公开(公告)号：US4675332A

公开(公告)日：1987-06-23

申请号：US788111

申请日：1985-10-21

Applicant: David T. Connor ,  Paul C. Unangst ,  S. Russell Stabler

Inventor： David T. Connor ,  Paul C. Unangst ,  S. Russell Stabler

IPC: A61K31/41 ,  A61P9/00 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D209/42 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D491/056

CPC classification number: C07D403/04 ,  C07D209/42 ,  C07D403/12

Abstract: Novel acidic indole compounds having use as antiallergic agents, methods of synthesis, compositions, and uses are claimed.

Abstract translation: 用作抗变应性剂的新型酸性吲哚化合物，合成方法，组合物和用途被要求保护。

公开(公告)号：US5208250A

公开(公告)日：1993-05-04

申请号：US702132

申请日：1991-05-13

Applicant: Wiaczeslaw A. Cetenko ,  David T. Connor ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Stephen S. Stabler

Inventor： Wiaczeslaw A. Cetenko ,  David T. Connor ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Stephen S. Stabler

IPC: A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  C07D233/78 ,  C07D233/86 ,  C07D233/96 ,  C07D263/44 ,  C07D263/46 ,  C07D277/20 ,  C07D277/34 ,  C07D417/06

CPC classification number: C07D263/44 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  C07D233/78 ,  C07D233/86 ,  C07D233/96 ,  C07D263/46 ,  C07D277/20 ,  C07D417/06

Abstract: The present invention is for selected novel compounds, as well as, pharmaceutical compositions and methods of use for known and the selected novel compounds both of the formula ##STR1## having activity useful for treating allergies and inflammation.

Abstract translation: 本发明涉及选择的新化合物，以及用于已知和所选新型化合物的药物组合物和方法，其具有可用于治疗过敏和炎症的活性。

公开(公告)号：US4868205A

公开(公告)日：1989-09-19

申请号：US167272

申请日：1988-03-11

Applicant: Mary E. Carethers ,  Wiaczeslaw A. Cetenko ,  David T. Connor ,  Elizabeth A. Johnson ,  John S. Kiely ,  Charles F. Schwender ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Robert F. Bruns

Inventor： Mary E. Carethers ,  Wiaczeslaw A. Cetenko ,  David T. Connor ,  Elizabeth A. Johnson ,  John S. Kiely ,  Charles F. Schwender ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Robert F. Bruns

IPC: C07D209/36 ,  C07D209/42 ,  C07D279/02 ,  C07D307/83 ,  C07D307/84 ,  C07D307/92 ,  C07D311/22 ,  C07D311/24 ,  C07D333/64 ,  C07D333/68 ,  C07D335/06 ,  C07D491/04

CPC classification number: C07D307/92 ,  C07D209/36 ,  C07D209/42 ,  C07D279/02 ,  C07D307/83 ,  C07D307/84 ,  C07D311/22 ,  C07D311/24 ,  C07D333/64 ,  C07D333/68 ,  C07D335/06 ,  C07D491/04

Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.

公开(公告)号：US4868199A

公开(公告)日：1989-09-19

申请号：US167264

申请日：1988-03-09

Applicant: Mary E. Carethers ,  Wiaczeslaw A. Cetenko ,  David T. Connor ,  Elizabeth A. Johnson ,  John S. Kiely ,  Charles F. Schwender ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Robert F. Bruns

Inventor： Mary E. Carethers ,  Wiaczeslaw A. Cetenko ,  David T. Connor ,  Elizabeth A. Johnson ,  John S. Kiely ,  Charles F. Schwender ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Robert F. Bruns

IPC: C07D209/36 ,  C07D209/42 ,  C07D279/02 ,  C07D307/83 ,  C07D307/84 ,  C07D307/92 ,  C07D311/22 ,  C07D311/24 ,  C07D333/64 ,  C07D333/68 ,  C07D335/06 ,  C07D491/04 ,  C07D491/048

CPC classification number: C07D307/92 ,  C07D209/36 ,  C07D209/42 ,  C07D279/02 ,  C07D307/83 ,  C07D307/84 ,  C07D311/22 ,  C07D311/24 ,  C07D333/64 ,  C07D333/68 ,  C07D335/06 ,  C07D491/04

Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.

