公开(公告)号：JP2001026565A

公开(公告)日：2001-01-30

申请号：JP2000188222

申请日：2000-06-22

Applicant: BASF AG

Inventor： KLATT MARTIN JOCHEN ,  MUELLER THOMAS ,  BOCKSTIEGEL BERNHARD DR

IPC: B01J31/18 ,  B01J31/22 ,  C07B61/00 ,  C07C45/34 ,  C07C45/86 ,  C07C49/403 ,  C07C49/603

Abstract: PROBLEM TO BE SOLVED: To obtain the subject compound by a method providing excellent yield, selectivity and space time yield by oxidizing a specific compound with molecular oxygen in a solvent in the presence of a base, a specific catalyst and a specific additive. SOLUTION: This compound is obtained by oxidizing (A) 3,5,5-trimethyl- cyclohex-3-ene-1-one with (B) molecular oxygen in the presence of (C) a base, (D) a catalyst of the formula R1 to R8 are each H, a halogen, NO2, COR9, SO3R9 (R9 is H or a 1-4C alkyl), or the like; M is Mn (II), Mn (III)(+)X(-) [X(-) is a counterion with a negative charge in the case of a metal used in an oxidation stage III], Co (II), or the like} and (E) an additive comprising an acetate of the formula (R10R11R12C-COO(-))mY(m+) (R10 to R12 are each H, F, a 1-4C alkyl, or the like; Y is NH4+ or a metal cation of the main groups 1-4 with 1-4 valence (s); (m) is 1-4) (e.g. lithium acetate) in (F) a solvent (e.g. dimethylformamide).

公开(公告)号：JP2003192638A

公开(公告)日：2003-07-09

申请号：JP2002351365

申请日：2002-12-03

Applicant: BASF AG

Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  ERHARDT MELANIE

IPC: C07D339/04 ,  C07C67/30 ,  C07C67/31 ,  C07C67/317 ,  C07C67/32 ,  C07C69/66 ,  C07C69/675

Abstract: PROBLEM TO BE SOLVED: To provide a method for producing a dihydroxycarboxylic ester of formula I as an intermediate for producing R-(+)-α-lipoic acid with a relative amount of complex hydrides in the absence of solvent in a high yield. SOLUTION: This method for producing the dihydroxycarboxylic ester represented by formula I [(n) is 1, 2, 3, 4, 5, 6 or 7; R 1 is a substituted or unsubstituted 1 to 20C alkyl, 2 to 20C alkenyl, 2 to 20C alkynyl or the like] comprises reacting a hydroxycarboxylic diester represented by formula II (R 2 is selected from R 1 independently from R 1 ) with the complex hydrides in the absence of solvent. COPYRIGHT: (C)2003,JPO

公开(公告)号：JP2002121134A

公开(公告)日：2002-04-23

申请号：JP2001207026

申请日：2001-07-06

Applicant: BASF AG

Inventor： KRAEMER KLAUS DR ,  KLATT MARTIN JOCHEN

IPC: A23K1/16 ,  A23L1/30 ,  A23L1/304 ,  A61K8/00 ,  A61K8/20 ,  A61K8/21 ,  A61K8/23 ,  A61K8/24 ,  A61K8/30 ,  A61K8/36 ,  A61K8/365 ,  A61K8/44 ,  A61K8/46 ,  A61K8/49 ,  A61K8/58 ,  A61K31/20 ,  A61K31/381 ,  A61K33/00 ,  A61K33/06 ,  A61K33/14 ,  A61K33/24 ,  A61K33/42 ,  A61P1/00 ,  A61P3/00 ,  A61P3/02 ,  A61P3/10 ,  A61P13/00 ,  A61P13/12 ,  A61P31/18 ,  A61P35/00 ,  A61P43/00 ,  A61Q90/00 ,  C07D339/04 ,  A61K7/00

Abstract: PROBLEM TO BE SOLVED: To obtain an organic chelator and a complexing agent or a salt- forming agent and an organic mineral compound having increased bioavailability as compared with that of inorganic mineral salts. SOLUTION: α-Lipoic acid or α-dihydrolipoic acid is used for increasing the bioavailability of the mineral salts.

