公开(公告)号：US4089960A

公开(公告)日：1978-05-16

申请号：US723125

申请日：1976-09-14

Applicant: Jacques Gosteli ,  Angelo Storni ,  Armin Zust

Inventor： Jacques Gosteli ,  Angelo Storni ,  Armin Zust

IPC: A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4412 ,  A61P1/08 ,  A61P25/18 ,  C07D213/78 ,  C07D213/79 ,  C07D213/80 ,  C07D213/85 ,  C07D453/02 ,  C07D455/02 ,  A61K31/455

CPC classification number: C07D213/78 ,  C07D213/80 ,  C07D453/02 ,  Y10S514/872

Abstract: The present invention provides new basically substituted pyridinecarboxamides having the formula I ##STR1## wherein R.sub.1 represents lower alkyl and --OR.sub.1 is in the adjacent position to the carboxamide group,R.sub.2 represents lower alkyl or an ethylene radical which is attached to one of the trivalent radicals designated as A and the nitrogen atom located between it to form a 6-membered ring,A represents a divalent saturated hydrocarbon radical which encompasses at most a single ring with 5 or 6 ring members and contains not more than 7 carbon atoms and whose two linkage positions are separated by (3-m) to 4 carbon atoms, or, if R.sub.2 is an ethylene radical, represents the 1-propanyl-3-ylidene radical, if m s 1, or the 1,2,4-butane-triyl radical, if m is 0,And one of the factors m and n is 0 and the other is 1, and, if desired, the ring B is further substituted, and the acid addition salts of the compounds of the formula I. These new substances possess useful pharmacological properties, in particular antiemetic, psychosomatic and antipsychotic activity and can be used for the treatment of thought disturbances and of states of psychomotor excitation. Specific embodiments are N-[(1-ethyl-2-pyrrolidinyl)-methyl]-2,6-dimethoxynicotinamide and the pharmaceutically acceptable acid addition salts thereof.

Abstract translation: 本发明提供了新的基本上取代的具有式I（I）的吡啶甲酰胺，其中R 1表示低级烷基，-OR 1在与羧酰胺基相邻的位置，R 2表示低级烷基或亚乙基， 指定为A的三价基团和位于其之间的氮原子形成6元环，A表示二价饱和烃基，其包含至多一个具有5或6个环成员的单环且含有不超过7个碳原子， 其两个连接位置被（3-m）分隔成4个碳原子，或者如果R 2是亚乙基，则表示1-丙基-3-亚基，如果ms 1或1,2,4-丁烷 三环基，如果m为0，且其中一个因子M和N为0，另一个为1，并且，如果所需，环B进一步被取代，以及式I化合物的酸加成盐。 这些新物质具有有用的药理学特性 特定的止吐，心身和抗精神病活动，可用于治疗思想障碍和精神运动激发状态。 具体实施方案是N - [（1-乙基-2-吡咯烷基） - 甲基] -2,6-二甲氧基烟酰胺及其药学上可接受的酸加成盐。

公开(公告)号：US06464962B2

公开(公告)日：2002-10-15

申请号：US09308380

申请日：1999-08-04

Applicant: René Heckendorn ,  Jacques Gosteli

Inventor： René Heckendorn ,  Jacques Gosteli

IPC: A61K716

CPC classification number: A61K8/69 ,  A61Q11/00 ,  C07C215/08

Abstract: Amine hydrofluorides of the general formula (I): R—N(CH2CH2OH)2.HF   (I) In which R is a straight-chain hydrocarbon residue having 10 to 20 carbon atoms exhibit antibacterial and caries-prophylactic activity and can be prepared in high purity. The amine hydrofluorides of the formula (I) can be formulated, optionally in combination with tin fluoride, into oral hygiene compositions such as toothpastes, mouthwashes or chewable tablets.