公开(公告)号：US4761424A

公开(公告)日：1988-08-02

申请号：US782623

申请日：1985-10-01

Applicant: Mary E. Carethers ,  Wiaczeslaw A. Cetenko ,  David T. Connor ,  Elizabeth A. Johnson ,  John S. Kiely ,  Charles F. Schwender ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Robert F. Bruns

Inventor： Mary E. Carethers ,  Wiaczeslaw A. Cetenko ,  David T. Connor ,  Elizabeth A. Johnson ,  John S. Kiely ,  Charles F. Schwender ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Robert F. Bruns

IPC: C07D491/048 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/38 ,  A61K31/381 ,  A61K31/382 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/54 ,  A61P9/00 ,  A61P11/00 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D209/12 ,  C07D209/36 ,  C07D209/42 ,  C07D279/02 ,  C07D307/68 ,  C07D307/83 ,  C07D307/84 ,  C07D307/92 ,  C07D311/22 ,  C07D311/24 ,  C07D333/60 ,  C07D333/64 ,  C07D333/68 ,  C07D333/70 ,  C07D335/06 ,  C07D491/04

CPC classification number: C07D307/92 ,  C07D209/36 ,  C07D209/42 ,  C07D279/02 ,  C07D307/83 ,  C07D307/84 ,  C07D311/22 ,  C07D311/24 ,  C07D333/64 ,  C07D333/68 ,  C07D335/06 ,  C07D491/04

Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.

Abstract translation: 本发明涉及新型烯醇酰胺型化合物，药物组合物及其使用方法，其可用于治疗其中脂肪氧合酶活性产物或白细胞三烯作用有助于病理状况的疾病。

公开(公告)号：US5565446A

公开(公告)日：1996-10-15

申请号：US444975

申请日：1995-05-19

Applicant: Diane H. Boschelli ,  David T. Connor ,  James B. Kramer ,  Paul C. Unangst

Inventor： Diane H. Boschelli ,  David T. Connor ,  James B. Kramer ,  Paul C. Unangst

IPC: C07D487/04 ,  A61K31/34 ,  A61K31/38 ,  A61K31/40 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  A61P29/00 ,  A61P31/12 ,  A61P37/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D495/04 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  C07D513/04

Abstract: Benzothiophene, benzofuran and indolethiazepinones, oxazepinones and diazepinones as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases; these compounds also inhibit the activation of human immunodeficiency virus (HIV).

Abstract translation: 苯并噻吩，苯并呋喃和吲哚噻嗪酮，氧氮杂酮和二氮杂酮及其制备方法被描述为抑制白细胞粘附于血管内皮的药剂，因此是用于治疗炎性疾病的有效治疗剂; 这些化合物也抑制人体免疫缺陷病毒（HIV）的活化。

公开(公告)号：US5489586A

公开(公告)日：1996-02-06

申请号：US351611

申请日：1994-12-12

Applicant: Diane H. Boschelli ,  David T. Connor ,  James B. Kramer ,  Paul C. Unangst

Inventor： Diane H. Boschelli ,  David T. Connor ,  James B. Kramer ,  Paul C. Unangst

IPC: C07D487/04 ,  A61K31/34 ,  A61K31/38 ,  A61K31/40 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  A61P29/00 ,  A61P31/12 ,  A61P37/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D495/04 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  C07D513/04

Abstract: Benzothiophene, benzofuran and indole-thiazepinones, oxazepinones and diazepinones as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases.

