公开(公告)号：USRE44186E1

公开(公告)日：2013-04-30

申请号：US13308658

申请日：2011-12-01

Applicant: Jeffrey A. Robl ,  Richard B. Sulsky ,  David J. Augeri ,  David R. Magnin ,  Lawrence G. Hamann ,  David A. Betebenner

Inventor： Jeffrey A. Robl ,  Richard B. Sulsky ,  David J. Augeri ,  David R. Magnin ,  Lawrence G. Hamann ,  David A. Betebenner

IPC: C07D209/02 ,  A61K31/403

CPC classification number: C07C271/22 ,  C07C2603/74 ,  C07D209/52 ,  C07D401/06 ,  C07D403/06

Abstract: Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where x is 0 or 1 and y is 0 or 1 (provided that x=1 when y=0 and x=0 when y=1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.

Abstract translation: 提供二肽基肽酶IV（DP 4）抑制化合物，其具有下式，其中x为0或1，y为0或1（当y = 0时x = 1，y = 1时x = 0）; n为0或1; X是H或CN; 并且其中R 1，R 2，R 3和R 4如本文所述。 还提供了一种用于治疗糖尿病和相关疾病，特别是II型糖尿病和本文所列的其它疾病的方法，其使用这种DP 4抑制剂*或这种DP 4抑制剂与一种或多种其它抗糖尿病药如二甲双胍的组合 ，格列本脲，曲格列酮，吡格列酮，罗格列酮和/或胰岛素和/或降血脂药和/或抗肥胖剂和/或其它治疗剂中的一种或多种。

公开(公告)号：US20100274025A1

公开(公告)日：2010-10-28

申请号：US12712958

申请日：2010-02-25

Applicant: Truc Chi Vu ,  David B. Brzozowski ,  Rita Fox ,  Jollie Duaine Godfrey, JR. ,  Ronald L. Hanson ,  Sergei V. Kolotuchin ,  John A. Mazzullo ,  Ramesh N. Patel ,  Jianji Wang ,  Kwok Wong ,  Jurong Yu ,  Jason J. Zhu ,  David R. Magnin ,  David J. Augeri ,  Lawrence G. Hamann

Inventor： Truc Chi Vu ,  David B. Brzozowski ,  Rita Fox ,  Jollie Duaine Godfrey, JR. ,  Ronald L. Hanson ,  Sergei V. Kolotuchin ,  John A. Mazzullo ,  Ramesh N. Patel ,  Jianji Wang ,  Kwok Wong ,  Jurong Yu ,  Jason J. Zhu ,  David R. Magnin ,  David J. Augeri ,  Lawrence G. Hamann

IPC: C07D209/52 ,  C07D207/22 ,  C07C57/28 ,  C12N1/19 ,  C12N1/21

CPC classification number: C07C69/757 ,  C07C62/06 ,  C07C69/635 ,  C07C69/675 ,  C07C229/28 ,  C07C271/22 ,  C07C2603/74 ,  C07D207/22 ,  C07D209/52

Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

Abstract translation: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。

公开(公告)号：US07420079B2

公开(公告)日：2008-09-02

申请号：US10716012

申请日：2003-11-18

Applicant: Truc Chi Vu ,  David B. Brzozowski ,  Rita Fox ,  Jollie Duaine Godfrey, Jr. ,  Ronald L. Hanson ,  Sergei V. Kolotuchin ,  John A. Mazzullo ,  Ramesh N. Patel ,  Jianji Wang ,  Kwok Wong ,  Jurong Yu ,  Jason J. Zhu ,  David R. Magnin ,  David J. Augeri ,  Lawrence G. Hamann

Inventor： Truc Chi Vu ,  David B. Brzozowski ,  Rita Fox ,  Jollie Duaine Godfrey, Jr. ,  Ronald L. Hanson ,  Sergei V. Kolotuchin ,  John A. Mazzullo ,  Ramesh N. Patel ,  Jianji Wang ,  Kwok Wong ,  Jurong Yu ,  Jason J. Zhu ,  David R. Magnin ,  David J. Augeri ,  Lawrence G. Hamann

IPC: C07C69/52 ,  C07C229/02

CPC classification number: C07C69/757 ,  C07C62/06 ,  C07C69/635 ,  C07C69/675 ,  C07C229/28 ,  C07C271/22 ,  C07C2603/74 ,  C07D207/22 ,  C07D209/52

Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

Abstract translation: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。

公开(公告)号：US06548529B1

公开(公告)日：2003-04-15

申请号：US09519079

申请日：2000-03-06

Applicant: Jeffrey A. Robl ,  Richard B. Sulsky ,  David R. Magnin

Inventor： Jeffrey A. Robl ,  Richard B. Sulsky ,  David R. Magnin

IPC: C07D23110

CPC classification number: C07D207/323 ,  A61K45/06 ,  C07D207/452 ,  C07D231/12 ,  C07D233/64 ,  C07D249/12 ,  C07D263/32 ,  C07D307/42 ,  C07D317/22 ,  C07D333/20 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D413/10

Abstract: aP2 inhibiting compounds are provided having the formula wherein R1, R2, R3, R4, X-Z and are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.