Abstract translation: 通式（I）的氨基氢氟酸：其中R是具有10〜20个碳原子的直链烃残基表现出抗菌和龋齿预防活性，可以制备高纯度。 式（I）的胺氢氟酸可以任选地与氟化锡组合配制成口腔卫生组合物如牙膏，漱口剂或咀嚼片。

公开(公告)号：US5606072A

公开(公告)日：1997-02-25

申请号：US418463

申请日：1995-04-07

Applicant: Gareth Griffiths ,  Ren e Imwinkelried ,  Jacques Gosteli

Inventor： Gareth Griffiths ,  Ren e Imwinkelried ,  Jacques Gosteli

IPC: C07D233/68 ,  C07D233/22 ,  C07D233/64

CPC classification number: C07D233/68

Abstract: 2-Substituted 5-chlorimidazoles of the general formula: ##STR1## are new intermediate products for the production of antihyperintensive pharmaceutical agents or of herbicidal compounds. A process for the production of these intermediate products as well as a new process for the further reaction of 2-substituted 5-chlorimidazoles of general formula I, wherein R.sub.1 is hydrogen, to the 2-substituted 5-chlorimidazole-4-carbaldehydes of the formula: ##STR2##

Abstract translation: 2-取代的以下通式的5-氯咪唑： I是用于生产抗高血压药物或除草化合物的新中间产物。 用于制备这些中间产物的方法以及用于将通式I的2-取代的5-氯咪唑（其中R 1是氢）进一步反应的2-取代的5-氯咪唑-4-甲醛的新方法 公式： II

公开(公告)号：US5442076A

公开(公告)日：1995-08-15

申请号：US92052

申请日：1993-07-15

Applicant: Jacques Gosteli ,  Gareth Griffiths ,  Rene Imwinkelried

Inventor： Jacques Gosteli ,  Gareth Griffiths ,  Rene Imwinkelried

IPC: C07D233/68 ,  C07D233/70

CPC classification number: C07D233/68 ,  C07D233/70

Abstract: Process for the production of 2-substituted 5-chlorimidazole-4-carbaldehydes of general formula: ##STR1## wherein R is alkyl, cycloalkyl, benzyl, or phenyl. These compounds form valuable intermediate products for the production of antihypertensive pharmaceutical agents or herbicidal compounds.

Abstract translation: 用于制备通式为：1或苯基的2-取代的5-氯咪唑-4-甲醛的方法。 这些化合物形成用于生产抗高血压药剂或除草化合物的有价值的中间产物。

公开(公告)号：US5292918A

公开(公告)日：1994-03-08

申请号：US934537

申请日：1992-10-06

Applicant: Jacques Gosteli ,  Ingrid Mergelsberg ,  Markus Tanner

Inventor： Jacques Gosteli ,  Ingrid Mergelsberg ,  Markus Tanner

IPC: B01J29/00 ,  C07B61/00 ,  C07C253/00 ,  C07C255/24 ,  C07C255/25 ,  C07C255/42 ,  C07C253/30

CPC classification number: C07C255/42 ,  C07C255/25

Abstract: A process for preparing an (S,S) or (R,R) diastereoisomer of the formula: ##STR1## or salts, esters or amides thereof, wherein R.sup.3 and R.sup.4 independently represent hydrogen, alkyl, aryl or aryl substituted with halogen, alkyl, nitro or alkoxy, and n and m independently represent integers from one to six, comprising combining a cyanide compound of the formula:M.sup.1 C.tbd.N (III)wherein M.sup.1 is hydrogen, trimethylsilyl or a metal, with an optional proton source, a solvent and a Lewis acid of the formula:M.sup.2 X.sub.4, AlCl.sub.3 or BF.sub.3 (IV)wherein M.sup.2 is Sn or Ti and X represents chloro, bromo, fluoro or iodo, with an .alpha.-amino acid compound or salts or esters thereof, followed by addition of an acyl or acetal compound to give the diastereoisomer of formula (X).

Abstract translation: PCT No.PCT / US91 / 02034第Sec。 371日期：1992年10月6日 102（e）日期1992年10月6日PCT 1991年3月29日PCT公布。 出版物WO91 / 17141 日期：1991年11月14日。一种制备下式的（S，S）或（R，R）非对映异构体的方法：（*化学结构*）（X）或其盐，酯或酰胺，其中R3和R4独立地 代表氢，烷基，芳基或被卤素，烷基，硝基或烷氧基取代的芳基，n和m独立地表示1至6的整数，包括将下式的氰化物化合物：M1C（三键）N（III） 是氢，三甲基甲硅烷基或金属，具有任选的质子源，溶剂和下式的路易斯酸：M2X4，AlCl3或BF3（Ⅳ），其中M2是Sn或Ti，X代表氯，溴，氟或碘，与 （α） - 氨基酸化合物或其盐或酯，然后加入酰基或缩醛化合物，得到式（X）的非对映异构体。