Abstract translation: 苯并噻吩，苯并呋喃和吲哚 - 硫氮酮，氧氮杂酮和二氮杂酮及其制备方法被描述为抑制白细胞粘附于血管内皮的试剂，因此是用于治疗炎性疾病的有效治疗剂。

公开(公告)号：US5312821A

公开(公告)日：1994-05-17

申请号：US54382

申请日：1993-04-28

Applicant: David T. Connor ,  Catherine R. Kostlan ,  Paul C. Unangst

Inventor： David T. Connor ,  Catherine R. Kostlan ,  Paul C. Unangst

IPC: A61K31/505 ,  A61K31/506 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  A61K31/52

CPC classification number: C07D403/04 ,  C07D413/04 ,  C07D417/04

Abstract: The present invention is novel compounds which are 2-heterocyclic-4,6-ditertiarybutyl-5-hydroxy-1,3-pyrimidines, where heterocyclic is selected from imidazole, thiazole, and oxazole, and pharmaceutically acceptable additional salts, bases, and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of, for example, inflammation.

Abstract translation: 本发明是2-杂环-4,6-二叔丁基-5-羟基-1,3-嘧啶的新化合物，其中杂环选自咪唑，噻唑和恶唑，以及其药学上可接受的另外的盐，碱和碱 其盐，药物组合物及其使用方法。 发现本发明化合物具有作为5-脂氧合酶和/或环加氧酶的抑制剂的活性，其提供例如炎症的治疗。

公开(公告)号：US5306822A

公开(公告)日：1994-04-26

申请号：US988562

申请日：1992-12-10

Applicant: Wiaczeslaw A. Cetenko ,  David T. Connor ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Stephen R. Stabler

Inventor： Wiaczeslaw A. Cetenko ,  David T. Connor ,  Roderick J. Sorenson ,  Paul C. Unangst ,  Stephen R. Stabler

IPC: A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  C07D233/78 ,  C07D233/86 ,  C07D233/96 ,  C07D263/44 ,  C07D263/46 ,  C07D277/20 ,  C07D277/34 ,  C07D417/06

CPC classification number: C07D263/44 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  C07D233/78 ,  C07D233/86 ,  C07D233/96 ,  C07D263/46 ,  C07D277/20 ,  C07D417/06

Abstract: The present invention is for selected novel compounds, as well as, pharmaceutical compositions and methods of use for known and the selected novel compounds both of the formula ##STR1## having activity useful for treating allergies and inflammation.

Abstract translation: 本发明用于选择的新化合物，以及用于已知和所选新型化合物的药物组合物和方法，其具有可用于治疗过敏和炎症的活性的式（*化学结构*）。

公开(公告)号：US5290800A

公开(公告)日：1994-03-01

申请号：US896299

申请日：1992-06-10

Applicant: Wiaczeslaw A. Cetenko ,  David T. Connor ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst

Inventor： Wiaczeslaw A. Cetenko ,  David T. Connor ,  Jagadish C. Sircar ,  Roderick J. Sorenson ,  Paul C. Unangst

IPC: A61K31/415 ,  A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61K31/426 ,  A61P29/00 ,  C07D233/96 ,  C07D263/40 ,  C07D263/46 ,  C07D263/48 ,  C07D277/20 ,  C07D277/34 ,  C07D277/36 ,  C07D277/48 ,  C07D277/50 ,  C07D277/54 ,  C07D203/40

CPC classification number: C07D277/20 ,  C07D233/96 ,  C07D263/46 ,  C07D263/48

Abstract: The novel 3,5-ditertiarybutyl-4-hydroxy-phenylmethylene derivative of 2-substituted thiazolidinones, oxazolidinones, and imidazolidinones as antiinflammatory agents having inhibiting activity for 5-lipoxygenase, cyclooxygenase, or both.

Abstract translation: 2-取代的噻唑烷酮，恶唑烷酮和咪唑啉酮的3,5-二叔丁基-4-羟基 - 苯基亚甲基衍生物作为具有5-脂氧合酶抑制活性，环氧合酶或两者的抗炎剂。