Abstract translation: 提供了具有如下所述的制剂的R1，R2，R3，R4，XZ的化合物的aP2抑制化合物。还提供了用于治疗糖尿病和相关疾病，特别是II型糖尿病的方法，其使用这种P 2抑制剂或这种P 2抑制剂的组合 和另一种抗糖尿病药如二甲双胍，格列本脲，曲格列酮和/或胰岛素。

公开(公告)号：US5712261A

公开(公告)日：1998-01-27

申请号：US493032

申请日：1995-06-21

Applicant: David R. Magnin ,  Scott A. Biller ,  John K. Dickson, Jr. ,  R. Michael Lawrence ,  Richard B. Sulsky

Inventor： David R. Magnin ,  Scott A. Biller ,  John K. Dickson, Jr. ,  R. Michael Lawrence ,  Richard B. Sulsky

IPC: C07F9/40 ,  C07F9/38 ,  A61K31/66

CPC classification number: A61K31/663 ,  C07F9/4025

Abstract: A method is provided for preventing and/or treating hypertriglyceridemia, and/or atherosclerosis and/or pancreatitis resulting from hypertriglyceridemia, employing a squalene synthetase inhibitor.

Abstract translation: 提供了使用角鲨烯合成酶抑制剂来预防和/或治疗高甘油三酯血症和/或由高甘油三酯血症引起的动脉粥样硬化和/或胰腺炎的方法。

公开(公告)号：US5567841A

公开(公告)日：1996-10-22

申请号：US464226

申请日：1995-06-05

Applicant: David R. Magnin ,  Scott A. Biller ,  John K. Dickson, Jr. ,  R. Michael Lawrence ,  Richard B. Sulsky

Inventor： David R. Magnin ,  Scott A. Biller ,  John K. Dickson, Jr. ,  R. Michael Lawrence ,  Richard B. Sulsky

IPC: A61K31/66 ,  A61P3/06 ,  A61P9/10 ,  A61P19/10 ,  C07B53/00 ,  C07F9/30 ,  C07F9/32 ,  C07F9/38 ,  C07F9/40 ,  C07F9/48 ,  C07F9/58 ,  C07F9/59 ,  C07F9/653 ,  C07F9/655 ,  C07F9/6553 ,  C07F9/6584

CPC classification number: C07F9/65848 ,  C07F9/302 ,  C07F9/3808 ,  C07F9/3826 ,  C07F9/383 ,  C07F9/3882 ,  C07F9/4006 ,  C07F9/4015 ,  C07F9/4056 ,  C07F9/4825 ,  C07F9/582 ,  C07F9/591 ,  C07F9/65324 ,  C07F9/65517 ,  C07F9/655345

Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R.sup.4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.

Abstract translation: 提供α-膦酸磺酸盐化合物，其抑制酶角鲨烯合成酶，从而抑制胆固醇生物合成。 这些化合物具有式“IMAGE”，其中R2是OR5或R5a; R3和R5独立地为H，烷基，芳烷基，芳基或环烷基; R5a是H，烷基，芳烷基或芳基; R4是H，烷基，芳基，芳基烷基或环烷基; Z是H，卤素，低级烷基或低级烯基; 并且R 1是含有至少7个碳原子并且是烷基，烯基，炔基，混合烯基 - 炔基，芳基，芳基烷基，环烷基，环烷基烷基，杂芳基，杂芳基烷基，环杂烷基，环杂烷基烷基的亲油基团。 如上面进一步定义的; 包括膦酸（次膦酸）和/或磺酸的药学上可接受的盐和/或前药酯。

公开(公告)号：US4970221A

公开(公告)日：1990-11-13

申请号：US386162

申请日：1989-07-28

Applicant: David R. Magnin ,  Eric M. Gordon

Inventor： David R. Magnin ,  Eric M. Gordon

IPC: C12N9/99 ,  A61K31/425 ,  A61K31/426 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D277/04 ,  C07D277/06 ,  C07D409/06 ,  C07D417/06

