Derek T Chalmers, 6034 Spruce St, Riverside, CT 06878

6420541, Jul 16, 2002

Dec 22, 2000

09/767013

Dominic P. Behan - San Diego CA
Derek T. Chalmers - Solana Beach CA
Chen W. Liaw - San Diego CA
Joseph F. Russo - San Diego CA
William J. Thomsen - Del Mar CA

Arena Pharmaceuticals, Inc. - San Diego CA

C07K 2104

536 231, 536 235, 4353201, 435325, 4352523, 435 691, 4351723, 435 71, 530300, 530350

Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT and human 5-HT receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT receptors. Yet further disclosed is a new class of compounds which act at the 5HT receptors.

6420563, Jul 16, 2002

Feb 25, 2000

09/513838

Nigel R. A. Beeley - Solana Beach CA
Dominic P. Behan - San Diego CA
Derek T. Chalmers - Cardiff CA
Frederique Menzaghi - San Diego CA

Arena Pharmaceuticals, Inc. - San Diego CA

C07D40112

5462731, 514338, 514341, 514378, 514387, 514397, 514398, 5462744, 5462114, 5463144, 5463154, 5463231, 548240

Disclosed herein are small molecule modulators of the G protein coupled receptor six, methods of making such compounds, and methods of using such compounds.

6541209, Apr 1, 2003

Apr 14, 1999

09/292072

Dominic P. Behan - San Diego CA
Derek T. Chalmers - Solana Beach CA
Chen W. Liaw - San Diego CA
Joseph F. Russo - San Diego CA
William J. Thomsen - Del Mar CA

Arena Pharmaceuticals, Inc. - San Diego CA

G01N 3350

435 71, 435 691, 435325, 4351723, 4352523, 536 243, 536 231, 530350

Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT and human 5-HT receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT receptors. Yet further disclosed is a new class of compounds which act at the 5HT receptors.

6555339, Apr 29, 2003

Oct 13, 1998

09/170496

Chen W. Liaw - San Diego CA
Dominic P. Behan - San Diego CA
Derek T. Chalmers - Solana Beach CA

Arena Pharmaceuticals, Inc. - San Diego CA

C12N 1500

435 691, 4353201, 435325, 4352523, 4351723, 435 681, 530333, 530300, 530350, 702 19, 702 20, 702 22, 536 231, 536 2431

Disclosed are constitutively activated, non-endogenous versions of endogenous human GPCRs comprising the following amino acid sequence region (C-terminus to N-terminus orientation) and/or the following nucleic acid sequence region (3â to 5â orientation) transversing the transmembrane-6 (TM6) and intracellular loop-3 (IC3) regions of the GPCR: and/or respectively. In a preferred embodiment, P and P are endogenous proline and an endogenous nucleic acid encoding region encoding proline, respectively, located within TM6 of the non-endogenous GPCR; AA and (AA-codon) are 15 endogenous amino acid residues and 15 codons encoding endogenous amino acid residues, respectively; and X and X are non-endogenous lysine and non-endogenous nucleic acid region encoding lysine, respectively, located within IC3 of the non-endogenous GPCR. The purified and isolated non-endogenous human GPCRs having these mutations, and the receptors incorporated into mammalian cells, are well within the present disclosure.

6586596, Jul 1, 2003

Apr 17, 2001

09/836069

Derek T. Chalmers - Solana Beach CA
Susumo Sato - Chiba, JP
Tadayuki Koda - Chiba, JP

SSP Co., Ltd. - Tokyo

C07D40106

546 84

Disclosed herein are quinoline derivatives having dual mechanistic properties, referred to in this patent document as âacetylcholine enhancersâ, i. e. , compounds which evidence acetylcholinesterase (AChE) inhibition activity, and 5-HT3 receptor antagonist activity. A particularly preferred compound is 2-[2-(1-benzylpiperizin-4-yl)ethyl]-2,3-dihydro-9-methoxy-1H-pyrrolo [3,4-b] quinolin-1-one hemifumarate, referred to herein as Compound A (âCm. Aâ).

6653086, Nov 25, 2003

Jul 30, 1999

09/364425

Dominic P. Behan - San Diego CA
Derek T. Chalmers - Solana Beach CA
Chen W. Liaw - San Diego CA
I Lin-Lin - San Diego CA
Kevin P. Lowitz - San Diego CA
Ruoping Chen - San Diego CA

Arena Pharmaceuticals, Inc. - San Diego CA

C12N 1500

435 71, 435 72, 435 721, 435 691, 435 701, 4353201, 4351723, 530300, 530350, 536 231, 4241921

Disclosed herein are techniques for directly identifying candidate compounds as agonists, partial agonists and/or, most preferably, inverse agonists, to endogenous, constitutively activated orphan G protein-coupled receptors. Such directly identified compounds can be utilized, most preferably, in pharmaceutical compositions.

6723841, Apr 20, 2004

Jun 13, 2001

09/881401

Timothy W. Lovenberg - Carlsbad CA
Tilman Oltersdorf - Cardiff CA
Chen Wang Liaw - San Diego CA
Dimitri E. Grigoriadis - Carlsbad CA
Derek T. Chalmers - Solana Beach CA
Errol B. DeSouza - Del Mar CA

Neurocrine Biosciences Inc. - San Diego CA

C12N 1563

536 2431, 536 235

The present invention provides isolated nucleic acid molecules encoding CRF receptors, recombinant expression vectors and host cells suitable for expressing such receptors, as well as compositions and methods which utilize such receptors.

6846919, Jan 25, 2005

Jun 19, 2002

10/176255

Dominic P Behan - San Diego CA, US
Derek T Chalmers - Solana Beach CA, US
Chen W Liaw - San Diego CA, US
Joseph F Russo - San Diego CA, US
William J Thomsen - Del Mar CA, US

Arena Pharmaceuticals, Inc. - San Diego CA

C07K 2104
C07K 1400
C12N 1509
C12N 1500

536 231, 435 71, 435 691, 4351723, 435325, 4353201, 4352351, 536 235, 530300, 530350

Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HTand human 5-HTreceptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HTreceptors. Yet further disclosed is a new class of compounds which act at the 5HTreceptors.