公开(公告)号：US06197976B1

公开(公告)日：2001-03-06

申请号：US09460526

申请日：1999-12-13

Applicant: Peter J. Harrington ,  Hiralal N. Khatri ,  George C. Schloemer

Inventor： Peter J. Harrington ,  Hiralal N. Khatri ,  George C. Schloemer

IPC: C07D20952

CPC classification number: C07D487/04

Abstract: 5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxamides of the formula where R1 is alkyl and R2 is optionally substituted phenyl, and the method for their preparation and their conversion to ketorolac and its pharmaceutically acceptable salts.

Abstract translation: 式R 1的5-苯甲酰基-2,3-二氢-1H-吡咯嗪-1-甲酰胺是烷基，R 2是任选取代的苯基，及其制备方法及其转化为酮咯酸及其药学上可接受的盐。

公开(公告)号：US06482957B2

公开(公告)日：2002-11-19

申请号：US10131244

申请日：2002-04-25

Applicant: Nobuya Katagiri ,  Chikara Kaneko ,  Junko Sato ,  Masahiro Torihara ,  Koichi Kanehira ,  Yoshin Tamai

Inventor： Nobuya Katagiri ,  Chikara Kaneko ,  Junko Sato ,  Masahiro Torihara ,  Koichi Kanehira ,  Yoshin Tamai

IPC: C07D20952

CPC classification number: C07F9/65616 ,  C07D209/52 ,  C07D473/40 ,  C07F9/5728

Abstract: A cyclopentenecarboxamide derivative represented by the formula (I): and a method for preparing the cyclopentencarboxamide derivative. A bicycloamide derivative represented by the formula (II): and a method for preparing the bicycloamide derivative.

Abstract translation: 由式（I）表示的环戊烯甲酰胺衍生物及其制备环戊烷羧酰胺衍生物的方法。 由式（II）表示的双环酰胺衍生物及其制备双环酰胺衍生物的方法。

公开(公告)号：US06313312B1

公开(公告)日：2001-11-06

申请号：US09467871

申请日：1999-12-20

Applicant: Bernard Joseph Banks ,  Robert James Crook ,  Stephen Paul Gibson ,  Graham Lunn ,  Alan John Pettman

Inventor： Bernard Joseph Banks ,  Robert James Crook ,  Stephen Paul Gibson ,  Graham Lunn ,  Alan John Pettman

IPC: C07D20952

CPC classification number: C07D401/04 ,  C07D209/52 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/06 ,  C07D409/06 ,  C07D409/10 ,  C07D413/12 ,  C07D417/06

Abstract: Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.

Abstract translation: 公开了其中取代基如本文所定义的式（I）化合物及其盐和前药，其用作阿片剂结合剂，其用于治疗阿片剂介导的病症。 还描述了制备这些物质的方法。

公开(公告)号：US06232473B1

公开(公告)日：2001-05-15

申请号：US09562129

申请日：2000-05-01

Applicant: Takashi Fukumoto ,  Rensuke Ikarashi

Inventor： Takashi Fukumoto ,  Rensuke Ikarashi

IPC: C07D20952

CPC classification number: C07D209/52

Abstract: 2-Azabicyclo[2.2.1]hept-5-en-3-one is prepared by a process comprising: continuously mixing a substituted sulfonyl cyanide represented by formula (I): R—SO2CN  (I), wherein R represents an alkyl group or a phenyl group or a substituted phenyl group, with cyclopentadiene; and then continuously adding the resultant reaction solution to water or to a mixed solvent comprising water and a hydrocarbon solvent under the condition that the pH of the present reaction mixture ranges from 4 to 7.

