公开(公告)号：US20130317035A1

公开(公告)日：2013-11-28

申请号：US13950853

申请日：2013-07-25

Applicant: Roland E. Dolle ,  Bertrand Le Bourdonnec ,  Allan James Goodman

Inventor： Roland E. Dolle ,  Bertrand Le Bourdonnec ,  Allan James Goodman

IPC: A61K31/4985 ,  A61K31/198 ,  C07D471/04

CPC classification number: A61K31/4985 ,  A61K31/198 ,  C07D471/04

Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.

公开(公告)号：US20120231543A1

公开(公告)日：2012-09-13

申请号：US13479622

申请日：2012-05-24

Applicant: Roland E. Dolle ,  Bertrand Le Bourdonnec ,  Allan James Goodman

Inventor： Roland E. Dolle ,  Bertrand Le Bourdonnec ,  Allan James Goodman

IPC: C07D471/04 ,  C12N5/071

CPC classification number: A61K31/4985 ,  A61K31/198 ,  C07D471/04

Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.

Abstract translation: 公开了某些喹嗪基和八氢吡啶并吡嗪化合物，药物组合物及其用途的方法，尤其是作为阿片受体拮抗剂。

公开(公告)号：US20100196269A1

公开(公告)日：2010-08-05

申请号：US12509549

申请日：2009-07-27

Applicant: Roland E. Dolle ,  Bertrand Le Bourdonnec ,  Guo-Hua Chu

Inventor： Roland E. Dolle ,  Bertrand Le Bourdonnec ,  Guo-Hua Chu

IPC: A61K31/55 ,  C07D405/04 ,  A61K31/438 ,  C07D221/20 ,  A61K31/5377 ,  A61K51/04 ,  A61P1/02 ,  A61P25/00 ,  A61P29/00

CPC classification number: C07D491/107 ,  C07D487/10

Abstract: Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ-opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ-opioid receptor-mediated diseases, disorders, and/or conditions.

Abstract translation: 公开了螺环杂环衍生物，含有这些化合物的药物组合物及其制药方法。 在某些实施方案中，螺环杂环衍生物是δ-阿片受体受体的配体，尤其可用于治疗和/或预防疼痛，焦虑，胃肠道疾病和其他δ-阿片受体介导的疾病，病症和 /或条件。

公开(公告)号：US20100173927A1

公开(公告)日：2010-07-08

申请号：US12750558

申请日：2010-03-30

Applicant: Bertrand Le Bourdonnec ,  Roland E. Dolle

Inventor： Bertrand Le Bourdonnec ,  Roland E. Dolle

IPC: A61K31/4353 ,  A61P25/00

CPC classification number: A61K31/4353

Abstract: This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs.

Abstract translation: 本公开内容提供了用贝洛塞平和/或贝洛塞平类似物治疗疼痛的方法。

公开(公告)号：US06995261B2

公开(公告)日：2006-02-07

申请号：US10668475

申请日：2003-09-22

Applicant: Roland E. Dolle ,  Denton W. Hoyer ,  Tina Morgan Ross ,  James M. Rinker ,  Stanley J. Schmidt ,  Mark A. Ator

Inventor： Roland E. Dolle ,  Denton W. Hoyer ,  Tina Morgan Ross ,  James M. Rinker ,  Stanley J. Schmidt ,  Mark A. Ator

IPC: C07D237/24 ,  C07D401/04 ,  C07F9/38 ,  A61K31/501 ,  A61P19/02

CPC classification number: C07D401/04 ,  C07D237/24 ,  C07D403/04

Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0–6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1β protease activity in a mammal utilizing the compounds and compositions.

Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐：化学式id =“CHEM-US-00001”num =“000

公开(公告)号：US06852713B2

公开(公告)日：2005-02-08

申请号：US10414802

申请日：2003-04-16

Applicant: Roland E. Dolle ,  Paul Anson Tuthill

Inventor： Roland E. Dolle ,  Paul Anson Tuthill

IPC: C07D223/10 ,  C07D225/02 ,  C07D267/22 ,  A61K31/395 ,  C07D281/02 ,  C07D403/00

CPC classification number: C07D225/02 ,  C07D223/10 ,  C07D267/22

Abstract: Lactam derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.

