C07D311/84

Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula ##STR1## where R.sub.2 is a radical selected from the group consisting of ##STR2## where m is an integer from 0 to 3.

Abstract translation: 提供了一类新的具有两条支链的抗痉挛化合物。 化合物具有通式“IMAGE”，其中R 2是选自下列的基团：其中m是0至3的整数。

公开(公告)号：US4898876A

公开(公告)日：1990-02-06

申请号：US796525

申请日：1985-11-12

Applicant: Setsuro Fujii ,  Eizou Hattori ,  Mitsuteru Hirata ,  Koichiro Watanabe ,  Kazuhiro Onogi ,  Masahiko Nagakura

Inventor： Setsuro Fujii ,  Eizou Hattori ,  Mitsuteru Hirata ,  Koichiro Watanabe ,  Kazuhiro Onogi ,  Masahiko Nagakura

IPC: C07D209/48 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54 ,  C07D217/26 ,  C07D237/28 ,  C07D241/44 ,  C07D261/18 ,  C07D295/192 ,  C07D307/79 ,  C07D307/84 ,  C07D307/86 ,  C07D311/12 ,  C07D311/58 ,  C07D311/84 ,  C07D317/68 ,  C07D319/18 ,  C07D333/54 ,  C07D333/60

CPC classification number: C07D209/48 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54 ,  C07D217/26 ,  C07D237/28 ,  C07D241/44 ,  C07D261/18 ,  C07D295/192 ,  C07D307/79 ,  C07D307/84 ,  C07D307/86 ,  C07D311/12 ,  C07D311/58 ,  C07D311/84 ,  C07D317/68 ,  C07D319/18 ,  C07D333/54 ,  C07D333/60

Abstract: A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group, excepting the case where A is a single bond, R.sub.1 is ##STR2## and R.sub.2 is a methyl group, exhibits excellent chymotrypsin inhibitive activity.

Abstract translation: 下式的苯甲酰基哌嗪酯：其中A表示单键或亚烷基，亚乙烯基，-O-亚烷基或次甲基，R 1表示可被低级烷基取代的双环碳环残基 ，低级烷氧基，氧代基或硝基或卤素原子，或可部分饱和; 可含有氧代基的芴残基; 亚芴基; 蒽残基; 可以被低级烷基取代的菲残基，或可以部分饱和; 可以被低级烷基或低级烷氧基取代的苯并呋喃残基或硫杂残基; 可被氧代基或苯基取代并部分饱和的苯并吡喃残基或苯并嗪残基; 邻苯二甲酰亚胺残基; 苯并二氮残基; 可以被低级烷基或苯基取代的异唑残基; 或亚烷基二氧基苯残基或呫吨残基; 除了A为单键，R 1为甲基，R 2为甲基的情况外，R 2表示烷基，环烷基，环烷基烷基或芳烷基，表现出优异的糜蛋白酶抑制活性。

公开(公告)号：US4571405A

公开(公告)日：1986-02-18

申请号：US615042

申请日：1984-05-29

Applicant: Trevor S. Abram ,  Peter Norman ,  Warren, Brian T.

Inventor： Trevor S. Abram ,  Peter Norman ,  Warren, Brian T.

IPC: C07D335/06 ,  A61K31/35 ,  A61K31/352 ,  A61K31/38 ,  A61K31/382 ,  A61P11/00 ,  A61P37/08 ,  C07C231/00 ,  C07C231/12 ,  C07C233/33 ,  C07C233/54 ,  C07C233/56 ,  C07C235/46 ,  C07C235/56 ,  C07C235/84 ,  C07D263/14 ,  C07D309/12 ,  C07D311/22 ,  C07D311/84 ,  C07D311/86 ,  C07D311/92 ,  C07D335/10 ,  C07D335/16 ,  C07D405/04 ,  C07D309/38 ,  C07D335/12

CPC classification number: C07D405/04 ,  C07D311/22 ,  C07D311/86 ,  C07D335/16

Abstract: Certain 5-substituted chromones and thiochromones and pharmacologically acceptable salts thereof are disclosed. The compounds possess antiallergic properties and are represented by the formula: ##STR1## wherein: X is selected from the group consisting of --O--, --S--, and --SO.sub.2 --;R.sub.1 and R.sub.2 are each independently H or lower alkyl having from 1 to 4 carbon atoms or together with C.sub.2 and C.sub.3 from a cyclohexane ring having the structure: ##STR2## wherein R.sub.3 and R.sub.4 are each independently H or a lower alkyl having from 1 to 4 carbon atoms.Also taught are valuable intermediates useful in the preparation of said 5-substituted chromones and thiochromones represented by the formula: ##STR3## wherein B is selected from the group consisting of --NHCOC(CH.sub.3).sub.3, 1,3-oxazolinyl and --CONHR, wherein R is methyl, phenyl, or t-butyl; Y is selected from the group consisting of CO.sub.2 H, CHO, CO.sub.2 R' and COR', wherein R' is a lower alkyl having from 1 to 4 carbon atoms; and A is H or tetrahydropyran.

