公开(公告)号：CA2055572A1

公开(公告)日：1992-06-19

申请号：CA2055572

申请日：1991-11-14

Applicant: KRONENTHAL DAVID ,  THOTTATHIL JOHN K ,  PATEL RAMESH N ,  SZARKA LASZLO J

Inventor： KRONENTHAL DAVID ,  THOTTATHIL JOHN K ,  PATEL RAMESH N ,  SZARKA LASZLO J

IPC: A61K31/34 ,  A61P7/02 ,  C07D493/08 ,  C12N9/18 ,  C12P17/04 ,  C12P17/18 ,  C12P41/00 ,  C12R1/38 ,  C07D493/18

Abstract: HA528 PROCESS AND INTERMEDIATES FOR THROMBOXANE RECEPTOR ANTAGONISTS Disclosed herein is a process for preparing a monoacyl of the formula in which the associated diacyl is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the -O-C-(O)-R1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. This acyl-alcohol is oxidized to the associated acylaldehydes, which are hydrolyzed with an alkali metal carbonate, bicarbonate or hydroxide to the cis furanol. The thromboxane receptor antagonist ¢lS-¢1.alpha.,2.alpha.(Z),3.alpha.,4.alpha.!!-7-¢3¢¢¢¢(1-oxoheptyl)-amino!acetyl!amino!methyl-7-oxabicyclo-¢2.2.1!-hept-2-yl!-5-heptenoic acid may be prepared using these processes.

公开(公告)号：CA2032091A1

公开(公告)日：1992-05-20

申请号：CA2032091

申请日：1990-12-12

Applicant: PATEL RAMESH N ,  SZARKA LASZLO J ,  MUELLER RICHARD H

Inventor： PATEL RAMESH N ,  SZARKA LASZLO J ,  MUELLER RICHARD H

IPC: C07D223/16 ,  C07D281/10 ,  C07D403/06 ,  C12P17/10 ,  C12P17/14 ,  C12P17/16 ,  C12R1/01

Abstract: HA466a MICROBIAL REDUCTION OF BENZAZEPINE AND BENZOTHIAZEPINE DERIVATIVES A novel process comprises reducing a benzazepine or benzothiazepine at the 3-position in d-cis configuration by treatment with reductasesupplying microorganisms or enzymes derived therefrom. The process can be catalyzed in a single stage by growing microbial cultures or in a two-stage fermentation/transformation by resting cell-suspensions. The enzymes derived from the microorganisms can be used in free state or immobilized form. The microorganisms and enzymes catalyzes the specific reduction with 90 to 99% conversion efficiency to 99% or greater optical purity of the desired enantiomer.

公开(公告)号：CA2008702A1

公开(公告)日：1990-08-27

申请号：CA2008702

申请日：1990-01-26

Applicant: HANSON RONALD L ,  PATEL RAMESH N ,  SZARKA LASZLO J

Inventor： HANSON RONALD L ,  PATEL RAMESH N ,  SZARKA LASZLO J

IPC: C12P13/04 ,  C12P13/08 ,  C12R1/07 ,  C12R1/085 ,  C12R1/72

Abstract: GC266 PROCESS FOR TRANSFORMATION OF HYDROXYKETO ACIDS TO HYDROXYAMINO ACIDS A novel process for preparation of hydroxyamino acids is disclosed. In this process, a hydroxyketo acid reacts with a nitrogen source when treated with an amino acid dehydrogenase, a transaminase, or microorganisms that produce such enzymes. This process allows production of compounds having the formula III from compounds having the formula IV GC266 wherein R3 and R4 are each independently hydrogen, alkyl, or aryl. In one embodiment of the invention, the transformation to hydroxyamino acid is combined with NADH regeneration by treatment with a dehydrogenase and its associated substrate.

公开(公告)号：CA2094191C

公开(公告)日：2003-09-23

申请号：CA2094191

申请日：1993-04-16

Applicant: PATEL RAMESH N ,  MCNAMEE CLYDE G ,  BANERJEE AMIT ,  SZARKA LASZLO J

Inventor： PATEL RAMESH N ,  MCNAMEE CLYDE G ,  BANERJEE AMIT ,  SZARKA LASZLO J

IPC: C07D319/06 ,  C07D405/06 ,  C12P7/62 ,  C12P17/16 ,  C12R1/01 ,  C12R1/365 ,  C12R1/645 ,  C12R1/78 ,  C12R1/84 ,  C12R1/865 ,  C12P17/06

Abstract: Microorganisms or reductases derived therefrom reduce a diketo ester (see formula I) to form the associated 3-hydroxy, 5-hydroxy, or 3,5-dihydroxy esters. Selected microorganisms produce the preferred stereoisomers (see formula II, III, IV) which can be used to prepare antihypercholesterolemic agents such as (see formula V)

公开(公告)号：CA2127972A1

公开(公告)日：1995-01-15

申请号：CA2127972

申请日：1994-07-13

Applicant: PATEL RAMESH N

Inventor： PATEL RAMESH N

IPC: C07D205/08 ,  C07D405/04 ,  C12P17/04 ,  C12P17/16 ,  C12P41/00 ,  C07D305/14

Abstract: ENZYMATIC PROCESSES FOR THE RESOLUTION OF ENANTIOMERIC MIXTURES OF COMPOUNDS USEFUL AS INTERMEDIATES IN THE PREPARATION OF TAXANES Methods for the enzymatic resolution of mixtures of enantiomers, such as .beta.-lactam compounds, which may be employed as intermediates in the preparation of taxanes bearing a C-13 sidechain containing a heterocyclic or cycloalkyl group, the latter useful in the pharmaceutical field.