公开(公告)号：JP2001031615A

公开(公告)日：2001-02-06

申请号：JP2000189393

申请日：2000-06-23

Applicant: BASF AG

Inventor： KLATT MARTIN JOCHEN ,  MUELLER THOMAS ,  BOCKSTIEGEL BERNHARD DR

IPC: B01J31/22 ,  B01J31/18 ,  C07B61/00 ,  C07C45/34 ,  C07C49/603

Abstract: PROBLEM TO BE SOLVED: To provide a method of oxidizing β-isophorone using a manganese- salen complex, in high efficiency, also in high yield, selectivity and space time yield each convertible to large industrial scale even in case of high starting material concentration. SOLUTION: This method comprises oxidizing 3,5,5-trimethylcyclohex-3-en-1- one with molecular oxygen in the presence of a base, a solvent and a catalyst to produce the objective 3,5,5-trimethylcyclohex-2-ene-1,4-dione; wherein a manganese-salen complex of the formula [R is hydrogen or Cl; M is Mn(II) or Mn(III)(+)Cl(-)] is used as the catalyst.

公开(公告)号：JP2000119217A

公开(公告)日：2000-04-25

申请号：JP27882199

申请日：1999-09-30

Applicant: BASF AG

Inventor： STUERMER RAINER ,  KLATT MARTIN JOCHEN ,  BOERMER ARMIN ,  HOLZ JENS ,  VOSS GUDRUN

IPC: B01J31/24 ,  C07B53/00 ,  C07B61/00 ,  C07C67/297 ,  C07C67/31 ,  C07C69/67 ,  C07C69/675 ,  C07C69/732

Abstract: PROBLEM TO BE SOLVED: To provide a method for producing the subject β-hydroxy ester in high yield by reacting a β-keto ester with hydrogen in the presence of a ruthenium catalyst. SOLUTION: This method is to react (A) a β-keto ester with (B) hydrogen in the presence of (C) a catalyst of the formula, LRuX2 [X is a halogen, acetate or aryl; and L is a bidentate phospholane of the formula (B is an 1-6C crosslink between 2 Ps; R1 is H or an 1-6C alkyl or the like; R2 is alkyl or aryl; (m) is 0 or 1; and R3 is H or the like)], pref., at 0 to 100 deg.C under a pressure of 0.1 to 300 bars in an alkanol-containing solvent. The weight ratio of the component C to component A is pref. (1 to 10) to (1 to 1000,000). In the above reaction, it is preferable to add (D) 0.5 to 2 mol equivalents of acid esp. strong acid, (e.g. mineral acid or trifluoroacetic acid) to the component C.

公开(公告)号：WO0210151A2

公开(公告)日：2002-02-07

申请号：PCT/EP0108523

申请日：2001-07-24

Applicant: BASF AG ,  KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

IPC: A61K31/20 ,  A61P3/10 ,  C07B53/00 ,  C07C303/38 ,  C07C309/66 ,  C07C319/08 ,  C07C319/18 ,  C07C319/28 ,  C07C321/04 ,  C07C323/52 ,  C07D339/04 ,  C07D339/00

CPC classification number: C07D339/04 ,  C07C319/18 ,  C07C321/04 ,  C07C323/52

Abstract: The invention relates to a method for producing R-lipoic acid and S-lipoic acid comprising a step selected from the following: (a) distillation of dihydrolipoic acid, (b) reaction of (2) or the stereoisomer thereof, wherein Ms represents SO2-R', and R and R' independently mean C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkylalkyl, aryl or aralkyl, with sodium sulphide and sulphur in ethanol and reaction with a complex hydride, (c) extraction of a protic solution of R dihydrolipoic acid or S-dihydrolipoic acid with an organic solvent at a pH value of 9 -10, or (d) extraction of R-dihydrolipoic acid or S-dihydrolipoic acid with an organic solvent from a protic solution at a pH value of 4 - 5, or a combination of individual or several steps (a) - (d). The invention also relates to a method for producing dihydrolipoic acid and the compound 1,6,8 octane triol.