Abstract translation: 公开了某些5-取代的色酮和硫代色酮及其药理学上可接受的盐。 这些化合物具有抗过敏性质并由下式表示：其中：X选自-O - ， - S - 和-SO 2 - ; - R 1和R 2各自独立地为具有1至4个碳原子的H或低级烷基或与来自具有以下结构的环己烷环的C2和C3一起形成：其中R 3和R 4各自独立地为H或具有1至 4个碳原子。 还教导了可用于制备由下式表示的所述5-取代的色酮和硫代色酮的有价值的中间体：其中B选自-NHCOC（CH 3）3，1,3-恶唑啉基和-CONHR， 其中R是甲基，苯基或叔丁基; Y选自CO 2 H，CHO，CO 2 R'和COR'，其中R'是具有1至4个碳原子的低级烷基; A是H或四氢吡喃。

公开(公告)号：US4503066A

公开(公告)日：1985-03-05

申请号：US377132

申请日：1982-05-11

Applicant: David R. Brittain ,  Robin Wood

Inventor： David R. Brittain ,  Robin Wood

IPC: A61K31/40 ,  A61P3/08 ,  A61P3/10 ,  C07D311/58 ,  C07D311/84 ,  C07D491/10 ,  C07D491/107 ,  A61K31/41

CPC classification number: C07D491/10 ,  C07D311/58 ,  C07D311/84

Abstract: The invention provides various medical compositions for use in treating or preventing certain of the side effects of diabetes or galactosemia. The active ingredients are selected from a series of novel aldose reductase inhibitory spiro-linked pyrrolidine-2,5-diones of the general formula: ##STR1## or a pharmaceutically acceptable salt, or a non-toxic, biodegradable precursor thereof. Processes for the production of these compounds are also provided. A particular compound suitable for use as an active ingredient is spiro[pyrrolidine-3,9'-xanthene]-2,5-dione.

Abstract translation: 本发明提供用于治疗或预防糖尿病或半乳糖血症的某些副作用的各种医药组合物。 活性成分选自一系列通式如下的新型醛糖还原酶抑制螺旋吡咯烷-2,5-二酮或其药学上可接受的盐或其无生物可降解的前体。 还提供了用于生产这些化合物的方法。 适合用作活性成分的特定化合物是螺[吡咯烷-3,9'-呫吨] -2,5-二酮。

公开(公告)号：US4048322A

公开(公告)日：1977-09-13

申请号：US673135

申请日：1976-04-02

Applicant: Egon Karpati ,  Laszlo Szporny ,  Mihaly Bartok ,  Jozsef Czombos ,  Karoly Felfoldi ,  Marta Laszlavik ,  Ferenc Notheisz

Inventor： Egon Karpati ,  Laszlo Szporny ,  Mihaly Bartok ,  Jozsef Czombos ,  Karoly Felfoldi ,  Marta Laszlavik ,  Ferenc Notheisz

IPC: C07D311/90 ,  A61K31/35 ,  A61K31/352 ,  A61K31/40 ,  A61P11/14 ,  A61P25/02 ,  C07D295/13 ,  C07D311/82 ,  C07D311/84

CPC classification number: C07D295/13 ,  C07D311/84

Abstract: The invention relates to new xanthene-9-carboxylates of the formula (I), ##STR1## wherein R.sub.1 and R.sub.3 are the same or different and each can represent a lower alkyl group,R.sub.2 is a lower alkyl group or a group of the formula (VI), ##STR2## WHEREIN M IS AN INTEGER OF 2 TO 5, OR R.sub.1 and R.sub.2 form, together with the adjacent nitrogen atom, a five- or six-membered heterocyclic group, and n and m each represent integers of 2 to 5, or salts thereof. These compounds possess cholinolytic and bronchospasmolytic effects and are completely devoid of harmful side-effects. Thus these compounds can be used to great advantage in therapy. The new compounds of the formula (I) or their salts can be prepared by reacting a diaminoalcohol of the formula (III), ##STR3## wherein R.sub.2 is lower alkyl or a group of formula -(CH.sub.2).sub.m -OH, with a reactive derivative of xanthene-9-carboxylic acid, and, if desired, converting the obtained product into its salt.

Abstract translation: 本发明涉及式（I）的新的呫吨-9-羧酸盐，其中R1和R3相同或不同并且各自表示低级烷基，R2是低级烷基或基团 式（VI），（VI），其中M为2至5的整数，或R 1和R 2与相邻的氮原子一起形成五元或六元杂环基，n和m 各自表示2至5的整数，或其盐。 这些化合物具有胆固醇和支气管痉挛的作用，完全没有有害的副作用。 因此，这些化合物可用于治疗中的极大优势。 式（I）的新化合物或其盐可以通过使式（III），（III）的二氨基醇与其中R 2为低级烷基或式 - （CH 2）m -OH的基团反应制备， 与呫吨-9-羧酸的反应性衍生物反应，如果需要，将得到的产物转化成其盐。