公开(公告)号：US5527799A

公开(公告)日：1996-06-18

申请号：US407740

申请日：1995-03-21

Applicant: Joseph P. Vacca ,  Bruce D. Dorsey ,  James P. Guare ,  M. Katharine Holloway ,  Randall W. Hungate ,  Rhonda B. Levin

Inventor： Joseph P. Vacca ,  Bruce D. Dorsey ,  James P. Guare ,  M. Katharine Holloway ,  Randall W. Hungate ,  Rhonda B. Levin

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/47 ,  A61K31/472 ,  A61K31/535 ,  A61K45/06 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07C237/20 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/495

CPC classification number: C07D401/06 ,  A61K31/70 ,  A61K45/06 ,  C07C237/20 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07C2102/08

Abstract: Compounds of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 其中R 1和R 2独立地是氢或任选被取代的C 1-4烷基或芳基，或者R 1和R 2连接在一起形成单环或双环环系的式“IMAGE”的化合物是HIV蛋白酶抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

公开(公告)号：US06306891B1

公开(公告)日：2001-10-23

申请号：US09323519

申请日：1999-06-01

Applicant: Harold G. Selnick ,  Melissa Egbertson ,  Daria Jean Hazuda ,  James P. Guare, Jr. ,  John S. Wai ,  Steven D. Young ,  David L. Clark ,  Julio C. Medina

Inventor： Harold G. Selnick ,  Melissa Egbertson ,  Daria Jean Hazuda ,  James P. Guare, Jr. ,  John S. Wai ,  Steven D. Young ,  David L. Clark ,  Julio C. Medina

IPC: A61K3140

CPC classification number: A61K45/06 ,  A61K31/40 ,  A61K31/445 ,  A61K2300/00

Abstract: Nitrogen-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 含氮杂芳基二氧代丁酸衍生物被描述为HIV整合酶的抑制剂和HIV复制抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

公开(公告)号：US06380249B1

公开(公告)日：2002-04-30

申请号：US09323417

申请日：1999-06-01

Applicant: Steven D. Young ,  Melissa Egbertson ,  Linda S. Payne ,  John S. Wai ,  Thorsten E. Fisher ,  James P. Guare, Jr. ,  Mark W. Embrey ,  Lekhanh Tran ,  Linghang Zhuang ,  Joseph P. Vacca ,  H. Marie Langford ,  Jeffrey Melamed ,  Juan C. Jaen ,  David L. Clark ,  Julio C. Medina

Inventor： Steven D. Young ,  Melissa Egbertson ,  Linda S. Payne ,  John S. Wai ,  Thorsten E. Fisher ,  James P. Guare, Jr. ,  Mark W. Embrey ,  Lekhanh Tran ,  Linghang Zhuang ,  Joseph P. Vacca ,  H. Marie Langford ,  Jeffrey Melamed ,  Juan C. Jaen ,  David L. Clark ,  Julio C. Medina

IPC: A61K31215

CPC classification number: C07D213/64 ,  C07C59/84 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C07C69/738 ,  C07C217/60 ,  C07C229/34 ,  C07C229/42 ,  C07C233/63 ,  C07C235/60 ,  C07C255/41 ,  C07C271/16 ,  C07C271/28 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2602/08 ,  C07C2602/10 ,  C07D209/12 ,  C07D241/12 ,  C07D253/08 ,  C07D263/58 ,  C07D295/088 ,  C07D295/155 ,  C07D295/192 ,  C07D333/22

Abstract: Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 某些六元芳族和杂芳族二氧代丁酸衍生物被描述为HIV整合酶的抑制剂和HIV复制的抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

公开(公告)号：US4686226A

公开(公告)日：1987-08-11

申请号：US771927

申请日：1985-09-03

Applicant: Joel R. Huff ,  John J. Baldwin ,  Yojiro Sakurai ,  Joseph P. Vacca ,  James P. Guare, Jr.

Inventor： Joel R. Huff ,  John J. Baldwin ,  Yojiro Sakurai ,  Joseph P. Vacca ,  James P. Guare, Jr.