Abstract translation: 为R-α-硫辛酸或S-硫辛酸的制剂，其包含选自（a）的二氢硫辛酸的蒸馏中选择的工艺步骤中，（b）中的反应或它的立体异构体，其中Ms“和R和R”是-SO 2 R独立地C 1 -C过程 C6烷基，C3-C8环烷基，C3-C8-环烷基烷基，芳基或芳烷基，与硫化钠和硫在乙醇中，用复合氢化物的反应中，（c）中R-二氢硫辛酸或S的质子溶液的提取 二氢硫辛酸与有机溶剂在pH值为9〜10，或（d）R-二氢硫辛酸或与来自一个的质子溶液或以4的pH值至5的有机溶剂S-二氢硫辛酸，或它们的组合的提取 更多的步骤（a）至（d）以及方法二氢硫辛酸的制备和化合物1,6,8 Oktantriol。

公开(公告)号：WO0244163A3

公开(公告)日：2003-01-30

申请号：PCT/EP0113955

申请日：2001-11-29

Applicant: BASF AG ,  KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

IPC: C07D339/04

CPC classification number: C07D339/04

Abstract: The invention relates to a method for producing R- and S-lipoic acid and R-dihydrolipoic acid comprising the following steps: (a) reaction of the compound of formula (2) with sodium sulphide and sulphur in methanol, whereby Ms represents SO R`, and R and R` independently of one another represent C1-C6 alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkylalkyl, aryl or aralkyl. The invention relates in particular to methods for producing pure R- or S-dihydrolipoic acid, which is either used directly or processed further to obtain R- and S-lipoic acid. The method is also used to produce medicaments. The invention also relates to a solution of sodium sulphide-trihydrate and sulphur in methanol, whereby the sulphur is present as a molar surplus in relation to the sodium sulphide-trihydrate, and to a kit that comprises the inventive solution.

Abstract translation: 本发明涉及一种方法，用于R-和S-硫辛酸和R-二氢硫辛酸的制备，其包括（a）使（I），其中MS是SO <2> R`和R和R`独立地为C1-C6烷基 ，C3-C8环烷基，C3-C8-环烷基烷基，芳基或芳烷基，与硫化钠和硫在甲醇中。 具体而言，本发明提供用于制备纯的R或S-二氢硫辛酸的，其直接或R-和S-硫辛酸涉及进一步的处理中使用的方法。 该方法也可用于制备药物。 本发明还涉及硫化酸钠三水合物和硫的甲醇溶液中，硫是存在的摩尔过量于Natriumsfulfid三水合物和包含本发明的

公开(公告)号：WO2006042728A2

公开(公告)日：2006-04-27

申请号：PCT/EP2005011147

申请日：2005-10-17

Applicant: BASF AG ,  KRAEMER KLAUS ,  HAUNERT FRANK ,  MATUSCHECK MARKUS ,  HASSELWANDER OLIVER ,  KLATT MARTIN JOCHEN

Inventor： KRAEMER KLAUS ,  HAUNERT FRANK ,  MATUSCHECK MARKUS ,  HASSELWANDER OLIVER ,  KLATT MARTIN JOCHEN

IPC: A61K31/44 ,  A61P1/18

CPC classification number: A61K31/44

Abstract: The invention relates to the use of stable ammonium a-liponate salts for the treatment of a series of disease states, in particular, diabetic disorders and disorders of diabetic origin. The salts (Lp) (A) are formed from a-liponic acid (Lp) and ammonium compounds (A) of general formula (II) or (III). Further application of the salts are related to the treatment of cardiovascular disorders, neurodegenerative disorders and diseases related to chronic kidney failure and/or dialysis treatment, retinopathies, nephropathies, proteinurias, hyperlipidaemias, hypertriglyceridaemias, hypercholesterinaemias, proliferations of smooth muscle cells in arteries, collagenoses, arthritis, fibromyalgias, kidney stones, inflammation, cancer, amyloidoses, osteoporoses, excess weight and obesity, HIV infections and AIDS, metabolic syndrome, oxidative stress and related diseases and the aging process.