Abstract translation: 披露了通式的内酰胺衍生物。 还公开了含有这些化合物的药物组合物及其使用方法。

公开(公告)号：US06624166B1

公开(公告)日：2003-09-23

申请号：US08625680

申请日：1996-04-03

Applicant: Roland E. Dolle ,  Denton W. Hoyer ,  Tina Morgan Ross ,  James M. Rinker ,  Stanley J. Schmidt ,  Mark A. Ator

Inventor： Roland E. Dolle ,  Denton W. Hoyer ,  Tina Morgan Ross ,  James M. Rinker ,  Stanley J. Schmidt ,  Mark A. Ator

IPC: C07D23724

CPC classification number: C07D401/04 ,  C07D237/24 ,  C07D403/04

Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1&bgr; protease activity in a mammal utilizing the compounds and compositions.

Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐：其中R1是卤素或含有芳香醚，烷基磺酸酯，芳基磺酸酯，烷基膦酸酯，芳基膦酸酯，磷酸烷基酯 或芳基磷酸酯; R2是COOR5，C（= O）NH（CHR5）m -COOR5，NH（CHR5）mCON（R5）R6，C（= O）N（R5）R6或NH（CHR5） H或烷基; R 4是H，取代或未取代的芳基，杂芳基或烷基; R 5和R 6独立地是H，低级烷基，芳基，羟基烷基，氨基烷基，杂芳基，低级亚烷基 - 芳基，低级亚烷基 - 杂芳基或低级环烷基; m = 0-6; 含有这些化合物的药物组合物; 以及利用该化合物和组合物抑制哺乳动物中白细胞介素-1β蛋白酶活性的方法。

公开(公告)号：US5677283A

公开(公告)日：1997-10-14

申请号：US732173

申请日：1996-10-16

Applicant: Roland E. Dolle ,  Jasbir Singh ,  David A. Whipple ,  Catherine Prouty ,  Prasad V. Chaturvedula ,  Stanley J. Schmidt ,  Mohamed M. A. Awad ,  Denton W. Hoyer ,  Tina Morgan Ross

Inventor： Roland E. Dolle ,  Jasbir Singh ,  David A. Whipple ,  Catherine Prouty ,  Prasad V. Chaturvedula ,  Stanley J. Schmidt ,  Mohamed M. A. Awad ,  Denton W. Hoyer ,  Tina Morgan Ross

IPC: C12N9/99 ,  A61K31/397 ,  A61K31/415 ,  A61K31/42 ,  A61K31/421 ,  A61K31/47 ,  A61K31/472 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/55 ,  A61K38/00 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07D205/04 ,  C07D207/38 ,  C07D209/12 ,  C07D215/14 ,  C07D217/16 ,  C07D223/08 ,  C07D231/20 ,  C07D231/22 ,  C07D261/12 ,  C07D263/06 ,  C07D265/06 ,  C07D265/30 ,  C07D311/46 ,  C07D311/50 ,  C07D311/56 ,  C07D401/12 ,  C07D409/12 ,  C07D413/04 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/09 ,  C07K5/097 ,  C07D231/04 ,  C07K5/00

CPC classification number: C07D401/12 ,  C07D207/38 ,  C07D231/20 ,  C07D231/22 ,  C07D261/12 ,  C07D311/46 ,  C07D311/56 ,  C07D409/12 ,  C07D413/04 ,  C07D417/12 ,  C07D453/02 ,  C07K5/0202 ,  A61K38/00

Abstract: Compounds which Inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is Independently L-valine or L-alanine; R.sub.1 is selected from the group consisting of N-�4(N,N-dimethylaminomethyl)!benzoyl, N-benzoyloxycarbonyl, N-methyl-N-�4-(pyridyl)methyl!, N-�4-(pyddyl)methyl!carbonyl, N-3-(piperidinopropionyl), N-�4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyddyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-�2-(4-pyridyl)ethyl!carbonyl, and N-(N-phenylpiperazino) carbonyl; and R.sub.8, R.sub.9 and R.sub.10 are as defined below.