Abstract translation: 2-氮杂双环[2.2.1]庚-5-烯-3-酮的制备方法包括：连续混合由式（I）表示的取代磺酰氰：其中R表示烷基或苯基或取代的 苯基，与环戊二烯; 然后在本反应混合物的pH为4〜7的条件下，将得到的反应溶液连续加入到水或包含水和烃溶剂的混合溶剂中。

公开(公告)号：US06559319B2

公开(公告)日：2003-05-06

申请号：US10233809

申请日：2002-09-03

Applicant: Douglas C. Caskey ,  John R. Duchek ,  Henry J. Buehler

Inventor： Douglas C. Caskey ,  John R. Duchek ,  Henry J. Buehler

IPC: C07D20952

CPC classification number: C07D207/337 ,  C07D487/04

Abstract: A multi-step method of synthesizing ketorolac, an analgesic compound, is shown. Several of the reactions and intermediate compounds are novel. The reaction sequence begins with the known compound N-2-bromoethylpyrrole.

公开(公告)号：US06328855B1

公开(公告)日：2001-12-11

申请号：US09807218

申请日：2001-04-11

Applicant: Norbert Bischof ,  Ernst Buschmann ,  Michael Henningsen ,  Georg Arnold Krei ,  Rainer Munschauer ,  Thomas Pfeiffer ,  Gerd Steiner ,  Wolfgang Viergutz

Inventor： Norbert Bischof ,  Ernst Buschmann ,  Michael Henningsen ,  Georg Arnold Krei ,  Rainer Munschauer ,  Thomas Pfeiffer ,  Gerd Steiner ,  Wolfgang Viergutz

IPC: C07D20952

CPC classification number: C07D209/52

Abstract: A process for preparing (+)-exo-6-phenyl-3-azabicyclo[3.2.0]heptanes of the formula I where R is hydrogen, chlorine, bromine, fluorine or methoxy, which comprises photocyclizing a bisallylammonium salt of the formula II where R has the meanings given above and X− is an anion, in an inert solvent in a glass apparatus with addition of sensitizer and precipitating using (−)-ditoluoyltartaric acid the desired (+)-exo-isomer I as ditoluoyltartrate from the resulting mixture, with or without recrystallization of this tartrate from an alcohol/water mixture.

Abstract translation: 制备式I的（+） - 外-6-苯基-3-氮杂双环[3.2.0]庚烷的方法，其中R是氢，氯，溴，氟或甲氧基，其包括将式II的双烯丙基铵盐光环化，其中R 具有上述含义，X-是阴离子，在玻璃装置的惰性溶剂中，加入敏化剂并使用（ - ） - 二甲酰基酒石酸从所得混合物中将所需的（+） - 外异构体I作为二异氰酸甲酯酒石酸盐沉淀， 有或没有酒石酸盐与酒精/水混合物重结晶。

公开(公告)号：US06310216B1

公开(公告)日：2001-10-30

申请号：US09463867

申请日：2000-02-18

Applicant: Elmar Vilsmaier ,  Torsten Goerz ,  Gunther Milch ,  Uwe Petersen ,  Axel Dalhoff ,  Gabriele Schmuck

Inventor： Elmar Vilsmaier ,  Torsten Goerz ,  Gunther Milch ,  Uwe Petersen ,  Axel Dalhoff ,  Gabriele Schmuck

IPC: C07D20952

CPC classification number: C07D471/14 ,  C07D209/52 ,  Y02P20/55

Abstract: 6-Amino-3-azabicyclo[3.1.0]hexanes of the formula wherein R1 and R2 independently of one another are C3-C4-alkenyl or Ar—CH(R′)— where R′ is hydrogen or C1-C4-alkyl and Ar is an optionally substituted C6-C10-aryl and R3 is hydrogen, C3-C4-alkenyl, Ar—CH(R′)— where R′ is hydrogen or C1-C4-alkyl and Ar is an optionally substituted C6-C10-aryl or COOR4 where R4 is C1-C4-alkyl or C2-C4-alkenyl. The invention also relates to a method for making these compounds and a method for using them.