CPC classification number: C07D417/06 ,  C07D277/06

Abstract: 3,5-Dihydroxypentanoic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-thiazolidine derivatives and have the structure ##STR1## wherein Z is ##STR2## R.sup.6 is an alkali metal, lower alkyl or H; R.sup.1 and R.sup.2 are the same or different and are H, lower alkyl or aryl;X is S, O, ##STR3## or a single bond; R.sup.7 is lower alkyl; R.sup.3 is lower alkyl or aryl; R.sup.4 and R.sup.5 are the same or different and are H or lower alkyl; and represents a single bond or a double bond, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, novel intermediates for use in preparing the above mevinic acid derivatives are also provided.

公开(公告)号：US08278462B2

公开(公告)日：2012-10-02

申请号：US12712958

申请日：2010-02-25

Applicant: Truc Chi Vu ,  David B. Brzozowski ,  Rita Fox ,  Jollie Duaine Godfrey, Jr. ,  Ronald L. Hanson ,  Sergei V. Kolotuchin ,  John A. Mazzullo ,  Ramesh N. Patel ,  Jianji Wang ,  Kwok Wong ,  Jurong Yu ,  Jason J. Zhu ,  David R. Magnin ,  David J. Augeri ,  Lawrence G. Hamann

Inventor： Truc Chi Vu ,  David B. Brzozowski ,  Rita Fox ,  Jollie Duaine Godfrey, Jr. ,  Ronald L. Hanson ,  Sergei V. Kolotuchin ,  John A. Mazzullo ,  Ramesh N. Patel ,  Jianji Wang ,  Kwok Wong ,  Jurong Yu ,  Jason J. Zhu ,  David R. Magnin ,  David J. Augeri ,  Lawrence G. Hamann

IPC: C07D209/52

CPC classification number: C07C69/757 ,  C07C62/06 ,  C07C69/635 ,  C07C69/675 ,  C07C229/28 ,  C07C271/22 ,  C07C2603/74 ,  C07D207/22 ,  C07D209/52

Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

Abstract translation: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。

公开(公告)号：US6066650A

公开(公告)日：2000-05-23

申请号：US898303

申请日：1997-07-21

Applicant: Scott A. Biller ,  John K. Dickson ,  R. Michael Lawrence ,  David R. Magnin ,  Michael A. Poss ,  Richard B. Sulsky ,  Joseph A. Tino ,  John E. Lawson ,  Henry M. Holava ,  Richard A. Partyka

Inventor： Scott A. Biller ,  John K. Dickson ,  R. Michael Lawrence ,  David R. Magnin ,  Michael A. Poss ,  Richard B. Sulsky ,  Joseph A. Tino ,  John E. Lawson ,  Henry M. Holava ,  Richard A. Partyka

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K31/535 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D211/00 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D211/98 ,  C07D215/38 ,  C07D217/00 ,  C07D217/22 ,  C07D221/16 ,  C07D241/04 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12

CPC classification number: C07D401/04 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12 ,  G01N2800/044

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.

Abstract translation: 提供抑制微粒体甘油三酯转运蛋白的化合物，因此可用于降低血清脂质和治疗动脉粥样硬化及相关疾病。 化合物具有其中R 1至R 7，Q，X和Y如本文所定义的结构。

公开(公告)号：US5712279A

公开(公告)日：1998-01-27

申请号：US548811

申请日：1996-01-11

Applicant: Scott A. Biller ,  John K. Dickson ,  R. Michael Lawrence ,  David R. Magnin ,  Michael A. Poss ,  Jeffrey A. Robl ,  Richard B. Sulsky ,  Joseph A. Tino

Inventor： Scott A. Biller ,  John K. Dickson ,  R. Michael Lawrence ,  David R. Magnin ,  Michael A. Poss ,  Jeffrey A. Robl ,  Richard B. Sulsky ,  Joseph A. Tino

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K31/535 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D211/00 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D211/98 ,  C07D215/38 ,  C07D217/00 ,  C07D217/22 ,  C07D221/16 ,  C07D241/04 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12

CPC classification number: C07D401/04 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12 ,  G01N2800/044

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein Z, X.sup.1, X.sup.2, x and R.sup.5 are as defined herein.

Abstract translation: 提供抑制微粒体甘油三酯转运蛋白的化合物，因此可用于降低血清脂质和治疗动脉粥样硬化及相关疾病。 化合物具有结构，其中Z，X1，X2，X和R5如本文所定义。