Abstract translation: 本发明涉及使用aLiponsäure的稳定铵盐用于治疗多种疾病状态，包括，特别是糖尿病病症和病症包括糖尿病原点。 盐（LP）（A）是由α-硫辛酸（LP）和通式（II）或（III）形成通式的氨基化合物（A）的。 盐的其它用途是在特定心血管疾病，神经变性疾病和慢性肾功能衰竭和/或透析治疗相关的疾病的治疗; 视网膜病，肾病，蛋白尿，高脂血症，高甘油三酯血症，高胆固醇血症，动脉的平滑肌细胞，结缔组织疾病，关节炎，纤维肌痛，肾结石，炎症，癌症，淀粉样变性，骨质疏松症，肥胖和肥胖，HIV感染和AIDS的增殖; 代谢综合征; 氧化应激和相关疾病; 并通过老化过程定向。

公开(公告)号：WO0222111A2

公开(公告)日：2002-03-21

申请号：PCT/EP0110501

申请日：2001-09-11

Applicant: BASF AG ,  HASSELWANDER OLIVER ,  KRAEMER KLAUS ,  BALDENIUS KAI UWE ,  KLATT MARTIN JOCHEN ,  SCHWEIKERT LONI

Inventor： HASSELWANDER OLIVER ,  KRAEMER KLAUS ,  BALDENIUS KAI-UWE ,  KLATT MARTIN JOCHEN ,  SCHWEIKERT LONI

IPC: A61K31/381 ,  A23L1/30 ,  A61K31/00 ,  A61K31/202 ,  A61K31/385 ,  A61P3/10 ,  A61P9/10 ,  A61P13/12 ,  A61P25/02 ,  A61P27/02

CPC classification number: A61K31/385 ,  A61K31/20 ,  A61K2300/00

Abstract: The invention relates to the use of lipoic acids, or a physiologically acceptable derivative or salt thereof, and a compound of formula (I): H3C-(CH2)n1-(CH=CH)n3-(CH2)n2-COOH - wherein n1 and n2 independently have the value of a whole number from 3 to 9, n3 has the value of a whole number from 2 to 6, and the number of carbon atoms amounts to 18, 20 or 22 - or a physiologically acceptable derivative or salt thereof, as food supplements, in functional foods and for therapeutic purposes in the treatment of diabetic disorders. The invention also relates to agents having a corresponding active ingredient combination and to agents in the form of commercial packs having corresponding combination preparations or monopreparations for combined use.

Abstract translation: 本发明涉及使用硫辛酸，生理学上可接受的衍生物或其盐，和式（I）的化合物：H 3 C-（CH 2）N1（CH = CH）N3（CH 2）N2-COOH，式中，n1， N2彼此独立地具有整数的3至9的值的，N3具有从2的整数的至6的值，并且是在功能的18，20或22，生理学上可接受的衍生物或其盐，膳食补充剂，碳原子数 食品（功能性食品）和糖尿病病症的治疗治疗目的。 还描述了装置与相应的活性成分组合物和组合物与相应的组合产品或单一成分的产品组合使用的商业包装的形式。

公开(公告)号：DE102004050353A1

公开(公告)日：2006-04-20

申请号：DE102004050353

申请日：2004-10-15

Applicant: BASF AG

Inventor： KRAEMER KLAUS ,  HAUNERT FRANK ,  MATUSCHEK MARKUS ,  HASSELWANDER OLIVER ,  KLATT MARTIN JOCHEN

IPC: A61K31/385 ,  A61K31/4436 ,  A61P3/10