Abstract translation: 提供了抑制白细胞介素-1β蛋白酶活性的化合物，含有这些化合物的药物组合物和使用该化合物的方法。 化合物具有式（1）其中n为0-2; 每个AA是独立的L-缬氨酸或L-丙氨酸; R1选自N- [4（N，N-二甲基氨基甲基）]苯甲酰基，N-苯甲酰氧基羰基，N-甲基-N- [4-（吡啶基）甲基]，N- [4-（吡啶基）甲基 ]羰基，N-3-（哌啶基丙酰基），N- [4-（吗啉代乙氧基）苯甲酰基，N-2-（奎宁环基）羰基，N-（3-吡啶基）甲氧基羰基，N-（2- N-甲基-N-苄基羰基，N-甲基-N- [2-（4-吡啶基）乙基]羰基和N-（N-苯基哌嗪基）羰基; 并且R 8，R 9和R 10如下所定义。

公开(公告)号：US5639745A

公开(公告)日：1997-06-17

申请号：US451108

申请日：1995-05-25

Applicant: Roland E. Dolle ,  Prasad V. Chaturvedula ,  Tina Morgan Ross ,  Stanley J. Schmidt

Inventor： Roland E. Dolle ,  Prasad V. Chaturvedula ,  Tina Morgan Ross ,  Stanley J. Schmidt

IPC: C07D487/04 ,  A61K31/535 ,  A61K31/55 ,  A61K38/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07D471/04 ,  C07D513/04 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078

CPC classification number: C07K5/06139 ,  C07K5/0202 ,  C07K5/021 ,  C07K5/06191 ,  A61K38/00

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.

Abstract translation: 公开了抑制白细胞介素-1β蛋白酶活性的化合物，组合物和方法。 醛和α-取代的甲基酮的化合物，双环衍生物具有本文所述的式（A）。

公开(公告)号：US5565430A

公开(公告)日：1996-10-15

申请号：US284861

申请日：1994-08-02

Applicant: Roland E. Dolle ,  Todd L. Graybill

Inventor： Roland E. Dolle ,  Todd L. Graybill

IPC: C07D231/22 ,  A61K31/195 ,  A61K31/198 ,  A61K31/215 ,  A61K31/27 ,  A61K31/40 ,  A61K31/66 ,  A61K38/00 ,  A61P11/00 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07C243/24 ,  C07C243/28 ,  C07C243/34 ,  C07C243/38 ,  C07D307/60 ,  C07F9/32 ,  C07K5/06 ,  C07K5/083 ,  A61K38/05 ,  C07C229/02 ,  C07K5/062

CPC classification number: C07K5/0808 ,  C07C243/28 ,  C07C243/34 ,  C07C243/38 ,  C07K5/06052 ,  A61K38/00

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukinprotease activity. The compounds, .alpha.-substituted acetamides a ##STR1## wherein: R.sub.2 =H or alkyl;R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5 ; ##STR2## where R.sup.4 and R.sup.5 =aryl;R.sup.6 =H, aryl or aralkyl;R.sup.7 =independently selected from R.sup.6, CF.sub.3 and CF.sub.2 CF.sub.3 ;R.sup.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO and amino acid.

Abstract translation: 公开了抑制白细胞间质蛋白酶活性的化合物，组合物和方法。 化合物，α-取代的乙酰胺a（A）其中：R2 = H或烷基; R3 =卤素，O（CO）0-1芳基，OPOR4R5; 其中R4和R5 =芳基; R6 = H，芳基或芳烷基; R7 =独立地选自R6，CF3和CF2CF3; R1 = R6-CO，杂芳基-CO，杂芳烷基-CO和氨基酸。