IPC: A61K31/435 ,  A61P1/00 ,  A61P3/04 ,  A61P3/08 ,  A61P7/02 ,  A61P9/12 ,  A61P25/02 ,  A61P25/24 ,  A61P25/26 ,  C07D455/06 ,  C07D471/14 ,  C07D491/14 ,  C07D491/147 ,  C07D495/14 ,  A61K31/38

CPC classification number: C07D471/14 ,  C07D455/06 ,  C07D491/14 ,  C07D495/14

Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.

Abstract translation: 取代的六氢芳基喹啉及其药学上可接受的盐是选择性α2-肾上腺素能受体拮抗剂，从而可用作抗抑郁药，抗高血压药，眼用抗高血压药，抗糖尿病药，抗肥胖药和血小板聚集抑制剂和胃肠运动性调节剂。

公开(公告)号：US5717097A

公开(公告)日：1998-02-10

申请号：US759203

申请日：1996-12-04

Applicant: Joseph P. Vacca ,  Bruce D. Dorsey ,  James P. Guare ,  M. Katharine Holloway ,  Randall W. Hungate ,  Rhonda B. Levin ,  Joel R. Huff

Inventor： Joseph P. Vacca ,  Bruce D. Dorsey ,  James P. Guare ,  M. Katharine Holloway ,  Randall W. Hungate ,  Rhonda B. Levin ,  Joel R. Huff

IPC: A61K45/06 ,  C07C237/20 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D495/04 ,  C07F7/18

CPC classification number: C07D495/04 ,  A61K31/70 ,  A61K45/06 ,  C07C237/20 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07F7/1856 ,  C07C2102/08

Abstract: Compounds of formula ##STR1## where A is usually carbonyl or --CH.sub.2 --, D is usually --CH.sub.2 --; R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 其中A通常为羰基或-CH 2 - ，D通常为-CH 2 - ; R1和R2独立地是氢或任选取代的C 1-4烷基或芳基，或者R 1和R 2连接在一起以形成单环或双环环系，是HIV蛋白酶抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

公开(公告)号：US5668132A

公开(公告)日：1997-09-16

申请号：US641720

申请日：1996-05-02

Applicant: Joseph P. Vacca ,  Bruce D. Dorsey ,  James P. Guare ,  M. Katharine Holloway ,  Randall W. Hungate ,  Rhonda B. Levin

Inventor： Joseph P. Vacca ,  Bruce D. Dorsey ,  James P. Guare ,  M. Katharine Holloway ,  Randall W. Hungate ,  Rhonda B. Levin

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/47 ,  A61K31/472 ,  A61K31/535 ,  A61K45/06 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07C237/20 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/44

CPC classification number: C07D401/06 ,  A61K31/70 ,  A61K45/06 ,  C07C237/20 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07C2102/08

Abstract: Compounds of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, and R.sup.1 also forms a heterocycle or heterocycle-C.sub.1-4 alkyl, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 其中R 1和R 2独立地为氢或任选取代的C 1-4烷基或芳基，R 1还形成杂环或杂环C 1-4烷基的式（I）的化合物是HIV蛋白酶抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

公开(公告)号：US5413999A

公开(公告)日：1995-05-09

申请号：US059038

申请日：1993-05-07

Applicant: Joseph P. Vacca ,  Bruce D. Dorsey ,  James P. Guare ,  M. Katharine Holloway ,  Randall W. Hungate ,  Rhonda B. Levin

Inventor： Joseph P. Vacca ,  Bruce D. Dorsey ,  James P. Guare ,  M. Katharine Holloway ,  Randall W. Hungate ,  Rhonda B. Levin

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/47 ,  A61K31/472 ,  A61K31/535 ,  A61K45/06 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07C237/20 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/495 ,  C07D241/02

CPC classification number: C07D401/06 ,  A61K31/70 ,  A61K45/06 ,  C07C237/20 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07C2102/08

Abstract: Compounds of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of treating infection by HIV are also described.

Abstract translation: 其中R 1和R 2独立地是氢或任选被取代的C 1-4烷基或芳基，或者R 1和R 2连接在一起形成单环或双环环系的式“IMAGE”的化合物是HIV蛋白酶抑制剂。 这些化合物可用于治疗HIV的感染和治疗AIDS，无论是作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗AIDS的方法和治疗HIV感染的方法。

公开(公告)号：US4710504A

公开(公告)日：1987-12-01

申请号：US848262

申请日：1986-04-04

Applicant: John J. Baldwin ,  Joel R. Huff ,  Joseph P. Vacca ,  Steven D. Young ,  Jane deSolms ,  James P. Guare, Jr.