公开(公告)号：US4990618A

公开(公告)日：1991-02-05

申请号：US517729

申请日：1990-05-02

Applicant: Jacques Gosteli ,  Aleksander Warm

Inventor： Jacques Gosteli ,  Aleksander Warm

IPC: C07D211/44 ,  C07D211/74 ,  C07D495/04 ,  C07D513/04

CPC classification number: C07D513/04 ,  C07D211/74

Abstract: The following intermediate compounds, namely, 4-Oxo-3-(2-propenyl)-piperidine-3-carboxylic acid ester of the formula: ##STR1## wherein R is hydrogen, a formyl group, an acetyl group or a benzoyl group or is a benzyl group, whose aromatic ring optionally is ring-substituted by at least one halogen atom, and R.sub.1 is an alkyl group with 1 to 4 C atoms.4-Oxo-3-(2-propenyl)-piperidine of the formula: ##STR2## wherein R is hydrogen, a formyl group, and acetyl group or a benzoyl group or is a benzyl group, whose aromatic ring optionally is ring-substituted by at least one halogen atom.

公开(公告)号：US4732999A

公开(公告)日：1988-03-22

申请号：US877784

申请日：1986-06-24

Applicant: Leander Tenud ,  Jacques Gosteli

Inventor： Leander Tenud ,  Jacques Gosteli

IPC: C07C229/22 ,  C07B31/00 ,  C07B53/00 ,  C07B57/00 ,  C07C51/00 ,  C07C51/41 ,  C07C59/255 ,  C07C67/00 ,  C07C213/00 ,  C07C213/10 ,  C07C215/40 ,  C07C253/00 ,  C07C255/26 ,  C07C121/43

CPC classification number: C07C59/255

Abstract: Process for the production of optically-active di-[3-chloro-2-oxy-propyltrimethylammonium]-tartrate. Racemic 3-chloro-2-oxy-propyltrimethylammonium-chloride is converted by racemate resolution with optically-active tartaric acid into the optically-active di-[3-chloro-2-oxy-propyltrimethylammonium]-tartrate. Such optically-active tartrate compound is dissociated in tartaric acid to optically-active 3-chloro-2-oxy-propyltrimethylammonium-chloride and the latter is converted with inorganic cyanides. From the product, the production of optically-active carnitine nitrile chloride can be achieved.

Abstract translation: 制备光学活性二 - [3-氯-2-羟基 - 丙基三甲基铵] - 酒石酸盐的方法。 外消旋3-氯-2-氧 - 丙基三甲基氯化铵通过外消旋物拆分与光学活性酒石酸转化成光学活性的二 - [3-氯-2-氧基 - 丙基三甲基铵] - 酒石酸盐。 这种光学活性酒石酸盐化合物在酒石酸中分解成光学活性的3-氯-2-氧 - 丙基三甲基氯化铵，后者用无机氰化物转化。 从产品出发，可以实现光学活性肉碱氯化腈的生产。

公开(公告)号：US4732709A

公开(公告)日：1988-03-22

申请号：US877786

申请日：1986-06-24

Applicant: Leander Tenud ,  Jacques Gosteli

Inventor： Leander Tenud ,  Jacques Gosteli

IPC: C07C229/22 ,  C07B31/00 ,  C07B53/00 ,  C07B57/00 ,  C07C51/00 ,  C07C51/41 ,  C07C59/255 ,  C07C67/00 ,  C07C213/00 ,  C07C213/10 ,  C07C215/40 ,  C07C253/00 ,  C07C255/26 ,  C07C87/30

CPC classification number: C07C59/255

Abstract: Process for the production of optically-active di-[3-chloro-2-oxy-propyltrimethylammonium]-tartrate. Racemic 3-chloro-2-oxy-propyltrimethylammonium-chloride is converted by racemate resolution with optically-active tartaric acid into the optically-active di-[3-chloro-2-oxy-propyltrimethylammonium]-tartrate. Such optically-active tartrate compound is dissociated in tartaric acid and optically-active 3-chloro-2-oxy-propyltrimethylammonium-chloride and the latter is converted with inorganic cyanides. From the product, the production of optically-active carnitine nitrile chloride can be achieved.