公开(公告)号：CA2125726A1

公开(公告)日：1994-12-16

申请号：CA2125726

申请日：1994-06-13

Applicant: HANSON RONALD L ,  PATEL RAMESH N ,  SZARKA LASZLO J

Inventor： HANSON RONALD L ,  PATEL RAMESH N ,  SZARKA LASZLO J

IPC: C12N1/20 ,  C07D305/14 ,  C12N9/14 ,  C12N9/18 ,  C12P17/02 ,  C12Q1/04 ,  C12R1/01 ,  C12Q1/24

Abstract: ENZYMATIC HYDROLYSIS METHODS FOR THE PREPARATION OF C-10 AND C-13 HYDROXYL-BEARING TAXANES, ENZYMATIC ESTERIFICATION METHOD FOR THE PREPARATION OF C-10 ACYLOXY-BEARING TAXANES, AND USE THEREOF IN THE PREPARATION OF C-13 ACYLOXY-BEARING TAXANES An enzymatic hydrolysis method, wherein one or more C-10 acyloxy-bearing taxanes are contacted with an enzyme or microorganism capable of hydrolyzing said acyloxy groups to hydroxyl groups. Also provided is an enzymatic esterification method, wherein one or more C-10 hydroxyl-bearing taxanes are contacted with an acylating agent and an enzyme or microorganism capable of esterifying said hydroxyl groups to form acyloxy groups. Further provided is an enzymatic hydrolysis method, wherein one or more C-13 acyloxy-bearing taxanes are contacted with an enzyme or microorganism capable of hydrolyzing said acyloxy groups to hydroxyl groups. The methods are especially useful for the preparation of compounds which may be employed as intermediates in the preparation of taxanes such as taxol.

公开(公告)号：GB2263848A

公开(公告)日：1993-08-04

申请号：GB9300996

申请日：1993-01-13

Applicant: PATEL RAMESH CHANDRA

Inventor： PATEL RAMESH CHANDRA

IPC: G08B13/24

Abstract: Apparatus for changing the magnetic state of a tag magnetisable material comprises an a.c. voltage source, a rectifier having an input derived from said a.c. voltage source and switch means having an output selectively connectable to either the a.c. voltage source or 10 the d.c. output of the rectifier. An electromagnet connected to the output of the switch means thereby selectively receives either an a.c. supply for demagnetising of the tag or a d.c. supply for magnetising (or remagnetising) of the tag.

公开(公告)号：CA2138674A1

公开(公告)日：1995-07-14

申请号：CA2138674

申请日：1994-12-21

Applicant: HANSON RONALD L ,  PATEL RAMESH N ,  SZARKA LASZLO J

Inventor： HANSON RONALD L ,  PATEL RAMESH N ,  SZARKA LASZLO J

IPC: C12N1/20 ,  C12N9/24 ,  C12P17/02 ,  C12P19/60 ,  C12Q1/02 ,  C12Q1/04 ,  C12Q1/34 ,  C12R1/01 ,  C12R1/07 ,  C12R1/09 ,  C12R1/265 ,  C12Q1/24

Abstract: An enzymatic hydrolysis method, wherein one or more C-7 sugar, preferably C-7 xylosyl-bearing taxanes are contacted with an enzyme or microorganism capable of hydrolyzing said sugar groups to hydroxyl groups.

公开(公告)号：CA2434312A1

公开(公告)日：1993-07-16

申请号：CA2434312

申请日：1993-01-15

Applicant: PATEL RAMESH N ,  PARTYKA RICHARD A ,  SZARKA LASZLO J

Inventor： PATEL RAMESH N ,  PARTYKA RICHARD A ,  SZARKA LASZLO J

IPC: C07D205/08 ,  C07D305/14 ,  C07D493/00 ,  C12P13/00 ,  C12P17/02 ,  C12P17/10 ,  C12P41/00 ,  C12R1/38 ,  C12R1/39 ,  C12R1/645 ,  C12R1/685 ,  C12R1/72 ,  C12R1/845

Abstract: Methods for the enzymatic resolution of mixtures of enantiomers, such as beta -lactam compounds, which may be employed as intermediates in the preparation of taxanes such as taxol, the latter useful in the pharmaceutical field.

公开(公告)号：CA2081069A1

公开(公告)日：1993-04-24

申请号：CA2081069

申请日：1992-10-21

Applicant: PATEL RAMESH N ,  LIU MARK ,  BANERJEE AMIT ,  SZARKA LASZLO J

Inventor： PATEL RAMESH N ,  LIU MARK ,  BANERJEE AMIT ,  SZARKA LASZLO J

IPC: C07D239/42 ,  C12P7/22 ,  C12P17/12 ,  C12P17/16 ,  C12R1/01 ,  C12R1/06 ,  C12R1/365 ,  C12R1/645 ,  C12R1/72 ,  C12R1/78 ,  C12R1/865

Abstract: HA583 STEREOSELECTIVE PREPARATION OF HALOPHENYL ALCOHOLS A process is described for selectively preparing a compound of the formula wherein: R1 is halogen; R2 is halogen, alkyl, cycloalkyl, aryl or ; and R3 is hydrogen, alkyl, cycloalkyl, aryl, or halogen; wherein the process comprises treating the associated ketone with an oxido-reductase or a microorganism comprising an oxidoreductase. Compounds prepared by this process are useful antipsychotic agents or useful intermediates therefor.