Abstract translation: 式R 1和R 2彼此独立的6-氨基-3-氮杂双环[3.1.0]己烷是C 3 -C 4 - 烯基或Ar-CH（R'） - ，其中R'是氢或C 1 -C 4烷基， Ar是任选取代的C 6 -C 10 - 芳基，R 3是氢，C 3 -C 4 - 烯基，Ar-CH（R'） - ，其中R'是氢或C 1 -C 4烷基，Ar是任选取代的C 6 -C 10 - 芳基或COOR 4，其中R 4是C 1 -C 4 - 烷基或C 2 -C 4 - 烯基。 本发明还涉及一种制备这些化合物的方法及其使用方法。

公开(公告)号：US06417371B1

公开(公告)日：2002-07-09

申请号：US09769742

申请日：2001-01-26

Applicant: Thomas Kammermeier ,  Stefan Laufer ,  Philipp Merckle ,  Hans-Guenter Striegel

Inventor： Thomas Kammermeier ,  Stefan Laufer ,  Philipp Merckle ,  Hans-Guenter Striegel

IPC: C07D20952

CPC classification number: C07D487/04

Abstract: The present invention relates to a process process for the preparation of the compound of the formula I where the compound of the formula III is reacted with oxalyl chloride and the product obtained is treated with hydrazine and an alkali metal hydroxide in the aqueous phase at elevated temperature, after treatment is complete a three-phase system is produced by addition of an ether and the compound of the formula I is obtained by acidifying the middle phase. The invention moreover relates to a polymorph of the compound of the formula I.

Abstract translation: 本发明涉及制备式I化合物的方法，其中式III的化合物与草酰氯反应，所得产物在水相中在水相中经肼和碱金属氢氧化物处理 处理完成，通过加入醚产生三相体系，通过酸化中间相获得式I化合物。本发明还涉及式I化合物的多晶型物。

公开(公告)号：US06407262B1

公开(公告)日：2002-06-18

申请号：US09990278

申请日：2001-11-23

Applicant: Zhi-Xian Wang ,  Cameron McPhail

Inventor： Zhi-Xian Wang ,  Cameron McPhail

IPC: C07D20952

CPC classification number: C07D209/52

Abstract: A process for separating diastereomeric mixtures of compounds of formula 1 and formula 2 wherein R1=H or R1 denotes a carboxyl-esterifying group selected from C1-C6 alkyl and C7-C8 aralkyl, by treating the mixture of 1 and 2 with a solvent or mixture of solvents to obtain a substantially pure compound of formula 1.

Abstract translation: 通过用溶剂或混合物处理1和2的混合物，分离式1和式2化合物的非对映体混合物的方法，其中R 1 = H或R 1表示选自C 1 -C 6烷基和C 7 -C 8芳烷基的羧基酯化基团 的溶剂以获得基本上纯的式1化合物。

公开(公告)号：US06407244B1

公开(公告)日：2002-06-18

申请号：US09491712

申请日：2000-01-26

Applicant: Madiraju S. R. Murthy ,  Nancy A. E. Steenaart ,  Roy A. Johnson ,  Gordon C. Shore

Inventor： Madiraju S. R. Murthy ,  Nancy A. E. Steenaart ,  Roy A. Johnson ,  Gordon C. Shore

IPC: C07D20952

CPC classification number: C07D403/14 ,  C07D207/44

Abstract: The present invention relates to novel Pyrrole-Type compounds, compositions comprising Pyrrole-Type compounds, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a composition comprising a Pyrrole-Type compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing a viral infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the replication and/or infectivity of a virus.

Abstract translation: 本发明涉及新颖的吡咯型化合物，包含吡咯型化合物的组合物和可用于治疗或预防癌症或肿瘤性疾病的方法，其包括施用包含吡咯型化合物的组合物。 本发明的化合物，组合物和方法也可用于抑制癌细胞或肿瘤细胞的生长。 本发明还涉及用于治疗或预防病毒感染的新型吡咯型化合物，组合物和方法。 本发明的化合物，组合物和方法也可用于抑制病毒的复制和/或感染性。