Abstract translation: 制备光学活性二 - [3-氯-2-羟基 - 丙基三甲基铵] - 酒石酸盐的方法。 外消旋3-氯-2-氧 - 丙基三甲基氯化铵通过外消旋物拆分与光学活性酒石酸转化成光学活性的二 - [3-氯-2-氧基 - 丙基三甲基铵] - 酒石酸盐。 这种光学活性酒石酸盐化合物在酒石酸和光学活性3-氯-2-氧 - 丙基三甲基氯化铵中解离，后者用无机氰化物转化。 从产品出发，可以实现光学活性肉碱氯化腈的生产。

公开(公告)号：US4692442A

公开(公告)日：1987-09-08

申请号：US208105

申请日：1980-11-18

Applicant: Jacques Gosteli ,  Ivan Ernest ,  Marc Lang ,  Robert B. Woodward

Inventor： Jacques Gosteli ,  Ivan Ernest ,  Marc Lang ,  Robert B. Woodward

IPC: A61K31/397 ,  A61K31/43 ,  A61P31/04 ,  C07D205/08 ,  C07D205/09 ,  C07D417/12 ,  C07D499/04 ,  C07D499/06 ,  C07D499/86 ,  C07D499/861 ,  C07D499/87 ,  C07D499/88 ,  C07D499/881 ,  C07D499/883 ,  C07D499/887 ,  C07D499/897 ,  C07F9/568 ,  C07D499/00

CPC classification number: C07D499/88 ,  C07D205/08 ,  C07D205/09 ,  C07F9/5683

Abstract: The invention relates to 2-penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.a represents an organic radical bonded by a carbon atom to the ring carbon atom, a free, etherified or esterified hydroxy or mercapto group or a halogen atom, R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom, or an etherified mercapto group, and R.sub.2 represents a hydroxy group or an R.sub.2.sup.A radical that together with the carbonyl grouping --C(.dbd.O)-- forms a protected carboxyl group, and to salts of such compounds with salt-forming groups, processes for the manufacture of such compounds, pharmaceutical preparations containing compounds of the formula I with pharmacological properties, and their use. The compounds have antibiotic activity.

Abstract translation: 本发明涉及式（Ⅰ）的2-青霉烯-3-羧酸化合物，其中Ra表示通过碳原子与环碳原子键合的有机基团，游离醚化或酯化的羟基或巯基 或卤素原子，R1表示氢，由碳原子键合至环碳原子的有机基团或醚化巯基，R 2表示与羰基-C（= O）一起形成的羟基或R2A基团 ）形成保护的羧基，以及这些化合物与成盐基团的盐，制备这些化合物的方法，含有药理学性质的式I化合物的药物制剂及其用途。 这些化合物具有抗生素活性。

公开(公告)号：US4670192A

公开(公告)日：1987-06-02

申请号：US877785

申请日：1986-06-24

Applicant: Leander Tenud ,  Jacques Gosteli

Inventor： Leander Tenud ,  Jacques Gosteli

IPC: C07C229/22 ,  C07B31/00 ,  C07B53/00 ,  C07B57/00 ,  C07C51/00 ,  C07C51/41 ,  C07C59/255 ,  C07C67/00 ,  C07C213/00 ,  C07C213/10 ,  C07C215/40 ,  C07C253/00 ,  C07C255/26 ,  C07C95/00

CPC classification number: C07C59/255

Abstract: Process for the production of optically-active di-[3-chloro-2-hydroxy-propyltrimethylammonium]-tartrate. Racemic 3-chloro-2-hydroxy-propyltrimethylammonium-chloride is converted by racemate resolution with optically-active tartaric acid into the optically-active di-[3-chloro-2-hydroxy-propyltrimethylammonium]-tartrate. Such optically-active tartrate compound is dissociated in tartaric acid and optically-active 3-chloro-2-hydroxy-propyltrimethylammonium-chloride and the latter is converted with inorganic cyanides. From the product, the production of optically-active carnitine nitrile chloride can be achieved.

Abstract translation: 制备光学活性二 - [3-氯-2-羟基 - 丙基三甲基铵] - 酒石酸盐的方法。 外消旋的3-氯-2-羟基 - 丙基三甲基氯化铵通过外消旋物拆分与光学活性酒石酸转化成光学活性的二 - [3-氯-2-羟基 - 丙基三甲基铵] - 酒石酸盐。 这种光学活性酒石酸盐化合物在酒石酸和光学活性3-氯-2-羟基 - 丙基三甲基氯化铵中解离，后者用无机氰化物转化。 从产品出发，可以实现光学活性肉碱氯化腈的生产。