Inventor： John J. Baldwin ,  Joel R. Huff ,  Joseph P. Vacca ,  Steven D. Young ,  Jane deSolms ,  James P. Guare, Jr.

IPC: C07D471/20 ,  C07D491/22 ,  C07D495/22 ,  C07D498/22 ,  C07D513/22 ,  A61K31/415 ,  A61K31/305 ,  C07D455/00

CPC classification number: C07D471/20 ,  C07D491/22 ,  C07D495/22 ,  C07D498/22 ,  C07D513/22

Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.

Abstract translation: 取代的六氢芳基喹啉及其药学上可接受的盐是选择性α2-肾上腺素能受体拮抗剂，因此可用作抗抑郁药，抗高血压药，眼用抗高血压药，抗糖尿病药，血小板聚集抑制剂，抗肥胖剂和消化道运动性改良剂。

公开(公告)号：US20110224447A1

公开(公告)日：2011-09-15

申请号：US13059491

申请日：2009-08-11

Applicant: Keith A. Bowman ,  James P. Guare, JR. ,  George D. Hartman ,  Rubina G. Parmar ,  Chandra Vargeese ,  Weimin Wang ,  Ye Zhang

Inventor： Keith A. Bowman ,  James P. Guare, JR. ,  George D. Hartman ,  Rubina G. Parmar ,  Chandra Vargeese ,  Weimin Wang ,  Ye Zhang

IPC: C07J9/00 ,  A61K31/713 ,  A61P1/16

CPC classification number: A61K9/5123 ,  A61K9/1272 ,  A61K9/1277 ,  A61K9/5192 ,  A61K47/28 ,  C07C217/42

Abstract: The instant invention provides for novel lipid nanoparticles and novel lipid nanoparticle components (specifically cationic lipids) that are useful for the delivery of nucleic acids, specifically siRNA, for therapeutic purposes.

Abstract translation: 本发明提供新颖的脂质纳米颗粒和新颖的脂质纳米颗粒组分（特别是阳离子脂质），其可用于递送核酸，特别是用于治疗目的的siRNA。

公开(公告)号：US06921759B2

公开(公告)日：2005-07-26

申请号：US09973853

申请日：2001-10-10

Applicant: Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Melissa Egbertson ,  John S. Wai ,  Linghang Zhuang ,  Mark Embrey ,  Jeffrey Y. Melamed ,  H. Marie Langford ,  James P. Guare ,  Thorsten E. Fisher ,  Samson M. Jolly ,  Michelle S. Kuo ,  Debra S. Perlow ,  Jennifer J. Bennett ,  Timothy W. Funk

Inventor： Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Melissa Egbertson ,  John S. Wai ,  Linghang Zhuang ,  Mark Embrey ,  Jeffrey Y. Melamed ,  H. Marie Langford ,  James P. Guare ,  Thorsten E. Fisher ,  Samson M. Jolly ,  Michelle S. Kuo ,  Debra S. Perlow ,  Jennifer J. Bennett ,  Timothy W. Funk

IPC: A61K31/4375 ,  A61K31/47 ,  A61K31/4985 ,  A61K31/541 ,  A61K31/554 ,  A61P31/12 ,  A61P31/18 ,  C07D20060101 ,  C07D215/48 ,  C07D221/00 ,  C07D241/00 ,  C07D471/00 ,  C07D471/04 ,  C07D471/16 ,  C07D487/00 ,  C07D519/00 ,  A61P31/00 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 描述了包括某些喹啉羧酰胺和萘啶甲酰胺衍生物的氮杂和多氮萘基甲酰胺衍生物。 这些化合物是HIV整合酶和HIV复制抑制剂的抑制剂，并且可用于预防或治疗HIV感染和治疗AIDS，作为化合物或药学上可接受的盐，或作为药物组合物中的成分，任选地与其它组合 抗病毒药，免疫调节剂，抗生素或疫苗。 还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。